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Assay Detail

CHEMBL4222279

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

Binding
Inhibition of recombinant wild-type HIV1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis
2
Total Activities
2
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 Intermediate

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Huang B, Liu X, Tian Y, Kang D, Zhou Z, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem Lett (2018) 28 : 1348 -1351
PubMed 29534929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.19 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236715 1 7.80
CHEMBL4225783 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236715 IC50 = 16.0 nM 7.80
CHEMBL4225783 IC50 = 264.0 nM 6.58