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Assay Detail

CHEMBL1659934

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

Functional
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
Tojo Y, Koh Y, Amano M, Aoki M, Das D, Kulkarni S, Anderson DD, Ghosh AK, Mitsuya H.
Antimicrob Agents Chemother (2010) 54 : 3460 -3470
PubMed 20439612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.87 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL571882 1 8.70
CHEMBL1323 DARUNAVIR 4.0 1 8.52
CHEMBL577560 1 8.40
CHEMBL1650599 1 7.85
CHEMBL571982 1 7.66
CHEMBL116 AMPRENAVIR 4.0 1 7.62
CHEMBL729 LOPINAVIR 4.0 1 7.41
CHEMBL222559 TIPRANAVIR 4.0 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL571882 EC50 = 2.0 nM 8.70
CHEMBL1323 DARUNAVIR EC50 = 3.0 nM 8.52
CHEMBL577560 EC50 = 4.0 nM 8.40
CHEMBL1650599 EC50 = 14.0 nM 7.85
CHEMBL571982 EC50 = 22.0 nM 7.66
CHEMBL116 AMPRENAVIR EC50 = 24.0 nM 7.62
CHEMBL729 LOPINAVIR EC50 = 39.0 nM 7.41
CHEMBL222559 TIPRANAVIR EC50 = 170.0 nM 6.77