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Assay Detail

CHEMBL900569

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Binding
Inhibition of HIV1 reverse transcriptase V106A mutant
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
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
Ki 30 6.75 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL394990 1 8.10
CHEMBL399016 1 8.00
CHEMBL239342 1 7.70
CHEMBL396816 1 7.70
CHEMBL239337 1 7.70
CHEMBL239064 1 7.52
CHEMBL239338 1 7.52
CHEMBL239281 1 7.40
CHEMBL238907 1 7.22
CHEMBL239120 1 7.05
CHEMBL240386 1 7.00
CHEMBL393696 1 6.85
CHEMBL241666 1 6.70
CHEMBL238701 1 6.40
CHEMBL239063 1 6.30
CHEMBL391164 1 6.30
CHEMBL239919 1 6.30
CHEMBL236161 1 6.30
CHEMBL239126 1 6.30
CHEMBL238700 1 6.30
CHEMBL240176 1 6.30
CHEMBL240770 1 6.30
CHEMBL427856 1 6.30
CHEMBL239717 1 6.16
CHEMBL239122 1 6.05
CHEMBL240769 1 5.54
CHEMBL57 NEVIRAPINE 4.0 1 5.00
CHEMBL238702 1 -
CHEMBL223228 EFAVIRENZ 4.0 1 -
CHEMBL240147 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL394990 Ki = 8.0 nM 8.10
CHEMBL399016 Ki = 10.0 nM 8.00
CHEMBL239342 Ki = 20.0 nM 7.70
CHEMBL396816 Ki = 20.0 nM 7.70
CHEMBL239337 Ki = 20.0 nM 7.70
CHEMBL239064 Ki = 30.0 nM 7.52
CHEMBL239338 Ki = 30.0 nM 7.52
CHEMBL239281 Ki = 40.0 nM 7.40
CHEMBL238907 Ki = 60.0 nM 7.22
CHEMBL239120 Ki = 90.0 nM 7.05
CHEMBL240386 Ki = 100.0 nM 7.00
CHEMBL393696 Ki = 140.0 nM 6.85
CHEMBL241666 Ki = 200.0 nM 6.70
CHEMBL238701 Ki = 400.0 nM 6.40
CHEMBL239063 Ki = 500.0 nM 6.30
CHEMBL391164 Ki = 500.0 nM 6.30
CHEMBL239919 Ki = 500.0 nM 6.30
CHEMBL236161 Ki = 500.0 nM 6.30
CHEMBL239126 Ki = 500.0 nM 6.30
CHEMBL238700 Ki = 500.0 nM 6.30
CHEMBL240176 Ki = 500.0 nM 6.30
CHEMBL240770 Ki = 500.0 nM 6.30
CHEMBL427856 Ki = 500.0 nM 6.30
CHEMBL239717 Ki = 700.0 nM 6.16
CHEMBL239122 Ki = 900.0 nM 6.05
CHEMBL240769 Ki = 2900.0 nM 5.54
CHEMBL57 NEVIRAPINE Ki = 10000.0 nM 5.00
CHEMBL238702 Ki > 40000.0 nM -
CHEMBL223228 EFAVIRENZ Ki - -
CHEMBL240147 Ki > 40000.0 nM -