Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4734695

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

Functional
Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
15
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type L929
Confidence 1 — Organism
Curated By Autocuration

Target

L929 (CHEMBL612267)
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors.
Wang Y,Ma H,Huang J,Yao Z,Yu J,Zhang W,Zhang L,Wang Z,Zhuang C
Eur J Med Chem (2021) 212 : 113030 -113030
PubMed 33248849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 5.88 6.21
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4800694 1 6.21
CHEMBL4751151 1 6.21
CHEMBL4764330 1 6.09
CHEMBL4747957 2 6.07
CHEMBL4786387 1 5.99
CHEMBL1720855 1 5.84
CHEMBL4756694 1 5.83
CHEMBL3105688 1 5.38
CHEMBL4303525 OMAVELOXOLONE 4.0 1 5.28
CHEMBL1093059 BARDOXOLONE 2.0 1 -
CHEMBL168 OLEANOLIC_ACID 1 -
CHEMBL230128 1 -
CHEMBL1762621 BARDOXOLONE METHYL 3.0 1 -
CHEMBL3582242 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4800694 EC50 = 620.0 nM 6.21
CHEMBL4751151 EC50 = 610.0 nM 6.21
CHEMBL4764330 EC50 = 820.0 nM 6.09
CHEMBL4747957 EC50 = 860.0 nM 6.07
CHEMBL4786387 EC50 = 1030.0 nM 5.99
CHEMBL1720855 EC50 = 1460.0 nM 5.84
CHEMBL4756694 EC50 = 1480.0 nM 5.83
CHEMBL3105688 EC50 = 4150.0 nM 5.38
CHEMBL4303525 OMAVELOXOLONE EC50 = 5250.0 nM 5.28
CHEMBL1093059 BARDOXOLONE EC50 > 10000.0 nM -
CHEMBL168 OLEANOLIC_ACID EC50 - -
CHEMBL230128 EC50 - -
CHEMBL1762621 BARDOXOLONE METHYL EC50 > 10000.0 nM -
CHEMBL3582242 EC50 > 10000.0 nM -
CHEMBL4747957 Inhibition - % -