Reaction Details |
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Target | Epithelial discoidin domain-containing receptor 1 |
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Ligand | BDBM50300690 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1681165 (CHEMBL4031442) |
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Kd | 81±n/a nM |
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Citation | Wang, A; Li, X; Chen, C; Wu, H; Qi, Z; Hu, C; Yu, K; Wu, J; Liu, J; Liu, X; Hu, Z; Wang, W; Wang, W; Wang, W; Wang, L; Wang, B; Liu, Q; Li, L; Ge, J; Ren, T; Zhang, S; Xia, R; Liu, J; Liu, Q Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. J Med Chem60:8407-8424 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Epithelial discoidin domain-containing receptor 1 |
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Name: | Epithelial discoidin domain-containing receptor 1 |
Synonyms: | CAK | DDR1 | DDR1_HUMAN | Discoidin domain receptor 1 (DDR1) | Discoidin domain-containing receptor 1 (DDR1) | Discoidin receptor tyrosine kinase | EDDR1 | Epithelial discoidin domain receptor 1 | Epithelial discoidin domain receptor 1 (DDR1) | Epithelial discoidin domain-containing receptor 1 | Epithelial discoidin domain-containing receptor 1 (DDR1) | HGK2 | Mammary carcinoma kinase 10 | NEP | NTRK4 | PTK3A | Protein-tyrosine kinase RTK 6 | RTK6 | TRKE | Tyrosine-protein kinase CAK |
Type: | Tyrosine-protein kinase |
Mol. Mass.: | 101130.02 |
Organism: | Homo sapiens (Human) |
Description: | Q08345 |
Residue: | 913 |
Sequence: | MGPEALSSLLLLLLVASGDADMKGHFDPAKCRYALGMQDRTIPDSDISASSSWSDSTAAR
HSRLESSDGDGAWCPAGSVFPKEEEYLQVDLQRLHLVALVGTQGRHAGGLGKEFSRSYRL
RYSRDGRRWMGWKDRWGQEVISGNEDPEGVVLKDLGPPMVARLVRFYPRADRVMSVCLRV
ELYGCLWRDGLLSYTAPVGQTMYLSEAVYLNDSTYDGHTVGGLQYGGLGQLADGVVGLDD
FRKSQELRVWPGYDYVGWSNHSFSSGYVEMEFEFDRLRAFQAMQVHCNNMHTLGARLPGG
VECRFRRGPAMAWEGEPMRHNLGGNLGDPRARAVSVPLGGRVARFLQCRFLFAGPWLLFS
EISFISDVVNNSSPALGGTFPPAPWWPPGPPPTNFSSLELEPRGQQPVAKAEGSPTAILI
GCLVAIILLLLLIIALMLWRLHWRRLLSKAERRVLEEELTVHLSVPGDTILINNRPGPRE
PPPYQEPRPRGNPPHSAPCVPNGSALLLSNPAYRLLLATYARPPRGPGPPTPAWAKPTNT
QAYSGDYMEPEKPGAPLLPPPPQNSVPHYAEADIVTLQGVTGGNTYAVPALPPGAVGDGP
PRVDFPRSRLRFKEKLGEGQFGEVHLCEVDSPQDLVSLDFPLNVRKGHPLLVAVKILRPD
ATKNARNDFLKEVKIMSRLKDPNIIRLLGVCVQDDPLCMITDYMENGDLNQFLSAHQLED
KAAEGAPGDGQAAQGPTISYPMLLHVAAQIASGMRYLATLNFVHRDLATRNCLVGENFTI
KIADFGMSRNLYAGDYYRVQGRAVLPIRWMAWECILMGKFTTASDVWAFGVTLWEVLMLC
RAQPFGQLTDEQVIENAGEFFRDQGRQVYLSRPPACPQGLYELMLRCWSRESEQRPPFSQ
LHRFLAEDALNTV
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BDBM50300690 |
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n/a |
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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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