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Assay Detail

CHEMBL982903

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

Binding
Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay
7
Total Activities
7
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 Autocuration

Target

Protease (CHEMBL2366517)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Kozísek M, Cígler P, Lepsík M, Fanfrlík J, Rezácová P, Brynda J, Pokorná J, Plesek J, Grüner B, Grantz Sasková K, Václavíková J, Král V, Konvalinka J.
J Med Chem (2008) 51 : 4839 -4843
PubMed 18598016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 10.26 10.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL729 LOPINAVIR 4.0 1 10.74
CHEMBL1163 ATAZANAVIR 4.0 1 10.62
CHEMBL114 SAQUINAVIR 4.0 1 10.40
CHEMBL584 NELFINAVIR 4.0 1 10.15
CHEMBL5483011 INDINAVIR 3.0 1 9.92
CHEMBL116 AMPRENAVIR 4.0 1 9.74
CHEMBL1323 DARUNAVIR 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL729 LOPINAVIR Ki = 0.018 nM 10.74
CHEMBL1163 ATAZANAVIR Ki = 0.024 nM 10.62
CHEMBL114 SAQUINAVIR Ki = 0.04 nM 10.40
CHEMBL584 NELFINAVIR Ki = 0.07 nM 10.15
CHEMBL5483011 INDINAVIR Ki = 0.12 nM 9.92
CHEMBL116 AMPRENAVIR Ki = 0.18 nM 9.74
CHEMBL1323 DARUNAVIR Ki = 0.0053 nM -