Reaction Details |
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Target | Ephrin type-A receptor 2 [596-900] |
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Ligand | BDBM209861 |
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Substrate/Competitor | n/a |
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Meas. Tech. | HotSpot Kinase Activity Assay |
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IC50 | 4.8±0.0 nM |
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Citation | Heinzlmeir, S; Kudlinzki, D; Sreeramulu, S; Klaeger, S; Gande, SL; Linhard, V; Wilhelm, M; Qiao, H; Helm, D; Ruprecht, B; Saxena, K; Médard, G; Schwalbe, H; Kuster, B Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs. ACS Chem Biol11:3400-3411 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Ephrin type-A receptor 2 [596-900] |
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Name: | Ephrin type-A receptor 2 [596-900] |
Synonyms: | ECK | EPHA2 | EPHA2_HUMAN | Ephrin type-A receptor 2 (EPHA2) |
Type: | Protein |
Mol. Mass.: | 34367.96 |
Organism: | Homo sapiens (Human) |
Description: | EPHA2 truncation (596-900 aa); 519U |
Residue: | 305 |
Sequence: | DPNQAVLKFTTEIHPSCVTRQKVIGAGEFGEVYKGMLKTSSGKKEVPVAIKTLKAGYTEK
QRVDFLGEAGIMGQFSHHNIIRLEGVISKYKPMMIITEYMENGALDKFLREKDGEFSVLQ
LVGMLRGIAAGMKYLANMNYVHRDLAARNILVNSNLVCKVSDFGLSRVLEDDPEATYTTS
GGKIPIRWTAPEAISYRKFTSASDVWSFGIVMWEVMTYGERPYWELSNHEVMKAINDGFR
LPTPMDCPSAIYQLMMQCWQQERARRPKFADIVSILDKLIRAPDSLKTLADFDPRVSIRL
PSTSG
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BDBM209861 |
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n/a |
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Name | BDBM209861 |
Synonyms: | 5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide | TAK-901 |
Type | Small organic molecule |
Emp. Form. | C28H32N4O3S |
Mol. Mass. | 504.644 |
SMILES | CCS(=O)(=O)c1cccc(c1)-c1cc(C(=O)NC2CCN(C)CC2)c(C)c2[nH]c3ncc(C)cc3c12 |
Structure |
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