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Assay Detail

CHEMBL1960054

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Binding
Inhibition of HIV1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rA)-oligo(dT)
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

Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
Chen X, Zhan P, Pannecouque C, Balzarini J, De Clercq E, Liu X.
Eur J Med Chem (2012) 51 : 60 -66
PubMed 22405288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.78 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308954 ETRAVIRINE 4.0 1 6.26
CHEMBL1957900 1 5.75
CHEMBL1957773 1 5.71
CHEMBL1957769 1 5.61
CHEMBL57 NEVIRAPINE 4.0 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308954 ETRAVIRINE IC50 = 550.0 nM 6.26
CHEMBL1957900 IC50 = 1770.0 nM 5.75
CHEMBL1957773 IC50 = 1970.0 nM 5.71
CHEMBL1957769 IC50 = 2460.0 nM 5.61
CHEMBL57 NEVIRAPINE IC50 = 2740.0 nM 5.56