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Assay Detail

CHEMBL4357205

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Binding
Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate measured every 5 mins for 120 mins by fluorescence based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

20S proteasome (CHEMBL3831201)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Novel Cell-Penetrating Peptide Conjugated Proteasome Inhibitors: Anticancer and Antifungal Investigations.
Patel KD, De Zoysa GH, Kanamala M, Patel K, Pilkington LI, Barker D, Reynisson J, Wu Z, Sarojini V.
J Med Chem (2020) 63 : 334 -348
PubMed 31801019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.97 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4587036 1 8.60
CHEMBL4581126 1 8.37
CHEMBL4447701 1 8.19
CHEMBL2141296 IXAZOMIB 3.0 1 7.82
CHEMBL4453814 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4587036 IC50 = 2.5 nM 8.60
CHEMBL4581126 IC50 = 4.28 nM 8.37
CHEMBL4447701 IC50 = 6.4 nM 8.19
CHEMBL2141296 IXAZOMIB IC50 = 15.0 nM 7.82
CHEMBL4453814 IC50 = 136.0 nM 6.87