Reaction Details |
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Target | Ephrin type-A receptor 2 [596-900] |
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Ligand | BDBM4552 |
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Substrate/Competitor | n/a |
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Meas. Tech. | HotSpot Kinase Activity Assay |
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IC50 | 2.0±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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BDBM4552 |
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n/a |
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Name | BDBM4552 |
Synonyms: | 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile | 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile | BOSUTINIB | CHEMBL288441 | SKI-606 |
Type | Small organic molecule |
Emp. Form. | C26H29Cl2N5O3 |
Mol. Mass. | 530.446 |
SMILES | COc1cc(Nc2c(cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)C#N)c(Cl)cc1Cl |
Structure |
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