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Assay Detail

CHEMBL5117637

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

Functional
Antiviral activity against HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
50
Total Activities
50
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

Discovery of novel biphenyl-substituted pyridone derivatives as potent non-nucleoside reverse transcriptase inhibitors with promising oral bioavailability.
Zhao LM, Wang S, Pannecouque C, De Clercq E, Piao HR, Chen FE.
Eur J Med Chem (2022) 240 : 114581 -114581
PubMed 35797898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 50 5.43 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308954 ETRAVIRINE 4.0 1 7.72
CHEMBL2364608 DORAVIRINE 4.0 1 7.60
CHEMBL5207106 1 7.27
CHEMBL5194948 1 7.24
CHEMBL5195851 1 6.92
CHEMBL5185466 1 6.75
CHEMBL5192706 1 6.68
CHEMBL5188535 1 6.47
CHEMBL5192492 1 6.35
CHEMBL5182552 1 6.35
CHEMBL5181319 1 5.33
CHEMBL5206584 1 5.32
CHEMBL5194139 1 5.32
CHEMBL5203008 1 5.30
CHEMBL5205877 1 5.26
CHEMBL5181444 1 5.22
CHEMBL5188268 1 5.22
CHEMBL5191658 1 5.20
CHEMBL5197565 1 5.20
CHEMBL5172391 1 5.16
CHEMBL5170086 1 5.15
CHEMBL5172383 1 5.12
CHEMBL5208344 1 5.08
CHEMBL5179563 1 5.06
CHEMBL5197675 1 5.05
CHEMBL5183448 1 4.92
CHEMBL5189516 1 4.87
CHEMBL5199298 1 4.85
CHEMBL5196297 1 4.83
CHEMBL5193241 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308954 ETRAVIRINE EC50 = 19.0 nM 7.72
CHEMBL2364608 DORAVIRINE EC50 = 25.0 nM 7.60
CHEMBL5207106 EC50 = 54.0 nM 7.27
CHEMBL5194948 EC50 = 58.0 nM 7.24
CHEMBL5195851 EC50 = 120.0 nM 6.92
CHEMBL5185466 EC50 = 180.0 nM 6.75
CHEMBL5192706 EC50 = 210.0 nM 6.68
CHEMBL5188535 EC50 = 340.0 nM 6.47
CHEMBL5192492 EC50 = 450.0 nM 6.35
CHEMBL5182552 EC50 = 450.0 nM 6.35
CHEMBL5181319 EC50 = 4690.0 nM 5.33
CHEMBL5206584 EC50 = 4840.0 nM 5.32
CHEMBL5194139 EC50 = 4750.0 nM 5.32
CHEMBL5203008 EC50 = 4970.0 nM 5.30
CHEMBL5205877 EC50 = 5540.0 nM 5.26
CHEMBL5181444 EC50 = 6030.0 nM 5.22
CHEMBL5188268 EC50 = 5960.0 nM 5.22
CHEMBL5191658 EC50 = 6380.0 nM 5.20
CHEMBL5197565 EC50 = 6260.0 nM 5.20
CHEMBL5172391 EC50 = 6910.0 nM 5.16
CHEMBL5170086 EC50 = 7140.0 nM 5.15
CHEMBL5172383 EC50 = 7510.0 nM 5.12
CHEMBL5208344 EC50 = 8360.0 nM 5.08
CHEMBL5179563 EC50 = 8640.0 nM 5.06
CHEMBL5197675 EC50 = 8830.0 nM 5.05
CHEMBL5183448 EC50 = 12140.0 nM 4.92
CHEMBL5189516 EC50 = 13430.0 nM 4.87
CHEMBL5199298 EC50 = 14150.0 nM 4.85
CHEMBL5196297 EC50 = 14720.0 nM 4.83
CHEMBL5193241 EC50 = 19440.0 nM 4.71
CHEMBL5176462 EC50 = 21330.0 nM 4.67
CHEMBL5207715 EC50 = 22270.0 nM 4.65
CHEMBL5172232 EC50 = 28600.0 nM 4.54
CHEMBL5208501 EC50 = 38810.0 nM 4.41
CHEMBL5172691 EC50 = 38750.0 nM 4.41
CHEMBL5176402 EC50 = 39050.0 nM 4.41
CHEMBL5200651 EC50 = 39590.0 nM 4.40
CHEMBL5181637 EC50 = 42250.0 nM 4.37
CHEMBL5204226 EC50 = 48320.0 nM 4.32
CHEMBL5209417 EC50 > 35000.0 nM -
CHEMBL5177801 EC50 > 35000.0 nM -
CHEMBL5169999 EC50 > 35000.0 nM -
CHEMBL5193795 EC50 > 35000.0 nM -
CHEMBL5206836 EC50 > 35000.0 nM -
CHEMBL5171525 EC50 > 35000.0 nM -
CHEMBL5175076 EC50 > 35000.0 nM -
CHEMBL5184356 EC50 > 35000.0 nM -
CHEMBL5191334 EC50 > 35000.0 nM -
CHEMBL5197858 EC50 > 35000.0 nM -
CHEMBL5192757 EC50 > 35000.0 nM -