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Assay Detail

CHEMBL702097

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

Binding
HIV integrase inhibitory potency was evaluated as IC50 on 3' processing of target DNA.
19
Total Activities
19
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

Styrylquinoline derivatives: a new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells.
Mekouar K, Mouscadet JF, Desmaële D, Subra F, Leh H, Savouré D, Auclair C, d'Angelo J.
J Med Chem (1998) 41 : 2846 -2857
PubMed 9667973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.79 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329488 1 6.58
CHEMBL37869 1 6.52
CHEMBL100082 1 6.10
CHEMBL97641 1 5.66
CHEMBL39092 1 5.62
CHEMBL59548 1 5.57
CHEMBL59446 1 5.52
CHEMBL36586 1 5.43
CHEMBL58057 1 5.13
CHEMBL58923 1 -
CHEMBL97679 1 -
CHEMBL58191 1 -
CHEMBL432775 1 -
CHEMBL61800 1 -
CHEMBL96959 1 -
CHEMBL418303 1 -
CHEMBL293788 1 -
CHEMBL61203 1 -
CHEMBL39823 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329488 IC50 = 260.0 nM 6.58
CHEMBL37869 IC50 = 300.0 nM 6.52
CHEMBL100082 IC50 = 800.0 nM 6.10
CHEMBL97641 IC50 = 2200.0 nM 5.66
CHEMBL39092 IC50 = 2400.0 nM 5.62
CHEMBL59548 IC50 = 2700.0 nM 5.57
CHEMBL59446 IC50 = 3000.0 nM 5.52
CHEMBL36586 IC50 = 3700.0 nM 5.43
CHEMBL58057 IC50 = 7400.0 nM 5.13
CHEMBL58923 IC50 > 100000.0 nM -
CHEMBL97679 IC50 > 100000.0 nM -
CHEMBL58191 IC50 > 100000.0 nM -
CHEMBL432775 IC50 > 100000.0 nM -
CHEMBL61800 IC50 > 100000.0 nM -
CHEMBL96959 IC50 > 100000.0 nM -
CHEMBL418303 IC50 > 100000.0 nM -
CHEMBL293788 IC50 > 100000.0 nM -
CHEMBL61203 IC50 > 100000.0 nM -
CHEMBL39823 IC50 > 100000.0 nM -