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Assay Detail

CHEMBL1051702

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Binding
Inhibition of human sEH
27
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Bifunctional epoxide hydrolase 2 (CHEMBL2409)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Shen HC, Ding FX, Wang S, Deng Q, Zhang X, Chen Y, Zhou G, Xu S, Chen HS, Tong X, Tong V, Mitra K, Kumar S, Tsai C, Stevenson AS, Pai LY, Alonso-Galicia M, Chen X, Soisson SM, Roy S, Zhang B, Tata JR, Berger JP, Colletti SL.
J Med Chem (2009) 52 : 5009 -5012
PubMed 19645482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.44 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215387 1 8.80
CHEMBL551058 1 8.40
CHEMBL559531 1 8.30
CHEMBL555347 1 8.15
CHEMBL551921 1 8.15
CHEMBL564757 1 8.15
CHEMBL552402 1 8.12
CHEMBL550242 1 8.10
CHEMBL552382 2 8.05
CHEMBL561788 1 8.05
CHEMBL552061 1 8.00
CHEMBL557032 1 7.89
CHEMBL562822 1 7.85
CHEMBL556487 1 7.85
CHEMBL564547 1 7.55
CHEMBL551517 1 7.48
CHEMBL562926 1 7.44
CHEMBL561259 1 7.27
CHEMBL562869 1 6.92
CHEMBL552381 1 6.89
CHEMBL561379 1 6.63
CHEMBL564975 1 6.37
CHEMBL559101 1 6.32
CHEMBL552196 1 5.96
CHEMBL563732 1 5.96
CHEMBL550652 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215387 IC50 = 1.6 nM 8.80
CHEMBL551058 IC50 = 4.0 nM 8.40
CHEMBL559531 IC50 = 5.0 nM 8.30
CHEMBL555347 IC50 = 7.0 nM 8.15
CHEMBL551921 IC50 = 7.0 nM 8.15
CHEMBL564757 IC50 = 7.0 nM 8.15
CHEMBL552402 IC50 = 7.5 nM 8.12
CHEMBL550242 IC50 = 8.0 nM 8.10
CHEMBL552382 IC50 = 9.0 nM 8.05
CHEMBL561788 IC50 = 9.0 nM 8.05
CHEMBL552061 IC50 = 10.0 nM 8.00
CHEMBL557032 IC50 = 13.0 nM 7.89
CHEMBL556487 IC50 = 14.0 nM 7.85
CHEMBL562822 IC50 = 14.0 nM 7.85
CHEMBL564547 IC50 = 28.0 nM 7.55
CHEMBL551517 IC50 = 33.0 nM 7.48
CHEMBL562926 IC50 = 36.0 nM 7.44
CHEMBL561259 IC50 = 54.0 nM 7.27
CHEMBL552382 IC50 = 62.0 nM 7.21
CHEMBL562869 IC50 = 120.0 nM 6.92
CHEMBL552381 IC50 = 130.0 nM 6.89
CHEMBL561379 IC50 = 235.0 nM 6.63
CHEMBL564975 IC50 = 430.0 nM 6.37
CHEMBL559101 IC50 = 480.0 nM 6.32
CHEMBL552196 IC50 = 1100.0 nM 5.96
CHEMBL563732 IC50 = 1100.0 nM 5.96
CHEMBL550652 IC50 = 8400.0 nM 5.08