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Assay Detail

CHEMBL4392472

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

Functional
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as reduction in viral yield measured after 4 days by EnduRen live cell substrate based luciferase reporter gene assay
13
Total Activities
13
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

Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.
A M Subbaiah M, Mandlekar S, Desikan S, Ramar T, Subramani L, Annadurai M, Desai SD, Sinha S, Jenkins SM, Krystal MR, Subramanian M, Sridhar S, Padmanabhan S, Bhutani P, Arla R, Singh S, Sinha J, Thakur M, Kadow JF, Meanwell NA.
J Med Chem (2019) 62 : 3553 -3574
PubMed 30938524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 9.06 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163 ATAZANAVIR 4.0 1 9.15
CHEMBL4300203 1 9.05
CHEMBL4522729 1 9.05
CHEMBL4437104 1 9.05
CHEMBL4474072 1 9.05
CHEMBL4460401 1 9.05
CHEMBL4554438 1 9.05
CHEMBL4447493 1 9.05
CHEMBL4463796 1 9.05
CHEMBL4525849 1 9.05
CHEMBL4542773 1 9.05
CHEMBL4573907 1 9.05
CHEMBL4574382 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163 ATAZANAVIR EC50 = 0.7 nM 9.15
CHEMBL4300203 EC50 = 0.9 nM 9.05
CHEMBL4522729 EC50 = 0.9 nM 9.05
CHEMBL4437104 EC50 = 0.9 nM 9.05
CHEMBL4474072 EC50 = 0.9 nM 9.05
CHEMBL4460401 EC50 = 0.9 nM 9.05
CHEMBL4554438 EC50 = 0.9 nM 9.05
CHEMBL4447493 EC50 = 0.9 nM 9.05
CHEMBL4463796 EC50 = 0.9 nM 9.05
CHEMBL4525849 EC50 = 0.9 nM 9.05
CHEMBL4542773 EC50 = 0.9 nM 9.05
CHEMBL4573907 EC50 = 0.9 nM 9.05
CHEMBL4574382 EC50 = 0.9 nM 9.05