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Assay Detail

CHEMBL2038367

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

Functional
Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
Agarwal HK, Chhikara BS, Quiterio M, Doncel GF, Parang K.
J Med Chem (2012) 55 : 2672 -2687
PubMed 22352809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 5.36 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035201 1 7.00
CHEMBL2035200 1 6.52
CHEMBL105318 ALOVUDINE 2.0 1 6.40
CHEMBL885 EMTRICITABINE 4.0 1 6.10
CHEMBL2035198 1 5.85
CHEMBL2035194 1 5.57
CHEMBL2035192 1 5.44
CHEMBL2035196 1 5.19
CHEMBL2035190 1 5.16
CHEMBL2035189 1 5.16
CHEMBL2035199 1 5.11
CHEMBL141 LAMIVUDINE 4.0 1 4.95
CHEMBL2035195 1 4.91
CHEMBL2035193 1 4.88
CHEMBL2035197 1 4.87
CHEMBL129 ZIDOVUDINE 4.0 1 4.85
CHEMBL2035188 1 4.54
CHEMBL2035191 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035201 EC50 = 100.0 nM 7.00
CHEMBL2035200 EC50 = 300.0 nM 6.52
CHEMBL105318 ALOVUDINE EC50 = 400.0 nM 6.40
CHEMBL885 EMTRICITABINE EC50 = 800.0 nM 6.10
CHEMBL2035198 EC50 = 1400.0 nM 5.85
CHEMBL2035194 EC50 = 2700.0 nM 5.57
CHEMBL2035192 EC50 = 3600.0 nM 5.44
CHEMBL2035196 EC50 = 6500.0 nM 5.19
CHEMBL2035190 EC50 = 6900.0 nM 5.16
CHEMBL2035189 EC50 = 6900.0 nM 5.16
CHEMBL2035199 EC50 = 7700.0 nM 5.11
CHEMBL141 LAMIVUDINE EC50 = 11300.0 nM 4.95
CHEMBL2035195 EC50 = 12300.0 nM 4.91
CHEMBL2035193 EC50 = 13100.0 nM 4.88
CHEMBL2035197 EC50 = 13400.0 nM 4.87
CHEMBL129 ZIDOVUDINE EC50 = 14200.0 nM 4.85
CHEMBL2035188 EC50 = 29100.0 nM 4.54
CHEMBL2035191 EC50 = 86400.0 nM 4.06