Compound name
JNJ-65355394
Target name
OGA
Affinity biochemical (nM)
1.3
Affinity on-target cellular (nM)
3.9
CG-Set
Other targets set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001561a
SMILES
CC(=O)Nc1ncc(CN2CCC[C@H](Cc3cc(C)nc(C)c3)C2)s1
InChIKey
CYFBRQHYEQKYHH-MRXNPFEDSA-N
NCBI gene ID
10724
UniProt ID
O60502
Synonyms
OGA, HEXC, KIAA0679, MEA5, MGEA5
Mode of action
Agonist/inhibitor
Negative control
JNJ-73924149
Affinity biochemical definition
IC50
Affinity biochemical assay type
Fluorescence-based enzymatic assay (recombinant full-length OGA, inhibition of the hydrolysis of fluorescein mono-β-D-N5 Acetyl-Glucosamine (FM-GlcNAc) by OGA)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!detailedpotencydataview/JNJ-65355394
Affinity biochemical relation
0
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cell-based OGA assay (in HEK293 cells overexpressing P301L mutant human Tau, OGA inhibition is evaluated through the immunocytochemical (ICC) detection of O-GlcNAcylated proteins by the use of a monoclonal antibody (CTD110.6))
Affinity on-target cellular source knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!detailedpotencydataview/JNJ-65355394
Affinity on-target cellular relation
0
Selectivity platform
CEREP panel (in-house data Janssen)
Selectivity platform number of targets
54
Selectivity remarks
Screened at 10 µM, closest targets as % of inhibition: OPRK1 (78%), rat ADORA2A (69%), human OPRM1 (55%); Screened at 10 µM against 45 GPCRs (PDSP screen), in-vitro potency of closest target: Ki(OPRK1) = 773.3 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!gpcrscandataview/JNJ-65355394
Selectivity Number of Off-targets
0