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Assay Detail

CHEMBL701716

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Binding
Inhibitory effect on strand transfer of proximal DNA into host DNA in an extracellular HIV-1 integrase assay in experiment 1
4
Total Activities
4
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 of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors.
Pais GC, Zhang X, Marchand C, Neamati N, Cowansage K, Svarovskaia ES, Pathak VK, Tang Y, Nicklaus M, Pommier Y, Burke TR.
J Med Chem (2002) 45 : 3184 -3194
PubMed 12109903 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.29 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3348565 1 5.72
CHEMBL22197 1 5.70
CHEMBL108423 1 5.11
CHEMBL16326 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3348565 IC50 = 1900.0 nM 5.72
CHEMBL22197 IC50 = 2000.0 nM 5.70
CHEMBL108423 IC50 = 7800.0 nM 5.11
CHEMBL16326 IC50 = 24200.0 nM 4.62