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Assay Detail

CHEMBL763242

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Functional
Inhibition of HIV protease
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism hiv
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

Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.
Lyle TA, Wiscount CM, Guare JP, Thompson WJ, Anderson PS, Darke PL, Zugay ZA, Emini EA, Schleif WA, Qunitero JC.
J Med Chem (1991) 34 : 1228 -1230
PubMed 2002466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.73 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419923 1 10.00
CHEMBL296115 1 9.52
CHEMBL20546 1 8.74
CHEMBL21041 1 8.72
CHEMBL20930 1 7.80
CHEMBL325107 1 7.72
CHEMBL2079666 1 7.68
CHEMBL279279 1 7.66
CHEMBL277034 1 6.96
CHEMBL439725 1 6.89
CHEMBL2092982 2 6.64
CHEMBL422928 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419923 IC50 = 0.1 nM 10.00
CHEMBL296115 IC50 = 0.3 nM 9.52
CHEMBL20546 IC50 = 1.8 nM 8.74
CHEMBL21041 IC50 = 1.9 nM 8.72
CHEMBL20930 IC50 = 16.0 nM 7.80
CHEMBL325107 IC50 = 19.0 nM 7.72
CHEMBL2079666 IC50 = 21.0 nM 7.68
CHEMBL279279 IC50 = 22.0 nM 7.66
CHEMBL277034 IC50 = 111.0 nM 6.96
CHEMBL439725 IC50 = 130.0 nM 6.89
CHEMBL2092982 IC50 = 229.0 nM 6.64
CHEMBL2092982 IC50 = 259.0 nM 6.59
CHEMBL422928 IC50 = 2800.0 nM 5.55