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Assay Detail

CHEMBL3240948

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

Functional
Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.
Costi R, Métifiot M, Chung S, Cuzzucoli Crucitti G, Maddali K, Pescatori L, Messore A, Madia VN, Pupo G, Scipione L, Tortorella S, Di Leva FS, Cosconati S, Marinelli L, Novellino E, Le Grice SF, Corona A, Pommier Y, Marchand C, Di Santo R.
J Med Chem (2014) 57 : 3223 -3234
PubMed 24684270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.46 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 7.85
CHEMBL254316 RALTEGRAVIR 4.0 1 7.63
CHEMBL456365 1 6.08
CHEMBL3238122 1 5.44
CHEMBL3238126 1 4.88
CHEMBL496454 1 4.85
CHEMBL3238124 1 4.79
CHEMBL3238130 1 4.77
CHEMBL3238120 1 4.68
CHEMBL3238132 1 4.58
CHEMBL3238121 1 4.48
CHEMBL3238131 1 -
CHEMBL3238129 1 -
CHEMBL3238133 1 -
CHEMBL3238134 1 -
CHEMBL3238128 1 -
CHEMBL3238127 1 -
CHEMBL3238125 1 -
CHEMBL3238123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204656 ELVITEGRAVIR EC50 = 14.2 nM 7.85
CHEMBL254316 RALTEGRAVIR EC50 = 23.6 nM 7.63
CHEMBL456365 EC50 = 830.0 nM 6.08
CHEMBL3238122 EC50 = 3600.0 nM 5.44
CHEMBL3238126 EC50 = 13200.0 nM 4.88
CHEMBL496454 EC50 = 14100.0 nM 4.85
CHEMBL3238124 EC50 = 16200.0 nM 4.79
CHEMBL3238130 EC50 = 17000.0 nM 4.77
CHEMBL3238120 EC50 = 20900.0 nM 4.68
CHEMBL3238132 EC50 = 26300.0 nM 4.58
CHEMBL3238121 EC50 = 33100.0 nM 4.48
CHEMBL3238131 EC50 > 50000.0 nM -
CHEMBL3238129 EC50 > 50000.0 nM -
CHEMBL3238133 EC50 > 50000.0 nM -
CHEMBL3238134 EC50 > 50000.0 nM -
CHEMBL3238128 EC50 > 50000.0 nM -
CHEMBL3238127 EC50 > 50000.0 nM -
CHEMBL3238125 EC50 > 50000.0 nM -
CHEMBL3238123 EC50 > 50000.0 nM -