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Assay Detail

CHEMBL5540956

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

Binding
Inhibition of recombinant mouse sEH using PHOME as substrate preincubated for 10 mins followed by substrate addition by fluorescence based assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bifunctional epoxide hydrolase 2 (CHEMBL4140)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and Synthesis of Dual-Targeting Inhibitors of sEH and HDAC6 for the Treatment of Neuropathic Pain and Lipopolysaccharide-Induced Mortality.
Chen Y, Sun J, Tong H, Wang J, Cao R, Xu H, Chen L, Morisseau C, Zhang M, Shi Y, Han C, Zhuang J, Jing Y, Liu Z, Hammock BD, Chen G.
J Med Chem (2024) 67 : 2095 -2117
PubMed 38236416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 9.25 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5592524 1 10.10
CHEMBL5564312 1 9.96
CHEMBL5571794 1 9.89
CHEMBL5570637 1 9.72
CHEMBL5569830 1 9.54
CHEMBL5573866 1 9.52
CHEMBL5571076 1 9.40
CHEMBL5564705 1 9.40
CHEMBL5564589 1 9.36
CHEMBL5570460 1 9.35
CHEMBL4869434 1 9.30
CHEMBL5566384 1 9.30
CHEMBL5574790 1 9.29
CHEMBL5571505 1 9.23
CHEMBL5567500 1 9.22
CHEMBL5571752 1 9.22
CHEMBL5591117 1 9.15
CHEMBL5567303 1 9.14
CHEMBL5574426 1 9.12
CHEMBL5564613 1 9.11
CHEMBL5570840 1 9.10
CHEMBL5590604 1 9.00
CHEMBL5571161 1 8.80
CHEMBL5573004 1 8.19
CHEMBL5563806 1 7.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5592524 IC50 = 0.08 nM 10.10
CHEMBL5564312 IC50 = 0.11 nM 9.96
CHEMBL5571794 IC50 = 0.13 nM 9.89
CHEMBL5570637 IC50 = 0.19 nM 9.72
CHEMBL5569830 IC50 = 0.29 nM 9.54
CHEMBL5573866 IC50 = 0.3 nM 9.52
CHEMBL5571076 IC50 = 0.4 nM 9.40
CHEMBL5564705 IC50 = 0.4 nM 9.40
CHEMBL5564589 IC50 = 0.44 nM 9.36
CHEMBL5570460 IC50 = 0.45 nM 9.35
CHEMBL4869434 IC50 = 0.5 nM 9.30
CHEMBL5566384 IC50 = 0.5 nM 9.30
CHEMBL5574790 IC50 = 0.51 nM 9.29
CHEMBL5571505 IC50 = 0.59 nM 9.23
CHEMBL5567500 IC50 = 0.6 nM 9.22
CHEMBL5571752 IC50 = 0.6 nM 9.22
CHEMBL5591117 IC50 = 0.7 nM 9.15
CHEMBL5567303 IC50 = 0.72 nM 9.14
CHEMBL5574426 IC50 = 0.75 nM 9.12
CHEMBL5564613 IC50 = 0.78 nM 9.11
CHEMBL5570840 IC50 = 0.8 nM 9.10
CHEMBL5590604 IC50 = 1.0 nM 9.00
CHEMBL5571161 IC50 = 1.6 nM 8.80
CHEMBL5573004 IC50 = 6.4 nM 8.19
CHEMBL5563806 IC50 = 11.7 nM 7.93