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Assay Detail

CHEMBL4767756

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

Functional
Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infection by luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type HEK293T
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Discovery, synthesis, and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root.
Xu C,Xin Y,Chen M,Ba M,Guo Q,Zhu C,Guo Y,Shi J
Eur J Med Chem (2020) 189 : 112071 -112071
PubMed 32004936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.62 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 8.70
CHEMBL4786649 1 7.40
CHEMBL4789248 1 6.75
CHEMBL4777503 1 5.67
CHEMBL4792750 1 5.62
CHEMBL57 NEVIRAPINE 4.0 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ EC50 = 2.0 nM 8.70
CHEMBL4786649 EC50 = 40.0 nM 7.40
CHEMBL4789248 EC50 = 180.0 nM 6.75
CHEMBL4777503 EC50 = 2130.0 nM 5.67
CHEMBL4792750 EC50 = 2410.0 nM 5.62
CHEMBL57 NEVIRAPINE EC50 = 2580.0 nM 5.59