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Assay Detail

CHEMBL3371144

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Binding
Inhibition of cathepsin D (unknown origin)
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cathepsin D (CHEMBL2581)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based optimization of non-peptidic Cathepsin D inhibitors.
Grädler U, Czodrowski P, Tsaklakidis C, Klein M, Werkmann D, Lindemann S, Maskos K, Leuthner B.
Bioorg Med Chem Lett (2014) 24 : 4141 -4150
PubMed 25086681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.78 7.07
Ki 1 9.15 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81927 2 9.15
CHEMBL68595 1 6.68
CHEMBL83114 1 6.60
CHEMBL296588 PEPSTATIN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81927 Ki = 0.7 nM 9.15
CHEMBL81927 IC50 = 85.0 nM 7.07
CHEMBL68595 IC50 = 210.0 nM 6.68
CHEMBL83114 IC50 = 250.0 nM 6.60
CHEMBL296588 PEPSTATIN IC50 < 1.0 nM -