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Assay Detail

CHEMBL763243

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Functional
Inhibition of HIV-1 protease
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 protease (CHEMBL243)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Vacca JP, Guare JP, deSolms SJ, Sanders WM, Giuliani EA, Young SD, Darke PL, Zugay J, Sigal IS, Schleif WA.
J Med Chem (1991) 34 : 1225 -1228
PubMed 2002465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.68 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085527 1 10.52
CHEMBL3085503 1 10.15
CHEMBL47480 1 9.82
CHEMBL283583 1 9.82
CHEMBL289195 1 9.22
CHEMBL282654 1 9.15
CHEMBL3143349 1 9.00
CHEMBL282041 1 8.85
CHEMBL3143353 1 8.22
CHEMBL423106 1 7.92
CHEMBL249788 1 7.92
CHEMBL3143341 1 7.70
CHEMBL277034 1 6.96
CHEMBL428686 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085527 IC50 = 0.03 nM 10.52
CHEMBL3085503 IC50 = 0.07 nM 10.15
CHEMBL47480 IC50 = 0.15 nM 9.82
CHEMBL283583 IC50 = 0.15 nM 9.82
CHEMBL289195 IC50 = 0.6 nM 9.22
CHEMBL282654 IC50 = 0.71 nM 9.15
CHEMBL3143349 IC50 = 1.0 nM 9.00
CHEMBL282041 IC50 = 1.4 nM 8.85
CHEMBL3143353 IC50 = 6.0 nM 8.22
CHEMBL423106 IC50 = 12.0 nM 7.92
CHEMBL249788 IC50 = 12.0 nM 7.92
CHEMBL3143341 IC50 = 20.0 nM 7.70
CHEMBL277034 IC50 = 111.0 nM 6.96
CHEMBL428686 IC50 = 470.0 nM 6.33