Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Ligand | BDBM50583749 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2158056 (CHEMBL5042806) |
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IC50 | 6.0±n/a nM |
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Citation | Weber, C; Sipos, M; Paczal, A; Balint, B; Kun, V; Foloppe, N; Dokurno, P; Massey, AJ; Walmsley, DL; Hubbard, RE; Murray, J; Benwell, K; Edmonds, T; Demarles, D; Bruno, A; Burbridge, M; Cruzalegui, F; Kotschy, A Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors. J Med Chem64:6745-6764 (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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BDBM50583749 |
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n/a |
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Name | BDBM50583749 |
Synonyms: | CHEMBL5089294 |
Type | Small organic molecule |
Emp. Form. | C16H20N6O |
Mol. Mass. | 312.3696 |
SMILES | COCCCn1c(C)nc2ccc(nc12)-c1cc(N)nc(N)c1 |
Structure |
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