Reaction Details |
| Report a problem with these data |
Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
---|
Ligand | BDBM50347388 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_754583 (CHEMBL1806286) |
---|
IC50 | 2100±n/a nM |
---|
Citation | Heathcote, DA; Patel, H; Kroll, SH; Hazel, P; Periyasamy, M; Alikian, M; Kanneganti, SK; Jogalekar, AS; Scheiper, B; Barbazanges, M; Blum, A; Brackow, J; Siwicka, A; Pace, RD; Fuchter, MJ; Snyder, JP; Liotta, DC; Freemont, PS; Aboagye, EO; Coombes, RC; Barrett, AG; Ali, S A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem53:8508-22 (2010) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
---|
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
|
|
|
BDBM50347388 |
---|
n/a |
---|
Name | BDBM50347388 |
Synonyms: | CHEMBL1234833 |
Type | Small organic molecule |
Emp. Form. | C20H27N5O3 |
Mol. Mass. | 385.4601 |
SMILES | CC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r| |
Structure |
|