Reaction Details Report a problem with these data
Target
Ephrin type-A receptor 2 [596-900]
Ligand
BDBM209858
Substrate
n/a
Meas. Tech.
HotSpot Kinase Activity Assay
IC50
4.4±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:
BDBM209858
Synonyms:
Danusertib | N-[5-[(2R)-2-methoxy-2-phenylacetyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide
Type:
Small organic molecule
Emp. Form.:
C26H30N6O3
Mol. Mass.:
474.5548
SMILES:
CO[C@@H](C(=O)N1Cc2[nH]nc(NC(=O)c3ccc(cc3)N3CCN(C)CC3)c2C1)c1ccccc1
Structure:
Search PDB for entries with ligand similarity: