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Assay Detail

CHEMBL1961053

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

Functional
Antiviral activity against HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
20
Total Activities
20
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 20 6.70 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1956096 1 7.56
CHEMBL1956092 1 7.50
CHEMBL240386 1 7.30
CHEMBL1956088 1 7.22
CHEMBL1956095 1 7.18
CHEMBL1956091 1 7.00
CHEMBL1956093 1 6.97
CHEMBL1956094 1 6.82
CHEMBL1956089 1 6.65
CHEMBL1956084 1 6.64
CHEMBL70663 DAPIVIRINE 3.0 1 6.48
CHEMBL1956083 1 6.18
CHEMBL1956087 1 6.08
CHEMBL1956090 1 5.99
CHEMBL1956085 1 5.85
CHEMBL223228 EFAVIRENZ 4.0 1 5.79
CHEMBL1955868 1 -
CHEMBL1956082 1 -
CHEMBL1956086 1 -
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1956096 EC50 = 27.4 nM 7.56
CHEMBL1956092 EC50 = 31.4 nM 7.50
CHEMBL240386 EC50 = 50.0 nM 7.30
CHEMBL1956088 EC50 = 60.0 nM 7.22
CHEMBL1956095 EC50 = 66.6 nM 7.18
CHEMBL1956091 EC50 = 100.2 nM 7.00
CHEMBL1956093 EC50 = 108.2 nM 6.97
CHEMBL1956094 EC50 = 151.1 nM 6.82
CHEMBL1956089 EC50 = 224.9 nM 6.65
CHEMBL1956084 EC50 = 230.4 nM 6.64
CHEMBL70663 DAPIVIRINE EC50 = 333.9 nM 6.48
CHEMBL1956083 EC50 = 652.8 nM 6.18
CHEMBL1956087 EC50 = 836.1 nM 6.08
CHEMBL1956090 EC50 = 1016.8 nM 5.99
CHEMBL1956085 EC50 = 1401.0 nM 5.85
CHEMBL223228 EFAVIRENZ EC50 = 1615.0 nM 5.79
CHEMBL1955868 EC50 > 2838.0 nM -
CHEMBL1956082 EC50 > 2500.0 nM -
CHEMBL1956086 EC50 > 2697.0 nM -
CHEMBL57 NEVIRAPINE EC50 > 7510.0 nM -