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Assay Detail

CHEMBL900566

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Binding
Inhibition of wild type HIV1 3B reverse transcriptase
26
Total Activities
26
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 26 6.94 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239063 1 8.52
CHEMBL236161 1 8.30
CHEMBL223228 EFAVIRENZ 4.0 1 7.52
CHEMBL396816 1 7.52
CHEMBL239281 1 7.40
CHEMBL239338 1 7.40
CHEMBL239337 1 7.40
CHEMBL238907 1 7.30
CHEMBL238701 1 7.30
CHEMBL399016 1 7.30
CHEMBL239064 1 7.22
CHEMBL239342 1 7.16
CHEMBL391164 1 7.10
CHEMBL240386 1 7.00
CHEMBL393696 1 7.00
CHEMBL394990 1 7.00
CHEMBL239717 1 7.00
CHEMBL239120 1 6.82
CHEMBL240770 1 6.70
CHEMBL239126 1 6.60
CHEMBL57 NEVIRAPINE 4.0 1 6.40
CHEMBL240769 1 6.16
CHEMBL238702 1 6.00
CHEMBL239122 1 5.70
CHEMBL241666 1 5.60
CHEMBL240147 1 4.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239063 Ki = 3.0 nM 8.52
CHEMBL236161 Ki = 5.0 nM 8.30
CHEMBL223228 EFAVIRENZ Ki = 30.0 nM 7.52
CHEMBL396816 Ki = 30.0 nM 7.52
CHEMBL239281 Ki = 40.0 nM 7.40
CHEMBL239338 Ki = 40.0 nM 7.40
CHEMBL239337 Ki = 40.0 nM 7.40
CHEMBL238907 Ki = 50.0 nM 7.30
CHEMBL238701 Ki = 50.0 nM 7.30
CHEMBL399016 Ki = 50.0 nM 7.30
CHEMBL239064 Ki = 60.0 nM 7.22
CHEMBL239342 Ki = 70.0 nM 7.16
CHEMBL391164 Ki = 80.0 nM 7.10
CHEMBL240386 Ki = 100.0 nM 7.00
CHEMBL393696 Ki = 100.0 nM 7.00
CHEMBL394990 Ki = 100.0 nM 7.00
CHEMBL239717 Ki = 100.0 nM 7.00
CHEMBL239120 Ki = 150.0 nM 6.82
CHEMBL240770 Ki = 200.0 nM 6.70
CHEMBL239126 Ki = 250.0 nM 6.60
CHEMBL57 NEVIRAPINE Ki = 400.0 nM 6.40
CHEMBL240769 Ki = 700.0 nM 6.16
CHEMBL238702 Ki = 1000.0 nM 6.00
CHEMBL239122 Ki = 2000.0 nM 5.70
CHEMBL241666 Ki = 2500.0 nM 5.60
CHEMBL240147 Ki = 11230.0 nM 4.95