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Assay Detail

CHEMBL699300

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

Binding
Inhibitory activity against Integrase in 3'-end- processing
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

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 9 5.75 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL37869 1 6.52
CHEMBL36640 1 6.16
CHEMBL289303 1 5.64
CHEMBL39092 1 5.62
CHEMBL39958 1 5.50
CHEMBL36586 1 5.43
CHEMBL37845 1 5.40
CHEMBL39725 1 -
CHEMBL36585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL37869 IC50 = 300.0 nM 6.52
CHEMBL36640 IC50 = 700.0 nM 6.16
CHEMBL289303 IC50 = 2300.0 nM 5.64
CHEMBL39092 IC50 = 2400.0 nM 5.62
CHEMBL39958 IC50 = 3200.0 nM 5.50
CHEMBL36586 IC50 = 3700.0 nM 5.43
CHEMBL37845 IC50 = 4000.0 nM 5.40
CHEMBL39725 IC50 > 100000.0 nM -
CHEMBL36585 IC50 > 100000.0 nM -