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Assay Detail

CHEMBL4822208

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

Binding
Inhibition of human chymotrypsin-like beta 5i subunit of iCP using suc-LLVY-AMC as flurogenic substrate for 90 mins by fluorescence-based assay
47
Total Activities
47
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 subunit beta type-8 (CHEMBL5620)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of selective fragment-sized immunoproteasome inhibitors.
Kollár L, Gobec M, Szilágyi B, Proj M, Knez D, Ábrányi-Balogh P, Petri L, Imre T, Bajusz D, Ferenczy GG, Gobec S, Keserű GM, Sosič I.
Eur J Med Chem (2021) 219 : 113455 -113455
PubMed 33894528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 4.55 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854282 1 5.75
CHEMBL4871166 1 5.52
CHEMBL1724381 1 5.39
CHEMBL227686 1 5.38
CHEMBL1500876 1 5.15
CHEMBL4849565 1 5.14
CHEMBL568708 1 5.05
CHEMBL4867541 1 5.05
CHEMBL4858322 1 5.04
CHEMBL4871650 1 5.01
CHEMBL4865958 1 5.00
CHEMBL4854219 1 4.96
CHEMBL4848759 1 4.96
CHEMBL4873906 1 4.89
CHEMBL111654 2-MERCAPTOBENZOTHIAZOLE 1 4.89
CHEMBL4877097 1 4.82
CHEMBL4858265 1 4.80
CHEMBL113414 1 4.77
CHEMBL4875943 1 4.75
CHEMBL4852689 1 4.70
CHEMBL4866283 1 4.58
CHEMBL4868002 1 4.57
CHEMBL4864399 1 4.55
CHEMBL4856216 1 4.52
CHEMBL1456330 1 4.50
CHEMBL4875672 1 4.44
CHEMBL4854026 1 4.37
CHEMBL4869230 1 4.31
CHEMBL4876125 1 4.22
CHEMBL69086 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854282 IC50 = 1800.0 nM 5.75
CHEMBL4871166 IC50 = 3000.0 nM 5.52
CHEMBL1724381 IC50 = 4100.0 nM 5.39
CHEMBL227686 IC50 = 4200.0 nM 5.38
CHEMBL1500876 IC50 = 7100.0 nM 5.15
CHEMBL4849565 IC50 = 7200.0 nM 5.14
CHEMBL568708 IC50 = 9000.0 nM 5.05
CHEMBL4867541 IC50 = 9000.0 nM 5.05
CHEMBL4858322 IC50 = 9100.0 nM 5.04
CHEMBL4871650 IC50 = 9700.0 nM 5.01
CHEMBL4865958 IC50 = 10000.0 nM 5.00
CHEMBL4854219 IC50 = 11000.0 nM 4.96
CHEMBL4848759 IC50 = 11000.0 nM 4.96
CHEMBL4873906 IC50 = 13000.0 nM 4.89
CHEMBL111654 2-MERCAPTOBENZOTHIAZOLE IC50 = 13000.0 nM 4.89
CHEMBL4877097 IC50 = 15000.0 nM 4.82
CHEMBL4858265 IC50 = 16000.0 nM 4.80
CHEMBL113414 IC50 = 17000.0 nM 4.77
CHEMBL4875943 IC50 = 18000.0 nM 4.75
CHEMBL4852689 IC50 = 20000.0 nM 4.70
CHEMBL4866283 IC50 = 26000.0 nM 4.58
CHEMBL4868002 IC50 = 27000.0 nM 4.57
CHEMBL4864399 IC50 = 28000.0 nM 4.55
CHEMBL4856216 IC50 = 30000.0 nM 4.52
CHEMBL1456330 IC50 = 32000.0 nM 4.50
CHEMBL4875672 IC50 = 36000.0 nM 4.44
CHEMBL4854026 IC50 = 43000.0 nM 4.37
CHEMBL4869230 IC50 = 49000.0 nM 4.31
CHEMBL4876125 IC50 = 60000.0 nM 4.22
CHEMBL69086 IC50 = 62000.0 nM 4.21
CHEMBL4859482 IC50 = 65000.0 nM 4.19
CHEMBL4875334 IC50 = 67000.0 nM 4.17
CHEMBL4872203 IC50 = 75000.0 nM 4.12
CHEMBL4856015 IC50 = 79000.0 nM 4.10
CHEMBL4857254 IC50 = 81000.0 nM 4.09
CHEMBL4873052 IC50 = 83000.0 nM 4.08
CHEMBL4861417 IC50 = 85000.0 nM 4.07
CHEMBL227086 IC50 = 94000.0 nM 4.03
CHEMBL4867840 IC50 = 95000.0 nM 4.02
CHEMBL99703 IC50 = 96000.0 nM 4.02
CHEMBL4877930 IC50 = 109000.0 nM 3.96
CHEMBL70141 2-MERCAPTOBENZIMIDAZOLE IC50 = 114000.0 nM 3.94
CHEMBL4877640 IC50 = 130000.0 nM 3.89
CHEMBL4876262 IC50 = 129000.0 nM 3.89
CHEMBL4868196 IC50 = 149000.0 nM 3.83
CHEMBL4877725 IC50 = 156000.0 nM 3.81
CHEMBL1580977 IC50 - -