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Assay Detail

CHEMBL4370445

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Binding
Inhibition of 20S constitutive proteasome beta 2 trypsin-like activity (unknown origin) by cell based ABPP assay
ChEMBL ↗
52
Total Activities
50
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 (CHEMBL3492) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits.
Xin BT, Huber EM, de Bruin G, Heinemeyer W, Maurits E, Espinal C, Du Y, Janssens M, Weyburne ES, Kisselev AF, Florea BI, Driessen C, van der Marel GA, Groll M, Overkleeft HS.
J Med Chem (2019) 62 : 1626 -1642
PubMed 30657666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.90 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4458756 — — 1 8.10
CHEMBL4590398 — — 1 8.10
CHEMBL4451682 — — 1 8.00
CHEMBL4440581 — — 1 7.96
CHEMBL4463326 — — 1 7.96
CHEMBL4471150 — — 1 7.89
CHEMBL4515041 — — 1 7.80
CHEMBL4550571 — — 1 7.77
CHEMBL4444586 — — 1 7.77
CHEMBL4450505 — — 1 7.75
CHEMBL4542603 — — 1 7.68
CHEMBL4471154 — — 1 7.64
CHEMBL4546121 — — 1 7.58
CHEMBL4549724 — — 1 7.54
CHEMBL4435519 — — 1 7.51
CHEMBL4457630 — — 1 7.50
CHEMBL4543211 — — 1 7.46
CHEMBL4467279 — — 1 7.46
CHEMBL4446148 — — 1 7.40
CHEMBL4465228 — — 1 7.39
CHEMBL4589564 — — 1 7.37
CHEMBL4455846 — — 1 7.33
CHEMBL4463454 — — 1 7.16
CHEMBL4539247 — — 1 7.14
CHEMBL4545073 — — 1 7.14
CHEMBL4565730 — — 1 7.14
CHEMBL4456245 — — 1 7.01
CHEMBL4442052 — — 2 7.00
CHEMBL4592602 — — 1 6.80
CHEMBL4447665 — — 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4458756 — IC50 = 8.0 nM 8.10
CHEMBL4590398 — IC50 = 8.0 nM 8.10
CHEMBL4451682 — IC50 = 10.0 nM 8.00
CHEMBL4440581 — IC50 = 11.0 nM 7.96
CHEMBL4463326 — IC50 = 11.0 nM 7.96
CHEMBL4471150 — IC50 = 13.0 nM 7.89
CHEMBL4515041 — IC50 = 16.0 nM 7.80
CHEMBL4550571 — IC50 = 17.0 nM 7.77
CHEMBL4444586 — IC50 = 17.0 nM 7.77
CHEMBL4450505 — IC50 = 18.0 nM 7.75
CHEMBL4542603 — IC50 = 21.0 nM 7.68
CHEMBL4471154 — IC50 = 23.0 nM 7.64
CHEMBL4546121 — IC50 = 26.0 nM 7.58
CHEMBL4549724 — IC50 = 29.0 nM 7.54
CHEMBL4435519 — IC50 = 31.0 nM 7.51
CHEMBL4457630 — IC50 = 32.0 nM 7.50
CHEMBL4543211 — IC50 = 35.0 nM 7.46
CHEMBL4467279 — IC50 = 35.0 nM 7.46
CHEMBL4446148 — IC50 = 40.0 nM 7.40
CHEMBL4465228 — IC50 = 41.0 nM 7.39
CHEMBL4589564 — IC50 = 43.0 nM 7.37
CHEMBL4455846 — IC50 = 47.0 nM 7.33
CHEMBL4463454 — IC50 = 69.0 nM 7.16
CHEMBL4565730 — IC50 = 72.0 nM 7.14
CHEMBL4539247 — IC50 = 73.0 nM 7.14
CHEMBL4545073 — IC50 = 72.0 nM 7.14
CHEMBL4456245 — IC50 = 97.0 nM 7.01
CHEMBL4442052 — IC50 = 100.0 nM 7.00
CHEMBL4592602 — IC50 = 160.0 nM 6.80
CHEMBL4447665 — IC50 = 210.0 nM 6.68
CHEMBL4450180 — IC50 = 210.0 nM 6.68
CHEMBL4577205 — IC50 = 215.0 nM 6.67
CHEMBL4532362 — IC50 = 240.0 nM 6.62
CHEMBL4436388 — IC50 = 265.0 nM 6.58
CHEMBL4442929 — IC50 = 280.0 nM 6.55
CHEMBL4438722 — IC50 = 290.0 nM 6.54
CHEMBL4446214 — IC50 = 320.0 nM 6.50
CHEMBL4541019 — IC50 = 380.0 nM 6.42
CHEMBL4568958 — IC50 = 510.0 nM 6.29
CHEMBL4444390 — IC50 = 2250.0 nM 5.65
CHEMBL4468562 — IC50 = 2750.0 nM 5.56
CHEMBL4445642 — IC50 = 2800.0 nM 5.55
CHEMBL4565742 — IC50 = 3100.0 nM 5.51
CHEMBL4581629 — IC50 = 3350.0 nM 5.47
CHEMBL4441494 — IC50 = 3600.0 nM 5.44
CHEMBL4461986 — IC50 = 4850.0 nM 5.31
CHEMBL4436388 — IC50 = 5000.0 nM 5.30
CHEMBL4533222 — IC50 = 5530.0 nM 5.26
CHEMBL4539341 — IC50 = 8400.0 nM 5.08
CHEMBL4442052 — IC50 > 10000.0 nM -