Compound name
BI-1935
Protein family
Protease
Target name
EPHX2@Protease
Affinity biochemical (nM)
7
Affinity on-target cellular (nM)
1
CG-Set
Other targets
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000542a
SMILES
CCOCCN1C=C(C=CC1=O)C(Nc1ccc(cn1)n1c(cc(c2cccnc2)n1)C(F)(F)F)=O
InChIKey
KMESAVNRPDKZCQ-UHFFFAOYSA-N
NCBI gene ID
2053
UniProt ID
P34913
Synonyms
ABHD20, CEH, SEH
Mode of action
Inhibitor
Negative control
BI-2049
Affinity biochemical definition
IC50
Affinity biochemical assay type
Human soluble epoxide hydrolase inhibition
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI-1935
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (inhibition of sEH in human Hep G2 cells)
Affinity on-target cellular relation
<
Selectivity remarks
Screened against human CYP epoxygenases (Boehringer panel) CYP2J2, CYP2C9, CYP2C19 and IL2: IC50 >1 µM for related targets (> 100-fold selective); Screened against 67 targets (Eurofins-Panlabs) at 10 µM, closest targets: TBXAS1 (96% inhibition, IC50 = 132 nM), 5-Lipoxygenase (66% inhibition, IC50 = 5.92 µM); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(SLC6A3) = 4.48 µM, Ki(SIGMAR1) = 6.28 µM; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: CHEK2 (0%), TYRO3 (0%), JAK1 (JH2domain-pseudokinase) (37%)
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI-1935