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Assay Detail

CHEMBL931815

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Binding
Inhibition of wild type HIV 3B reverse transcriptase in MT2 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Cell Type MT2
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 anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.
Boojamra CG, Mackman RL, Markevitch DY, Prasad V, Ray AS, Douglas J, Grant D, Kim CU, Cihlar T.
Bioorg Med Chem Lett (2008) 18 : 1120 -1123
PubMed 18164198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.41 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 7.30
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 6.42
CHEMBL271681 1 6.40
CHEMBL420843 1 6.22
CHEMBL252036 GS-9148 -1.0 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE IC50 = 50.0 nM 7.30
CHEMBL483 TENOFOVIR ANHYDROUS IC50 = 380.0 nM 6.42
CHEMBL271681 IC50 = 400.0 nM 6.40
CHEMBL420843 IC50 = 600.0 nM 6.22
CHEMBL252036 GS-9148 IC50 = 1900.0 nM 5.72