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Assay Detail

CHEMBL4688809

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

Functional
Antiviral activity against HIV-3B infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
Gao P,Song S,Frutos-Beltrán E,Li W,Sun B,Kang D,Zou J,Zhang J,Pannecouque C,De Clercq E,Menéndez-Arias L,Zhan P,Liu X
Bioorg Med Chem (2021) 30 : 115927 -115927
PubMed 33352387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.30 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 8.00
CHEMBL308954 ETRAVIRINE 4.0 1 8.00
CHEMBL253629 1 5.44
CHEMBL223228 EFAVIRENZ 4.0 1 5.07
CHEMBL4760121 1 5.01
CHEMBL4752899 1 -
CHEMBL4751528 1 -
CHEMBL4762273 1 -
CHEMBL4798626 1 -
CHEMBL4741996 1 -
CHEMBL4796270 1 -
CHEMBL4754387 1 -
CHEMBL4755224 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE EC50 = 10.0 nM 8.00
CHEMBL308954 ETRAVIRINE EC50 = 10.0 nM 8.00
CHEMBL253629 EC50 = 3600.0 nM 5.44
CHEMBL223228 EFAVIRENZ EC50 = 8500.0 nM 5.07
CHEMBL4760121 EC50 = 9740.0 nM 5.01
CHEMBL4752899 EC50 > 6500.0 nM -
CHEMBL4751528 EC50 > 2100.0 nM -
CHEMBL4762273 EC50 > 51800.0 nM -
CHEMBL4798626 EC50 > 43600.0 nM -
CHEMBL4741996 EC50 = 125400.0 nM -
CHEMBL4796270 EC50 > 155200.0 nM -
CHEMBL4754387 EC50 > 178000.0 nM -
CHEMBL4755224 EC50 > 29000.0 nM -