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Assay Detail

CHEMBL861104

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Binding
Inhibition of strand transfer process of HIV1 integrase
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 Expert

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Guare JP, Wai JS, Gomez RP, Anthony NJ, Jolly SM, Cortes AR, Vacca JP, Felock PJ, Stillmock KA, Schleif WA, Moyer G, Gabryelski LJ, Jin L, Chen IW, Hazuda DJ, Young SD.
Bioorg Med Chem Lett (2006) 16 : 2900 -2904
PubMed 16554152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.55 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210234 1 8.15
CHEMBL379658 1 8.00
CHEMBL378029 1 7.82
CHEMBL210233 1 7.70
CHEMBL377759 1 7.60
CHEMBL209872 1 7.60
CHEMBL199145 1 7.48
CHEMBL209307 1 7.40
CHEMBL426686 1 7.40
CHEMBL441683 1 7.40
CHEMBL208776 1 7.24
CHEMBL379132 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210234 IC50 = 7.0 nM 8.15
CHEMBL379658 IC50 = 10.0 nM 8.00
CHEMBL378029 IC50 = 15.0 nM 7.82
CHEMBL210233 IC50 = 20.0 nM 7.70
CHEMBL377759 IC50 = 25.0 nM 7.60
CHEMBL209872 IC50 = 25.0 nM 7.60
CHEMBL199145 IC50 = 33.0 nM 7.48
CHEMBL209307 IC50 = 40.0 nM 7.40
CHEMBL426686 IC50 = 40.0 nM 7.40
CHEMBL441683 IC50 = 40.0 nM 7.40
CHEMBL208776 IC50 = 58.0 nM 7.24
CHEMBL379132 IC50 = 156.0 nM 6.81