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Assay Detail

CHEMBL768622

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Binding
Inhibition of HIV-1 protease was determined in vitro
16
Total Activities
16
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

A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Holloway MK, Wai JM, Halgren TA, Fitzgerald PM, Vacca JP, Dorsey BD, Levin RB, Thompson WJ, Chen LJ, deSolms SJ.
J Med Chem (1995) 38 : 305 -317
PubMed 7830273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.42 10.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17612 1 10.27
CHEMBL319408 1 10.22
CHEMBL114 SAQUINAVIR 4.0 1 9.64
CHEMBL109952 1 9.16
CHEMBL322037 1 8.89
CHEMBL312788 1 8.27
CHEMBL322577 1 8.12
CHEMBL106530 1 7.28
CHEMBL69604 1 6.64
CHEMBL320099 1 6.25
CHEMBL107259 1 6.23
CHEMBL111175 1 5.90
CHEMBL9618 1 5.86
CHEMBL110144 1 5.52
CHEMBL106005 1 5.33
CHEMBL323225 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17612 IC50 = 0.054 nM 10.27
CHEMBL319408 IC50 = 0.05998 nM 10.22
CHEMBL114 SAQUINAVIR IC50 = 0.2291 nM 9.64
CHEMBL109952 IC50 = 0.6918 nM 9.16
CHEMBL322037 IC50 = 1.288 nM 8.89
CHEMBL312788 IC50 = 5.4 nM 8.27
CHEMBL322577 IC50 = 7.586 nM 8.12
CHEMBL106530 IC50 = 52.8 nM 7.28
CHEMBL69604 IC50 = 228.98 nM 6.64
CHEMBL320099 IC50 = 567.94 nM 6.25
CHEMBL107259 IC50 = 588.98 nM 6.23
CHEMBL111175 IC50 = 1269.11 nM 5.90
CHEMBL9618 IC50 = 1374.99 nM 5.86
CHEMBL110144 IC50 = 3019.95 nM 5.52
CHEMBL106005 IC50 = 4677.35 nM 5.33
CHEMBL323225 IC50 = 6760.83 nM 5.17