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Assay Detail

CHEMBL3271226

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

Functional
Antiretroviral activity against HIV-1 3B infected in human CEM/0 cells expressing thymidine kinase assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type CEM/0
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
Velanguparackel W, Hamon N, Balzarini J, McGuigan C, Westwell AD.
Bioorg Med Chem Lett (2014) 24 : 2240 -2243
PubMed 24751439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.83 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105318 ALOVUDINE 2.0 1 8.21
CHEMBL3260474 1 7.77
CHEMBL3260470 1 7.50
CHEMBL3260473 1 7.44
CHEMBL3260469 1 7.32
CHEMBL3260118 1 7.00
CHEMBL3260471 1 6.92
CHEMBL3260464 1 6.89
CHEMBL3260466 1 6.80
CHEMBL3260120 1 6.54
CHEMBL3260465 1 6.37
CHEMBL3260117 1 6.26
CHEMBL3260467 1 6.25
CHEMBL3260472 1 6.19
CHEMBL3260119 1 6.12
CHEMBL3260468 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105318 ALOVUDINE EC50 = 6.2 nM 8.21
CHEMBL3260474 EC50 = 17.0 nM 7.77
CHEMBL3260470 EC50 = 32.0 nM 7.50
CHEMBL3260473 EC50 = 36.0 nM 7.44
CHEMBL3260469 EC50 = 48.0 nM 7.32
CHEMBL3260118 EC50 = 100.0 nM 7.00
CHEMBL3260471 EC50 = 120.0 nM 6.92
CHEMBL3260464 EC50 = 130.0 nM 6.89
CHEMBL3260466 EC50 = 160.0 nM 6.80
CHEMBL3260120 EC50 = 290.0 nM 6.54
CHEMBL3260465 EC50 = 430.0 nM 6.37
CHEMBL3260117 EC50 = 550.0 nM 6.26
CHEMBL3260467 EC50 = 560.0 nM 6.25
CHEMBL3260472 EC50 = 650.0 nM 6.19
CHEMBL3260119 EC50 = 750.0 nM 6.12
CHEMBL3260468 EC50 = 2300.0 nM 5.64