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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50162287
Substrate
n/a
Meas. Tech.
ChEMBL_2294024
IC50
19±n/a nM
Citation
 Pathak, A; Rohilla, A; Gupta, T; Akhtar, MJ; Haider, MR; Sharma, K; Haider, K; Yar, MS DYRK1A kinase inhibition with emphasis on neurodegeneration: A comprehensive evolution story-cum-perspective. Eur J Med Chem 158:559-592 (2018) [PubMed] 
Target
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:
Human
Description:
Q13627
Residue:
763
Sequence:
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
  
Inhibitor
Name:
BDBM50162287
Synonyms:
(Rebeccamycin)1,11-dichloro-12-(3,4-dihydroxy-6-hydroxymethyl-5-methoxytetrahydro-2H-2-pyranyl)-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione | 1,11-dichloro-12-(3,4-dihydroxy-6-hydroxymethyl-5-methoxytetrahydro-2H-2-pyranyl)-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione | 1,11-dichloro-12-(3,4-dihydroxy-6-hydroxymethyl-5-methoxytetrahydro-2H-2-pyranyl)-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione(rebeccamycin) | 1,11-dichloro-12-[3,4-dihydroxy-6-hydroxymethyl-5-methoxy-(2R,3R,4S,5R,6R)-tetrahydro-2H-2-pyranyl]-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione | CHEMBL370100 | Rebeccamycin
Type:
Small organic molecule
Emp. Form.:
C27H21Cl2N3O7
Mol. Mass.:
570.378
SMILES:
CO[C@@H]1[C@@H](CO)O[C@H]([C@H](O)[C@H]1O)n1c2c(Cl)cccc2c2c3C(=O)NC(=O)c3c3c4cccc(Cl)c4[nH]c3c12 |r|
Structure:
Search PDB for entries with ligand similarity: