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Assay Detail

CHEMBL4222273

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Huang B, Liu X, Tian Y, Kang D, Zhou Z, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem Lett (2018) 28 : 1348 -1351
PubMed 29534929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.98 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236715 1 8.54
CHEMBL308954 ETRAVIRINE 4.0 1 8.41
CHEMBL223228 EFAVIRENZ 4.0 1 8.32
CHEMBL4225783 1 8.26
CHEMBL57 NEVIRAPINE 4.0 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236715 EC50 = 2.9 nM 8.54
CHEMBL308954 ETRAVIRINE EC50 = 3.9 nM 8.41
CHEMBL223228 EFAVIRENZ EC50 = 4.8 nM 8.32
CHEMBL4225783 EC50 = 5.5 nM 8.26
CHEMBL57 NEVIRAPINE EC50 = 440.0 nM 6.36