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Assay Detail

CHEMBL2034200

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Binding
Inhibition of chymotrypsin-like activity of proteasome by fluorogenic assay
ChEMBL ↗
43
Total Activities
43
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 43 6.18 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030278 — — 1 6.82
CHEMBL2030276 — — 1 6.75
CHEMBL2030284 — — 1 6.66
CHEMBL2030458 — — 1 6.66
CHEMBL2030453 — — 1 6.64
CHEMBL2030455 — — 1 6.64
CHEMBL2030457 — — 1 6.64
CHEMBL2030274 — — 1 6.55
CHEMBL2030281 — — 1 6.52
CHEMBL2030277 — — 1 6.52
CHEMBL2030459 — — 1 6.40
CHEMBL2030456 — — 1 6.40
CHEMBL2030460 — — 1 6.33
CHEMBL2030454 — — 1 6.32
CHEMBL2030283 — — 1 6.29
CHEMBL2030462 — — 1 6.27
CHEMBL2030461 — — 1 6.24
CHEMBL2030463 — — 1 6.22
CHEMBL2030464 — — 1 6.20
CHEMBL2030282 — — 1 6.19
CHEMBL2030275 — — 1 6.14
CHEMBL2030465 — — 1 6.06
CHEMBL2030269 — — 1 5.79
CHEMBL2030280 — — 1 5.71
CHEMBL2030279 — — 1 5.61
CHEMBL2030270 — — 1 5.52
CHEMBL2030273 — — 1 5.39
CHEMBL2030271 — — 1 5.38
CHEMBL2030272 — — 1 5.38
CHEMBL2030466 — — 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030278 — IC50 = 150.0 nM 6.82
CHEMBL2030276 — IC50 = 180.0 nM 6.75
CHEMBL2030458 — IC50 = 220.0 nM 6.66
CHEMBL2030284 — IC50 = 220.0 nM 6.66
CHEMBL2030453 — IC50 = 230.0 nM 6.64
CHEMBL2030455 — IC50 = 230.0 nM 6.64
CHEMBL2030457 — IC50 = 230.0 nM 6.64
CHEMBL2030274 — IC50 = 280.0 nM 6.55
CHEMBL2030281 — IC50 = 300.0 nM 6.52
CHEMBL2030277 — IC50 = 300.0 nM 6.52
CHEMBL2030459 — IC50 = 400.0 nM 6.40
CHEMBL2030456 — IC50 = 400.0 nM 6.40
CHEMBL2030460 — IC50 = 470.0 nM 6.33
CHEMBL2030454 — IC50 = 480.0 nM 6.32
CHEMBL2030283 — IC50 = 510.0 nM 6.29
CHEMBL2030462 — IC50 = 540.0 nM 6.27
CHEMBL2030461 — IC50 = 570.0 nM 6.24
CHEMBL2030463 — IC50 = 600.0 nM 6.22
CHEMBL2030464 — IC50 = 630.0 nM 6.20
CHEMBL2030282 — IC50 = 650.0 nM 6.19
CHEMBL2030275 — IC50 = 730.0 nM 6.14
CHEMBL2030465 — IC50 = 880.0 nM 6.06
CHEMBL2030269 — IC50 = 1610.0 nM 5.79
CHEMBL2030280 — IC50 = 1970.0 nM 5.71
CHEMBL2030279 — IC50 = 2470.0 nM 5.61
CHEMBL2030270 — IC50 = 3000.0 nM 5.52
CHEMBL2030273 — IC50 = 4050.0 nM 5.39
CHEMBL2030271 — IC50 = 4200.0 nM 5.38
CHEMBL2030272 — IC50 = 4200.0 nM 5.38
CHEMBL2030466 — IC50 = 5700.0 nM 5.24
CHEMBL2030467 — IC50 > 10000.0 nM -
CHEMBL1342041 — IC50 > 30000.0 nM -
CHEMBL2030468 — IC50 > 30000.0 nM -
CHEMBL2030469 — IC50 > 30000.0 nM -
CHEMBL2030470 — IC50 > 30000.0 nM -
CHEMBL2030471 — IC50 > 100000.0 nM -
CHEMBL2030472 — IC50 > 100000.0 nM -
CHEMBL2030473 — IC50 > 5000.0 nM -
CHEMBL2030474 — IC50 > 5000.0 nM -
CHEMBL2030475 — IC50 > 5000.0 nM -
CHEMBL2030477 — IC50 > 5000.0 nM -
CHEMBL2030476 — IC50 > 5000.0 nM -
CHEMBL2030478 — IC50 > 100.0 nM -