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Assay Detail

CHEMBL890163

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Binding
Inhibition of HIV1 recombinant 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 and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems.
Sakamoto T, Cullen MD, Hartman TL, Watson KM, Buckheit RW, Pannecouque C, De Clercq E, Cushman M.
J Med Chem (2007) 50 : 3314 -3321
PubMed 17579385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.40 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226735 1 7.70
CHEMBL389466 1 6.26
CHEMBL389237 1 6.22
CHEMBL226787 1 6.17
CHEMBL226786 1 6.07
CHEMBL428685 1 6.00
CHEMBL267920 1 -
CHEMBL226788 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226735 IC50 = 20.0 nM 7.70
CHEMBL389466 IC50 = 550.0 nM 6.26
CHEMBL389237 IC50 = 600.0 nM 6.22
CHEMBL226787 IC50 = 670.0 nM 6.17
CHEMBL226786 IC50 = 850.0 nM 6.07
CHEMBL428685 IC50 = 1000.0 nM 6.00
CHEMBL267920 IC50 > 100000.0 nM -
CHEMBL226788 IC50 > 100000.0 nM -