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THPP-1

Protein target name:
PDE10AMechanism of action:
InhibitorRecommended Concentration for use in cells:
10 nM
Reviewer suggested Concentration for use in cells:
50-200 nM
Probe Availability
Probe Information
In vitro validation
Potency:
Ki0.99 nM
Potency assay:
Phosphodiesterase (PDE) activity was determined using an IMAP® FP kitPDB ID for probe-target interaction (3D structure):
3UI7Probe Selectivity in Vitro:
PDE selectivity: closest hit is PDE6A (44 fold)
In cell validation
Potency in cells:
IC5049 nM
Potency assay (cells):
cAMP Gs dynamic kitProbe Selectivity in Cell:
Closest off-targets (Panlabs): Adenosine transporter (guinea pig): IC50 = 1.61 µM @ 10 µM
In vivo validation
Organism:
RatDogRhesus MonkeyDose:
1-10 mg/KgRoute of delivery:
OralSystemic clearance:
6-7.7 mL/min/kgFraction of probe bound to plasma protein:
47% Rat79% Dog31% MonkeyTmax:
1.4 h Rat, Monkey7.2 h DogOrgan (O):
BrainPrimary Reference
External Resources
Available data:
SGC additional analysis