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Assay Detail

CHEMBL4359408

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

Functional
Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in absence of test compound assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.
Kang D, Feng D, Sun Y, Fang Z, Wei F, De Clercq E, Pannecouque C, Liu X, Zhan P.
J Med Chem (2020) 63 : 4837 -4848
PubMed 32293182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.08 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 9.05
CHEMBL3929927 1 8.96
CHEMBL223228 EFAVIRENZ 4.0 1 8.80
CHEMBL308954 ETRAVIRINE 4.0 1 8.57
CHEMBL4094163 1 8.57
CHEMBL4526732 1 8.39
CHEMBL129 ZIDOVUDINE 4.0 1 7.90
CHEMBL57 NEVIRAPINE 4.0 1 7.06
CHEMBL483 TENOFOVIR ANHYDROUS 3.0 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE EC50 = 0.9 nM 9.05
CHEMBL3929927 EC50 = 1.1 nM 8.96
CHEMBL223228 EFAVIRENZ EC50 = 1.6 nM 8.80
CHEMBL308954 ETRAVIRINE EC50 = 2.7 nM 8.57
CHEMBL4094163 EC50 = 2.7 nM 8.57
CHEMBL4526732 EC50 = 4.1 nM 8.39
CHEMBL129 ZIDOVUDINE EC50 = 12.7 nM 7.90
CHEMBL57 NEVIRAPINE EC50 = 87.9 nM 7.06
CHEMBL483 TENOFOVIR ANHYDROUS EC50 = 4140.0 nM 5.38