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Assay Detail

CHEMBL4040187

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

Functional
Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured on day 10 post infection in presence of IL-2 by ELISA
11
Total Activities
11
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

Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs.
Luo M, Groaz E, Andrei G, Snoeck R, Kalkeri R, Ptak RG, Hartman T, Buckheit RW, Schols D, De Jonghe S, Herdewijn P.
J Med Chem (2017) 60 : 6220 -6238
PubMed 28682067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.05 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2107825 TENOFOVIR ALAFENAMIDE 4.0 1 9.00
CHEMBL4070180 1 8.52
CHEMBL4089642 1 7.70
CHEMBL4073327 1 7.58
CHEMBL4099787 1 7.52
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE 4.0 1 7.10
CHEMBL329554 1 6.55
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 6.42
CHEMBL519667 1 5.92
CHEMBL93006 1 5.85
CHEMBL482465 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2107825 TENOFOVIR ALAFENAMIDE IC50 = 1.0 nM 9.00
CHEMBL4070180 IC50 = 3.0 nM 8.52
CHEMBL4089642 IC50 = 20.0 nM 7.70
CHEMBL4073327 IC50 = 26.0 nM 7.58
CHEMBL4099787 IC50 = 30.0 nM 7.52
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE IC50 = 80.0 nM 7.10
CHEMBL329554 IC50 = 280.0 nM 6.55
CHEMBL483 TENOFOVIR ANHYDROUS IC50 = 380.0 nM 6.42
CHEMBL519667 IC50 = 1190.0 nM 5.92
CHEMBL93006 IC50 = 1420.0 nM 5.85
CHEMBL482465 IC50 = 4040.0 nM 5.39