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Assay Detail

CHEMBL4829379

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

Binding
Inhibition of human 20S proteasome X using Ac-WLA-AMC as fluorogenic substrate measured every minute for 1 hr by fluorescence assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 20 5.43 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4867231 1 5.97
CHEMBL4877277 1 5.33
CHEMBL4863075 1 5.33
CHEMBL4879354 1 5.32
CHEMBL4863666 1 5.30
CHEMBL4875393 1 5.30
CHEMBL4845896 1 -
CHEMBL4649310 1 -
CHEMBL4879280 1 -
CHEMBL4646371 1 -
CHEMBL4863407 1 -
CHEMBL4864020 1 -
CHEMBL4867229 1 -
CHEMBL4870740 1 -
CHEMBL4855585 1 -
CHEMBL4869559 1 -
CHEMBL4854647 1 -
CHEMBL4866610 1 -
CHEMBL4849360 1 -
CHEMBL4859824 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4867231 IC50 = 1081.0 nM 5.97
CHEMBL4877277 IC50 = 4640.0 nM 5.33
CHEMBL4863075 IC50 = 4640.0 nM 5.33
CHEMBL4879354 IC50 = 4766.0 nM 5.32
CHEMBL4863666 IC50 = 4998.0 nM 5.30
CHEMBL4875393 IC50 = 4998.0 nM 5.30
CHEMBL4845896 IC50 > 10000.0 nM -
CHEMBL4649310 IC50 > 10000.0 nM -
CHEMBL4879280 IC50 > 10000.0 nM -
CHEMBL4646371 IC50 > 10000.0 nM -
CHEMBL4863407 IC50 > 10000.0 nM -
CHEMBL4864020 IC50 > 10000.0 nM -
CHEMBL4867229 IC50 > 10000.0 nM -
CHEMBL4870740 IC50 > 10000.0 nM -
CHEMBL4855585 IC50 > 10000.0 nM -
CHEMBL4869559 IC50 > 10000.0 nM -
CHEMBL4854647 IC50 > 10000.0 nM -
CHEMBL4866610 IC50 > 10000.0 nM -
CHEMBL4849360 IC50 > 10000.0 nM -
CHEMBL4859824 IC50 > 10000.0 nM -