Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Ligand | BDBM50538091 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1972149 (CHEMBL4604967) |
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IC50 | 17±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 |
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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BDBM50538091 |
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n/a |
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Name | BDBM50538091 |
Synonyms: | CHEMBL4640465 |
Type | Small organic molecule |
Emp. Form. | C18H14N4 |
Mol. Mass. | 286.3306 |
SMILES | Nc1cc(ccn1)-c1cn(-c2ccccc2)c2cnccc12 |
Structure |
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