Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Ligand | BDBM50305006 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_606925 (CHEMBL1072668) |
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IC50 | 440±n/a nM |
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Citation | Harris, CM; Ericsson, AM; Argiriadi, MA; Barberis, C; Borhani, DW; Burchat, A; Calderwood, DJ; Cunha, GA; Dixon, RW; Frank, KE; Johnson, EF; Kamens, J; Kwak, S; Li, B; Mullen, KD; Perron, DC; Wang, L; Wishart, N; Wu, X; Zhang, X; Zmetra, TR; Talanian, RV 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. Bioorg Med Chem Lett20:334-7 (2010) [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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BDBM50305006 |
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n/a |
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Name | BDBM50305006 |
Synonyms: | 5-(2-aminoethyl)-7-(7-(benzo[b]thiophen-2-yl)-1H-indazol-5-yl)-5H-pyrrolo[3,2-d]pyrimidin-2-amine | CHEMBL590109 |
Type | Small organic molecule |
Emp. Form. | C23H19N7S |
Mol. Mass. | 425.509 |
SMILES | NCCn1cc(-c2cc(-c3cc4ccccc4s3)c3[nH]ncc3c2)c2nc(N)ncc12 |
Structure |
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