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Assay Detail

CHEMBL701281

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Binding
Inhibitory activity against HIV-1 Integrase in 3'-end- processing
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture.
Zouhiri F, Mouscadet JF, Mekouar K, Desmaële D, Savouré D, Leh H, Subra F, Le Bret M, Auclair C, d'Angelo J.
J Med Chem (2000) 43 : 1533 -1540
PubMed 10780910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.63 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL37139 1 6.05
CHEMBL431508 1 5.92
CHEMBL39301 1 5.89
CHEMBL39481 1 5.85
CHEMBL418613 1 5.80
CHEMBL40170 1 5.55
CHEMBL287903 1 5.47
CHEMBL39883 1 5.46
CHEMBL39143 1 5.39
CHEMBL37431 1 5.31
CHEMBL40148 1 5.28
CHEMBL39823 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL37139 IC50 = 900.0 nM 6.05
CHEMBL431508 IC50 = 1200.0 nM 5.92
CHEMBL39301 IC50 = 1300.0 nM 5.89
CHEMBL39481 IC50 = 1400.0 nM 5.85
CHEMBL418613 IC50 = 1600.0 nM 5.80
CHEMBL40170 IC50 = 2800.0 nM 5.55
CHEMBL287903 IC50 = 3400.0 nM 5.47
CHEMBL39883 IC50 = 3500.0 nM 5.46
CHEMBL39143 IC50 = 4100.0 nM 5.39
CHEMBL37431 IC50 = 4900.0 nM 5.31
CHEMBL40148 IC50 = 5300.0 nM 5.28
CHEMBL39823 IC50 > 100000.0 nM -