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Assay Detail

CHEMBL5548162

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

Functional
Antiviral activity against NNRTI-resistant HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect 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
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Discovery of Novel Aryl Triazolone Dihydropyridines (ATDPs) Targeting Highly Conserved Residue W229 as Promising HIV-1 NNRTIs.
Sun Y, Zhou Z, Wang N, Zhao F, Liu Y, Xu X, Wang X, Gou Z, De Clercq E, Pannecouque C, Zhan P, Kang D, Liu X.
J Med Chem (2024) 67 : 6570 -6584
PubMed 38613773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 4.56 4.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5564750 1 4.78
CHEMBL5575003 1 4.75
CHEMBL5593560 1 4.64
CHEMBL5573421 1 4.60
CHEMBL5573653 1 4.59
CHEMBL5575200 1 4.57
CHEMBL5571067 1 4.54
CHEMBL5563055 1 4.38
CHEMBL2364608 DORAVIRINE 4.0 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5564750 EC50 = 16500.0 nM 4.78
CHEMBL5575003 EC50 = 17700.0 nM 4.75
CHEMBL5593560 EC50 = 22900.0 nM 4.64
CHEMBL5573421 EC50 = 24900.0 nM 4.60
CHEMBL5573653 EC50 = 25800.0 nM 4.59
CHEMBL5575200 EC50 = 26900.0 nM 4.57
CHEMBL5571067 EC50 = 29200.0 nM 4.54
CHEMBL5563055 EC50 = 41800.0 nM 4.38
CHEMBL2364608 DORAVIRINE EC50 = 67800.0 nM 4.17