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Assay Detail

CHEMBL615354

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Binding
Inhibition of chymotrypsin-like activity of 20S proteasome
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 2 — Organism
Curated By Expert

Target

Proteasome (CHEMBL612443)
Type SUBCELLULAR

Publication

Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.
Lum RT, Nelson MG, Joly A, Horsma AG, Lee G, Meyer SM, Wick MM, Schow SR.
Bioorg Med Chem Lett (1998) 8 : 209 -214
PubMed 9871656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.05 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67885 1 6.85
CHEMBL304784 1 6.82
CHEMBL66044 1 6.70
CHEMBL409140 1 6.47
CHEMBL70065 1 6.31
CHEMBL70075 1 6.15
CHEMBL303651 1 6.05
CHEMBL305527 1 6.03
CHEMBL303973 1 5.72
CHEMBL304822 1 5.66
CHEMBL67617 1 5.06
CHEMBL68747 1 4.80
CHEMBL303505 1 -
CHEMBL65851 1 -
CHEMBL420362 1 -
CHEMBL66696 1 -
CHEMBL431170 1 -
CHEMBL66580 1 -
CHEMBL307565 1 -
CHEMBL308888 1 -
CHEMBL305474 1 -
CHEMBL70171 1 -
CHEMBL69001 1 -
CHEMBL69112 1 -
CHEMBL303215 1 -
CHEMBL302082 1 -
CHEMBL69100 1 -
CHEMBL302813 1 -
CHEMBL66282 1 -
CHEMBL65787 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67885 IC50 = 140.0 nM 6.85
CHEMBL304784 IC50 = 150.0 nM 6.82
CHEMBL66044 IC50 = 200.0 nM 6.70
CHEMBL409140 IC50 = 340.0 nM 6.47
CHEMBL70065 IC50 = 490.0 nM 6.31
CHEMBL70075 IC50 = 710.0 nM 6.15
CHEMBL303651 IC50 = 890.0 nM 6.05
CHEMBL305527 IC50 = 930.0 nM 6.03
CHEMBL303973 IC50 = 1900.0 nM 5.72
CHEMBL304822 IC50 = 2200.0 nM 5.66
CHEMBL67617 IC50 = 8700.0 nM 5.06
CHEMBL68747 IC50 = 16000.0 nM 4.80
CHEMBL304969 IC50 > 20000.0 nM -
CHEMBL304751 IC50 > 20000.0 nM -
CHEMBL303449 IC50 > 20000.0 nM -
CHEMBL65845 IC50 > 18000.0 nM -
CHEMBL69633 IC50 > 16000.0 nM -
CHEMBL303505 IC50 > 20000.0 nM -
CHEMBL65851 IC50 > 20000.0 nM -
CHEMBL420362 IC50 > 20000.0 nM -
CHEMBL66696 IC50 > 20000.0 nM -
CHEMBL431170 IC50 > 16000.0 nM -
CHEMBL66580 IC50 > 20000.0 nM -
CHEMBL307565 IC50 > 20000.0 nM -
CHEMBL308888 IC50 > 18000.0 nM -
CHEMBL305474 IC50 > 19000.0 nM -
CHEMBL70171 IC50 > 16000.0 nM -
CHEMBL69001 IC50 > 20000.0 nM -
CHEMBL69112 IC50 > 20000.0 nM -
CHEMBL303215 IC50 > 20000.0 nM -
CHEMBL302082 IC50 > 17000.0 nM -
CHEMBL69100 IC50 > 18000.0 nM -
CHEMBL302813 IC50 > 18000.0 nM -
CHEMBL66282 IC50 > 20000.0 nM -
CHEMBL65787 IC50 > 20000.0 nM -