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Assay Detail

CHEMBL3389542

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Functional
Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay
25
Total Activities
25
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

Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
Famiglini V, La Regina G, Coluccia A, Pelliccia S, Brancale A, Maga G, Crespan E, Badia R, Riveira-Muñoz E, Esté JA, Ferretti R, Cirilli R, Zamperini C, Botta M, Schols D, Limongelli V, Agostino B, Novellino E, Silvestri R.
J Med Chem (2014) 57 : 9945 -9957
PubMed 25418038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.94 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358170 1 9.10
CHEMBL3358176 1 8.68
CHEMBL3358161 1 8.66
CHEMBL308954 ETRAVIRINE 4.0 1 8.22
CHEMBL3358159 1 7.80
CHEMBL1766221 1 7.75
CHEMBL3358160 1 7.18
CHEMBL3358172 1 7.17
CHEMBL3358165 1 7.06
CHEMBL1766233 1 6.97
CHEMBL3358175 1 6.89
CHEMBL223228 EFAVIRENZ 4.0 1 6.80
CHEMBL3358173 1 6.80
CHEMBL3358171 1 6.80
CHEMBL3358167 1 6.66
CHEMBL3358166 1 6.64
CHEMBL3358174 1 6.17
CHEMBL3263468 1 6.14
CHEMBL3358169 1 5.83
CHEMBL3358164 1 5.60
CHEMBL79797 1 5.29
CHEMBL3358162 1 4.37
CHEMBL3358168 1 -
CHEMBL57 NEVIRAPINE 4.0 1 -
CHEMBL3358163 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358170 EC50 = 0.8 nM 9.10
CHEMBL3358176 EC50 = 2.1 nM 8.68
CHEMBL3358161 EC50 = 2.2 nM 8.66
CHEMBL308954 ETRAVIRINE EC50 = 6.0 nM 8.22
CHEMBL3358159 EC50 = 16.0 nM 7.80
CHEMBL1766221 EC50 = 18.0 nM 7.75
CHEMBL3358160 EC50 = 66.0 nM 7.18
CHEMBL3358172 EC50 = 68.0 nM 7.17
CHEMBL3358165 EC50 = 87.0 nM 7.06
CHEMBL1766233 EC50 = 107.0 nM 6.97
CHEMBL3358175 EC50 = 128.0 nM 6.89
CHEMBL223228 EFAVIRENZ EC50 = 160.0 nM 6.80
CHEMBL3358173 EC50 = 160.0 nM 6.80
CHEMBL3358171 EC50 = 160.0 nM 6.80
CHEMBL3358167 EC50 = 220.0 nM 6.66
CHEMBL3358166 EC50 = 230.0 nM 6.64
CHEMBL3358174 EC50 = 670.0 nM 6.17
CHEMBL3263468 EC50 = 720.0 nM 6.14
CHEMBL3358169 EC50 = 1474.0 nM 5.83
CHEMBL3358164 EC50 = 2526.0 nM 5.60
CHEMBL79797 EC50 = 5174.0 nM 5.29
CHEMBL3358162 EC50 = 42719.0 nM 4.37
CHEMBL3358168 EC50 > 20000.0 nM -
CHEMBL57 NEVIRAPINE EC50 > 3756.0 nM -
CHEMBL3358163 EC50 > 55073.0 nM -