Compound name
JNJ-73924149
Target name
OGA
Affinity biochemical (nM)
10000
Affinity on-target cellular (nM)
1000
CG-Set
Other targets set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001562a
SMILES
CC(=O)Nc1nc(CN2CCC[C@H](Cc3cc(C)nc(C)c3)C2)cs1
InChIKey
VKYYOTCDIVOPRO-MRXNPFEDSA-N
NCBI gene ID
10724
UniProt ID
O60502
Synonyms
OGA, HEXC, KIAA0679, MEA5, MGEA5
Mode of action
negative control for JNJ-65355394
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
>
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
>
Selectivity platform
GPCR panel (PDSP screen)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, in-vitro potencies of closest targets: Ki(SIGMAR1) = 63.33 nM, Ki(TMEM97) = 1399.16 nM, Ki(SLC6A4) = 2614.09 nM, Ki(ADRA2B) = 3691.26 nM, Ki(SLC6A3) = 5284.45 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!gpcrscandataview/JNJ-65355394
Selectivity Number of Off-targets
1