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Assay Detail

CHEMBL1020405

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

Functional
Antiviral activity against HIV1 BaL in human PBMC assessed as blockade of reverse transcriptase activity
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
Hazen R, Harvey R, Ferris R, Craig C, Yates P, Griffin P, Miller J, Kaldor I, Ray J, Samano V, Furfine E, Spaltenstein A, Hale M, Tung R, St Clair M, Hanlon M, Boone L.
Antimicrob Agents Chemother (2007) 51 : 3147 -3154
PubMed 17620375 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.92 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206031 BRECANAVIR 2.0 1 9.38
CHEMBL1323 DARUNAVIR 4.0 1 8.55
CHEMBL1163 ATAZANAVIR 4.0 1 8.36
CHEMBL584 NELFINAVIR 4.0 1 7.44
CHEMBL116 AMPRENAVIR 4.0 1 7.24
CHEMBL222559 TIPRANAVIR 4.0 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL206031 BRECANAVIR EC50 = 0.42 nM 9.38
CHEMBL1323 DARUNAVIR EC50 = 2.8 nM 8.55
CHEMBL1163 ATAZANAVIR EC50 = 4.4 nM 8.36
CHEMBL584 NELFINAVIR EC50 = 36.0 nM 7.44
CHEMBL116 AMPRENAVIR EC50 = 57.0 nM 7.24
CHEMBL222559 TIPRANAVIR EC50 = 304.0 nM 6.52