Compound name
JNJ-42396302
Target name
PDE10A
Affinity biochemical (nM)
13
Affinity on-target cellular (nM)
2.3
CG-Set
Other targets set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001570a
SMILES
COCCc1ccc(-c2c(C)nc3c(N4CCOCC4)ccnn23)cn1
InChIKey
BPLVDYJDAVYLRQ-UHFFFAOYSA-N
NCBI gene ID
10846
UniProt ID
Q9Y233
Synonyms
PDE10A
Mode of action
Inhibitor
Negative control
JNJ-40573663
Affinity biochemical definition
Ki
Affinity biochemical assay type
Scintillation proximity assay with human PDE10A
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/JNJ-42396302
Affinity biochemical relation
0
Affinity on-target cellular definition
fold
Affinity on-target cellular assay type
Luciferase activity assay (measuring increase in cAMP level at 1 µM in HEK293 cells stably transfected with mouse PDE10A1 and transiently co-transfected with pCRE-Luc plasmid)
Affinity on-target cellular source knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!detailedpotencydataview/JNJ-42396302
Affinity on-target cellular relation
0
Selectivity platform
PDE panel (in-house data Janssen)
Selectivity platform number of targets
11
Selectivity remarks
Selective versus other PDE family members (>250 fold in Scintillation proximity assays): Ki(hPDE1B1) = 3.4 µM, Ki(hPDE2A) = 32 µM, Ki(hPDE3A) = 49 µM, Ki(hPDE4D3) = 15 µM, Ki(hPDE5A3) = 8.5 µM, Ki(hPDE6AB) = 85 µM, Ki(hPDE7A1) = 23 µM, Ki(hPDE8A1) = 41 µM, Ki(hPDE9A) >33 µM, Ki(hPDE10A2) = 0.013 µM, Ki(hPDE11A4) = 46 µM; Screened at 10 µM in CEREP panel against 50 receptors and other enzymes: clean selectivity profile; Screened at 10 µM against 230 kinases (Millipore panel): clean selectivity profile with no inhibition of kinases <50%; Screened at 10 µM against 45 GPCRs (PDSP screen), in-vitro potencies of closest targets: Ki(ADRA2B) >10 µM, Ki(HTR2C) = 2.197 µM, Ki(HTR2B) = 2.293 µM, Ki(HTR7) = 8.745 µM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/JNJ-42396302
Selectivity Number of Off-targets
0