Reaction Details |
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Target | Ephrin type-A receptor 3 |
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Ligand | BDBM50345579 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_751823 (CHEMBL1785578) |
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IC50 | 1.2±n/a nM |
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Citation | Thomas, M; Huang, WS; Wen, D; Zhu, X; Wang, Y; Metcalf, CA; Liu, S; Chen, I; Romero, J; Zou, D; Sundaramoorthi, R; Li, F; Qi, J; Cai, L; Zhou, T; Commodore, L; Xu, Q; Keats, J; Wang, F; Wardwell, S; Ning, Y; Snodgrass, JT; Broudy, MI; Russian, K; Iuliucci, J; Rivera, VM; Sawyer, TK; Dalgarno, DC; Clackson, T; Shakespeare, WC Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. Bioorg Med Chem Lett21:3743-8 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Ephrin type-A receptor 3 |
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Name: | Ephrin type-A receptor 3 |
Synonyms: | EPHA3 | EPHA3_HUMAN | ETK | ETK1 | Ephrin receptor | Ephrin type-A receptor 3 | Ephrin type-A receptor 3 (EPHA3) | HEK | TYRO4 |
Type: | Protein |
Mol. Mass.: | 110131.95 |
Organism: | Homo sapiens (Human) |
Description: | P29320 |
Residue: | 983 |
Sequence: | MDCQLSILLLLSCSVLDSFGELIPQPSNEVNLLDSKTIQGELGWISYPSHGWEEISGVDE
HYTPIRTYQVCNVMDHSQNNWLRTNWVPRNSAQKIYVELKFTLRDCNSIPLVLGTCKETF
NLYYMESDDDHGVKFREHQFTKIDTIAADESFTQMDLGDRILKLNTEIREVGPVNKKGFY
LAFQDVGACVALVSVRVYFKKCPFTVKNLAMFPDTVPMDSQSLVEVRGSCVNNSKEEDPP
RMYCSTEGEWLVPIGKCSCNAGYEERGFMCQACRPGFYKALDGNMKCAKCPPHSSTQEDG
SMNCRCENNYFRADKDPPSMACTRPPSSPRNVISNINETSVILDWSWPLDTGGRKDVTFN
IICKKCGWNIKQCEPCSPNVRFLPRQFGLTNTTVTVTDLLAHTNYTFEIDAVNGVSELSS
PPRQFAAVSITTNQAAPSPVLTIKKDRTSRNSISLSWQEPEHPNGIILDYEVKYYEKQEQ
ETSYTILRARGTNVTISSLKPDTIYVFQIRARTAAGYGTNSRKFEFETSPDSFSISGESS
QVVMIAISAAVAIILLTVVIYVLIGRFCGYKSKHGADEKRLHFGNGHLKLPGLRTYVDPH
TYEDPTQAVHEFAKELDATNISIDKVVGAGEFGEVCSGRLKLPSKKEISVAIKTLKVGYT
EKQRRDFLGEASIMGQFDHPNIIRLEGVVTKSKPVMIVTEYMENGSLDSFLRKHDAQFTV
IQLVGMLRGIASGMKYLSDMGYVHRDLAARNILINSNLVCKVSDFGLSRVLEDDPEAAYT
TRGGKIPIRWTSPEAIAYRKFTSASDVWSYGIVLWEVMSYGERPYWEMSNQDVIKAVDEG
YRLPPPMDCPAALYQLMLDCWQKDRNNRPKFEQIVSILDKLIRNPGSLKIITSAAARPSN
LLLDQSNVDITTFRTTGDWLNGVWTAHCKEIFTGVEYSSCDTIAKISTDDMKKVGVTVVG
PQKKIISSIKALETQSKNGPVPV
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BDBM50345579 |
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n/a |
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Name | BDBM50345579 |
Synonyms: | 5-((5-(4-((4-(2-hydroxyethyl)piperazin-1-yl)methyl)-3-(trifluoromethyl)phenylcarbamoyl)-2-methylphenyl)ethynyl)-N,1-dimethyl-1H-imidazole-2-carboxamide | CHEMBL1784637 |
Type | Small organic molecule |
Emp. Form. | C30H33F3N6O3 |
Mol. Mass. | 582.6166 |
SMILES | CNC(=O)c1ncc(C#Cc2cc(ccc2C)C(=O)Nc2ccc(CN3CCN(CCO)CC3)c(c2)C(F)(F)F)n1C |
Structure |
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