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DO264 | DO264 : Inhibitor of ABHD12
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ABHD12
  • IC50:11 nM
  • IC50:26 nM
Inhibitor
20-200 nM ideal, up to 1 uM acceptable
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
ABPP studies of DO264 (46) and other representative (thio)urea inhibitors of ABHD12 confirmed excell ...

Potency
Cellular
In Vitro

ABHD12

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-018-0155-8

In Vivo Validations

Mouse
Dose: 30 mg/Kg, 60 mg/Kg
Route of delivery: Intraperitoneal, Oral
Organ of interest (O): Brain

DOI Reference: 10.1038/s41589-018-0155-8

Negative Control Compounds

canSAR3136718

Chemical Information

Molecular Formula C23H20Cl2F3N5O2S
SMILEs FC(F)(F)Oc1ccc(Oc2ccnc(N3CCC(NC(=S)Nc4cccnc4)CC3)c2Cl)c(Cl)c1
InChI InChI=1S/C23H20Cl2F3N5O2S/c24-17-12-16(35-23(26,27)28)3-4-18(17)34-19-5-9-30-21(20(19)25)33-10-6-14(7-11-33)31-22(36)32-15-2-1-8-29-13-15/h1-5,8-9,12-14H,6-7,10-11H2,(H2,31,32,36)
Molecular weight 557.07 Da
AlogP 6.429700000000003
HBond acceptors 7
HBond donors 2
Atoms 56

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 13 Aug 2020 )
Cellular Use Rating
In Model Organisms
DO264 is a high quality probe for reversible inhibition of human and mouse lyso-PS lipase ABHD12. The probe is effective and has excellent selectivity in cell lysates, in cell culture models, and can...
by SERP
(on 5 Sept 2020 )
Cellular Use Rating
In Model Organisms
This probe is of reasonable high quality, but there are two concerns, based on the lack of available data (as opposed to existing negative data). 1) How selective is the probe outside of the serine...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria