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Target
Ribosomal protein S6 kinase alpha-5
Ligand
BDBM50300690
Substrate
n/a
Meas. Tech.
ChEMBL_655922 (CHEMBL1244966)
Kd
>10000±n/a nM
Citation
 Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114:2984-92 (2009) [PubMed]  Article 
Target
Name:
Ribosomal protein S6 kinase alpha-5
Synonyms:
90 kDa ribosomal protein S6 kinase 5 | KS6A5_HUMAN | MSK1 | Mitogen- and Stress-Activated Protein Kinase 1 (MSK1) | Nuclear mitogen- and stress-activated protein kinase 1 | Nuclear mitogen- and stress-activated protein kinase 1 (MSK1) | RPS6KA5 | RPS6KA5(Kin.Dom.2 - C-terminal) | RSK-like protein kinase | RSKL | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha 5 | Ribosomal protein S6 kinase alpha-5
Type:
Serine/threonine-protein kinase
Mol. Mass.:
89874.44
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
802
Sequence:
MEEEGGSSGGAAGTSADGGDGGEQLLTVKHELRTANLTGHAEKVGIENFELLKVLGTGAYGKVFLVRKISGHDTGKLYAMKVLKKATIVQKAKTTEHTRTERQVLEHIRQSPFLVTLHYAFQTETKLHLILDYINGGELFTHLSQRERFTEHEVQIYVGEIVLALEHLHKLGIIYRDIKLENILLDSNGHVVLTDFGLSKEFVADETERAYSFCGTIEYMAPDIVRGGDSGHDKAVDWWSLGVLMYELLTGASPFTVDGEKNSQAEISRRILKSEPPYPQEMSALAKDLIQRLLMKDPKKRLGCGPRDADEIKEHLFFQKINWDDLAAKKVPAPFKPVIRDELDVSNFAEEFTEMDPTYSPAALPQSSEKLFQGYSFVAPSILFKRNAAVIDPLQFHMGVERPGVTNVARSAMMKDSPFYQHYDLDLKDKPLGEGSFSICRKCVHKKSNQAFAVKIISKRMEANTQKEITALKLCEGHPNIVKLHEVFHDQLHTFLVMELLNGGELFERIKKKKHFSETEASYIMRKLVSAVSHMHDVGVVHRDLKPENLLFTDENDNLEIKIIDFGFARLKPPDNQPLKTPCFTLHYAAPELLNQNGYDESCDLWSLGVILYTMLSGQVPFQSHDRSLTCTSAVEIMKKIKKGDFSFEGEAWKNVSQEAKDLIQGLLTVDPNKRLKMSGLRYNEWLQDGSQLSSNPLMTPDILGSSGAAVHTCVKATFHAFNKYKREGFCLQNVDKAPLAKRRKMKKTSTSTETRSSSSESSHSSSSHSHGKTTPTKTLQPSNPADSNNPETLFQFSDSVA
  
Inhibitor
Name:
BDBM50300690
Synonyms:
1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morpholin-4-Yl)ethoxy]imidazo[2,1-B][1,3]benzothiazol-2-Yl}phenyl)urea | AC 010220 | AC 220 | AC-220 | AC010220 | AC220 | ASP-2689 | CHEMBL576982 | N-(5-tert-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea | Quizartinib | Quizartinib (AC220) | US10266535, Compound AC220 | US11542261, Compound quizartinib | US9216997, Quizartinib (positive compound)
Type:
Small organic molecule
Emp. Form.:
C29H32N6O4S
Mol. Mass.:
560.667
SMILES:
CC(C)(C)c1cc(NC(=O)Nc2ccc(cc2)-c2cn3c(n2)sc2cc(OCCN4CCOCC4)ccc32)no1
Structure:
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