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Assay Detail

CHEMBL763585

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Binding
Tested for inhibitory concentration against HIV-1 protease
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands.
Ghosh AK, Thompson WJ, Holloway MK, McKee SP, Duong TT, Lee HY, Munson PM, Smith AM, Wai JM, Darke PL.
J Med Chem (1993) 36 : 2300 -2310
PubMed 8360874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 9.21 10.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17612 1 10.27
CHEMBL75904 1 10.22
CHEMBL310924 1 10.15
CHEMBL73934 1 9.96
CHEMBL307918 1 9.92
CHEMBL309175 1 9.82
CHEMBL306974 1 9.80
CHEMBL114 SAQUINAVIR 4.0 1 9.64
CHEMBL432924 1 9.62
CHEMBL74472 1 9.41
CHEMBL76352 1 9.30
CHEMBL306570 1 9.22
CHEMBL75082 1 9.15
CHEMBL307926 1 8.59
CHEMBL265026 1 8.55
CHEMBL74077 1 8.48
CHEMBL312788 1 8.27
CHEMBL306810 1 7.41
CHEMBL418902 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17612 IC50 = 0.054 nM 10.27
CHEMBL75904 IC50 = 0.06 nM 10.22
CHEMBL310924 IC50 = 0.071 nM 10.15
CHEMBL73934 IC50 = 0.11 nM 9.96
CHEMBL307918 IC50 = 0.12 nM 9.92
CHEMBL309175 IC50 = 0.15 nM 9.82
CHEMBL306974 IC50 = 0.16 nM 9.80
CHEMBL114 SAQUINAVIR IC50 = 0.23 nM 9.64
CHEMBL432924 IC50 = 0.24 nM 9.62
CHEMBL74472 IC50 = 0.39 nM 9.41
CHEMBL76352 IC50 = 0.5 nM 9.30
CHEMBL306570 IC50 = 0.6 nM 9.22
CHEMBL75082 IC50 = 0.7 nM 9.15
CHEMBL307926 IC50 = 2.6 nM 8.59
CHEMBL265026 IC50 = 2.83 nM 8.55
CHEMBL74077 IC50 = 3.3 nM 8.48
CHEMBL312788 IC50 = 5.4 nM 8.27
CHEMBL306810 IC50 = 39.0 nM 7.41
CHEMBL418902 IC50 = 67.9 nM 7.17