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Assay Detail

CHEMBL2399731

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

Binding
Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carbonate conversion to 6-methoxy-2-naphthaldehyde preincubated for 5 mins prior to substrate addition by fluorescence assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bifunctional epoxide hydrolase 2 (CHEMBL2409)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.
Hwang SH, Wecksler AT, Zhang G, Morisseau C, Nguyen LV, Fu SH, Hammock BD.
Bioorg Med Chem Lett (2013) 23 : 3732 -3737
PubMed 23726028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 9.02 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946170 REGORAFENIB 4.0 1 9.30
CHEMBL2397149 1 9.30
CHEMBL2397137 1 9.30
CHEMBL2397138 1 9.30
CHEMBL2397139 1 9.30
CHEMBL2397140 1 9.30
CHEMBL2397147 1 9.30
CHEMBL2397146 1 9.30
CHEMBL2397143 1 9.30
CHEMBL2397142 1 9.30
CHEMBL2397141 1 9.30
CHEMBL2397136 1 9.30
CHEMBL2397148 1 9.05
CHEMBL2397145 1 9.00
CHEMBL242459 1 8.82
CHEMBL1257634 1 8.54
CHEMBL1258904 1 8.43
CHEMBL2397144 1 8.07
CHEMBL1336 SORAFENIB 4.0 1 7.92
CHEMBL535 SUNITINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946170 REGORAFENIB IC50 = 0.5 nM 9.30
CHEMBL2397149 IC50 = 0.5 nM 9.30
CHEMBL2397137 IC50 = 0.5 nM 9.30
CHEMBL2397138 IC50 = 0.5 nM 9.30
CHEMBL2397139 IC50 = 0.5 nM 9.30
CHEMBL2397140 IC50 = 0.5 nM 9.30
CHEMBL2397147 IC50 = 0.5 nM 9.30
CHEMBL2397146 IC50 = 0.5 nM 9.30
CHEMBL2397143 IC50 = 0.5 nM 9.30
CHEMBL2397142 IC50 = 0.5 nM 9.30
CHEMBL2397141 IC50 = 0.5 nM 9.30
CHEMBL2397136 IC50 = 0.5 nM 9.30
CHEMBL2397148 IC50 = 0.9 nM 9.05
CHEMBL2397145 IC50 = 1.0 nM 9.00
CHEMBL242459 IC50 = 1.5 nM 8.82
CHEMBL1257634 IC50 = 2.9 nM 8.54
CHEMBL1258904 IC50 = 3.7 nM 8.43
CHEMBL2397144 IC50 = 8.6 nM 8.07
CHEMBL1336 SORAFENIB IC50 = 12.0 nM 7.92
CHEMBL535 SUNITINIB IC50 > 10000.0 nM -