Compound name
TTBK1-IN-1
Protein family
Protein Kinase
Target name
TTBK2
Affinity biochemical (nM)
2.7
Affinity on-target cellular (nM)
315
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002107a
SMILES
O[C@@](C)(CC)C#CC1=CC2=C(C=CN2C3=CC(OC)=NC(N)=N3)C=N1
InChIKey
HPJVZSVEIGCFJP-SFHVURJKSA-N
NCBI gene ID
146057
UniProt ID
Q6IQ55
Synonyms
KIAA0847
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
LANCE Ultra TR-FRET assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/33944571/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
HTRF assay (TBK1 mediated Tau-Ser422 phosphorylation in HEK-293T cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/33944571/
Affinity on-target cellular relation
=
Selectivity platform
KINOMEscan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, closest targets as % of control: CIT(20%), CSNK1D (5%), CSNK1E (2.4%), CSNK1G2 (23%), NIK (22%), PAK6 (12%), PAK7 (14%), PIKFYVE (0%), PKNB(4.2%), PRKD1 (2%), PRKD2 (1.7%), PRKD3 (16%), TAOK1 (5%), TSSK3 (0%), MAP3K19 (0.2%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/33944571/;
Screened at 1 µM, against 468 kinases, KinomeScan(DiscoverX), closest targets as % of control: CSNK1D (22%), CSNK1E (43%), PKNB(8.5%),PRKD1 (5.5%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/33944571/;
In-vitro potency (enzymatic assay): IC50(NIK) = 1097 nM, IC50(PIP5K1C) >10000 nM, IC50(CSNK1D) = 40 nM, IC50(DRAK) >10000 nM, IC50(JAK2) >10000 nM, IC50(PAK5) = 824 nM, IC50(TAOK1) = 225 nM, IC50(TAOK2) = 889 nM, IC50(TYK2) = 1091 nM, https://pubmed.ncbi.nlm.nih.gov/33944571/;
Screened at 1 µM, against 468 kinases, KinomeScan(DiscoverX), closest targets as % of control: CSNK1D (22%), CSNK1E (43%), PKNB(8.5%),PRKD1 (5.5%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/33944571/;
In-vitro potency (enzymatic assay): IC50(NIK) = 1097 nM, IC50(PIP5K1C) >10000 nM, IC50(CSNK1D) = 40 nM, IC50(DRAK) >10000 nM, IC50(JAK2) >10000 nM, IC50(PAK5) = 824 nM, IC50(TAOK1) = 225 nM, IC50(TAOK2) = 889 nM, IC50(TYK2) = 1091 nM, https://pubmed.ncbi.nlm.nih.gov/33944571/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/33944571/
Selectivity Number of Off-targets
9