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Assay Detail

CHEMBL998726

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Binding
Inhibition of HIV1 integrase 3'-processing 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

Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors.
Pasquini S, Mugnaini C, Tintori C, Botta M, Trejos A, Arvela RK, Larhed M, Witvrouw M, Michiels M, Christ F, Debyser Z, Corelli F.
J Med Chem (2008) 51 : 5125 -5129
PubMed 18665580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.04 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 7.30
CHEMBL522229 1 4.78
CHEMBL458483 1 -
CHEMBL497489 1 -
CHEMBL526269 1 -
CHEMBL498491 1 -
CHEMBL496491 1 -
CHEMBL496476 1 -
CHEMBL497506 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR IC50 = 50.0 nM 7.30
CHEMBL522229 IC50 = 16600.0 nM 4.78
CHEMBL458483 IC50 > 100000.0 nM -
CHEMBL497489 IC50 > 100000.0 nM -
CHEMBL526269 IC50 > 100000.0 nM -
CHEMBL498491 IC50 > 100000.0 nM -
CHEMBL496491 IC50 > 100000.0 nM -
CHEMBL496476 IC50 > 100000.0 nM -
CHEMBL497506 IC50 > 100000.0 nM -