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Assay Detail

CHEMBL1001485

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

Binding
Inhibition of SDS-activated 20S proteasome activity in rabbit muscle
ChEMBL ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Muscle tissue
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

3D-QSAR studies of boron-containing dipeptides as proteasome inhibitors with CoMFA and CoMSIA methods.
Zhu YQ, Lei M, Lu AJ, Zhao X, Yin XJ, Gao QZ.
Eur J Med Chem (2009) 44 : 1486 -1499
PubMed 18771818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 58 8.87 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485865 — — 1 10.52
CHEMBL519164 — — 1 10.12
CHEMBL520452 — — 1 10.08
CHEMBL484282 — — 1 10.06
CHEMBL446205 — — 1 10.00
CHEMBL520966 — — 1 9.89
CHEMBL484701 — — 1 9.85
CHEMBL483482 — — 1 9.85
CHEMBL483063 — — 1 9.85
CHEMBL484286 — — 1 9.82
CHEMBL483062 — — 1 9.82
CHEMBL2304766 — — 1 9.82
CHEMBL487920 — — 1 9.77
CHEMBL482658 — — 1 9.77
CHEMBL485649 — — 1 9.77
CHEMBL484687 — — 1 9.72
CHEMBL482870 — — 1 9.70
CHEMBL527210 — — 1 9.64
CHEMBL483060 — — 1 9.60
CHEMBL482450 — — 1 9.55
CHEMBL483266 — — 1 9.38
CHEMBL490256 — — 1 9.29
CHEMBL325041 BORTEZOMIB 3.0 1 9.22
CHEMBL2304744 — — 1 9.14
CHEMBL519975 — — 1 9.12
CHEMBL482630 — — 1 9.09
CHEMBL2304777 — — 1 9.08
CHEMBL520965 — — 1 9.02
CHEMBL483275 — — 1 9.02
CHEMBL487918 — — 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485865 — Ki = 0.0302 nM 10.52
CHEMBL519164 — Ki = 0.07586 nM 10.12
CHEMBL520452 — Ki = 0.08318 nM 10.08
CHEMBL484282 — Ki = 0.0871 nM 10.06
CHEMBL446205 — Ki = 0.1 nM 10.00
CHEMBL520966 — Ki = 0.1288 nM 9.89
CHEMBL484701 — Ki = 0.1413 nM 9.85
CHEMBL483482 — Ki = 0.1413 nM 9.85
CHEMBL483063 — Ki = 0.1413 nM 9.85
CHEMBL484286 — Ki = 0.1514 nM 9.82
CHEMBL483062 — Ki = 0.1514 nM 9.82
CHEMBL2304766 — Ki = 0.1514 nM 9.82
CHEMBL485649 — Ki = 0.1698 nM 9.77
CHEMBL482658 — Ki = 0.1698 nM 9.77
CHEMBL487920 — Ki = 0.1698 nM 9.77
CHEMBL484687 — Ki = 0.1905 nM 9.72
CHEMBL482870 — Ki = 0.1995 nM 9.70
CHEMBL527210 — Ki = 0.2291 nM 9.64
CHEMBL483060 — Ki = 0.2512 nM 9.60
CHEMBL482450 — Ki = 0.2818 nM 9.55
CHEMBL483266 — Ki = 0.4169 nM 9.38
CHEMBL490256 — Ki = 0.5129 nM 9.29
CHEMBL325041 BORTEZOMIB Ki = 0.6026 nM 9.22
CHEMBL2304744 — Ki = 0.7244 nM 9.14
CHEMBL519975 — Ki = 0.7586 nM 9.12
CHEMBL482630 — Ki = 0.8128 nM 9.09
CHEMBL2304777 — Ki = 0.8318 nM 9.08
CHEMBL520965 — Ki = 0.955 nM 9.02
CHEMBL483275 — Ki = 0.955 nM 9.02
CHEMBL487918 — Ki = 1.096 nM 8.96
CHEMBL484903 — Ki = 1.096 nM 8.96
CHEMBL490257 — Ki = 1.288 nM 8.89
CHEMBL520310 — Ki = 1.288 nM 8.89
CHEMBL483061 — Ki = 1.413 nM 8.85
CHEMBL2304846 — Ki = 1.698 nM 8.77
CHEMBL484082 — Ki = 1.995 nM 8.70
CHEMBL484081 — Ki = 2.188 nM 8.66
CHEMBL484688 — Ki = 2.188 nM 8.66
CHEMBL488939 — Ki = 2.818 nM 8.55
CHEMBL482641 — Ki = 3.02 nM 8.52
CHEMBL484285 — Ki = 3.02 nM 8.52
CHEMBL2304742 — Ki = 3.89 nM 8.41
CHEMBL520139 — Ki = 4.365 nM 8.36
CHEMBL445542 — Ki = 5.37 nM 8.27
CHEMBL483286 — Ki = 5.754 nM 8.24
CHEMBL520618 — Ki = 6.026 nM 8.22
CHEMBL450116 — Ki = 6.31 nM 8.20
CHEMBL520295 — Ki = 6.31 nM 8.20
CHEMBL483273 — Ki = 7.079 nM 8.15
CHEMBL490055 — Ki = 7.586 nM 8.12