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Assay Detail

CHEMBL1693648

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

Functional
Antiviral activity against HIV1 NL4-3.Luc in human PBMC assessed as infectivity treated for 24 hrs by luciferase assay
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
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 4 8.22 9.52
EC95 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 2 9.52
CHEMBL254316 RALTEGRAVIR 4.0 2 8.62
CHEMBL57 NEVIRAPINE 4.0 2 7.39
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE 4.0 2 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR EC50 = 0.3 nM 9.52
CHEMBL254316 RALTEGRAVIR EC50 = 2.4 nM 8.62
CHEMBL57 NEVIRAPINE EC50 = 41.0 nM 7.39
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE EC50 = 46.0 nM 7.34
CHEMBL254316 RALTEGRAVIR EC95 = 0.048 uM -
CHEMBL204656 ELVITEGRAVIR EC95 = 0.0074 uM -
CHEMBL1486 TENOFOVIR DISOPROXIL FUMARATE EC95 = 0.72 uM -
CHEMBL57 NEVIRAPINE EC95 = 0.69 uM -