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Target
Inhibitor of nuclear factor kappa-B kinase subunit alpha
Ligand
BDBM50300690
Substrate
n/a
Meas. Tech.
ChEMBL_655413 (CHEMBL1244457)
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:
Inhibitor of nuclear factor kappa-B kinase subunit alpha
Synonyms:
CHUK | Conserved helix-loop-helix ubiquitous kinase | I-kappa-B kinase 1 | I-kappa-B kinase alpha | IKK-A | IKK-alpha | IKK1 | IKK2/IKK1 | IKKA | IKKA_HUMAN | IkBKA | IkappaB kinase | Inhibitor of NF-kappa-B kinase alpha/beta | NFKBIKA | Nuclear factor NF-kappa-B inhibitor kinase alpha | TCF-16 | TCF16 | Transcription factor 16
Type:
PROTEIN
Mol. Mass.:
84642.21
Organism:
Homo sapiens (Human)
Description:
ChEMBL_327453
Residue:
745
Sequence:
MERPPGLRPGAGGPWEMRERLGTGGFGNVCLYQHRELDLKIAIKSCRLELSTKNRERWCHEIQIMKKLNHANVVKACDVPEELNILIHDVPLLAMEYCSGGDLRKLLNKPENCCGLKESQILSLLSDIGSGIRYLHENKIIHRDLKPENIVLQDVGGKIIHKIIDLGYAKDVDQGSLCTSFVGTLQYLAPELFENKPYTATVDYWSFGTMVFECIAGYRPFLHHLQPFTWHEKIKKKDPKCIFACEEMSGEVRFSSHLPQPNSLCSLVVEPMENWLQLMLNWDPQQRGGPVDLTLKQPRCFVLMDHILNLKIVHILNMTSAKIISFLLPPDESLHSLQSRIERETGINTGSQELLSETGISLDPRKPASQCVLDGVRGCDSYMVYLFDKSKTVYEGPFASRSLSDCVNYIVQDSKIQLPIIQLRKVWAEAVHYVSGLKEDYSRLFQGQRAAMLSLLRYNANLTKMKNTLISASQQLKAKLEFFHKSIQLDLERYSEQMTYGISSEKMLKAWKEMEEKAIHYAEVGVIGYLEDQIMSLHAEIMELQKSPYGRRQGDLMESLEQRAIDLYKQLKHRPSDHSYSDSTEMVKIIVHTVQSQDRVLKELFGHLSKLLGCKQKIIDLLPKVEVALSNIKEADNTVMFMQGKRQKEIWHLLKIACTQSSARSLVGSSLEGAVTPQTSAWLPPTSAEHDHSLSCVVTPQDGETSAQMIEENLNCLGHLSTIIHEANEEQGNSMMNLDWSWLTE
  
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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