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Assay Detail

CHEMBL3788090

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Binding
Inhibition of wild type HIV1 Reverse transcriptase assessed as reduction of biotin deoxyuridine triphosphate incorporation into the wild type HIV1 reverse transcriptase after 1 hr by ELISA
3
Total Activities
3
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

Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
Meng Q, Chen X, Kang D, Huang B, Li W, Zhan P, Daelemans D, De Clercq E, Pannecouque C, Liu X.
Eur J Med Chem (2016) 115 : 53 -62
PubMed 26994843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.90 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786091 1 7.14
CHEMBL308954 ETRAVIRINE 4.0 1 5.51
CHEMBL57 NEVIRAPINE 4.0 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786091 IC50 = 72.7 nM 7.14
CHEMBL308954 ETRAVIRINE IC50 = 3100.0 nM 5.51
CHEMBL57 NEVIRAPINE IC50 = 8800.0 nM 5.06