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Assay Detail

CHEMBL903664

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Binding
Inhibition of HIV1 integrase 3'-end processing activity
40
Total Activities
40
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 and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.
Patil S, Kamath S, Sanchez T, Neamati N, Schinazi RF, Buolamwini JK.
Bioorg Med Chem (2007) 15 : 1212 -1228
PubMed 17158051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 4.64 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225681 1 5.16
CHEMBL389930 1 5.05
CHEMBL218227 S-1360 2.0 1 4.96
CHEMBL226484 1 4.96
CHEMBL375484 1 4.64
CHEMBL226485 1 4.60
CHEMBL226434 1 4.58
CHEMBL226489 1 4.50
CHEMBL375956 1 4.27
CHEMBL226490 1 4.27
CHEMBL225682 1 4.04
CHEMBL226318 1 -
CHEMBL3706870 1 -
CHEMBL3706871 1 -
CHEMBL3706872 1 -
CHEMBL226375 1 -
CHEMBL226432 1 -
CHEMBL389881 1 -
CHEMBL389931 1 -
CHEMBL376550 1 -
CHEMBL226259 1 -
CHEMBL226473 1 -
CHEMBL3706873 1 -
CHEMBL387679 1 -
CHEMBL387677 1 -
CHEMBL225669 1 -
CHEMBL225725 1 -
CHEMBL225661 1 -
CHEMBL226374 1 -
CHEMBL226433 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225681 IC50 = 7000.0 nM 5.16
CHEMBL389930 IC50 = 9000.0 nM 5.05
CHEMBL218227 S-1360 IC50 = 11000.0 nM 4.96
CHEMBL226484 IC50 = 11000.0 nM 4.96
CHEMBL375484 IC50 = 23000.0 nM 4.64
CHEMBL226485 IC50 = 25000.0 nM 4.60
CHEMBL226434 IC50 = 26000.0 nM 4.58
CHEMBL226489 IC50 = 32000.0 nM 4.50
CHEMBL226490 IC50 = 54000.0 nM 4.27
CHEMBL375956 IC50 = 54000.0 nM 4.27
CHEMBL225682 IC50 = 92000.0 nM 4.04
CHEMBL3706872 IC50 > 500000.0 nM -
CHEMBL436140 IC50 > 500000.0 nM -
CHEMBL3706871 IC50 > 500000.0 nM -
CHEMBL3706870 IC50 > 500000.0 nM -
CHEMBL226318 IC50 > 500000.0 nM -
CHEMBL225823 IC50 = 300000.0 nM -
CHEMBL226258 IC50 > 500000.0 nM -
CHEMBL226257 IC50 > 500000.0 nM -
CHEMBL387894 IC50 > 500000.0 nM -
CHEMBL225724 IC50 > 500000.0 nM -
CHEMBL225723 IC50 > 500000.0 nM -
CHEMBL387678 IC50 > 1000000.0 nM -
CHEMBL225667 IC50 > 1000000.0 nM -
CHEMBL225666 IC50 = 1000000.0 nM -
CHEMBL226375 IC50 > 500000.0 nM -
CHEMBL226432 IC50 > 500000.0 nM -
CHEMBL389881 IC50 > 100000.0 nM -
CHEMBL389931 IC50 > 100000.0 nM -
CHEMBL376550 IC50 > 500000.0 nM -
CHEMBL226259 IC50 > 500000.0 nM -
CHEMBL226473 IC50 > 500000.0 nM -
CHEMBL3706873 IC50 = 500000.0 nM -
CHEMBL387679 IC50 = 500000.0 nM -
CHEMBL387677 IC50 = 449000.0 nM -
CHEMBL225669 IC50 = 225000.0 nM -
CHEMBL225725 IC50 = 206000.0 nM -
CHEMBL225661 IC50 > 500000.0 nM -
CHEMBL226374 IC50 = 400000.0 nM -
CHEMBL226433 IC50 = 102000.0 nM -