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Assay Detail

CHEMBL2317017

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

Binding
Inhibition of wild type HIV1 integrase 3'-processing activity using 5'-end 32P-labeled linear oligonucleotide as substrate preincubated for 30 mins
38
Total Activities
38
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

Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions.
Sanchez TW, Debnath B, Christ F, Otake H, Debyser Z, Neamati N.
Bioorg Med Chem (2013) 21 : 957 -963
PubMed 23306052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 4.24 4.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2311867 1 4.77
CHEMBL2311873 1 4.54
CHEMBL2094513 1 4.16
CHEMBL2311887 1 4.11
CHEMBL2311881 1 4.05
CHEMBL2311882 1 4.05
CHEMBL2311878 1 4.00
CHEMBL2311897 1 -
CHEMBL2311912 1 -
CHEMBL2311911 1 -
CHEMBL2311910 1 -
CHEMBL1976649 1 -
CHEMBL2311908 1 -
CHEMBL2311906 1 -
CHEMBL2311904 1 -
CHEMBL2311903 1 -
CHEMBL2311902 1 -
CHEMBL2311898 1 -
CHEMBL1597979 1 -
CHEMBL2311866 1 -
CHEMBL199592 1 -
CHEMBL200144 1 -
CHEMBL569410 1 -
CHEMBL2311868 1 -
CHEMBL390195 1 -
CHEMBL2311870 1 -
CHEMBL2311872 1 -
CHEMBL2311874 1 -
CHEMBL2311877 1 -
CHEMBL2094455 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2311867 IC50 = 17000.0 nM 4.77
CHEMBL2311873 IC50 = 29000.0 nM 4.54
CHEMBL2094513 IC50 = 69000.0 nM 4.16
CHEMBL2311887 IC50 = 77000.0 nM 4.11
CHEMBL2311881 IC50 = 90000.0 nM 4.05
CHEMBL2311882 IC50 = 90000.0 nM 4.05
CHEMBL2311878 IC50 = 100000.0 nM 4.00
CHEMBL2311908 IC50 > 100000.0 nM -
CHEMBL2311879 IC50 > 100000.0 nM -
CHEMBL2311906 IC50 > 100000.0 nM -
CHEMBL2311904 IC50 > 100000.0 nM -
CHEMBL2311903 IC50 > 100000.0 nM -
CHEMBL2311902 IC50 > 100000.0 nM -
CHEMBL2311898 IC50 > 100000.0 nM -
CHEMBL2311912 IC50 > 100000.0 nM -
CHEMBL2311896 IC50 > 100000.0 nM -
CHEMBL2311893 IC50 > 100000.0 nM -
CHEMBL2311891 IC50 > 100000.0 nM -
CHEMBL2311890 IC50 > 100000.0 nM -
CHEMBL2311889 IC50 > 100000.0 nM -
CHEMBL2311888 IC50 > 100000.0 nM -
CHEMBL2311885 IC50 > 100000.0 nM -
CHEMBL1976649 IC50 > 100000.0 nM -
CHEMBL2311910 IC50 > 100000.0 nM -
CHEMBL2311911 IC50 > 100000.0 nM -
CHEMBL2311897 IC50 > 100000.0 nM -
CHEMBL1597979 IC50 < 100000.0 nM -
CHEMBL2311866 IC50 > 100000.0 nM -
CHEMBL199592 IC50 > 100000.0 nM -
CHEMBL200144 IC50 > 100000.0 nM -
CHEMBL569410 IC50 > 100000.0 nM -
CHEMBL2311868 IC50 > 100000.0 nM -
CHEMBL390195 IC50 > 100000.0 nM -
CHEMBL2311870 IC50 > 100000.0 nM -
CHEMBL2311872 IC50 > 100000.0 nM -
CHEMBL2311874 IC50 > 100000.0 nM -
CHEMBL2311877 IC50 > 100000.0 nM -
CHEMBL2094455 IC50 > 100000.0 nM -