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Assay Detail

CHEMBL903666

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

Functional
Antiviral activity against HIV1 LAI replication in human PBMC after 5 days
11
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

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

Publication

Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.
Patil S, Kamath S, Sanchez T, Neamati N, Schinazi RF, Buolamwini JK.
Bioorg Med Chem (2007) 15 : 1212 -1228
PubMed 17158051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.73 9.14
EC90 5 - -
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 2 9.14
CHEMBL226485 2 5.10
CHEMBL375484 2 4.58
CHEMBL389930 2 4.08
CHEMBL226490 2 -
CHEMBL19977 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 0.73 nM 9.14
CHEMBL226485 EC50 = 8000.0 nM 5.10
CHEMBL375484 EC50 = 26600.0 nM 4.58
CHEMBL389930 EC50 = 83700.0 nM 4.08
CHEMBL129 ZIDOVUDINE EC90 = 0.019 uM -
CHEMBL226490 EC50 > 100000.0 nM -
CHEMBL226490 EC90 > 100.0 uM -
CHEMBL389930 EC90 > 100.0 uM -
CHEMBL375484 EC90 > 100.0 uM -
CHEMBL226485 EC90 = 72.8 uM -
CHEMBL19977 Activity - -