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Assay Detail

CHEMBL5588326

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

Binding
Activation of human recombinant his-sumo tagged ClpP expressed in Escherichia coli BL21 (DE3) using FITC-casein as substrate preincubated for 30 mins followed by substrate addition and measured every 60 secs for 30 mins by fluorescence based microplate reader analysis
20
Total Activities
20
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

Publication

Discovery of Dehydrogenated Imipridone Derivatives as Activators of Human Caseinolytic Protease P.
Jiang J, Xie G, Li T, Ding H, Tang R, Luo J, Li Q, Lu W, Xiao Y, Sun H.
J Med Chem (2024) 67 : 15328 -15352
PubMed 39172943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.57 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5597011 1 7.10
CHEMBL5596220 1 7.05
CHEMBL5597441 1 7.05
CHEMBL5596597 1 6.92
CHEMBL5598515 1 6.89
CHEMBL5597008 1 6.89
CHEMBL5597414 1 6.85
CHEMBL5597713 1 6.64
CHEMBL5598503 1 6.62
CHEMBL5597740 1 6.58
CHEMBL5596563 1 6.58
CHEMBL5596404 1 6.50
CHEMBL5287669 1 6.41
CHEMBL5596606 1 6.38
CHEMBL5590920 1 6.32
CHEMBL5598320 1 6.28
CHEMBL4650311 ONC-206 1.0 1 6.25
CHEMBL5597516 1 6.16
CHEMBL5596968 1 6.07
CHEMBL4297310 DORDAVIPRONE 3.0 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5597011 EC50 = 80.0 nM 7.10
CHEMBL5596220 EC50 = 90.0 nM 7.05
CHEMBL5597441 EC50 = 90.0 nM 7.05
CHEMBL5596597 EC50 = 120.0 nM 6.92
CHEMBL5598515 EC50 = 130.0 nM 6.89
CHEMBL5597008 EC50 = 130.0 nM 6.89
CHEMBL5597414 EC50 = 140.0 nM 6.85
CHEMBL5597713 EC50 = 230.0 nM 6.64
CHEMBL5598503 EC50 = 240.0 nM 6.62
CHEMBL5597740 EC50 = 260.0 nM 6.58
CHEMBL5596563 EC50 = 260.0 nM 6.58
CHEMBL5596404 EC50 = 320.0 nM 6.50
CHEMBL5287669 EC50 = 390.0 nM 6.41
CHEMBL5596606 EC50 = 420.0 nM 6.38
CHEMBL5590920 EC50 = 480.0 nM 6.32
CHEMBL5598320 EC50 = 530.0 nM 6.28
CHEMBL4650311 ONC-206 EC50 = 560.0 nM 6.25
CHEMBL5597516 EC50 = 700.0 nM 6.16
CHEMBL5596968 EC50 = 850.0 nM 6.07
CHEMBL4297310 DORDAVIPRONE EC50 = 1720.0 nM 5.76