Compound name
BPKDi
Protein family
Protein Kinase
Target name
PRKD2
Affinity biochemical (nM)
9
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002083a
SMILES
O=C(C1=CC(N2CCNCC2)=NC(C3=CC=NC(NC4CCCCC4)=C3)=C1)N
InChIKey
XNWDRALEEPGBHB-UHFFFAOYSA-N
NCBI gene ID
25865
UniProt ID
Q9BZL6
Synonyms
PKD2, HSPC187, DKFZP586E0820
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay (20 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/20018189/
Affinity biochemical relation
=
Selectivity platform
Invitrogen Selectscreen
Selectivity platform number of targets
198
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: PRKD3 (109%), PRKD1(102%), PRKD2 (102%), IKBKB (57%), STK24 (47%), full screening data availabale as supporting information, https://pubs.acs.org/doi/10.1021/jm100076w;
In-vitro potency (enzymatic assay): IC50(a1AR) = 3000 nM, https://pubs.acs.org/doi/10.1021/jm100076w;
In-vitro potency (enzymatic assay): IC50(ß1AR) = 8300 nM, https://pubs.acs.org/doi/10.1021/jm100076w;
In-vitro potency (enzymatic assay): IC50(a1AR) = 3000 nM, https://pubs.acs.org/doi/10.1021/jm100076w;
In-vitro potency (enzymatic assay): IC50(ß1AR) = 8300 nM, https://pubs.acs.org/doi/10.1021/jm100076w;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/jm100076w
Selectivity Number of Off-targets
0