Reaction Details Report a problem with these data
Target
Ephrin type-A receptor 2 [596-900]
Ligand
BDBM50100615
Substrate
n/a
Meas. Tech.
HotSpot Kinase Activity Assay
IC50
13±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:
BDBM50100615
Synonyms:
E-7050 | E7050 | Golvatinib
Type:
Small organic molecule
Emp. Form.:
C33H37F2N7O4
Mol. Mass.:
633.6882
SMILES:
CN1CCN(CC1)C1CCN(CC1)C(=O)Nc1cc(Oc2ccc(NC(=O)C3(CC3)C(=O)Nc3ccc(F)cc3)c(F)c2)ccn1
Structure:
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