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Assay Detail

CHEMBL2034202

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

Binding
Inhibition of trypsin-like activity of proteasome by fluorogenic assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Proteasome
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors.
Ge Y, Kazi A, Marsilio F, Luo Y, Jain S, Brooks W, Daniel KG, Guida WC, Sebti SM, Lawrence HR.
J Med Chem (2012) 55 : 1978 -1998
PubMed 22220566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.76 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030283 1 6.70
CHEMBL2030453 1 6.26
CHEMBL2030462 1 6.24
CHEMBL2030461 1 6.12
CHEMBL2030464 1 5.96
CHEMBL2030465 1 5.94
CHEMBL2030458 1 5.89
CHEMBL2030459 1 5.87
CHEMBL2030463 1 5.86
CHEMBL2030460 1 5.84
CHEMBL2030454 1 5.81
CHEMBL2030455 1 5.73
CHEMBL2030281 1 5.70
CHEMBL2030457 1 5.70
CHEMBL2030275 1 5.63
CHEMBL2030276 1 5.62
CHEMBL2030456 1 5.55
CHEMBL2030278 1 5.38
CHEMBL2030274 1 5.38
CHEMBL2030284 1 5.32
CHEMBL2030277 1 5.16
CHEMBL2030279 1 5.14
CHEMBL2030282 1 -
CHEMBL2030269 1 -
CHEMBL2030280 1 -
CHEMBL2030273 1 -
CHEMBL2030272 1 -
CHEMBL2030271 1 -
CHEMBL2030270 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030283 IC50 = 200.0 nM 6.70
CHEMBL2030453 IC50 = 550.0 nM 6.26
CHEMBL2030462 IC50 = 570.0 nM 6.24
CHEMBL2030461 IC50 = 750.0 nM 6.12
CHEMBL2030464 IC50 = 1100.0 nM 5.96
CHEMBL2030465 IC50 = 1140.0 nM 5.94
CHEMBL2030458 IC50 = 1300.0 nM 5.89
CHEMBL2030459 IC50 = 1350.0 nM 5.87
CHEMBL2030463 IC50 = 1380.0 nM 5.86
CHEMBL2030460 IC50 = 1450.0 nM 5.84
CHEMBL2030454 IC50 = 1550.0 nM 5.81
CHEMBL2030455 IC50 = 1850.0 nM 5.73
CHEMBL2030281 IC50 = 2000.0 nM 5.70
CHEMBL2030457 IC50 = 2000.0 nM 5.70
CHEMBL2030275 IC50 = 2350.0 nM 5.63
CHEMBL2030276 IC50 = 2370.0 nM 5.62
CHEMBL2030456 IC50 = 2800.0 nM 5.55
CHEMBL2030278 IC50 = 4200.0 nM 5.38
CHEMBL2030274 IC50 = 4220.0 nM 5.38
CHEMBL2030284 IC50 = 4800.0 nM 5.32
CHEMBL2030277 IC50 = 7000.0 nM 5.16
CHEMBL2030279 IC50 = 7200.0 nM 5.14
CHEMBL2030282 IC50 - -
CHEMBL2030269 IC50 - -
CHEMBL2030280 IC50 - -
CHEMBL2030273 IC50 - -
CHEMBL2030272 IC50 - -
CHEMBL2030271 IC50 - -
CHEMBL2030270 IC50 - -