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Assay Detail

CHEMBL3362706

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Binding
Inhibition of wild type HIV1 reverse transcriptase assessed as inhibition of DNA primer extension using [8-3H(N)]-dATP by scintillation proximity assay
14
Total Activities
14
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

Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase.
Lacbay CM, Mancuso J, Lin YS, Bennett N, Götte M, Tsantrizos YS.
J Med Chem (2014) 57 : 7435 -7449
PubMed 25144111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.34 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3327156 1 5.96
CHEMBL3327148 1 5.82
CHEMBL3327153 1 5.75
CHEMBL3327158 1 5.62
CHEMBL666 FOSCARNET 4.0 1 5.60
CHEMBL3327159 1 5.15
CHEMBL3327160 1 5.08
CHEMBL3327155 1 5.05
CHEMBL3327152 1 5.00
CHEMBL3357472 1 4.98
CHEMBL3327157 1 4.70
CHEMBL3327154 1 -
CHEMBL3327150 1 -
CHEMBL3327149 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3327156 IC50 = 1100.0 nM 5.96
CHEMBL3327148 IC50 = 1500.0 nM 5.82
CHEMBL3327153 IC50 = 1800.0 nM 5.75
CHEMBL3327158 IC50 = 2400.0 nM 5.62
CHEMBL666 FOSCARNET IC50 = 2500.0 nM 5.60
CHEMBL3327159 IC50 = 7100.0 nM 5.15
CHEMBL3327160 IC50 = 8300.0 nM 5.08
CHEMBL3327155 IC50 = 9000.0 nM 5.05
CHEMBL3327152 IC50 = 10000.0 nM 5.00
CHEMBL3357472 IC50 = 10400.0 nM 4.98
CHEMBL3327157 IC50 = 20000.0 nM 4.70
CHEMBL3327154 IC50 > 50000.0 nM -
CHEMBL3327150 IC50 > 50000.0 nM -
CHEMBL3327149 IC50 > 50000.0 nM -