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Assay Detail

CHEMBL3300993

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

Functional
Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
15
Total Activities
15
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 15 7.50 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70663 DAPIVIRINE 3.0 1 9.00
CHEMBL308954 ETRAVIRINE 4.0 1 9.00
CHEMBL223228 EFAVIRENZ 4.0 1 8.70
CHEMBL240386 1 8.40
CHEMBL3298051 1 8.00
CHEMBL114 SAQUINAVIR 4.0 1 8.00
CHEMBL3297960 1 7.40
CHEMBL3297961 1 7.30
CHEMBL57 NEVIRAPINE 4.0 1 7.22
CHEMBL3298048 1 7.16
CHEMBL35033 EMIVIRINE 2.0 1 7.10
CHEMBL3298130 1 7.00
CHEMBL129 ZIDOVUDINE 4.0 1 6.70
CHEMBL3298049 1 6.52
CHEMBL3298050 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70663 DAPIVIRINE EC50 = 1.0 nM 9.00
CHEMBL308954 ETRAVIRINE EC50 = 1.0 nM 9.00
CHEMBL223228 EFAVIRENZ EC50 = 2.0 nM 8.70
CHEMBL240386 EC50 = 4.0 nM 8.40
CHEMBL3298051 EC50 = 10.0 nM 8.00
CHEMBL114 SAQUINAVIR EC50 = 10.0 nM 8.00
CHEMBL3297960 EC50 = 40.0 nM 7.40
CHEMBL3297961 EC50 = 50.0 nM 7.30
CHEMBL57 NEVIRAPINE EC50 = 60.0 nM 7.22
CHEMBL3298048 EC50 = 70.0 nM 7.16
CHEMBL35033 EMIVIRINE EC50 = 80.0 nM 7.10
CHEMBL3298130 EC50 = 100.0 nM 7.00
CHEMBL129 ZIDOVUDINE EC50 = 200.0 nM 6.70
CHEMBL3298049 EC50 = 300.0 nM 6.52
CHEMBL3298050 EC50 = 11000.0 nM 4.96