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Assay Detail

CHEMBL4333216

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

Binding
Activation of Keap1/Cul3/Nrf2 in human BEAS2B cells assessed as increase in NQO1 levels measured after 48 hrs
8
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.
Boehm J, Davis R, Murar CE, Li T, McCleland B, Dong S, Yan H, Kerns J, Moody CJ, Wilson AJ, Graves AP, Mentzer M, Qi H, Yonchuk J, Kou JP, Foley J, Sanchez Y, Podolin PL, Bolognese B, Booth-Genthe C, Galop M, Wolfe L, Carr R, Callahan JF.
Bioorg Med Chem (2019) 27 : 579 -588
PubMed 30626555 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.10 8.06
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762621 BARDOXOLONE METHYL 3.0 1 8.06
CHEMBL4573284 1 5.80
CHEMBL4245297 1 5.80
CHEMBL4554334 1 5.80
CHEMBL4514848 1 5.80
CHEMBL4474353 2 5.78
CHEMBL48802 SULFORAPHANE 3.0 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762621 BARDOXOLONE METHYL EC50 = 8.71 nM 8.06
CHEMBL4573284 EC50 = 1584.89 nM 5.80
CHEMBL4245297 EC50 = 1584.89 nM 5.80
CHEMBL4554334 EC50 = 1584.89 nM 5.80
CHEMBL4514848 EC50 = 1584.89 nM 5.80
CHEMBL4474353 EC50 = 1659.59 nM 5.78
CHEMBL48802 SULFORAPHANE EC50 = 2089.3 nM 5.68
CHEMBL4474353 Activity - -