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Assay Detail

CHEMBL3242251

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Binding
Inhibition of HIV-1 integrase strand transfer activity using 3'-end biotin labelled oligonucleotide/5'-end digoxigenin labelled oligonucleotide as substrate after 1 hr by ELISA
6
Total Activities
6
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

A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.
Ferro S, De Luca L, Lo Surdo G, Morreale F, Christ F, Debyser Z, Gitto R, Chimirri A.
Bioorg Med Chem (2014) 22 : 2269 -2279
PubMed 24618511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.20 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259011 1 6.85
CHEMBL3233021 1 6.58
CHEMBL3233908 1 6.38
CHEMBL3233907 1 5.96
CHEMBL3233898 1 5.81
CHEMBL3233902 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259011 IC50 = 140.0 nM 6.85
CHEMBL3233021 IC50 = 260.0 nM 6.58
CHEMBL3233908 IC50 = 420.0 nM 6.38
CHEMBL3233907 IC50 = 1090.0 nM 5.96
CHEMBL3233898 IC50 = 1550.0 nM 5.81
CHEMBL3233902 IC50 = 2510.0 nM 5.60