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Assay Detail

CHEMBL3301000

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

Functional
Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
8
Total Activities
8
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 Autocuration

Target

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

Publication

Synthesis of novel fluoro analogues of MKC442 as microbicides.
Loksha YM, Pedersen EB, Loddo R, Sanna G, Collu G, Giliberti G, La Colla P.
J Med Chem (2014) 57 : 5169 -5178
PubMed 24805780 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.97 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 8.00
CHEMBL114 SAQUINAVIR 4.0 1 7.70
CHEMBL223228 EFAVIRENZ 4.0 1 7.22
CHEMBL70663 DAPIVIRINE 3.0 1 7.00
CHEMBL308954 ETRAVIRINE 4.0 1 7.00
CHEMBL240386 1 6.16
CHEMBL3298051 1 5.70
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 10.0 nM 8.00
CHEMBL114 SAQUINAVIR EC50 = 20.0 nM 7.70
CHEMBL223228 EFAVIRENZ EC50 = 60.0 nM 7.22
CHEMBL70663 DAPIVIRINE EC50 = 100.0 nM 7.00
CHEMBL308954 ETRAVIRINE EC50 = 100.0 nM 7.00
CHEMBL240386 EC50 = 700.0 nM 6.16
CHEMBL3298051 EC50 = 2000.0 nM 5.70
CHEMBL57 NEVIRAPINE EC50 > 20000.0 nM -