Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1004782

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

Binding
Inhibition of recombinant HIV1 integrase strand transfer activity by gel-based assay in presence of magnesium
23
Total Activities
23
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

Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities.
Di Santo R, Costi R, Roux A, Miele G, Crucitti GC, Iacovo A, Rosi F, Lavecchia A, Marinelli L, Di Giovanni C, Novellino E, Palmisano L, Andreotti M, Amici R, Galluzzo CM, Nencioni L, Palamara AT, Pommier Y, Marchand C.
J Med Chem (2008) 51 : 4744 -4750
PubMed 18646746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.12 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497501 1 7.77
CHEMBL498697 1 7.30
CHEMBL512195 1 7.22
CHEMBL498713 1 7.12
CHEMBL497688 1 6.96
CHEMBL498698 1 6.80
CHEMBL496454 1 6.75
CHEMBL504621 1 6.64
CHEMBL496652 1 6.40
CHEMBL458064 1 6.36
CHEMBL524807 1 6.29
CHEMBL458275 1 5.92
CHEMBL456158 1 5.75
CHEMBL496455 1 5.68
CHEMBL456580 1 5.64
CHEMBL456365 1 5.57
CHEMBL457850 1 5.52
CHEMBL456791 1 5.44
CHEMBL456991 1 5.28
CHEMBL514422 1 5.28
CHEMBL492335 1 4.77
CHEMBL497314 1 4.25
CHEMBL497313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497501 IC50 = 17.0 nM 7.77
CHEMBL498697 IC50 = 50.0 nM 7.30
CHEMBL512195 IC50 = 60.0 nM 7.22
CHEMBL498713 IC50 = 75.0 nM 7.12
CHEMBL497688 IC50 = 110.0 nM 6.96
CHEMBL498698 IC50 = 160.0 nM 6.80
CHEMBL496454 IC50 = 180.0 nM 6.75
CHEMBL504621 IC50 = 230.0 nM 6.64
CHEMBL496652 IC50 = 400.0 nM 6.40
CHEMBL458064 IC50 = 440.0 nM 6.36
CHEMBL524807 IC50 = 510.0 nM 6.29
CHEMBL458275 IC50 = 1200.0 nM 5.92
CHEMBL456158 IC50 = 1800.0 nM 5.75
CHEMBL496455 IC50 = 2100.0 nM 5.68
CHEMBL456580 IC50 = 2300.0 nM 5.64
CHEMBL456365 IC50 = 2700.0 nM 5.57
CHEMBL457850 IC50 = 3000.0 nM 5.52
CHEMBL456791 IC50 = 3600.0 nM 5.44
CHEMBL456991 IC50 = 5200.0 nM 5.28
CHEMBL514422 IC50 = 5200.0 nM 5.28
CHEMBL492335 IC50 = 17000.0 nM 4.77
CHEMBL497314 IC50 = 56000.0 nM 4.25
CHEMBL497313 IC50 = 224000.0 nM -