Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL900568

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

Binding
Inhibition of HIV1 reverse transcriptase L100I mutant
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 5.44 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396816 1 6.75
CHEMBL236161 1 6.52
CHEMBL239281 1 6.51
CHEMBL238701 1 6.05
CHEMBL240386 1 6.00
CHEMBL239342 1 5.70
CHEMBL239337 1 5.60
CHEMBL393696 1 5.48
CHEMBL238907 1 5.40
CHEMBL239064 1 5.30
CHEMBL239120 1 5.30
CHEMBL57 NEVIRAPINE 4.0 1 5.05
CHEMBL240770 1 5.00
CHEMBL391164 1 5.00
CHEMBL239063 1 5.00
CHEMBL239338 1 5.00
CHEMBL239126 1 5.00
CHEMBL239717 1 5.00
CHEMBL241666 1 5.00
CHEMBL240769 1 4.82
CHEMBL394990 1 4.75
CHEMBL399016 1 -
CHEMBL239122 1 -
CHEMBL238702 1 -
CHEMBL240147 1 -
CHEMBL223228 EFAVIRENZ 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396816 Ki = 180.0 nM 6.75
CHEMBL236161 Ki = 300.0 nM 6.52
CHEMBL239281 Ki = 310.0 nM 6.51
CHEMBL238701 Ki = 900.0 nM 6.05
CHEMBL240386 Ki = 1000.0 nM 6.00
CHEMBL239342 Ki = 2000.0 nM 5.70
CHEMBL239337 Ki = 2500.0 nM 5.60
CHEMBL393696 Ki = 3300.0 nM 5.48
CHEMBL238907 Ki = 4000.0 nM 5.40
CHEMBL239064 Ki = 5000.0 nM 5.30
CHEMBL239120 Ki = 5000.0 nM 5.30
CHEMBL57 NEVIRAPINE Ki = 9000.0 nM 5.05
CHEMBL240770 Ki = 10000.0 nM 5.00
CHEMBL391164 Ki = 10000.0 nM 5.00
CHEMBL239063 Ki = 10000.0 nM 5.00
CHEMBL239338 Ki = 10000.0 nM 5.00
CHEMBL239126 Ki = 10000.0 nM 5.00
CHEMBL239717 Ki = 10000.0 nM 5.00
CHEMBL241666 Ki = 10000.0 nM 5.00
CHEMBL240769 Ki = 15000.0 nM 4.82
CHEMBL394990 Ki = 18000.0 nM 4.75
CHEMBL399016 Ki > 20000.0 nM -
CHEMBL239122 Ki - -
CHEMBL238702 Ki > 20000.0 nM -
CHEMBL240147 Ki > 20000.0 nM -
CHEMBL223228 EFAVIRENZ Ki - -