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Assay Detail

CHEMBL906565

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Binding
Inhibition of HIV1 reverse transcriptase
8
Total Activities
8
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, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.
Mackman RL, Zhang L, Prasad V, Boojamra CG, Douglas J, Grant D, Hui H, Kim CU, Laflamme G, Parrish J, Stoycheva AD, Swaminathan S, Wang K, Cihlar T.
Bioorg Med Chem (2007) 15 : 5519 -5528
PubMed 17562366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.40 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 7.30
CHEMBL991 STAVUDINE 4.0 1 7.22
CHEMBL444314 1 6.92
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 6.42
CHEMBL485652 STAVUDINE TRIPHOSPHATE -1.0 1 6.41
CHEMBL122885 1 6.41
CHEMBL229284 1 5.27
CHEMBL229111 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE IC50 = 50.0 nM 7.30
CHEMBL991 STAVUDINE IC50 = 60.0 nM 7.22
CHEMBL444314 IC50 = 120.0 nM 6.92
CHEMBL483 TENOFOVIR ANHYDROUS IC50 = 380.0 nM 6.42
CHEMBL485652 STAVUDINE TRIPHOSPHATE IC50 = 390.0 nM 6.41
CHEMBL122885 IC50 = 390.0 nM 6.41
CHEMBL229284 IC50 = 5400.0 nM 5.27
CHEMBL229111 IC50 = 5400.0 nM 5.27