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Assay Detail

CHEMBL699441

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

Binding
In vitro inhibition of recombinant integrase activity in a standard 3'-processing assay.
20
Total Activities
20
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

Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.
Bénard C, Zouhiri F, Normand-Bayle M, Danet M, Desmaële D, Leh H, Mouscadet JF, Mbemba G, Thomas CM, Bonnenfant S, Le Bret M, d'Angelo J.
Bioorg Med Chem Lett (2004) 14 : 2473 -2476
PubMed 15109635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.46 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36640 1 6.16
CHEMBL312608 1 6.05
CHEMBL82986 1 5.82
CHEMBL289303 1 5.64
CHEMBL39092 1 5.62
CHEMBL310321 1 5.52
CHEMBL39958 1 5.50
CHEMBL82633 1 5.30
CHEMBL81182 1 5.30
CHEMBL81714 1 5.30
CHEMBL40148 1 5.28
CHEMBL80008 1 5.19
CHEMBL83746 1 5.19
CHEMBL420026 1 4.52
CHEMBL309885 1 -
CHEMBL81284 1 -
CHEMBL82359 1 -
CHEMBL83419 1 -
CHEMBL82029 1 -
CHEMBL81686 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36640 IC50 = 700.0 nM 6.16
CHEMBL312608 IC50 = 900.0 nM 6.05
CHEMBL82986 IC50 = 1500.0 nM 5.82
CHEMBL289303 IC50 = 2300.0 nM 5.64
CHEMBL39092 IC50 = 2400.0 nM 5.62
CHEMBL310321 IC50 = 3000.0 nM 5.52
CHEMBL39958 IC50 = 3200.0 nM 5.50
CHEMBL82633 IC50 = 5000.0 nM 5.30
CHEMBL81182 IC50 = 5000.0 nM 5.30
CHEMBL81714 IC50 = 5000.0 nM 5.30
CHEMBL40148 IC50 = 5300.0 nM 5.28
CHEMBL80008 IC50 = 6500.0 nM 5.19
CHEMBL83746 IC50 = 6500.0 nM 5.19
CHEMBL420026 IC50 = 30000.0 nM 4.52
CHEMBL309885 IC50 > 100000.0 nM -
CHEMBL81284 IC50 > 100000.0 nM -
CHEMBL82359 IC50 > 100000.0 nM -
CHEMBL83419 IC50 > 100000.0 nM -
CHEMBL82029 IC50 > 100000.0 nM -
CHEMBL81686 IC50 > 100000.0 nM -