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Assay Detail

CHEMBL2038371

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

Functional
Antiviral activity against NNRTI-resistant HIV1 clade B A-17 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infection assay
8
Total Activities
4
Compounds Tested
2
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

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
IC50 4 7.54 7.89
IC90 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035198 2 7.89
CHEMBL129 ZIDOVUDINE 4.0 2 7.66
CHEMBL105318 ALOVUDINE 2.0 2 7.58
CHEMBL141 LAMIVUDINE 4.0 2 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035198 IC50 = 12.9 nM 7.89
CHEMBL129 ZIDOVUDINE IC50 = 21.7 nM 7.66
CHEMBL105318 ALOVUDINE IC50 = 26.0 nM 7.58
CHEMBL141 LAMIVUDINE IC50 = 92.1 nM 7.04
CHEMBL141 LAMIVUDINE IC90 = 282.9 nM -
CHEMBL105318 ALOVUDINE IC90 = 87.2 nM -
CHEMBL129 ZIDOVUDINE IC90 = 152.3 nM -
CHEMBL2035198 IC90 = 28.3 nM -