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Assay Detail

CHEMBL863032

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Binding
Inhibition of HIV integrase
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Triketoacid inhibitors of HIV-integrase: a new chemotype useful for probing the integrase pharmacophore.
Walker MA, Johnson T, Ma Z, Banville J, Remillard R, Kim O, Zhang Y, Staab A, Wong H, Torri A, Samanta H, Lin Z, Deminie C, Terry B, Krystal M, Meanwell N.
Bioorg Med Chem Lett (2006) 16 : 2920 -2924
PubMed 16546383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.38 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL211028 1 8.00
CHEMBL50605 1 7.70
CHEMBL108760 1 7.10
CHEMBL211014 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL211028 IC50 = 10.0 nM 8.00
CHEMBL50605 IC50 = 20.0 nM 7.70
CHEMBL108760 IC50 = 80.0 nM 7.10
CHEMBL211014 IC50 = 200.0 nM 6.70