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Assay Detail

CHEMBL5733757

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Binding
Determination of Beta5 Activity: Measurement of Beta5 inhibition is performed in 384 well format based on fluorescence intensity assay.Purified human constitutive proteasome (1.25 nM) and serial diluted compounds in DMSO (range of concentrations from 30 μM to 15 μM) or controls are incubated for 20 minutes at 25° C. in assay buffer containing 50 mM Tris pH 7.4, 0.03% SDS, 1 mM EDTA and 1% DMSO. The reaction is initiated by the addition of the fluorogenic peptide substrate, Suc-LLVY-AMC (Bachem 1-1395), at a concentration of 40 μM. After 60 minutes of incubation at 37° C., fluorescence intensity is measured at λex=350 nm and λem=450 nm with a fluorescence reader (Perkin Elmer Envision reader or equivalent).
ChEMBL ↗
408
Total Activities
135
Compounds Tested
3
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

Substituted boronic acids and boronate esters as immunoproteasome inhibitors
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 136 5.92 6.56
kon 136 - -
k_off 136 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5790819 — — 3 6.56
CHEMBL5952321 — — 3 6.56
CHEMBL5749544 — — 3 6.56
CHEMBL6037298 — — 3 6.56
CHEMBL5913340 — — 3 6.56
CHEMBL5808438 — — 3 6.56
CHEMBL5792961 — — 3 6.56
CHEMBL5825213 — — 3 6.56
CHEMBL6014336 — — 3 6.56
CHEMBL5880539 — — 3 6.56
CHEMBL5823614 — — 3 6.56
CHEMBL5850280 — — 3 6.56
CHEMBL5781322 — — 3 6.56
CHEMBL5784483 — — 3 6.56
CHEMBL5790523 — — 3 6.56
CHEMBL5805387 — — 3 6.56
CHEMBL5813052 — — 3 6.56
CHEMBL5190088 — — 3 6.56
CHEMBL5174892 — — 3 6.56
CHEMBL5894027 — — 3 6.56
CHEMBL5927929 — — 3 6.56
CHEMBL5767445 — — 3 6.56
CHEMBL6004747 — — 3 6.56
CHEMBL5966663 — — 3 6.56
CHEMBL5892751 — — 3 6.56
CHEMBL5170541 — — 3 6.56
CHEMBL5175217 — — 3 6.56
CHEMBL6058604 — — 3 6.56
CHEMBL6049906 — — 3 6.56
CHEMBL5990732 — — 3 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5175217 — IC50 = 275.0 nM 6.56
CHEMBL6004747 — IC50 = 275.0 nM 6.56
CHEMBL5823614 — IC50 = 275.0 nM 6.56
CHEMBL5913340 — IC50 = 275.0 nM 6.56
CHEMBL5966663 — IC50 = 275.0 nM 6.56
CHEMBL5880539 — IC50 = 275.0 nM 6.56
CHEMBL5892751 — IC50 = 275.0 nM 6.56
CHEMBL5170541 — IC50 = 275.0 nM 6.56
CHEMBL5808438 — IC50 = 275.0 nM 6.56
CHEMBL5790819 — IC50 = 275.0 nM 6.56
CHEMBL5910598 — IC50 = 275.0 nM 6.56
CHEMBL5825213 — IC50 = 275.0 nM 6.56
CHEMBL5990732 — IC50 = 275.0 nM 6.56
CHEMBL5792961 — IC50 = 275.0 nM 6.56
CHEMBL6049906 — IC50 = 275.0 nM 6.56
CHEMBL6014336 — IC50 = 275.0 nM 6.56
CHEMBL6058604 — IC50 = 275.0 nM 6.56
CHEMBL6037298 — IC50 = 275.0 nM 6.56
CHEMBL5805387 — IC50 = 275.0 nM 6.56
CHEMBL5813052 — IC50 = 275.0 nM 6.56
CHEMBL5790523 — IC50 = 275.0 nM 6.56
CHEMBL5190088 — IC50 = 275.0 nM 6.56
CHEMBL5930810 — IC50 = 275.0 nM 6.56
CHEMBL5952321 — IC50 = 275.0 nM 6.56
CHEMBL5784483 — IC50 = 275.0 nM 6.56
CHEMBL5174892 — IC50 = 275.0 nM 6.56
CHEMBL5781322 — IC50 = 275.0 nM 6.56
CHEMBL5185591 — IC50 = 275.0 nM 6.56
CHEMBL5850280 — IC50 = 275.0 nM 6.56
CHEMBL5894027 — IC50 = 275.0 nM 6.56
CHEMBL5749544 — IC50 = 275.0 nM 6.56
CHEMBL5927929 — IC50 = 275.0 nM 6.56
CHEMBL5767445 — IC50 = 275.0 nM 6.56
CHEMBL5196780 — IC50 = 275.0 nM 6.56
CHEMBL5749561 — IC50 = 2750.0 nM 5.56
CHEMBL5980168 — IC50 = 2750.0 nM 5.56
CHEMBL5899725 — IC50 = 2750.0 nM 5.56
CHEMBL6033633 — IC50 = 2750.0 nM 5.56
CHEMBL5812694 — IC50 = 2750.0 nM 5.56
CHEMBL6033738 — IC50 = 2750.0 nM 5.56
CHEMBL5874400 — IC50 = 2750.0 nM 5.56
CHEMBL5997384 — IC50 = 2750.0 nM 5.56
CHEMBL5185756 — IC50 = 2750.0 nM 5.56
CHEMBL6002998 — IC50 = 2750.0 nM 5.56
CHEMBL5908786 — IC50 = 2750.0 nM 5.56
CHEMBL6042926 — IC50 = 2750.0 nM 5.56
CHEMBL6025208 — IC50 = 2750.0 nM 5.56
CHEMBL5928304 — IC50 = 2750.0 nM 5.56
CHEMBL5816234 — IC50 = 2750.0 nM 5.56
CHEMBL5742606 — IC50 = 2750.0 nM 5.56