Reaction Details |
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Target | Epithelial discoidin domain-containing receptor 1 |
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Ligand | BDBM50430857 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_945426 (CHEMBL2342537) |
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IC50 | 6.1±n/a nM |
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Citation | Gao, M; Duan, L; Luo, J; Zhang, L; Lu, X; Zhang, Y; Zhang, Z; Tu, Z; Xu, Y; Ren, X; Ding, K Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. J Med Chem56:3281-95 (2013) [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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BDBM50430857 |
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n/a |
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Name | BDBM50430857 |
Synonyms: | CHEMBL2336021 |
Type | Small organic molecule |
Emp. Form. | C23H15F3N4O |
Mol. Mass. | 420.3866 |
SMILES | Cc1ccc(cc1C#Cc1cnc2ccnn2c1)C(=O)Nc1cccc(c1)C(F)(F)F |
Structure |
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