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Assay Detail

CHEMBL987043

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

Binding
Inhibition of recombinant HIV1 integrase strand transfer activity using immobilized DNA substrate
8
Total Activities
8
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

Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Melamed JY, Egbertson MS, Varga S, Vacca JP, Moyer G, Gabryelski L, Felock PJ, Stillmock KA, Witmer MV, Schleif W, Hazuda DJ, Leonard Y, Jin L, Ellis JD, Young SD.
Bioorg Med Chem Lett (2008) 18 : 5307 -5310
PubMed 18774711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.50 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476564 1 7.85
CHEMBL476357 1 7.70
CHEMBL514836 1 7.62
CHEMBL514555 1 7.58
CHEMBL478239 1 7.48
CHEMBL199145 1 7.48
CHEMBL476565 1 7.40
CHEMBL478452 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476564 IC50 = 14.0 nM 7.85
CHEMBL476357 IC50 = 20.0 nM 7.70
CHEMBL514836 IC50 = 24.0 nM 7.62
CHEMBL514555 IC50 = 26.0 nM 7.58
CHEMBL478239 IC50 = 33.0 nM 7.48
CHEMBL199145 IC50 = 33.0 nM 7.48
CHEMBL476565 IC50 = 40.0 nM 7.40
CHEMBL478452 IC50 = 123.0 nM 6.91