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Assay Detail

CHEMBL3583198

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

Functional
Antiviral activity against HIV-1 3B infected in human HeLa-CD4-LTR-beta-gal cells assessed as inhibition of viral replication by SpectraMax GEMINI-XS plate reader analysis
55
Total Activities
55
Compounds Tested
1
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

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase.
Pescatori L, Métifiot M, Chung S, Masoaka T, Cuzzucoli Crucitti G, Messore A, Pupo G, Madia VN, Saccoliti F, Scipione L, Tortorella S, Di Leva FS, Cosconati S, Marinelli L, Novellino E, Le Grice SF, Pommier Y, Marchand C, Costi R, Di Santo R.
J Med Chem (2015) 58 : 4610 -4623
PubMed 25961960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 55 5.30 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204656 ELVITEGRAVIR 4.0 1 7.85
CHEMBL254316 RALTEGRAVIR 4.0 1 7.63
CHEMBL3582044 1 6.24
CHEMBL3582058 1 6.06
CHEMBL3582038 1 6.00
CHEMBL3582039 1 5.82
CHEMBL2236598 RDS-1624 1 5.77
CHEMBL3582057 1 5.58
CHEMBL2236589 20, RDS-2163 1 5.58
CHEMBL3582080 1 5.32
CHEMBL2236601 RDS-1984 1 5.09
CHEMBL2236602 1 5.07
CHEMBL2236588 1 5.03
CHEMBL3582046 1 5.01
CHEMBL3582052 1 5.00
CHEMBL3582055 1 4.96
CHEMBL3582062 1 4.86
CHEMBL3582056 1 4.81
CHEMBL3582064 1 4.79
CHEMBL3582074 1 4.77
CHEMBL3582053 1 4.76
CHEMBL3582070 1 4.63
CHEMBL2236599 1 4.55
CHEMBL3582049 1 4.52
CHEMBL3582041 1 4.51
CHEMBL3582047 1 4.49
CHEMBL3582072 1 4.30
CHEMBL3582071 1 -
CHEMBL3582061 1 -
CHEMBL3582069 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
CHEMBL3582044 EC50 = 580.0 nM 6.24
CHEMBL3582058 EC50 = 870.0 nM 6.06
CHEMBL3582038 EC50 = 1000.0 nM 6.00
CHEMBL3582039 EC50 = 1500.0 nM 5.82
CHEMBL2236598 RDS-1624 EC50 = 1700.0 nM 5.77
CHEMBL3582057 EC50 = 2600.0 nM 5.58
CHEMBL2236589 20, RDS-2163 EC50 = 2600.0 nM 5.58
CHEMBL3582080 EC50 = 4800.0 nM 5.32
CHEMBL2236601 RDS-1984 EC50 = 8100.0 nM 5.09
CHEMBL2236602 EC50 = 8500.0 nM 5.07
CHEMBL2236588 EC50 = 9300.0 nM 5.03
CHEMBL3582046 EC50 = 9800.0 nM 5.01
CHEMBL3582052 EC50 = 10000.0 nM 5.00
CHEMBL3582055 EC50 = 11000.0 nM 4.96
CHEMBL3582062 EC50 = 13800.0 nM 4.86
CHEMBL3582056 EC50 = 15500.0 nM 4.81
CHEMBL3582064 EC50 = 16200.0 nM 4.79
CHEMBL3582074 EC50 = 17000.0 nM 4.77
CHEMBL3582053 EC50 = 17400.0 nM 4.76
CHEMBL3582070 EC50 = 23400.0 nM 4.63
CHEMBL2236599 EC50 = 28200.0 nM 4.55
CHEMBL3582049 EC50 = 30200.0 nM 4.52
CHEMBL3582041 EC50 = 30900.0 nM 4.51
CHEMBL3582047 EC50 = 32400.0 nM 4.49
CHEMBL3582072 EC50 = 50000.0 nM 4.30
CHEMBL3582054 EC50 > 50000.0 nM -
CHEMBL3582059 EC50 > 50000.0 nM -
CHEMBL2236603 RDS-2161 EC50 > 50000.0 nM -
CHEMBL3582068 EC50 > 50000.0 nM -
CHEMBL3582051 EC50 > 50000.0 nM -
CHEMBL3582050 EC50 > 50000.0 nM -
CHEMBL3582048 EC50 > 50000.0 nM -
CHEMBL2236600 EC50 < 200.0 nM -
CHEMBL3582045 EC50 > 50000.0 nM -
CHEMBL3582040 EC50 > 50000.0 nM -
CHEMBL3582043 EC50 > 50000.0 nM -
CHEMBL3582042 EC50 > 50000.0 nM -
CHEMBL3582082 EC50 > 50000.0 nM -
CHEMBL3582081 EC50 > 50000.0 nM -
CHEMBL3582079 EC50 > 50000.0 nM -
CHEMBL3582078 EC50 > 50000.0 nM -
CHEMBL3582077 EC50 > 50000.0 nM -
CHEMBL3582076 EC50 > 50000.0 nM -
CHEMBL3582075 EC50 > 50000.0 nM -
CHEMBL3582073 EC50 > 50000.0 nM -
CHEMBL3582069 EC50 > 50000.0 nM -
CHEMBL3582061 EC50 > 50000.0 nM -
CHEMBL3582071 EC50 > 50000.0 nM -