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Assay Detail

CHEMBL4710313

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

Functional
Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay
29
Total Activities
29
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

New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
Nalli M,Armijos Rivera JI,Masci D,Coluccia A,Badia R,Riveira-Muñoz E,Brambilla A,Cinquina E,Turriziani O,Falasca F,Catalano M,Limatola C,Esté JA,Maga G,Silvestri R,Crespan E,La Regina G
Eur J Med Chem (2020) 208 : 112696 -112696
PubMed 32883642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 6.09 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308954 ETRAVIRINE 4.0 1 8.34
CHEMBL4784247 1 8.21
CHEMBL129 ZIDOVUDINE 4.0 1 7.80
CHEMBL4755777 1 7.63
CHEMBL4759261 1 6.96
CHEMBL1766209 1 6.52
CHEMBL4800322 1 6.48
CHEMBL4743821 1 6.22
CHEMBL85059 1 6.19
CHEMBL4749320 1 6.18
CHEMBL127012 1 6.16
CHEMBL4747527 1 6.15
CHEMBL4780972 1 6.01
CHEMBL4776949 1 5.95
CHEMBL4745751 1 5.74
CHEMBL4744227 1 5.49
CHEMBL4739864 1 5.48
CHEMBL4776145 1 5.45
CHEMBL4788245 1 5.44
CHEMBL4760961 1 5.37
CHEMBL4788280 1 5.33
CHEMBL4800185 1 5.28
CHEMBL4747243 1 5.21
CHEMBL283950 L-737126 1 5.10
CHEMBL4794256 1 4.85
CHEMBL4776821 1 4.71
CHEMBL57 NEVIRAPINE 4.0 1 -
CHEMBL223228 EFAVIRENZ 4.0 1 -
CHEMBL4798552 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308954 ETRAVIRINE EC50 = 4.6 nM 8.34
CHEMBL4784247 EC50 = 6.2 nM 8.21
CHEMBL129 ZIDOVUDINE EC50 = 16.0 nM 7.80
CHEMBL4755777 EC50 = 23.5 nM 7.63
CHEMBL4759261 EC50 = 110.0 nM 6.96
CHEMBL1766209 EC50 = 300.0 nM 6.52
CHEMBL4800322 EC50 = 331.0 nM 6.48
CHEMBL4743821 EC50 = 600.0 nM 6.22
CHEMBL85059 EC50 = 650.0 nM 6.19
CHEMBL4749320 EC50 = 662.0 nM 6.18
CHEMBL127012 EC50 = 700.0 nM 6.16
CHEMBL4747527 EC50 = 704.0 nM 6.15
CHEMBL4780972 EC50 = 967.0 nM 6.01
CHEMBL4776949 EC50 = 1123.0 nM 5.95
CHEMBL4745751 EC50 = 1808.0 nM 5.74
CHEMBL4744227 EC50 = 3237.0 nM 5.49
CHEMBL4739864 EC50 = 3292.0 nM 5.48
CHEMBL4776145 EC50 = 3555.0 nM 5.45
CHEMBL4788245 EC50 = 3667.0 nM 5.44
CHEMBL4760961 EC50 = 4307.0 nM 5.37
CHEMBL4788280 EC50 = 4621.0 nM 5.33
CHEMBL4800185 EC50 = 5240.0 nM 5.28
CHEMBL4747243 EC50 = 6089.0 nM 5.21
CHEMBL283950 L-737126 EC50 = 8000.0 nM 5.10
CHEMBL4794256 EC50 = 14270.0 nM 4.85
CHEMBL4776821 EC50 = 19533.0 nM 4.71
CHEMBL57 NEVIRAPINE EC50 > 3756.0 nM -
CHEMBL223228 EFAVIRENZ EC50 > 317.0 nM -
CHEMBL4798552 EC50 > 19718.0 nM -