Reaction Details Report a problem with these data
Target
Ephrin type-A receptor 2 [596-900]
Ligand
BDBM13216
Substrate
n/a
Meas. Tech.
Kinobeads Competition Assay
Kd
2.8±0.0 nM
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 Biol 11:3400-3411 (2016) [PubMed]  Article 
Target
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:
DPNQAVLKFTTEIHPSCVTRQKVIGAGEFGEVYKGMLKTSSGKKEVPVAIKTLKAGYTEKQRVDFLGEAGIMGQFSHHNIIRLEGVISKYKPMMIITEYMENGALDKFLREKDGEFSVLQLVGMLRGIAAGMKYLANMNYVHRDLAARNILVNSNLVCKVSDFGLSRVLEDDPEATYTTSGGKIPIRWTAPEAISYRKFTSASDVWSFGIVMWEVMTYGERPYWELSNHEVMKAINDGFRLPTPMDCPSAIYQLMMQCWQQERARRPKFADIVSILDKLIRAPDSLKTLADFDPRVSIRLPSTSG
  
Inhibitor
Name:
BDBM13216
Synonyms:
BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide | N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide | US10294227, Code Dasatinib | US20230348453, Compound A8 | cid_3062316 | med.21724, Compound Dasatinib
Type:
Small organic molecule
Emp. Form.:
C22H26ClN7O2S
Mol. Mass.:
488.006
SMILES:
Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCN(CCO)CC1
Structure:
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