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Assay Detail

CHEMBL4813299

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Binding
Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into cDNA measured after 1 hr by ELISA
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

Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
Fu Z, Zhang T, Zhou Z, Kang D, Sun L, Gao S, Cherukupalli S, De Clercq E, Pannecouque C, Liu X, Zhan P.
Bioorg Med Chem (2021) 42 : 116239 -116239
PubMed 34090079 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.42 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308954 ETRAVIRINE 4.0 1 7.32
CHEMBL4870132 1 6.89
CHEMBL4857180 1 6.64
CHEMBL4865294 1 5.70
CHEMBL4875791 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308954 ETRAVIRINE IC50 = 48.0 nM 7.32
CHEMBL4870132 IC50 = 130.0 nM 6.89
CHEMBL4857180 IC50 = 230.0 nM 6.64
CHEMBL4865294 IC50 = 1980.0 nM 5.70
CHEMBL4875791 IC50 = 2980.0 nM 5.53