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Assay Detail

CHEMBL4704261

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Binding
Inhibition of human constitutive 20S proteasome beta 5 chymotrypsin-like activity
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proteasome Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.
Zhan W,Singh PK,Ban Y,Qing X,Ah Kioon MD,Fan H,Zhao Q,Wang R,Sukenick G,Salmon J,Warren JD,Ma X,Barrat FJ,Nathan CF,Lin G
J Med Chem (2020) 63 : 13103 -13123
PubMed 33095579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.57 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784015 1 7.26
CHEMBL4759896 1 7.23
CHEMBL4764833 1 7.00
CHEMBL4764897 1 6.92
CHEMBL4747215 1 6.77
CHEMBL4758484 1 6.61
CHEMBL4751044 1 6.53
CHEMBL4754892 1 6.52
CHEMBL4746069 1 6.51
CHEMBL4784875 1 6.37
CHEMBL4782251 1 6.29
CHEMBL4796570 1 6.21
CHEMBL4798821 1 6.01
CHEMBL4763630 1 5.98
CHEMBL4758527 1 5.88
CHEMBL4741140 1 5.84
CHEMBL4764343 1 5.83
CHEMBL4779742 1 5.59
CHEMBL4776824 1 5.46
CHEMBL4763116 1 5.26
CHEMBL4782050 1 4.97
CHEMBL4762794 1 4.89
CHEMBL4764263 1 4.88
CHEMBL4799140 1 4.86
CHEMBL4744524 1 4.84
CHEMBL4784421 1 4.73
CHEMBL4776510 1 4.68
CHEMBL4745016 1 4.64
CHEMBL4754559 1 4.57
CHEMBL4516988 1 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784015 IC50 = 55.0 nM 7.26
CHEMBL4759896 IC50 = 59.2 nM 7.23
CHEMBL4764833 IC50 = 101.0 nM 7.00
CHEMBL4764897 IC50 = 120.0 nM 6.92
CHEMBL4747215 IC50 = 170.0 nM 6.77
CHEMBL4758484 IC50 = 244.0 nM 6.61
CHEMBL4751044 IC50 = 296.0 nM 6.53
CHEMBL4754892 IC50 = 300.0 nM 6.52
CHEMBL4746069 IC50 = 307.0 nM 6.51
CHEMBL4784875 IC50 = 424.0 nM 6.37
CHEMBL4782251 IC50 = 514.0 nM 6.29
CHEMBL4796570 IC50 = 610.0 nM 6.21
CHEMBL4798821 IC50 = 980.0 nM 6.01
CHEMBL4763630 IC50 = 1040.0 nM 5.98
CHEMBL4758527 IC50 = 1320.0 nM 5.88
CHEMBL4741140 IC50 = 1456.0 nM 5.84
CHEMBL4764343 IC50 = 1467.0 nM 5.83
CHEMBL4779742 IC50 = 2570.0 nM 5.59
CHEMBL4776824 IC50 = 3480.0 nM 5.46
CHEMBL4763116 IC50 = 5520.0 nM 5.26
CHEMBL4782050 IC50 = 10730.0 nM 4.97
CHEMBL4762794 IC50 = 12730.0 nM 4.89
CHEMBL4764263 IC50 = 13060.0 nM 4.88
CHEMBL4799140 IC50 = 13740.0 nM 4.86
CHEMBL4744524 IC50 = 14340.0 nM 4.84
CHEMBL4784421 IC50 = 18520.0 nM 4.73
CHEMBL4776510 IC50 = 20950.0 nM 4.68
CHEMBL4745016 IC50 = 22730.0 nM 4.64
CHEMBL4754559 IC50 = 27230.0 nM 4.57
CHEMBL4516988 IC50 = 32400.0 nM 4.49
CHEMBL4745162 IC50 = 41080.0 nM 4.39
CHEMBL4795707 IC50 = 47670.0 nM 4.32
CHEMBL4764229 IC50 = 53700.0 nM 4.27
CHEMBL4741411 IC50 = 59030.0 nM 4.23
CHEMBL4752685 IC50 = 90630.0 nM 4.04
CHEMBL4779108 IC50 > 100000.0 nM -
CHEMBL4753220 IC50 > 100000.0 nM -
CHEMBL4761864 IC50 > 100000.0 nM -
CHEMBL4762145 IC50 > 100000.0 nM -
CHEMBL4754415 IC50 > 100000.0 nM -
CHEMBL4740404 IC50 > 100000.0 nM -
CHEMBL4762452 IC50 > 100000.0 nM -