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Assay Detail

CHEMBL1961049

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

Functional
Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay
6
Total Activities
6
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

Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
Rotili D, Tarantino D, Artico M, Nawrozkij MB, Gonzalez-Ortega E, Clotet B, Samuele A, Esté JA, Maga G, Mai A.
J Med Chem (2011) 54 : 3091 -3096
PubMed 21438533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.92 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70663 DAPIVIRINE 3.0 1 9.52
CHEMBL1956096 1 9.09
CHEMBL1956088 1 8.11
CHEMBL240386 1 6.69
CHEMBL223228 EFAVIRENZ 4.0 1 6.20
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70663 DAPIVIRINE EC50 = 0.3 nM 9.52
CHEMBL1956096 EC50 = 0.82 nM 9.09
CHEMBL1956088 EC50 = 7.8 nM 8.11
CHEMBL240386 EC50 = 204.6 nM 6.69
CHEMBL223228 EFAVIRENZ EC50 = 633.5 nM 6.20
CHEMBL57 NEVIRAPINE EC50 > 18850.0 nM -