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Assay Detail

CHEMBL4040184

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 TZM-bl cells assessed as inhibition of virus-induced cytopathic effect preincubated with cells for 30 mins followed by viral infection measured after 48 hrs in presence of p-24 HIV-1 Ag by luciferase reporter gene assay
17
Total Activities
17
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
EC50 17 5.52 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4070180 1 8.00
CHEMBL4089642 1 7.14
CHEMBL4073327 1 6.85
CHEMBL4099787 1 6.80
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 5.40
CHEMBL93006 1 5.34
CHEMBL329554 1 5.32
CHEMBL519667 1 5.22
CHEMBL482465 1 4.53
CHEMBL4082499 1 4.38
CHEMBL4062343 1 4.27
CHEMBL270618 1 4.26
CHEMBL2030736 1 4.25
CHEMBL4097362 1 -
CHEMBL4078094 1 -
CHEMBL4081770 1 -
CHEMBL4080837 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4070180 EC50 = 10.0 nM 8.00
CHEMBL4089642 EC50 = 73.0 nM 7.14
CHEMBL4073327 EC50 = 140.0 nM 6.85
CHEMBL4099787 EC50 = 160.0 nM 6.80
CHEMBL483 TENOFOVIR ANHYDROUS EC50 = 4000.0 nM 5.40
CHEMBL93006 EC50 = 4570.0 nM 5.34
CHEMBL329554 EC50 = 4810.0 nM 5.32
CHEMBL519667 EC50 = 5950.0 nM 5.22
CHEMBL482465 EC50 = 29240.0 nM 4.53
CHEMBL4082499 EC50 = 41860.0 nM 4.38
CHEMBL4062343 EC50 = 54110.0 nM 4.27
CHEMBL270618 EC50 = 54800.0 nM 4.26
CHEMBL2030736 EC50 = 56770.0 nM 4.25
CHEMBL4097362 EC50 > 100000.0 nM -
CHEMBL4078094 EC50 > 43440.0 nM -
CHEMBL4081770 EC50 > 54190.0 nM -
CHEMBL4080837 EC50 > 68980.0 nM -