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Assay Detail

CHEMBL2411985

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of 3'-processing activity of HIV1 integrase using 32P-5'-TGTGGAAAATCTCTAGCAGT-3' and 5'-ACTGCTAGAGATTTTCCACA-3' as substrate after 1 hr by ELISA
4
Total Activities
4
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

4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.
Billamboz M, Suchaud V, Bailly F, Lion C, Demeulemeester J, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.
ACS Med Chem Lett (2013) 4 : 606 -611
PubMed 24900718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.18 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2407287 1 7.22
CHEMBL254316 RALTEGRAVIR 4.0 1 6.05
CHEMBL2407277 1 5.80
CHEMBL2407284 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2407287 IC50 = 60.0 nM 7.22
CHEMBL254316 RALTEGRAVIR IC50 = 900.0 nM 6.05
CHEMBL2407277 IC50 = 1580.0 nM 5.80
CHEMBL2407284 IC50 = 2350.0 nM 5.63