Reaction Details
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Dual specificity tyrosine-phosphorylation-regulated kinase 2
Ligand
BDBM50347750
Substrate
n/a
Meas. Tech.
ChEMBL_2214249 (CHEMBL5127381)
IC50
14±n/a nM
Citation
Tahtouh, T; Durieu, E; Villiers, B; Bruyère, C; Nguyen, TL; Fant, X; Ahn, KH; Khurana, L; Deau, E; Lindberg, MF; Sévère, E; Miege, F; Roche, D; Limanton, E; L'Helgoual'ch, JM; Burgy, G; Guiheneuf, S; Herault, Y; Kendall, DA; Carreaux, F; Bazureau, JP; Meijer, L Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. J Med Chem 65:1396-1417 (2022) [PubMed] More Info.:
Target
Name:
Dual specificity tyrosine-phosphorylation-regulated kinase 2
Synonyms:
DYRK2 | DYRK2_HUMAN | Dual-specificity tyrosine-phosphorylation regulated kinase 2
Type:
PROTEIN
Mol. Mass.:
66690.69
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1508025
Residue:
601
Sequence:
MLTRKPSAAAPAAYPTGRGGDSAVRQLQASPGLGAGATRSGVGTGPPSPIALPPLRASNAAAAAHTIGGSKHTMNDHLHVGSHAHGQIQVQQLFEDNSNKRTVLTTQPNGLTTVGKTGLPVVPERQLDSIHRRQGSSTSLKSMEGMGKVKATPMTPEQAMKQYMQKLTAFEHHEIFSYPEIYFLGLNAKKRQGMTGGPNNGGYDDDQGSYVQVPHDHVAYRYEVLKVIGKGSFGQVVKAYDHKVHQHVALKMVRNEKRFHRQAAEEIRILEHLRKQDKDNTMNVIHMLENFTFRNHICMTFELLSMNLYELIKKNKFQGFSLPLVRKFAHSILQCLDALHKNRIIHCDLKPENILLKQQGRSGIKVIDFGSSCYEHQRVYTYIQSRFYRAPEVILGARYGMPIDMWSLGCILAELLTGYPLLPGEDEGDQLACMIELLGMPSQKLLDASKRAKNFVSSKGYPRYCTVTTLSDGSVVLNGGRSRRGKLRGPPESREWGNALKGCDDPLFLDFLKQCLEWDPAVRMTPGQALRHPWLRRRLPKPPTGEKTSVKRITESTGAITSISKLPPPSSSASKLRTNLAQMTDANGNIQQRTVLPKLVS
Inhibitor
Name:
BDBM50347750
Synonyms:
CHEMBL1802358
Type:
Small organic molecule
Emp. Form.:
C17H13N3O3
Mol. Mass.:
307.3034
SMILES:
O=C1NC(Nc2ccccc2)=NC1=Cc1ccc2OCOc2c1 |w:13.15,c:11|
Structure:
