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Assay Detail

CHEMBL917591

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Binding
Inhibition of human leukocyte elastase using [14C]GS7340 substrate
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

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Birkus G, Wang R, Liu X, Kutty N, MacArthur H, Cihlar T, Gibbs C, Swaminathan S, Lee W, McDermott M.
Antimicrob Agents Chemother (2007) 51 : 543 -550
PubMed 17145787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.52 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24983 1 5.52
CHEMBL374508 E-64 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24983 IC50 = 3000.0 nM 5.52
CHEMBL374508 E-64 IC50 > 300000.0 nM -