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Assay Detail

CHEMBL5098053

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

Functional
Antiviral activity against HIV 1 infected in human HeLa-MAGI cells assessed as inhibition of viral replication measured 24 hrs post infection by fluorescence based analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.
Messore A, Corona A, Madia VN, Saccoliti F, Tudino V, De Leo A, Ialongo D, Scipione L, De Vita D, Amendola G, Novellino E, Cosconati S, Métifiot M, Andreola ML, Esposito F, Grandi N, Tramontano E, Costi R, Di Santo R.
J Med Chem (2021) 64 : 8579 -8598
PubMed 34106711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.22 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 6.28
CHEMBL5185855 1 5.76
CHEMBL5198310 1 5.60
CHEMBL5207685 1 5.54
CHEMBL5176128 1 5.27
CHEMBL5173288 1 5.08
CHEMBL5183730 1 4.95
CHEMBL5188823 1 4.93
CHEMBL5197780 1 4.88
CHEMBL5191403 1 4.84
CHEMBL5198940 1 4.79
CHEMBL5182942 1 4.75
CHEMBL5202973 1 -
CHEMBL5207303 1 -
CHEMBL5194402 1 -
CHEMBL5187082 1 -
CHEMBL5174596 1 -
CHEMBL5172754 1 -
CHEMBL5191482 1 -
CHEMBL5184868 1 -
CHEMBL5172266 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ EC50 = 530.0 nM 6.28
CHEMBL5185855 EC50 = 1730.0 nM 5.76
CHEMBL5198310 EC50 = 2500.0 nM 5.60
CHEMBL5207685 EC50 = 2900.0 nM 5.54
CHEMBL5176128 EC50 = 5400.0 nM 5.27
CHEMBL5173288 EC50 = 8400.0 nM 5.08
CHEMBL5183730 EC50 = 11300.0 nM 4.95
CHEMBL5188823 EC50 = 11700.0 nM 4.93
CHEMBL5197780 EC50 = 13300.0 nM 4.88
CHEMBL5191403 EC50 = 14600.0 nM 4.84
CHEMBL5198940 EC50 = 16100.0 nM 4.79
CHEMBL5182942 EC50 = 17800.0 nM 4.75
CHEMBL5202973 EC50 > 50000.0 nM -
CHEMBL5207303 EC50 > 50000.0 nM -
CHEMBL5194402 EC50 > 50000.0 nM -
CHEMBL5187082 EC50 > 50000.0 nM -
CHEMBL5174596 EC50 > 100000.0 nM -
CHEMBL5172754 EC50 > 100000.0 nM -
CHEMBL5191482 EC50 > 50000.0 nM -
CHEMBL5184868 EC50 > 16000.0 nM -
CHEMBL5172266 EC50 > 50000.0 nM -