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Assay Detail

CHEMBL3796231

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

Binding
Inhibition of chymotrypsin like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by spectrofluorimetric analysis
ChEMBL ↗
85
Total Activities
45
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

3D-QSAR-aided design, synthesis, in vitro and in vivo evaluation of dipeptidyl boronic acid proteasome inhibitors and mechanism studies.
Lei M, Feng H, Wang C, Li H, Shi J, Wang J, Liu Z, Chen S, Hu S, Zhu Y.
Bioorg Med Chem (2016) 24 : 2576 -2588
PubMed 27117691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 85 8.23 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3793848 — — 2 9.12
CHEMBL3794168 — — 2 8.95
CHEMBL3793581 — — 2 8.94
CHEMBL3793238 — — 2 8.94
CHEMBL3794310 — — 2 8.94
CHEMBL499361 — — 2 8.92
CHEMBL3794136 — — 2 8.90
CHEMBL3794207 — — 2 8.87
CHEMBL3793242 — — 2 8.84
CHEMBL499504 — — 2 8.80
CHEMBL606394 — — 2 8.72
CHEMBL3792511 — — 2 8.72
CHEMBL325041 BORTEZOMIB 3.0 2 8.72
CHEMBL3792573 — — 2 8.63
CHEMBL3793093 — — 2 8.61
CHEMBL3793863 — — 2 8.56
CHEMBL3792854 — — 2 8.49
CHEMBL3793683 — — 2 8.48
CHEMBL3793066 — — 2 8.47
CHEMBL3794171 — — 2 8.44
CHEMBL3793344 — — 2 8.38
CHEMBL1169560 — — 2 8.37
CHEMBL499083 — — 2 8.36
CHEMBL3793107 — — 1 8.34
CHEMBL3794440 — — 2 8.31
CHEMBL3792730 — — 2 8.29
CHEMBL3793876 — — 2 8.28
CHEMBL3792602 — — 2 8.21
CHEMBL3792587 — — 2 8.17
CHEMBL3793192 — — 2 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3793848 — IC50 = 0.76 nM 9.12
CHEMBL3794168 — IC50 = 1.12 nM 8.95
CHEMBL3793581 — IC50 = 1.15 nM 8.94
CHEMBL3793238 — IC50 = 1.16 nM 8.94
CHEMBL3794310 — IC50 = 1.16 nM 8.94
CHEMBL499361 — IC50 = 1.2 nM 8.92
CHEMBL3794136 — IC50 = 1.26 nM 8.90
CHEMBL3794207 — IC50 = 1.34 nM 8.87
CHEMBL3793242 — IC50 = 1.46 nM 8.84
CHEMBL499504 — IC50 = 1.6 nM 8.80
CHEMBL606394 — IC50 = 1.92 nM 8.72
CHEMBL3792511 — IC50 = 1.92 nM 8.72
CHEMBL325041 BORTEZOMIB IC50 = 1.9 nM 8.72
CHEMBL3792573 — IC50 = 2.34 nM 8.63
CHEMBL3793093 — IC50 = 2.46 nM 8.61
CHEMBL3793863 — IC50 = 2.73 nM 8.56
CHEMBL3792854 — IC50 = 3.21 nM 8.49
CHEMBL3793683 — IC50 = 3.34 nM 8.48
CHEMBL3793066 — IC50 = 3.37 nM 8.47
CHEMBL3794171 — IC50 = 3.67 nM 8.44
CHEMBL3793344 — IC50 = 4.18 nM 8.38
CHEMBL1169560 — IC50 = 4.26 nM 8.37
CHEMBL499083 — IC50 = 4.37 nM 8.36
CHEMBL3793107 — IC50 = 4.6 nM 8.34
CHEMBL3794440 — IC50 = 4.85 nM 8.31
CHEMBL3792730 — IC50 = 5.17 nM 8.29
CHEMBL3793876 — IC50 = 5.24 nM 8.28
CHEMBL3792602 — IC50 = 6.12 nM 8.21
CHEMBL3792587 — IC50 = 6.7 nM 8.17
CHEMBL3793192 — IC50 = 6.96 nM 8.16
CHEMBL1169561 — IC50 = 7.63 nM 8.12
CHEMBL3794347 — IC50 = 8.32 nM 8.08
CHEMBL3794303 — IC50 = 8.46 nM 8.07
CHEMBL3792405 — IC50 = 14.2 nM 7.85
CHEMBL3793068 — IC50 = 16.4 nM 7.79
CHEMBL3794131 — IC50 = 17.2 nM 7.76
CHEMBL3793540 — IC50 = 25.02 nM 7.60
CHEMBL3794075 — IC50 = 26.24 nM 7.58
CHEMBL3792403 — IC50 = 39.0 nM 7.41
CHEMBL3794482 — IC50 = 41.2 nM 7.38
CHEMBL3792495 — IC50 = 42.61 nM 7.37
CHEMBL3793633 — IC50 = 49.5 nM 7.30
CHEMBL3793665 — IC50 = 114.0 nM 6.94
CHEMBL3793010 — IC50 = 120.2 nM 6.92
CHEMBL3792846 — IC50 = 471.0 nM 6.33
CHEMBL3794207 — IC50 = 741310241.3 nM -
CHEMBL3793848 — IC50 = 758577575.03 nM -
CHEMBL3793093 — IC50 = 407380277.8 nM -
CHEMBL3794310 — IC50 = 862978547.77 nM -
CHEMBL3794303 — IC50 = 117489755.49 nM -