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Assay Detail

CHEMBL1042353

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

Binding
Inhibition of para-aminophenylmercuric acetate-activated human pro-MMP8 after 4 hrs by fluorimetry
20
Total Activities
20
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

Neutrophil collagenase (CHEMBL4588)
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 20 6.32 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179288 1 8.80
CHEMBL573715 1 8.29
CHEMBL572780 1 7.27
CHEMBL573934 1 7.06
CHEMBL573936 1 7.00
CHEMBL584365 1 6.92
CHEMBL573714 1 6.55
CHEMBL573935 1 6.54
CHEMBL584147 1 6.54
CHEMBL574370 1 6.43
CHEMBL574605 1 6.41
CHEMBL575896 1 6.21
CHEMBL574589 1 6.00
CHEMBL579067 1 5.92
CHEMBL584122 1 5.72
CHEMBL579068 1 5.72
CHEMBL575881 1 5.70
CHEMBL576762 1 5.04
CHEMBL575895 1 4.14
CHEMBL585376 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179288 IC50 = 1.6 nM 8.80
CHEMBL573715 IC50 = 5.1 nM 8.29
CHEMBL572780 IC50 = 54.0 nM 7.27
CHEMBL573934 IC50 = 87.0 nM 7.06
CHEMBL573936 IC50 = 99.0 nM 7.00
CHEMBL584365 IC50 = 120.0 nM 6.92
CHEMBL573714 IC50 = 280.0 nM 6.55
CHEMBL573935 IC50 = 290.0 nM 6.54
CHEMBL584147 IC50 = 290.0 nM 6.54
CHEMBL574370 IC50 = 370.0 nM 6.43
CHEMBL574605 IC50 = 390.0 nM 6.41
CHEMBL575896 IC50 = 620.0 nM 6.21
CHEMBL574589 IC50 = 1000.0 nM 6.00
CHEMBL579067 IC50 = 1200.0 nM 5.92
CHEMBL584122 IC50 = 1900.0 nM 5.72
CHEMBL579068 IC50 = 1900.0 nM 5.72
CHEMBL575881 IC50 = 2000.0 nM 5.70
CHEMBL576762 IC50 = 9200.0 nM 5.04
CHEMBL575895 IC50 = 72000.0 nM 4.14
CHEMBL585376 IC50 = 74000.0 nM 4.13