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Assay Detail

CHEMBL935830

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

Functional
Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Intermediate

Target

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

Publication

A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.
Amano M, Koh Y, Das D, Li J, Leschenko S, Wang YF, Boross PI, Weber IT, Ghosh AK, Mitsuya H.
Antimicrob Agents Chemother (2007) 51 : 2143 -2155
PubMed 17371811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.64 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL178593 1 8.62
CHEMBL1323 DARUNAVIR 4.0 1 8.48
CHEMBL1163 ATAZANAVIR 4.0 1 7.68
CHEMBL114 SAQUINAVIR 4.0 1 7.62
CHEMBL729 LOPINAVIR 4.0 1 7.62
CHEMBL163 RITONAVIR 4.0 1 7.29
CHEMBL116 AMPRENAVIR 4.0 1 7.22
CHEMBL5483011 INDINAVIR 3.0 1 6.57
CHEMBL584 NELFINAVIR 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL178593 EC50 = 2.4 nM 8.62
CHEMBL1323 DARUNAVIR EC50 = 3.3 nM 8.48
CHEMBL1163 ATAZANAVIR EC50 = 21.0 nM 7.68
CHEMBL114 SAQUINAVIR EC50 = 24.0 nM 7.62
CHEMBL729 LOPINAVIR EC50 = 24.0 nM 7.62
CHEMBL163 RITONAVIR EC50 = 51.0 nM 7.29
CHEMBL116 AMPRENAVIR EC50 = 60.0 nM 7.22
CHEMBL5483011 INDINAVIR EC50 = 270.0 nM 6.57
CHEMBL584 NELFINAVIR EC50 > 1000.0 nM -