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Assay Detail

CHEMBL832854

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

Binding
Inhibitory concentration against HIV-1 protease (NL4-3)
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 protease (CHEMBL243)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Kim RM, Rouse EA, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Emini EA, Tata JR.
Bioorg Med Chem Lett (2004) 14 : 4651 -4654
PubMed 15324882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 10.26 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361443 1 11.00
CHEMBL360212 1 11.00
CHEMBL364376 1 11.00
CHEMBL364409 1 11.00
CHEMBL364407 1 10.70
CHEMBL364404 1 10.70
CHEMBL435095 1 10.70
CHEMBL434342 1 9.62
CHEMBL366293 1 9.49
CHEMBL364552 1 9.40
CHEMBL361062 1 9.32
CHEMBL5483011 INDINAVIR 3.0 1 9.22
CHEMBL366299 1 -
CHEMBL361292 1 -
CHEMBL364855 1 -
CHEMBL187111 1 -
CHEMBL184010 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361443 IC50 = 0.01 nM 11.00
CHEMBL360212 IC50 = 0.01 nM 11.00
CHEMBL364376 IC50 = 0.01 nM 11.00
CHEMBL364409 IC50 = 0.01 nM 11.00
CHEMBL364407 IC50 = 0.02 nM 10.70
CHEMBL364404 IC50 = 0.02 nM 10.70
CHEMBL435095 IC50 = 0.02 nM 10.70
CHEMBL434342 IC50 = 0.24 nM 9.62
CHEMBL366293 IC50 = 0.32 nM 9.49
CHEMBL364552 IC50 = 0.4 nM 9.40
CHEMBL361062 IC50 = 0.48 nM 9.32
CHEMBL5483011 INDINAVIR IC50 = 0.6 nM 9.22
CHEMBL366299 IC50 < 0.01 nM -
CHEMBL361292 IC50 < 0.01 nM -
CHEMBL364855 IC50 < 0.01 nM -
CHEMBL187111 IC50 < 0.01 nM -
CHEMBL184010 IC50 < 0.01 nM -