| Reaction Details |
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 | Report a problem with these data |
| Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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| Ligand | BDBM50466158 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1803673 (CHEMBL4275965) |
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| IC50 | 14±n/a nM |
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| Citation |  Darwish, SS; Abdel-Halim, M; ElHady, AK; Salah, M; Abadi, AH; Becker, W; Engel, M Development of novel amide-derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification. Eur J Med Chem158:270-285 (2018) [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 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 85616.61 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q13627 |
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| Residue: | 763 |
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| Sequence: | MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
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| BDBM50466158 |
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| n/a |
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| Name | BDBM50466158 |
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| Synonyms: | CHEMBL4290247 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H16FN3OS |
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| Mol. Mass. | 389.445 |
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| SMILES | Fc1ccc(CC(=O)Nc2cncc(c2)-c2cc(cs2)-c2cccnc2)cc1 |
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| Structure | 
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