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Assay Detail

CHEMBL765174

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

Binding
Inhibitory activity against HIV-1 protease
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.
Tamamura H, Koh Y, Ueda S, Sasaki Y, Yamasaki T, Aoki M, Maeda K, Watai Y, Arikuni H, Otaka A, Mitsuya H, Fujii N.
J Med Chem (2003) 46 : 1764 -1768
PubMed 12699395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 9.72 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299578 1 10.00
CHEMBL49002 1 9.92
CHEMBL114 SAQUINAVIR 4.0 1 9.72
CHEMBL5483011 INDINAVIR 3.0 1 9.55
CHEMBL50945 1 9.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299578 Ki = 0.1 nM 10.00
CHEMBL49002 Ki = 0.12 nM 9.92
CHEMBL114 SAQUINAVIR Ki = 0.19 nM 9.72
CHEMBL5483011 INDINAVIR Ki = 0.28 nM 9.55
CHEMBL50945 Ki = 0.38 nM 9.42