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Assay Detail

CHEMBL1693641

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

Functional
Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to virus immediately after 3 times compound washout
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type HeLaT4
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
Koh Y, Haim H, Engelman A.
Antimicrob Agents Chemother (2011) 55 : 42 -49
PubMed 21060108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.21 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 7.22
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE 4.0 1 6.92
CHEMBL254316 RALTEGRAVIR 4.0 1 5.34
CHEMBL129 ZIDOVUDINE 4.0 1 5.34
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR EC50 = 60.0 nM 7.22
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE EC50 = 120.0 nM 6.92
CHEMBL254316 RALTEGRAVIR EC50 = 4600.0 nM 5.34
CHEMBL129 ZIDOVUDINE EC50 = 4600.0 nM 5.34
CHEMBL57 NEVIRAPINE EC50 > 100000.0 nM -