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Assay Detail

CHEMBL5254891

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

Functional
Antiviral activity against HIV LAI infected in human MT-2 cells assessed as inhibition of viral growth
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus
Cell Type MT2
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus (CHEMBL613758)
Type ORGANISM
Organism Human immunodeficiency virus

Publication

Evaluation of darunavir-derived HIV-1 protease inhibitors incorporating P2' amide-derivatives: Synthesis, biological evaluation and structural studies.
Ghosh AK, Shahabi D, Kipfmiller M, Ghosh AK, Johnson M, Wang YF, Agniswamy J, Amano M, Weber IT, Mitsuya H.
Bioorg Med Chem Lett (2023) 83 : 129168 -129168
PubMed 36738797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.26 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1323 DARUNAVIR 4.0 1 8.80
CHEMBL5284706 1 7.60
CHEMBL5291125 1 7.54
CHEMBL5288746 1 7.51
CHEMBL5287201 1 7.50
CHEMBL5267260 1 7.41
CHEMBL5271223 1 7.03
CHEMBL5280093 1 6.55
CHEMBL5278603 1 6.37
CHEMBL5268648 1 6.27
CHEMBL5274743 1 -
CHEMBL5287711 1 -
CHEMBL5281851 1 -
CHEMBL5266228 1 -
CHEMBL5271083 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1323 DARUNAVIR IC50 = 1.6 nM 8.80
CHEMBL5284706 IC50 = 25.0 nM 7.60
CHEMBL5291125 IC50 = 29.0 nM 7.54
CHEMBL5288746 IC50 = 31.0 nM 7.51
CHEMBL5287201 IC50 = 32.0 nM 7.50
CHEMBL5267260 IC50 = 39.0 nM 7.41
CHEMBL5271223 IC50 = 93.0 nM 7.03
CHEMBL5280093 IC50 = 280.0 nM 6.55
CHEMBL5278603 IC50 = 430.0 nM 6.37
CHEMBL5268648 IC50 = 540.0 nM 6.27
CHEMBL5274743 IC50 > 1000.0 nM -
CHEMBL5287711 IC50 - -
CHEMBL5281851 IC50 - -
CHEMBL5266228 IC50 > 1000.0 nM -
CHEMBL5271083 IC50 > 1000.0 nM -