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Assay Detail

CHEMBL1671068

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

Binding
Inhibition of human soluble epoxide hydrolase
19
Total Activities
19
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

1-(1-acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia.
Anandan SK, Webb HK, Chen D, Wang YX, Aavula BR, Cases S, Cheng Y, Do ZN, Mehra U, Tran V, Vincelette J, Waszczuk J, White K, Wong KR, Zhang LN, Jones PD, Hammock BD, Patel DV, Whitcomb R, MacIntyre DE, Sabry J, Gless R.
Bioorg Med Chem Lett (2011) 21 : 983 -988
PubMed 21211973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.03 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668928 1 9.10
CHEMBL1668937 1 8.80
CHEMBL1668940 1 8.80
CHEMBL1668935 1 8.72
CHEMBL1668939 1 8.54
CHEMBL1668936 1 8.43
CHEMBL1668930 1 8.22
CHEMBL1668938 1 8.19
CHEMBL436774 AR9281 2.0 1 8.10
CHEMBL1668933 1 8.00
CHEMBL1668932 1 7.96
CHEMBL1668934 1 7.92
CHEMBL1668929 1 7.89
CHEMBL1668926 1 7.85
CHEMBL1668925 1 7.60
CHEMBL1668927 1 7.54
CHEMBL1668923 1 7.24
CHEMBL1668924 1 6.92
CHEMBL1668931 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668928 IC50 = 0.8 nM 9.10
CHEMBL1668937 IC50 = 1.6 nM 8.80
CHEMBL1668940 IC50 = 1.6 nM 8.80
CHEMBL1668935 IC50 = 1.9 nM 8.72
CHEMBL1668939 IC50 = 2.9 nM 8.54
CHEMBL1668936 IC50 = 3.7 nM 8.43
CHEMBL1668930 IC50 = 6.0 nM 8.22
CHEMBL1668938 IC50 = 6.4 nM 8.19
CHEMBL436774 AR9281 IC50 = 8.0 nM 8.10
CHEMBL1668933 IC50 = 10.0 nM 8.00
CHEMBL1668932 IC50 = 11.0 nM 7.96
CHEMBL1668934 IC50 = 12.0 nM 7.92
CHEMBL1668929 IC50 = 13.0 nM 7.89
CHEMBL1668926 IC50 = 14.0 nM 7.85
CHEMBL1668925 IC50 = 25.0 nM 7.60
CHEMBL1668927 IC50 = 29.0 nM 7.54
CHEMBL1668923 IC50 = 58.0 nM 7.24
CHEMBL1668924 IC50 = 120.0 nM 6.92
CHEMBL1668931 IC50 = 185.0 nM 6.73