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Assay Detail

CHEMBL5341333

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

Functional
Antiviral activity against wild type HIV1 IIIB infected in human TZM-bl cells
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type TZM-bl
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

<i>N</i>-Phenyl-1-(phenylsulfonyl)-1<i>H</i>-1,2,4-triazol-3-amine as a New Class of HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor.
Lane T, Makarov V, Nelson JAE, Meeker RB, Sanna G, Riabova O, Kazakova E, Monakhova N, Tsedilin A, Urbina F, Jones T, Suchy A, Ekins S.
J Med Chem (2023) 66 : 6193 -6217
PubMed 37130343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.93 9.66
IC50 3 9.58 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5439006 1 9.66
CHEMBL5412528 1 9.64
CHEMBL5397495 1 9.62
CHEMBL5395699 1 9.58
CHEMBL175691 RILPIVIRINE 4.0 1 9.48
CHEMBL5417242 1 9.38
CHEMBL5439895 1 9.22
CHEMBL223228 EFAVIRENZ 4.0 1 9.17
CHEMBL5424813 1 9.06
CHEMBL5430523 1 9.01
CHEMBL5426382 1 8.75
CHEMBL5432903 1 7.97
CHEMBL5432006 1 7.50
CHEMBL5408046 1 -
CHEMBL5407783 1 -
CHEMBL5402762 1 -
CHEMBL5411690 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5439006 EC50 = 0.22 nM 9.66
CHEMBL5412528 IC50 = 0.23 nM 9.64
CHEMBL5397495 IC50 = 0.24 nM 9.62
CHEMBL5395699 EC50 = 0.263 nM 9.58
CHEMBL175691 RILPIVIRINE IC50 = 0.33 nM 9.48
CHEMBL5417242 EC50 = 0.42 nM 9.38
CHEMBL5439895 EC50 = 0.598 nM 9.22
CHEMBL223228 EFAVIRENZ EC50 = 0.68 nM 9.17
CHEMBL5424813 EC50 = 0.879 nM 9.06
CHEMBL5430523 EC50 = 0.98 nM 9.01
CHEMBL5426382 EC50 = 1.77 nM 8.75
CHEMBL5432903 EC50 = 10.6 nM 7.97
CHEMBL5432006 EC50 = 32.0 nM 7.50
CHEMBL5408046 EC50 < 100.0 nM -
CHEMBL5407783 EC50 < 100.0 nM -
CHEMBL5402762 EC50 < 100.0 nM -
CHEMBL5411690 EC50 > 1000.0 nM -