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Assay Detail

CHEMBL4276409

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Functional
Antiviral activity against Atazanavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay
6
Total Activities
6
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

Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.
Ghosh AK, Williams JN, Ho RY, Simpson HM, Hattori SI, Hayashi H, Agniswamy J, Wang YF, Weber IT, Mitsuya H.
J Med Chem (2018) 61 : 9722 -9737
PubMed 30354121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.29 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1323 DARUNAVIR 4.0 1 7.72
CHEMBL4277539 1 7.48
CHEMBL4292006 1 7.44
CHEMBL729 LOPINAVIR 4.0 1 6.51
CHEMBL116 AMPRENAVIR 4.0 1 -
CHEMBL1163 ATAZANAVIR 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1323 DARUNAVIR IC50 = 19.0 nM 7.72
CHEMBL4277539 IC50 = 33.0 nM 7.48
CHEMBL4292006 IC50 = 36.0 nM 7.44
CHEMBL729 LOPINAVIR IC50 = 311.0 nM 6.51
CHEMBL116 AMPRENAVIR IC50 > 1000.0 nM -
CHEMBL1163 ATAZANAVIR IC50 > 1000.0 nM -