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Assay Detail

CHEMBL3384153

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

Functional
Inhibition of LPS-induced NO production in C57BL/6 mouse macrophages preincubated with compound for 1 hr before LPS challenge measured after 24 hrs by Griess method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Macrophage (CHEMBL612578)
Type CELL-LINE

Publication

Novel nitric oxide-releasing derivatives of brusatol as anti-inflammatory agents: design, synthesis, biological evaluation, and nitric oxide release studies.
Tang W, Xie J, Xu S, Lv H, Lin M, Yuan S, Bai J, Hou Q, Yu S.
J Med Chem (2014) 57 : 7600 -7612
PubMed 25179783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.36 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342212 1 7.33
CHEMBL450464 BRUSATOL 1 7.30
CHEMBL3342220 1 7.17
CHEMBL3342210 1 7.05
CHEMBL3342214 1 6.68
CHEMBL3342215 1 6.42
CHEMBL3342211 1 6.16
CHEMBL3342217 1 5.96
CHEMBL3342221 1 5.89
CHEMBL3342213 1 5.68
CHEMBL3342218 1 5.66
CHEMBL3342219 1 4.96
CHEMBL3342216 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342212 IC50 = 47.0 nM 7.33
CHEMBL450464 BRUSATOL IC50 = 50.0 nM 7.30
CHEMBL3342220 IC50 = 67.0 nM 7.17
CHEMBL3342210 IC50 = 89.0 nM 7.05
CHEMBL3342214 IC50 = 210.0 nM 6.68
CHEMBL3342215 IC50 = 380.0 nM 6.42
CHEMBL3342211 IC50 = 690.0 nM 6.16
CHEMBL3342217 IC50 = 1100.0 nM 5.96
CHEMBL3342221 IC50 = 1300.0 nM 5.89
CHEMBL3342213 IC50 = 2100.0 nM 5.68
CHEMBL3342218 IC50 = 2200.0 nM 5.66
CHEMBL3342219 IC50 = 11000.0 nM 4.96
CHEMBL3342216 IC50 > 10000.0 nM -