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Assay Detail

CHEMBL5042639

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

Binding
Inhibition of recombinant human C-terminal sEH (222 to 555 residues) expressed in Escherichia coli BL21-DE3 using PHOME as substrate assessed as reduction in 6-methoxy-2-naphthaldehyde formation incubated for 30 mins followed by substarte addition and measured after 30 mins by fluorescence based assay
3
Total Activities
3
Compounds Tested
2
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

Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
Hartmann M, Bibli SI, Tews D, Ni X, Kircher T, Kramer JS, Kilu W, Heering J, Hernandez-Olmos V, Weizel L, Scriba GKE, Krait S, Knapp S, Chaikuad A, Merk D, Fleming I, Fischer-Posovszky P, Proschak E.
J Med Chem (2021) 64 : 2815 -2828
PubMed 33620196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.30 7.89
EC50 1 6.62 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1258904 1 7.89
CHEMBL5077503 1 6.70
CHEMBL5075221 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1258904 IC50 = 13.0 nM 7.89
CHEMBL5077503 IC50 = 200.0 nM 6.70
CHEMBL5075221 EC50 = 240.0 nM 6.62