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Assay Detail

CHEMBL899467

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Functional
Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method
ChEMBL ↗
47
Total Activities
47
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 47 6.71 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396816 — — 1 9.22
CHEMBL239338 — — 1 9.15
CHEMBL239337 — — 1 8.70
CHEMBL223228 EFAVIRENZ 4.0 1 8.22
CHEMBL442246 — — 1 8.00
CHEMBL239343 — — 1 7.85
CHEMBL240386 — — 1 7.85
CHEMBL239064 — — 1 7.52
CHEMBL238882 — — 1 7.52
CHEMBL239719 — — 1 7.52
CHEMBL394990 — — 1 7.41
CHEMBL238856 — — 1 7.30
CHEMBL239281 — — 1 7.22
CHEMBL239342 — — 1 7.16
CHEMBL394482 — — 1 7.15
CHEMBL239063 — — 1 7.05
CHEMBL236161 — — 1 7.01
CHEMBL238907 — — 1 7.00
CHEMBL239934 — — 1 6.85
CHEMBL395404 — — 1 6.85
CHEMBL238466 — — 1 6.85
CHEMBL239918 — — 1 6.37
CHEMBL393696 — — 1 6.37
CHEMBL238921 — — 1 6.37
CHEMBL391165 — — 1 6.30
CHEMBL238700 — — 1 6.24
CHEMBL241666 — — 1 6.15
CHEMBL239718 — — 1 6.15
CHEMBL239919 — — 1 6.10
CHEMBL57 NEVIRAPINE 4.0 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396816 — EC50 = 0.6 nM 9.22
CHEMBL239338 — EC50 = 0.7 nM 9.15
CHEMBL239337 — EC50 = 2.0 nM 8.70
CHEMBL223228 EFAVIRENZ EC50 = 6.0 nM 8.22
CHEMBL442246 — EC50 = 10.0 nM 8.00
CHEMBL239343 — EC50 = 14.0 nM 7.85
CHEMBL240386 — EC50 = 14.0 nM 7.85
CHEMBL239064 — EC50 = 30.0 nM 7.52
CHEMBL238882 — EC50 = 30.0 nM 7.52
CHEMBL239719 — EC50 = 30.0 nM 7.52
CHEMBL394990 — EC50 = 39.0 nM 7.41
CHEMBL238856 — EC50 = 50.0 nM 7.30
CHEMBL239281 — EC50 = 60.0 nM 7.22
CHEMBL239342 — EC50 = 70.0 nM 7.16
CHEMBL394482 — EC50 = 71.0 nM 7.15
CHEMBL239063 — EC50 = 90.0 nM 7.05
CHEMBL236161 — EC50 = 97.0 nM 7.01
CHEMBL238907 — EC50 = 100.0 nM 7.00
CHEMBL239934 — EC50 = 140.0 nM 6.85
CHEMBL395404 — EC50 = 140.0 nM 6.85
CHEMBL238466 — EC50 = 140.0 nM 6.85
CHEMBL238921 — EC50 = 430.0 nM 6.37
CHEMBL239918 — EC50 = 430.0 nM 6.37
CHEMBL393696 — EC50 = 430.0 nM 6.37
CHEMBL391165 — EC50 = 500.0 nM 6.30
CHEMBL238700 — EC50 = 570.0 nM 6.24
CHEMBL241666 — EC50 = 710.0 nM 6.15
CHEMBL239718 — EC50 = 710.0 nM 6.15
CHEMBL239919 — EC50 = 790.0 nM 6.10
CHEMBL57 NEVIRAPINE EC50 = 870.0 nM 6.06
CHEMBL238464 — EC50 = 1140.0 nM 5.94
CHEMBL239699 — EC50 = 1290.0 nM 5.89
CHEMBL239717 — EC50 = 1820.0 nM 5.74
CHEMBL391164 — EC50 = 3600.0 nM 5.44
CHEMBL240387 — EC50 = 3600.0 nM 5.44
CHEMBL394989 — EC50 = 3600.0 nM 5.44
CHEMBL427856 — EC50 = 3600.0 nM 5.44
CHEMBL240388 — EC50 = 3600.0 nM 5.44
CHEMBL238702 — EC50 = 3600.0 nM 5.44
CHEMBL240148 — EC50 = 3600.0 nM 5.44
CHEMBL391762 — EC50 = 5150.0 nM 5.29
CHEMBL397172 — EC50 = 5720.0 nM 5.24
CHEMBL240770 — EC50 > 10000.0 nM -
CHEMBL240769 — EC50 > 10000.0 nM -
CHEMBL239120 — EC50 > 10000.0 nM -
CHEMBL396683 — EC50 > 10000.0 nM -
CHEMBL238701 — EC50 > 10000.0 nM -