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Assay Detail

CHEMBL699301

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Binding
Inhibitory activity against HIV-1 integrase.
26
Total Activities
13
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

6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays.
Costi R, Di Santo R, Artico M, Roux A, Ragno R, Massa S, Tramontano E, La Colla M, Loddo R, Marongiu ME, Pani A, La Colla P.
Bioorg Med Chem Lett (2004) 14 : 1745 -1749
PubMed 15026063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 4.51 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50605 2 6.52
CHEMBL49201 2 5.16
CHEMBL48381 2 5.12
CHEMBL46032 2 4.66
CHEMBL49473 2 4.42
CHEMBL49387 2 4.35
CHEMBL417356 2 4.30
CHEMBL299873 2 4.30
CHEMBL49363 2 4.25
CHEMBL48573 2 4.21
CHEMBL301161 2 4.14
CHEMBL301183 2 4.12
CHEMBL45578 2 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50605 IC50 = 300.0 nM 6.52
CHEMBL50605 IC50 = 2000.0 nM 5.70
CHEMBL49201 IC50 = 7000.0 nM 5.16
CHEMBL48381 IC50 = 7500.0 nM 5.12
CHEMBL49201 IC50 = 7900.0 nM 5.10
CHEMBL48381 IC50 = 8900.0 nM 5.05
CHEMBL46032 IC50 = 22000.0 nM 4.66
CHEMBL49473 IC50 = 38000.0 nM 4.42
CHEMBL46032 IC50 = 41000.0 nM 4.39
CHEMBL49387 IC50 = 45000.0 nM 4.35
CHEMBL49473 IC50 = 50000.0 nM 4.30
CHEMBL417356 IC50 = 50000.0 nM 4.30
CHEMBL299873 IC50 = 50000.0 nM 4.30
CHEMBL49363 IC50 = 56000.0 nM 4.25
CHEMBL49387 IC50 = 57000.0 nM 4.24
CHEMBL48573 IC50 = 61000.0 nM 4.21
CHEMBL417356 IC50 = 65000.0 nM 4.19
CHEMBL299873 IC50 = 65000.0 nM 4.19
CHEMBL49363 IC50 = 67000.0 nM 4.17
CHEMBL48573 IC50 = 72000.0 nM 4.14
CHEMBL301161 IC50 = 73000.0 nM 4.14
CHEMBL301183 IC50 = 76000.0 nM 4.12
CHEMBL301161 IC50 = 88000.0 nM 4.06
CHEMBL45578 IC50 = 87000.0 nM 4.06
CHEMBL301183 IC50 = 92000.0 nM 4.04
CHEMBL45578 IC50 = 95000.0 nM 4.02