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Assay Detail

CHEMBL3821236

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

Binding
Inhibition of recombinant human sHE assessed as product formation preincubated for 30 mins followed by addition of (3-phenyl-cyano-(6-methoxy-2-naphthalenyl)methyl ester-2-oxirane-acetic acid as substrate measured after 30 mins by fluorescence analysis
16
Total Activities
16
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

Design and synthesis of fused soluble epoxide hydrolase/peroxisome proliferator-activated receptor modulators
Blocher R, Lamers C, Wittmann SK, Diehl O, Hanke T, Merk D, Steinhilber D, Schubert-Zsilavecz M, Kahnt AS, Proschak E
Medchemcomm (2016) 7 : 1209 -1216
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.75 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818537 1 7.64
CHEMBL3818149 1 7.57
CHEMBL3818107 1 7.57
CHEMBL3819103 1 7.40
CHEMBL3819337 1 7.19
CHEMBL3817950 1 7.12
CHEMBL3818875 GSK2256294 2.0 1 6.96
CHEMBL1231797 1 6.85
CHEMBL3818683 1 6.52
CHEMBL3818601 1 6.24
CHEMBL3818059 1 6.07
CHEMBL3818976 1 5.92
CHEMBL3818218 1 5.89
CHEMBL3819535 1 5.60
CHEMBL3318038 1 -
CHEMBL264374 BEZAFIBRATE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818537 IC50 = 23.0 nM 7.64
CHEMBL3818149 IC50 = 27.0 nM 7.57
CHEMBL3818107 IC50 = 27.0 nM 7.57
CHEMBL3819103 IC50 = 40.0 nM 7.40
CHEMBL3819337 IC50 = 64.0 nM 7.19
CHEMBL3817950 IC50 = 75.0 nM 7.12
CHEMBL3818875 GSK2256294 IC50 = 110.0 nM 6.96
CHEMBL1231797 IC50 = 140.0 nM 6.85
CHEMBL3818683 IC50 = 300.0 nM 6.52
CHEMBL3818601 IC50 = 570.0 nM 6.24
CHEMBL3818059 IC50 = 850.0 nM 6.07
CHEMBL3818976 IC50 = 1200.0 nM 5.92
CHEMBL3818218 IC50 = 1300.0 nM 5.89
CHEMBL3819535 IC50 = 2500.0 nM 5.60
CHEMBL3318038 IC50 - -
CHEMBL264374 BEZAFIBRATE IC50 - -