Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Ligand | BDBM50347760 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_756286 (CHEMBL1805099) |
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IC50 | 240±n/a nM |
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Citation | Debdab, M; Carreaux, F; Renault, S; Soundararajan, M; Fedorov, O; Filippakopoulos, P; Lozach, O; Babault, L; Tahtouh, T; Baratte, B; Ogawa, Y; Hagiwara, M; Eisenreich, A; Rauch, U; Knapp, S; Meijer, L; Bazureau, JP Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem54:4172-86 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Name: | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
Synonyms: | DYR1A_RAT | Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A | Dyrk | Dyrk1a |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 85573.59 |
Organism: | RAT |
Description: | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A 0 RAT::Q63470 |
Residue: | 763 |
Sequence: | MHTGGETSACKPSSVRLAPSFSFHAAGLQMAAQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWSLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFAAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
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BDBM50347760 |
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n/a |
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Name | BDBM50347760 |
Synonyms: | CHEMBL1803071 |
Type | Small organic molecule |
Emp. Form. | C19H17N3O4 |
Mol. Mass. | 351.356 |
SMILES | COc1ccc(NC2=NC(=Cc3ccc4OCOc4c3)C(=O)N2C)cc1 |w:10.10,t:7| |
Structure |
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