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Assay Detail

CHEMBL1816188

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

Binding
Inhibition of HIV1 recombinant integrase 3'-processing and strand transfer activity using 21-mer U5B/U5A duplex oligonucleotides after 1 hr
12
Total Activities
12
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

Ethyl malonate amides: a diketo acid offspring fragment for HIV integrase inhibition.
Serafin K, Mazur P, Bak A, Laine E, Tchertanov L, Mouscadet JF, Polanski J.
Bioorg Med Chem (2011) 19 : 5000 -5005
PubMed 21767953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.77 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254316 RALTEGRAVIR 4.0 1 8.30
CHEMBL36640 1 6.16
CHEMBL1813126 1 5.70
CHEMBL1813127 1 4.38
CHEMBL1456957 1 4.30
CHEMBL1813133 1 -
CHEMBL1813132 1 -
CHEMBL1813131 1 -
CHEMBL1813130 1 -
CHEMBL1813129 1 -
CHEMBL1813128 1 -
CHEMBL1813134 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254316 RALTEGRAVIR IC50 = 5.0 nM 8.30
CHEMBL36640 IC50 = 700.0 nM 6.16
CHEMBL1813126 IC50 = 2000.0 nM 5.70
CHEMBL1813127 IC50 = 42000.0 nM 4.38
CHEMBL1456957 IC50 = 50000.0 nM 4.30
CHEMBL1813133 IC50 > 100000.0 nM -
CHEMBL1813132 IC50 - -
CHEMBL1813131 IC50 > 300000.0 nM -
CHEMBL1813130 IC50 - -
CHEMBL1813129 IC50 > 100000.0 nM -
CHEMBL1813128 IC50 > 100000.0 nM -
CHEMBL1813134 IC50 = 500000.0 nM -