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Assay Detail

CHEMBL1003960

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 [32P]-labeled linear oligonucleotide substrate by polyacrylamide gel electrophoresis
34
Total Activities
34
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

Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: effects of the phenyl substituent and the linker orientation.
Zeng LF, Jiang XH, Sanchez T, Zhang HS, Dayam R, Neamati N, Long YQ.
Bioorg Med Chem (2008) 16 : 7777 -7787
PubMed 18644730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 4.26 4.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492770 1 4.72
CHEMBL454190 1 4.64
CHEMBL467380 1 4.58
CHEMBL467149 1 4.26
CHEMBL443890 1 4.25
CHEMBL452223 1 4.04
CHEMBL513666 1 4.04
CHEMBL444974 1 4.03
CHEMBL467361 1 4.00
CHEMBL469071 1 4.00
CHEMBL468235 1 -
CHEMBL467360 1 -
CHEMBL513321 1 -
CHEMBL476930 1 -
CHEMBL467381 1 -
CHEMBL448880 1 -
CHEMBL467351 1 -
CHEMBL465864 1 -
CHEMBL505776 1 -
CHEMBL464340 1 -
CHEMBL452876 1 -
CHEMBL511423 1 -
CHEMBL452111 1 -
CHEMBL467159 1 -
CHEMBL449221 1 -
CHEMBL467169 1 -
CHEMBL469069 1 -
CHEMBL469070 1 -
CHEMBL467389 1 -
CHEMBL467359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492770 IC50 = 19000.0 nM 4.72
CHEMBL454190 IC50 = 23000.0 nM 4.64
CHEMBL467380 IC50 = 26000.0 nM 4.58
CHEMBL467149 IC50 = 55000.0 nM 4.26
CHEMBL443890 IC50 = 56000.0 nM 4.25
CHEMBL452223 IC50 = 91000.0 nM 4.04
CHEMBL513666 IC50 = 92000.0 nM 4.04
CHEMBL444974 IC50 = 94000.0 nM 4.03
CHEMBL467361 IC50 = 99000.0 nM 4.00
CHEMBL469071 IC50 = 99000.0 nM 4.00
CHEMBL513321 IC50 > 100000.0 nM -
CHEMBL468234 IC50 > 100000.0 nM -
CHEMBL476930 IC50 > 100000.0 nM -
CHEMBL467381 IC50 > 100000.0 nM -
CHEMBL448880 IC50 > 100000.0 nM -
CHEMBL467351 IC50 > 100000.0 nM -
CHEMBL465864 IC50 > 100000.0 nM -
CHEMBL505776 IC50 > 100000.0 nM -
CHEMBL464340 IC50 > 100000.0 nM -
CHEMBL502238 IC50 > 100000.0 nM -
CHEMBL468233 IC50 > 100000.0 nM -
CHEMBL512106 IC50 > 100000.0 nM -
CHEMBL467360 IC50 > 100000.0 nM -
CHEMBL468235 IC50 > 100000.0 nM -
CHEMBL452876 IC50 > 100000.0 nM -
CHEMBL511423 IC50 > 100000.0 nM -
CHEMBL452111 IC50 > 100000.0 nM -
CHEMBL467159 IC50 > 100000.0 nM -
CHEMBL449221 IC50 > 100000.0 nM -
CHEMBL467169 IC50 > 100000.0 nM -
CHEMBL469069 IC50 > 100000.0 nM -
CHEMBL469070 IC50 > 100000.0 nM -
CHEMBL467389 IC50 > 100000.0 nM -
CHEMBL467359 IC50 > 100000.0 nM -