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Assay Detail

CHEMBL3119249

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

Binding
Non-competitive inhibition of HIV-1 integrase expressed in Escherichia coli using [32P]-labeled U5B/U5A DNA as substrate after 1 hr by double-reciprocal plot analysis in presence of Mn2+
2
Total Activities
2
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

Specific features of HIV-1 integrase inhibition by bisphosphonate derivatives.
Agapkina J, Yanvarev D, Anisenko A, Korolev S, Vepsäläinen J, Kochetkov S, Gottikh M.
Eur J Med Chem (2014) 73 : 73 -82
PubMed 24378711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.68 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3116306 1 6.00
CHEMBL34249 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3116306 Ki = 1000.0 nM 6.00
CHEMBL34249 Ki = 4400.0 nM 5.36