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Assay Detail

CHEMBL925064

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Binding
Inhibition of HIV1 integrase strand transfer activity
9
Total Activities
9
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 Autocuration

Target

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

Publication

Development of integrase inhibitors for treatment of AIDS: an overview.
Dubey S, Satyanarayana YD, Lavania H.
Eur J Med Chem (2007) 42 : 1159 -1168
PubMed 17367896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.77 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 8.14
CHEMBL252700 1 5.75
CHEMBL252905 1 5.68
CHEMBL254727 1 5.58
CHEMBL404423 1 5.47
CHEMBL19977 1 5.46
CHEMBL49201 1 5.10
CHEMBL254527 1 5.00
CHEMBL32865 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR IC50 = 7.2 nM 8.14
CHEMBL252700 IC50 = 1800.0 nM 5.75
CHEMBL252905 IC50 = 2100.0 nM 5.68
CHEMBL254727 IC50 = 2600.0 nM 5.58
CHEMBL404423 IC50 = 3400.0 nM 5.47
CHEMBL19977 IC50 = 3500.0 nM 5.46
CHEMBL49201 IC50 = 7900.0 nM 5.10
CHEMBL254527 IC50 = 10000.0 nM 5.00
CHEMBL32865 IC50 = 10000.0 nM -