Target
Ephrin type-A receptor 2 [596-900]
Ligand
BDBM209862
Substrate
n/a
Meas. Tech.
Kinobeads Competition Assay
Kd
265±0.0 nM
Citation
 Heinzlmeir, SKudlinzki, DSreeramulu, SKlaeger, SGande, SLLinhard, VWilhelm, MQiao, HHelm, DRuprecht, BSaxena, KMédard, GSchwalbe, HKuster, 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:
BDBM209862
Synonyms:
4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]cyclohexane-1-carboxylic acid | MK-5108
Type:
Small organic molecule
Emp. Form.:
C22H21ClFN3O3S
Mol. Mass.:
461.937
SMILES:
OC(=O)C1(Cc2cccc(Nc3nccs3)n2)CCC(CC1)Oc1cccc(Cl)c1F |(6.1,3.85,;7.64,3.85,;8.41,5.18,;8.41,2.52,;9.18,3.85,;10.72,3.85,;11.49,5.18,;13.03,5.18,;13.8,3.85,;13.03,2.52,;13.8,1.18,;15.35,1.18,;16.25,-.06,;17.71,.41,;17.71,1.95,;16.25,2.43,;11.49,2.52,;7.08,1.75,;7.08,.21,;8.41,-.56,;9.75,.21,;9.75,1.75,;8.41,-2.1,;7.08,-2.87,;7.08,-4.41,;5.75,-5.18,;4.41,-4.41,;4.41,-2.87,;3.08,-2.1,;5.75,-2.1,;5.75,-.56,)|
Structure:
Search PDB for entries with ligand similarity: