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Assay Detail

CHEMBL1020342

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

Binding
Binding affinity to HIV1 wild type reverse transcriptase p66/p51 expressed in Escherichia coli assessed as incorporation of drug to DNA by gel electrophoresis
5
Total Activities
5
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

In vitro suppression of K65R reverse transcriptase-mediated tenofovir- and adefovir-5'-diphosphate resistance conferred by the boranophosphonate derivatives.
Frangeul A, Barral K, Alvarez K, Canard B.
Antimicrob Agents Chemother (2007) 51 : 3162 -3167
PubMed 17620380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 4.91 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2448397 1 5.19
CHEMBL335538 1 5.12
CHEMBL1162433 ADEFOVIR DIPHOSPHATE -1.0 1 5.10
CHEMBL1236349 1 4.64
CHEMBL2448398 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2448397 Kd = 6500.0 nM 5.19
CHEMBL335538 Kd = 7500.0 nM 5.12
CHEMBL1162433 ADEFOVIR DIPHOSPHATE Kd = 7900.0 nM 5.10
CHEMBL1236349 Kd = 23000.0 nM 4.64
CHEMBL2448398 Kd = 33000.0 nM 4.48