Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Ligand | BDBM50581214 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2150107 (CHEMBL5034569) |
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IC50 | 3.0±n/a nM |
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Citation | Lee Walmsley, D; Murray, JB; Dokurno, P; Massey, AJ; Benwell, K; Fiumana, A; Foloppe, N; Ray, S; Smith, J; Surgenor, AE; Edmonds, T; Demarles, D; Burbridge, M; Cruzalegui, F; Kotschy, A; Hubbard, RE Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B. J Med Chem64:8971-8991 (2021) [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_HUMAN | DYRK | DYRK1A | Dual specificity YAK1-related kinase | Dual specificity YAK1-related kinase 1A (Dyrk1A) | Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) | Dual-specificity tyrosine-phosphorylation regulated kinase 1A | Dual-specificity tyrosine-regulated kinases 1A | HP86 | MNB | MNBH |
Type: | Enzyme |
Mol. Mass.: | 85616.61 |
Organism: | Homo sapiens (Human) |
Description: | Q13627 |
Residue: | 763 |
Sequence: | MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
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BDBM50581214 |
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n/a |
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Name | BDBM50581214 |
Synonyms: | CHEMBL5078833 |
Type | Small organic molecule |
Emp. Form. | C19H15N5O2 |
Mol. Mass. | 345.3547 |
SMILES | Cc1nc(-c2ccc3OCOc3c2)c2c(c[nH]c2n1)-c1ccnc(N)c1 |
Structure |
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