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Assay Detail

CHEMBL763581

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

Binding
Tested against S2-binding site of HIV-1 protease
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
Ghosh AK, Thompson WJ, Lee HY, McKee SP, Munson PM, Duong TT, Darke PL, Zugay JA, Emini EA, Schleif WA.
J Med Chem (1993) 36 : 924 -927
PubMed 8464047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.55 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114 SAQUINAVIR 4.0 1 9.64
CHEMBL18067 1 8.52
CHEMBL17600 1 8.27
CHEMBL414648 1 8.05
CHEMBL261340 1 7.96
CHEMBL18068 1 7.94
CHEMBL353815 1 7.92
CHEMBL279326 1 7.88
CHEMBL277801 1 7.65
CHEMBL170576 1 7.52
CHEMBL18031 1 7.28
CHEMBL273317 1 7.12
CHEMBL275389 1 6.85
CHEMBL18389 1 6.80
CHEMBL18253 1 6.77
CHEMBL354897 1 6.16
CHEMBL17704 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114 SAQUINAVIR IC50 = 0.23 nM 9.64
CHEMBL18067 IC50 = 3.0 nM 8.52
CHEMBL17600 IC50 = 5.4 nM 8.27
CHEMBL414648 IC50 = 9.0 nM 8.05
CHEMBL261340 IC50 = 11.0 nM 7.96
CHEMBL18068 IC50 = 11.4 nM 7.94
CHEMBL353815 IC50 = 12.0 nM 7.92
CHEMBL279326 IC50 = 13.1 nM 7.88
CHEMBL277801 IC50 = 22.3 nM 7.65
CHEMBL170576 IC50 = 30.0 nM 7.52
CHEMBL18031 IC50 = 52.4 nM 7.28
CHEMBL273317 IC50 = 75.0 nM 7.12
CHEMBL275389 IC50 = 140.0 nM 6.85
CHEMBL18389 IC50 = 160.0 nM 6.80
CHEMBL18253 IC50 = 169.0 nM 6.77
CHEMBL354897 IC50 = 694.0 nM 6.16
CHEMBL17704 IC50 = 1030.0 nM 5.99