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Assay Detail

CHEMBL4724691

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

Functional
Potentiation of vorinostat-induced reactivation of latent HIV-1 infected in human Jurkat 2C4 cells assessed as increase in HIV-1 transcription incubated for 24 hrs in presence of vorinostat by Steady-Glo luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type 2C4
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.
Bukhtiyarova M,Cook EM,Hancock PJ,Hruza AW,Shaw AW,Adam GC,Barnard RJO,McKenna PM,Holloway MK,Bell IM,Carroll S,Cornella-Taracido I,Cox CD,Kutchukian PS,Powell DA,Strickland C,Trotter BW,Tudor M,Wolkenberg S,Li J,Tellers DM
ACS Med Chem Lett (2021) 12 : 99 -106
PubMed 33488970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.40 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279433 L-778123 FREE BASE 1.0 1 6.77
CHEMBL4758112 1 6.47
CHEMBL4781419 1 5.96
CHEMBL4759194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279433 L-778123 FREE BASE EC50 = 170.0 nM 6.77
CHEMBL4758112 EC50 = 340.0 nM 6.47
CHEMBL4781419 EC50 = 1100.0 nM 5.96
CHEMBL4759194 EC50 > 8000.0 nM -