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Assay Detail

CHEMBL887178

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

Binding
Inhibition of HIV1 recombinant integrase strand transfer activity
16
Total Activities
16
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

Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
Sriram D, Yogeeswari P, Senchani G, Banerjee D.
Bioorg Med Chem Lett (2007) 17 : 2372 -2375
PubMed 17376679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.74 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396688 1 4.92
CHEMBL241495 1 4.92
CHEMBL396907 1 4.89
CHEMBL392565 1 4.87
CHEMBL239176 1 4.77
CHEMBL239177 1 4.75
CHEMBL1237046 ROLITETRACYCLINE 2.0 1 4.47
CHEMBL396686 1 4.36
CHEMBL1440 TETRACYCLINE 4.0 1 -
CHEMBL396687 1 -
CHEMBL561 LOMEFLOXACIN 4.0 1 -
CHEMBL1434 MINOCYCLINE 4.0 1 -
CHEMBL239813 1 -
CHEMBL392612 1 -
CHEMBL392611 1 -
CHEMBL241293 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396688 IC50 = 12000.0 nM 4.92
CHEMBL241495 IC50 = 12000.0 nM 4.92
CHEMBL396907 IC50 = 13000.0 nM 4.89
CHEMBL392565 IC50 = 13500.0 nM 4.87
CHEMBL239176 IC50 = 17000.0 nM 4.77
CHEMBL239177 IC50 = 18000.0 nM 4.75
CHEMBL1237046 ROLITETRACYCLINE IC50 = 34000.0 nM 4.47
CHEMBL396686 IC50 = 44000.0 nM 4.36
CHEMBL1440 TETRACYCLINE IC50 = 188000.0 nM -
CHEMBL396687 IC50 - -
CHEMBL561 LOMEFLOXACIN IC50 - -
CHEMBL1434 MINOCYCLINE IC50 - -
CHEMBL239813 IC50 - -
CHEMBL392612 IC50 - -
CHEMBL392611 IC50 - -
CHEMBL241293 IC50 - -