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Assay Detail

CHEMBL4019416

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

Binding
Inhibition of recombinant human sEH using PHOME as substrate preincubated for 30 mins followed by substrate addition measured for 30 mins by fluorescence photometric method
39
Total Activities
39
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

A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis.
Schmidt J, Rotter M, Weiser T, Wittmann S, Weizel L, Kaiser A, Heering J, Goebel T, Angioni C, Wurglics M, Paulke A, Geisslinger G, Kahnt A, Steinhilber D, Proschak E, Merk D.
J Med Chem (2017) 60 : 7703 -7724
PubMed 28845983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.97 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066332 1 8.39
CHEMBL4087681 1 8.05
CHEMBL4095371 1 7.40
CHEMBL4064739 1 6.92
CHEMBL4094881 1 6.86
CHEMBL4076701 1 6.80
CHEMBL4088582 1 6.77
CHEMBL4092436 1 6.66
CHEMBL4084686 1 6.66
CHEMBL381544 1 6.55
CHEMBL4074393 1 6.41
CHEMBL1300445 1 6.37
CHEMBL4091019 1 6.29
CHEMBL4100178 1 6.24
CHEMBL4061980 1 6.19
CHEMBL4071919 1 6.18
CHEMBL4076274 1 6.17
CHEMBL4083383 1 6.04
CHEMBL4098909 1 5.95
CHEMBL4081891 1 5.92
CHEMBL4102626 1 5.92
CHEMBL4060350 1 5.84
CHEMBL4072573 1 5.79
CHEMBL4072936 1 5.72
CHEMBL4096300 1 5.69
CHEMBL4091164 1 5.46
CHEMBL4094234 1 5.38
CHEMBL4093640 1 5.34
CHEMBL4067723 1 5.30
CHEMBL4068899 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066332 IC50 = 4.1 nM 8.39
CHEMBL4087681 IC50 = 8.9 nM 8.05
CHEMBL4095371 IC50 = 40.0 nM 7.40
CHEMBL4064739 IC50 = 120.0 nM 6.92
CHEMBL4094881 IC50 = 137.0 nM 6.86
CHEMBL4076701 IC50 = 157.0 nM 6.80
CHEMBL4088582 IC50 = 170.0 nM 6.77
CHEMBL4092436 IC50 = 220.0 nM 6.66
CHEMBL4084686 IC50 = 220.0 nM 6.66
CHEMBL381544 IC50 = 280.0 nM 6.55
CHEMBL4074393 IC50 = 390.0 nM 6.41
CHEMBL1300445 IC50 = 430.0 nM 6.37
CHEMBL4091019 IC50 = 510.0 nM 6.29
CHEMBL4100178 IC50 = 570.0 nM 6.24
CHEMBL4061980 IC50 = 650.0 nM 6.19
CHEMBL4071919 IC50 = 660.0 nM 6.18
CHEMBL4076274 IC50 = 680.0 nM 6.17
CHEMBL4083383 IC50 = 910.0 nM 6.04
CHEMBL4098909 IC50 = 1120.0 nM 5.95
CHEMBL4081891 IC50 = 1200.0 nM 5.92
CHEMBL4102626 IC50 = 1200.0 nM 5.92
CHEMBL4060350 IC50 = 1430.0 nM 5.84
CHEMBL4072573 IC50 = 1630.0 nM 5.79
CHEMBL4072936 IC50 = 1900.0 nM 5.72
CHEMBL4096300 IC50 = 2050.0 nM 5.69
CHEMBL4091164 IC50 = 3500.0 nM 5.46
CHEMBL4094234 IC50 = 4200.0 nM 5.38
CHEMBL4093640 IC50 = 4600.0 nM 5.34
CHEMBL4067723 IC50 = 5040.0 nM 5.30
CHEMBL4068899 IC50 = 8100.0 nM 5.09
CHEMBL4095466 IC50 = 10000.0 nM 5.00
CHEMBL4102078 IC50 = 10500.0 nM 4.98
CHEMBL4067074 IC50 = 12700.0 nM 4.90
CHEMBL4063293 IC50 = 18200.0 nM 4.74
CHEMBL4088942 IC50 = 18500.0 nM 4.73
CHEMBL4093296 IC50 = 19000.0 nM 4.72
CHEMBL4096637 IC50 = 20000.0 nM 4.70
CHEMBL4104050 IC50 = 20300.0 nM 4.69
CHEMBL4073326 IC50 - -