| 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 | BDBM50538096 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1972149 (CHEMBL4604967) |
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| IC50 | 25±n/a nM |
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| Citation |  Liu, YA; Jin, Q; Zou, Y; Ding, Q; Yan, S; Wang, Z; Hao, X; Nguyen, B; Zhang, X; Pan, J; Mo, T; Jacobsen, K; Lam, T; Wu, TY; Petrassi, HM; Bursulaya, B; DiDonato, M; Gordon, WP; Liu, B; Baaten, J; Hill, R; Nguyen-Tran, V; Qiu, M; Zhang, YQ; Kamireddy, A; Espinola, S; Deaton, L; Ha, S; Harb, G; Jia, Y; Li, J; Shen, W; Schumacher, AM; Colman, K; Glynne, R; Pan, S; McNamara, P; Laffitte, B; Meeusen, S; Molteni, V; Loren, J Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem63:2958-2973 (2020) [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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| BDBM50538096 |
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| n/a |
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| Name | BDBM50538096 |
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| Synonyms: | CHEMBL4641672 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H25N5O3 |
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| Mol. Mass. | 407.4656 |
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| SMILES | O=C(Nc1cc(ccn1)-c1cn(C2CCOCC2)c2cnccc12)N1CCOCC1 |
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| Structure | 
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