Reaction Details |
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Target | Epithelial discoidin domain-containing receptor 1 |
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Ligand | BDBM50173334 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1579230 (CHEMBL3812310) |
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IC50 | 126±n/a nM |
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Citation | Wang, Q; Liu, F; Wang, B; Zou, F; Chen, C; Liu, X; Wang, A; Qi, S; Wang, W; Qi, Z; Zhao, Z; Hu, Z; Wang, W; Wang, L; Zhang, S; Wang, Y; Liu, J; Liu, Q Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). J Med Chem59:3964-79 (2016) [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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BDBM50173334 |
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n/a |
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Name | BDBM50173334 |
Synonyms: | CHEMBL3809935 |
Type | Small organic molecule |
Emp. Form. | C26H24F3N3O3 |
Mol. Mass. | 483.4823 |
SMILES | Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1OC1CCN(CC1)C(=O)c1ccncc1 |
Structure |
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