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Assay Detail

CHEMBL4362915

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

Functional
Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
16
Total Activities
16
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 indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing.
Zhao T, Meng Q, Kang D, Ji J, De Clercq E, Pannecouque C, Liu X, Zhan P.
Eur J Med Chem (2019) 182 : 111619 -111619
PubMed 31434039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.26 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 8.31
CHEMBL308954 ETRAVIRINE 4.0 1 8.21
CHEMBL4473354 1 7.96
CHEMBL85059 1 7.77
CHEMBL223228 EFAVIRENZ 4.0 1 7.36
CHEMBL4560034 1 6.98
CHEMBL57 NEVIRAPINE 4.0 1 5.91
CHEMBL4522009 1 5.85
CHEMBL4580502 1 5.66
CHEMBL141 LAMIVUDINE 4.0 1 5.50
CHEMBL4448112 1 5.36
CHEMBL4472347 1 5.17
CHEMBL4474373 1 5.09
CHEMBL4558281 1 5.05
CHEMBL4435269 1 5.00
CHEMBL4535880 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 4.9 nM 8.31
CHEMBL308954 ETRAVIRINE EC50 = 6.2 nM 8.21
CHEMBL4473354 EC50 = 11.0 nM 7.96
CHEMBL85059 EC50 = 17.0 nM 7.77
CHEMBL223228 EFAVIRENZ EC50 = 44.0 nM 7.36
CHEMBL4560034 EC50 = 104.0 nM 6.98
CHEMBL57 NEVIRAPINE EC50 = 1240.0 nM 5.91
CHEMBL4522009 EC50 = 1410.0 nM 5.85
CHEMBL4580502 EC50 = 2170.0 nM 5.66
CHEMBL141 LAMIVUDINE EC50 = 3140.0 nM 5.50
CHEMBL4448112 EC50 = 4400.0 nM 5.36
CHEMBL4472347 EC50 = 6810.0 nM 5.17
CHEMBL4474373 EC50 = 8170.0 nM 5.09
CHEMBL4558281 EC50 = 8860.0 nM 5.05
CHEMBL4435269 EC50 = 10020.0 nM 5.00
CHEMBL4535880 EC50 = 10940.0 nM 4.96