Compound name
MU1250
Protein family
Protein Kinase
Target name
CSNK1A1
Affinity biochemical (nM)
67
Affinity on-target cellular (nM)
539.8
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001203a
SMILES
Cn1ccc(Cn2cnc(-c3ccc(F)cc3)c2-c2ccnc3[nH]ccc23)n1
InChIKey
KINPMBFCIYMYBU-UHFFFAOYSA-N
NCBI gene ID
1452
UniProt ID
P48729
Synonyms
CK1, CK1a, CK1alpha, CKIa, CKIalpha
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Tracer competition assays (Reaction Biology, 10 mM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/36625768/
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Kinobeads competition binding assays (using K-562, COLO-205, and MV-4-11 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/36625768/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Eurofins)
Selectivity platform number of targets
413
Selectivity remarks
Screened at 1 µM, using ATP conc. = Km, closest targets as % of activity: CSNK1A1 (7%), CSNK1E (-1%), CSNK1D (-6%), TNIK (12%), MAP4K4 (47%), MAP2K3 (43%), SAPK2a (41%), full screening data are available as supporting information, https://onlinelibrary.wiley.com/action/downloadSupplement?doi=10.1002%2Fanie.202217532&file=anie202217532-sup-0001-misc_information.pdf;
Screened at 1 µM, Kinobeads pulldown experiments (Kinobeads competition binding assays, using K-562, COLO-205, and MV-4-11 cells), EC50(CSNK1A) = 539.9 nM, EC50(CSNK1D) = 12.9 nM, EC50(CSNK1E) = 51.8 nM, EC50(GAPVD1) = 137.7 nM, full screening data, with additional conc. are available as a supplemental table, https://pubmed.ncbi.nlm.nih.gov/36625768/;
Screened at 1 µM, Kinobeads pulldown experiments (Kinobeads competition binding assays, using K-562, COLO-205, and MV-4-11 cells), EC50(CSNK1A) = 539.9 nM, EC50(CSNK1D) = 12.9 nM, EC50(CSNK1E) = 51.8 nM, EC50(GAPVD1) = 137.7 nM, full screening data, with additional conc. are available as a supplemental table, https://pubmed.ncbi.nlm.nih.gov/36625768/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/36625768/
Selectivity Number of Off-targets
0