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Assay Detail

CHEMBL803234

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

Binding
Compound was evaluated for aspartyl protease inhibition selectivity relative to renin
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties
Sawyer T, Fisher J, Hester J, Smith C, Tomasselli A, Tarpley W, Burton P, Hui J, McQuade T, Conradi R, Bradford V, Liu L, Kinner J, Tustin J, Alexander D, Harrison A, Emmert D, Staples D, Maggiora L, Zhang Y, Poorman R, Dunna B, Rao C, Scarborough P, Lowther W, Craik C, DeCamp D, Moon J, Howe W, Heinrikson R
Bioorg Med Chem Lett (1993) 3 : 819 -824
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.50 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL165706 1 8.70
CHEMBL3350189 1 8.70
CHEMBL167514 1 6.67
CHEMBL166175 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL165706 Ki = 2.0 nM 8.70
CHEMBL3350189 Ki = 2.0 nM 8.70
CHEMBL167514 Ki = 212.0 nM 6.67
CHEMBL166175 Ki = 1200.0 nM 5.92