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Assay Detail

CHEMBL4829383

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

Binding
Inhibition of human 20S proteasome LMP2 activity in human RPMI-8226 cells using Ac-PAL-AMC as fluorogenic substrate incubated for 72 hrs by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type RPMI-8226
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proteasome subunit beta type-9 (CHEMBL1944495)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer's Disease.
Lee MJ, Bhattarai D, Jang H, Baek A, Yeo IJ, Lee S, Miller Z, Lee S, Hong JT, Kim DE, Lee W, Kim KB.
J Med Chem (2021) 64 : 10934 -10950
PubMed 34309393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.49 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4845896 1 7.55
CHEMBL4646371 1 7.51
CHEMBL4877277 1 7.49
CHEMBL4879354 1 7.47
CHEMBL4867231 1 7.45
CHEMBL4867229 1 -
CHEMBL4870740 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4845896 IC50 = 28.0 nM 7.55
CHEMBL4646371 IC50 = 30.9 nM 7.51
CHEMBL4877277 IC50 = 32.7 nM 7.49
CHEMBL4879354 IC50 = 33.9 nM 7.47
CHEMBL4867231 IC50 = 35.8 nM 7.45
CHEMBL4867229 IC50 > 10000.0 nM -
CHEMBL4870740 IC50 > 10000.0 nM -