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Assay Detail

CHEMBL4370448

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Binding
Inhibition of 20S immunoproteasome beta 2 in human Raji cell lysates after 1 hr by competitive ABPP assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proteasome subunit beta type-10 (CHEMBL3317334)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits.
Xin BT, Huber EM, de Bruin G, Heinemeyer W, Maurits E, Espinal C, Du Y, Janssens M, Weyburne ES, Kisselev AF, Florea BI, Driessen C, van der Marel GA, Groll M, Overkleeft HS.
J Med Chem (2019) 62 : 1626 -1642
PubMed 30657666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.17 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326533 1 7.70
CHEMBL4577205 1 7.24
CHEMBL4590398 1 6.96
CHEMBL4451682 1 6.85
CHEMBL4446214 1 6.75
CHEMBL4513509 1 6.72
CHEMBL4440581 1 6.64
CHEMBL4544868 1 6.42
CHEMBL4450505 1 6.38
CHEMBL4546121 1 5.60
CHEMBL4518685 1 5.60
CHEMBL4592602 1 5.54
CHEMBL4442929 1 5.51
CHEMBL4545073 1 5.40
CHEMBL4550552 1 4.92
CHEMBL4443899 1 4.47
CHEMBL4452605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326533 IC50 = 20.0 nM 7.70
CHEMBL4577205 IC50 = 57.0 nM 7.24
CHEMBL4590398 IC50 = 110.0 nM 6.96
CHEMBL4451682 IC50 = 140.0 nM 6.85
CHEMBL4446214 IC50 = 180.0 nM 6.75
CHEMBL4513509 IC50 = 190.0 nM 6.72
CHEMBL4440581 IC50 = 230.0 nM 6.64
CHEMBL4544868 IC50 = 380.0 nM 6.42
CHEMBL4450505 IC50 = 420.0 nM 6.38
CHEMBL4546121 IC50 = 2500.0 nM 5.60
CHEMBL4518685 IC50 = 2500.0 nM 5.60
CHEMBL4592602 IC50 = 2900.0 nM 5.54
CHEMBL4442929 IC50 = 3100.0 nM 5.51
CHEMBL4545073 IC50 = 4000.0 nM 5.40
CHEMBL4550552 IC50 = 12000.0 nM 4.92
CHEMBL4443899 IC50 = 34000.0 nM 4.47
CHEMBL4452605 IC50 > 100000.0 nM -