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Assay Detail

CHEMBL5036668

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

Binding
Inhibition of human recombinant sEH using CMNPC as substrate incubated for 5 mins by fluorescent based assay
18
Total Activities
18
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

From the Design to the <i>In Vivo</i> Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis.
Codony S, Calvó-Tusell C, Valverde E, Osuna S, Morisseau C, Loza MI, Brea J, Pérez C, Rodríguez-Franco MI, Pizarro-Delgado J, Corpas R, Griñán-Ferré C, Pallàs M, Sanfeliu C, Vázquez-Carrera M, Hammock BD, Feixas F, Vázquez S.
J Med Chem (2021) 64 : 5429 -5446
PubMed 33945278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.22 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5084744 1 9.40
CHEMBL4752759 1 9.40
CHEMBL5093683 1 9.30
CHEMBL242459 1 9.30
CHEMBL5081862 1 9.05
CHEMBL5080024 1 9.00
CHEMBL5081815 1 8.51
CHEMBL1818385 1 8.11
CHEMBL436774 AR9281 2.0 1 8.10
CHEMBL4779073 1 8.05
CHEMBL5083623 1 7.70
CHEMBL4797443 1 7.67
CHEMBL5084924 1 7.55
CHEMBL4759592 1 7.52
CHEMBL5090478 1 6.86
CHEMBL5083763 1 6.03
CHEMBL5094924 1 -
CHEMBL5083283 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5084744 IC50 = 0.4 nM 9.40
CHEMBL4752759 IC50 = 0.4 nM 9.40
CHEMBL5093683 IC50 = 0.5 nM 9.30
CHEMBL242459 IC50 = 0.5 nM 9.30
CHEMBL5081862 IC50 = 0.9 nM 9.05
CHEMBL5080024 IC50 = 1.0 nM 9.00
CHEMBL5081815 IC50 = 3.1 nM 8.51
CHEMBL1818385 IC50 = 7.7 nM 8.11
CHEMBL436774 AR9281 IC50 = 8.0 nM 8.10
CHEMBL4779073 IC50 = 9.0 nM 8.05
CHEMBL5083623 IC50 = 20.0 nM 7.70
CHEMBL4797443 IC50 = 21.3 nM 7.67
CHEMBL5084924 IC50 = 28.0 nM 7.55
CHEMBL4759592 IC50 = 29.9 nM 7.52
CHEMBL5090478 IC50 = 138.0 nM 6.86
CHEMBL5083763 IC50 = 941.0 nM 6.03
CHEMBL5094924 IC50 > 10000.0 nM -
CHEMBL5083283 IC50 > 10000.0 nM -