Compound name
DCLK1-IN-1
Protein family
Protein Kinase
Target name
DCLK1
Affinity biochemical (nM)
9.5
Affinity on-target cellular (nM)
279
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001463a
SMILES
COc1cc(N2CCN(C)CC2)ccc1Nc1ncc2c(n1)N(C)c1ccccc1C(=O)N2CC(F)(F)F
InChIKey
OQFCHSFVWSLDAO-UHFFFAOYSA-N
NCBI gene ID
9201
UniProt ID
O15075
Synonyms
KIAA0369, DCLK, DCDC3A
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Binding assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/32251410/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/32251410/
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
489
Selectivity remarks
Screened at 1 µM, closest targets as % of control: DCAMKL2(1.9%), DCAMKL1(5.9%), HIPK4 (44%), ABL1 (44%), full screening data available as supporting information; Screened at 2.5 µM, in activity-based proteomic profiling against 250 kinases using KiNativ assay profiling in PATU-8988T cell lysates, closest targets as % of inhibition: DCAMKL1 (52.3%), TBK1 (43.6%), DCAMKL1 (40.1%), MAPK15(36%), full screening data available as supporting informatio, https://pubmed.ncbi.nlm.nih.gov/32251410/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/32251410/
Selectivity Number of Off-targets
0