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Assay Detail

CHEMBL899466

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

Functional
Antiviral activity against HIV1 with reverse transcriptase K103N mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method
43
Total Activities
43
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 Intermediate

Target

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

Publication

Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
Mai A, Artico M, Rotili D, Tarantino D, Clotet-Codina I, Armand-Ugón M, Ragno R, Simeoni S, Sbardella G, Nawrozkij MB, Samuele A, Maga G, Esté JA.
J Med Chem (2007) 50 : 5412 -5424
PubMed 17910429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 6.55 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239338 1 8.22
CHEMBL396816 1 8.00
CHEMBL239337 1 7.70
CHEMBL240386 1 7.30
CHEMBL238856 1 7.10
CHEMBL223228 EFAVIRENZ 4.0 1 7.05
CHEMBL239919 1 6.92
CHEMBL394482 1 6.81
CHEMBL393696 1 6.75
CHEMBL239343 1 6.71
CHEMBL236161 1 6.65
CHEMBL238907 1 6.60
CHEMBL442246 1 6.49
CHEMBL239281 1 6.43
CHEMBL239063 1 6.41
CHEMBL239342 1 6.28
CHEMBL394990 1 6.12
CHEMBL239719 1 5.92
CHEMBL239064 1 5.91
CHEMBL57 NEVIRAPINE 4.0 1 5.75
CHEMBL238702 1 5.74
CHEMBL239717 1 5.62
CHEMBL239934 1 5.36
CHEMBL239718 1 5.34
CHEMBL240769 1 -
CHEMBL239120 1 -
CHEMBL238701 1 -
CHEMBL238700 1 -
CHEMBL427856 1 -
CHEMBL397172 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239338 EC50 = 6.0 nM 8.22
CHEMBL396816 EC50 = 10.0 nM 8.00
CHEMBL239337 EC50 = 20.0 nM 7.70
CHEMBL240386 EC50 = 50.0 nM 7.30
CHEMBL238856 EC50 = 80.0 nM 7.10
CHEMBL223228 EFAVIRENZ EC50 = 90.0 nM 7.05
CHEMBL239919 EC50 = 120.0 nM 6.92
CHEMBL394482 EC50 = 155.0 nM 6.81
CHEMBL393696 EC50 = 180.0 nM 6.75
CHEMBL239343 EC50 = 193.0 nM 6.71
CHEMBL236161 EC50 = 225.0 nM 6.65
CHEMBL238907 EC50 = 250.0 nM 6.60
CHEMBL442246 EC50 = 322.0 nM 6.49
CHEMBL239281 EC50 = 370.0 nM 6.43
CHEMBL239063 EC50 = 390.0 nM 6.41
CHEMBL239342 EC50 = 520.0 nM 6.28
CHEMBL394990 EC50 = 750.0 nM 6.12
CHEMBL239719 EC50 = 1200.0 nM 5.92
CHEMBL239064 EC50 = 1240.0 nM 5.91
CHEMBL57 NEVIRAPINE EC50 = 1800.0 nM 5.75
CHEMBL238702 EC50 = 1830.0 nM 5.74
CHEMBL239717 EC50 = 2400.0 nM 5.62
CHEMBL239934 EC50 = 4400.0 nM 5.36
CHEMBL239718 EC50 = 4600.0 nM 5.34
CHEMBL391165 EC50 > 10000.0 nM -
CHEMBL238882 EC50 > 10000.0 nM -
CHEMBL396683 EC50 > 10000.0 nM -
CHEMBL241666 EC50 > 10000.0 nM -
CHEMBL238464 EC50 > 10000.0 nM -
CHEMBL238921 EC50 > 10000.0 nM -
CHEMBL239699 EC50 > 10000.0 nM -
CHEMBL239918 EC50 > 10000.0 nM -
CHEMBL391164 EC50 > 10000.0 nM -
CHEMBL240770 EC50 > 10000.0 nM -
CHEMBL391762 EC50 > 10000.0 nM -
CHEMBL395404 EC50 > 10000.0 nM -
CHEMBL238466 EC50 > 10000.0 nM -
CHEMBL397172 EC50 > 10000.0 nM -
CHEMBL427856 EC50 > 10000.0 nM -
CHEMBL238700 EC50 > 10000.0 nM -
CHEMBL238701 EC50 > 10000.0 nM -
CHEMBL239120 EC50 > 10000.0 nM -
CHEMBL240769 EC50 > 10000.0 nM -