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Assay Detail

CHEMBL5381164

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Binding
Inhibition of recombinant mouse soluble epoxide hydrolase using PHOME as substrate assessed as 6-methoxynaphthaldehyde product formation preincubated with compound for 10 mins followed by substrate addition and measured by fluorescence based analysis
ChEMBL ↗
54
Total Activities
54
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

Structure-Directed Discovery of Potent Soluble Epoxide Hydrolase Inhibitors for the Treatment of Inflammatory Diseases.
Chen Y, Chen L, Xu H, Cao R, Morisseau C, Zhang M, Shi Y, Hammock BD, Wang J, Zhuang J, Liu Z, Chen G.
J Med Chem (2023) 66 : 2979 -3009
PubMed 36689364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 9.42 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5415121 — — 1 10.22
CHEMBL5427173 — — 1 10.15
CHEMBL5428998 — — 1 10.05
CHEMBL5430033 — — 1 9.96
CHEMBL5435557 — — 1 9.92
CHEMBL5424246 — — 1 9.92
CHEMBL5433624 — — 1 9.92
CHEMBL5433817 — — 1 9.89
CHEMBL5425833 — — 1 9.85
CHEMBL5422052 — — 1 9.82
CHEMBL5405764 — — 1 9.82
CHEMBL5431410 — — 1 9.80
CHEMBL5399478 — — 1 9.74
CHEMBL5410521 — — 1 9.74
CHEMBL5396859 — — 1 9.74
CHEMBL5430146 — — 1 9.64
CHEMBL5425040 — — 1 9.64
CHEMBL5432207 — — 1 9.59
CHEMBL5397730 — — 1 9.59
CHEMBL5429256 — — 1 9.54
CHEMBL5403016 — — 1 9.49
CHEMBL5431497 — — 1 9.49
CHEMBL5430521 — — 1 9.46
CHEMBL5417426 — — 1 9.46
CHEMBL5417008 — — 1 9.46
CHEMBL5431392 — — 1 9.42
CHEMBL5394017 — — 1 9.41
CHEMBL5421307 — — 1 9.39
CHEMBL5438968 — — 1 9.36
CHEMBL5423765 — — 1 9.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5415121 — IC50 = 0.06 nM 10.22
CHEMBL5427173 — IC50 = 0.07 nM 10.15
CHEMBL5428998 — IC50 = 0.09 nM 10.05
CHEMBL5430033 — IC50 = 0.11 nM 9.96
CHEMBL5435557 — IC50 = 0.12 nM 9.92
CHEMBL5424246 — IC50 = 0.12 nM 9.92
CHEMBL5433624 — IC50 = 0.12 nM 9.92
CHEMBL5433817 — IC50 = 0.13 nM 9.89
CHEMBL5425833 — IC50 = 0.14 nM 9.85
CHEMBL5422052 — IC50 = 0.15 nM 9.82
CHEMBL5405764 — IC50 = 0.15 nM 9.82
CHEMBL5431410 — IC50 = 0.16 nM 9.80
CHEMBL5396859 — IC50 = 0.18 nM 9.74
CHEMBL5410521 — IC50 = 0.18 nM 9.74
CHEMBL5399478 — IC50 = 0.18 nM 9.74
CHEMBL5430146 — IC50 = 0.23 nM 9.64
CHEMBL5425040 — IC50 = 0.23 nM 9.64
CHEMBL5432207 — IC50 = 0.26 nM 9.59
CHEMBL5397730 — IC50 = 0.26 nM 9.59
CHEMBL5429256 — IC50 = 0.29 nM 9.54
CHEMBL5403016 — IC50 = 0.32 nM 9.49
CHEMBL5431497 — IC50 = 0.32 nM 9.49
CHEMBL5430521 — IC50 = 0.35 nM 9.46
CHEMBL5417426 — IC50 = 0.35 nM 9.46
CHEMBL5417008 — IC50 = 0.35 nM 9.46
CHEMBL5431392 — IC50 = 0.38 nM 9.42
CHEMBL5394017 — IC50 = 0.39 nM 9.41
CHEMBL5421307 — IC50 = 0.41 nM 9.39
CHEMBL5438968 — IC50 = 0.44 nM 9.36
CHEMBL5423765 — IC50 = 0.47 nM 9.33
CHEMBL5433621 — IC50 = 0.53 nM 9.28
CHEMBL5399542 — IC50 = 0.53 nM 9.28
CHEMBL5435276 — IC50 = 0.55 nM 9.26
CHEMBL5412026 — IC50 = 0.55 nM 9.26
CHEMBL5437028 — IC50 = 0.55 nM 9.26
CHEMBL5421374 — IC50 = 0.55 nM 9.26
CHEMBL5434178 — IC50 = 0.56 nM 9.25
CHEMBL5406085 — IC50 = 0.58 nM 9.24
CHEMBL5429531 — IC50 = 0.58 nM 9.24
CHEMBL5410982 — IC50 = 0.61 nM 9.21
CHEMBL5435879 — IC50 = 0.62 nM 9.21
CHEMBL5414609 — IC50 = 0.61 nM 9.21
CHEMBL5423755 — IC50 = 0.67 nM 9.17
CHEMBL5404352 — IC50 = 0.8 nM 9.10
CHEMBL5419231 — IC50 = 0.8 nM 9.10
CHEMBL5431664 — IC50 = 0.9 nM 9.05
CHEMBL5404981 — IC50 = 1.1 nM 8.96
CHEMBL5437010 — IC50 = 1.25 nM 8.90
CHEMBL5435984 — IC50 = 1.3 nM 8.89
CHEMBL5414179 — IC50 = 1.3 nM 8.89