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Assay Detail

CHEMBL5341334

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

Functional
Antiviral activity against HIV1 harboring A17 mutant infected in human TZM-bl cells
18
Total Activities
17
Compounds Tested
3
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 11 7.27 9.16
IC50 4 8.54 9.10
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397495 2 9.16
CHEMBL175691 RILPIVIRINE 4.0 1 9.10
CHEMBL5395699 1 8.89
CHEMBL223228 EFAVIRENZ 4.0 1 7.75
CHEMBL5439006 1 7.61
CHEMBL5417242 1 7.40
CHEMBL5412528 1 7.26
CHEMBL5439895 1 6.82
CHEMBL5430523 1 6.76
CHEMBL5424813 1 6.51
CHEMBL5426382 1 6.15
CHEMBL5432903 1 -
CHEMBL5408046 1 -
CHEMBL5407783 1 -
CHEMBL5402762 1 -
CHEMBL5432006 1 -
CHEMBL5411690 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397495 EC50 = 0.689 nM 9.16
CHEMBL175691 RILPIVIRINE IC50 = 0.8 nM 9.10
CHEMBL5395699 IC50 = 1.3 nM 8.89
CHEMBL5397495 IC50 = 1.3 nM 8.89
CHEMBL223228 EFAVIRENZ EC50 = 18.0 nM 7.75
CHEMBL5439006 EC50 = 24.5 nM 7.61
CHEMBL5417242 EC50 = 39.6 nM 7.40
CHEMBL5412528 IC50 = 55.0 nM 7.26
CHEMBL5439895 EC50 = 153.0 nM 6.82
CHEMBL5430523 EC50 = 175.0 nM 6.76
CHEMBL5424813 EC50 = 306.0 nM 6.51
CHEMBL5426382 EC50 = 705.0 nM 6.15
CHEMBL5402762 Activity - -
CHEMBL5408046 Activity - -
CHEMBL5407783 Activity - -
CHEMBL5432903 EC50 > 1000.0 nM -
CHEMBL5432006 EC50 > 1000.0 nM -
CHEMBL5411690 EC50 > 1000.0 nM -