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Assay Detail

CHEMBL974532

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

Functional
Antiviral activity against HIV1-infected in human H9/HTLV 3B cells after 4 days
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
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
EC50 24 5.47 6.77
EC95 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496454 1 6.77
CHEMBL50605 1 6.00
CHEMBL512195 1 5.93
CHEMBL498713 1 5.50
CHEMBL456365 1 5.39
CHEMBL497501 1 5.37
CHEMBL458064 1 4.46
CHEMBL496652 1 4.34
CHEMBL497314 1 -
CHEMBL492335 1 -
CHEMBL504621 1 -
CHEMBL32865 1 -
CHEMBL524807 1 -
CHEMBL497688 1 -
CHEMBL498698 1 -
CHEMBL498697 1 -
CHEMBL497313 1 -
CHEMBL496455 1 -
CHEMBL457850 1 -
CHEMBL458275 1 -
CHEMBL514422 1 -
CHEMBL456991 1 -
CHEMBL456158 1 -
CHEMBL456791 1 -
CHEMBL456580 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496454 EC50 = 170.0 nM 6.77
CHEMBL50605 EC50 = 1000.0 nM 6.00
CHEMBL512195 EC50 = 1170.0 nM 5.93
CHEMBL498713 EC50 = 3200.0 nM 5.50
CHEMBL456365 EC50 = 4100.0 nM 5.39
CHEMBL497501 EC50 = 4290.0 nM 5.37
CHEMBL458064 EC50 = 34800.0 nM 4.46
CHEMBL496652 EC50 = 46100.0 nM 4.34
CHEMBL497314 EC50 - -
CHEMBL492335 EC50 - -
CHEMBL504621 EC50 > 50000.0 nM -
CHEMBL32865 EC95 = 0.39 uM -
CHEMBL524807 EC50 > 50000.0 nM -
CHEMBL497688 EC50 > 50000.0 nM -
CHEMBL498698 EC50 > 50000.0 nM -
CHEMBL498697 EC50 > 50000.0 nM -
CHEMBL497313 EC50 - -
CHEMBL496455 EC50 - -
CHEMBL457850 EC50 - -
CHEMBL458275 EC50 > 50000.0 nM -
CHEMBL514422 EC50 > 50000.0 nM -
CHEMBL456991 EC50 > 50000.0 nM -
CHEMBL456158 EC50 > 50000.0 nM -
CHEMBL456791 EC50 - -
CHEMBL456580 EC50 > 50000.0 nM -