EUB0000751a_PDE10A

Chemical structure of compound EUB0000751a
Compound name
THPP-1
Protein family
PDE
Target name
PDE10A
Affinity biochemical (nM)
0.99
Affinity on-target cellular (nM)
49
CG-Set
Other targets
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000751a
SMILES
COCCOC1=NC(C2=CC=C(Cl)N=C2)=NC3=C1CN(C(C4=C5C=CC=CN5C=N4)=O)CC3
InChIKey
JBHLOPKIPKTRSU-UHFFFAOYSA-N
NCBI gene ID
10846
UniProt ID
Q9Y233
Synonyms
PDE10A
Mode of action
Inhibitor
Negative control
THPP-1-NC
Affinity biochemical definition
Ki
Affinity biochemical assay type
Fluorescence polarization assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.neuropharm.2012.06.013
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/THPP-1
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cell-based assay
Affinity on-target cellular relation
=
Selectivity platform
PDE panel, literature
Selectivity platform number of targets
11
Selectivity remarks
Targets tested in PDE activity assays, closest targets: Ki(PDE6) = 44 nM (44-fold selective), Ki(PDE5A) = 116 nM (116-fold selective), Ki(PDE298) = 298 nM (300-fold selective), others >1000-fold selective
Selectivity Source Knowledge
https://doi.org/10.1016/j.bmcl.2012.07.072
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/THPP-1
Selectivity Number of Off-targets
1