Target
Ephrin type-A receptor 2
Ligand
BDBM50021626
Substrate
n/a
Meas. Tech.
ChEMBL_1368133 (CHEMBL3301278)
IC50
>10000±n/a nM
Citation
 Casuscelli, FArdini, EAvanzi, NCasale, ECervi, GD'Anello, MDonati, DFaiardi, DFerguson, RDFogliatto, GGalvani, AMarsiglio, AMirizzi, DGMontemartini, MOrrenius, CPapeo, GPiutti, CSalom, BFelder, ER Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. Bioorg Med Chem 21:7364-80 (2013) [PubMed]  Article 
Target
Name:
Ephrin type-A receptor 2
Synonyms:
ECK | EPHA2 | EPHA2_HUMAN | Ephrin receptor | Epithelial cell kinase | Tyrosine-protein kinase receptor ECK
Type:
PROTEIN
Mol. Mass.:
108260.70
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1505248
Residue:
976
Sequence:
MELQAARACFALLWGCALAAAAAAQGKEVVLLDFAAAGGELGWLTHPYGKGWDLMQNIMNDMPIYMYSVCNVMSGDQDNWLRTNWVYRGEAERIFIELKFTVRDCNSFPGGASSCKETFNLYYAESDLDYGTNFQKRLFTKIDTIAPDEITVSSDFEARHVKLNVEERSVGPLTRKGFYLAFQDIGACVALLSVRVYYKKCPELLQGLAHFPETIAGSDAPSLATVAGTCVDHAVVPPGGEEPRMHCAVDGEWLVPIGQCLCQAGYEKVEDACQACSPGFFKFEASESPCLECPEHTLPSPEGATSCECEEGFFRAPQDPASMPCTRPPSAPHYLTAVGMGAKVELRWTPPQDSGGREDIVYSVTCEQCWPESGECGPCEASVRYSEPPHGLTRTSVTVSDLEPHMNYTFTVEARNGVSGLVTSRSFRTASVSINQTEPPKVRLEGRSTTSLSVSWSIPPPQQSRVWKYEVTYRKKGDSNSYNVRRTEGFSVTLDDLAPDTTYLVQVQALTQEGQGAGSKVHEFQTLSPEGSGNLAVIGGVAVGVVLLLVLAGVGFFIHRRRKNQRARQSPEDVYFSKSEQLKPLKTYVDPHTYEDPNQAVLKFTTEIHPSCVTRQKVIGAGEFGEVYKGMLKTSSGKKEVPVAIKTLKAGYTEKQRVDFLGEAGIMGQFSHHNIIRLEGVISKYKPMMIITEYMENGALDKFLREKDGEFSVLQLVGMLRGIAAGMKYLANMNYVHRDLAARNILVNSNLVCKVSDFGLSRVLEDDPEATYTTSGGKIPIRWTAPEAISYRKFTSASDVWSFGIVMWEVMTYGERPYWELSNHEVMKAINDGFRLPTPMDCPSAIYQLMMQCWQQERARRPKFADIVSILDKLIRAPDSLKTLADFDPRVSIRLPSTSGSEGVPFRTVSEWLESIKMQQYTEHFMAAGYTAIEKVVQMTNDDIKRIGVRLPGHQKRIAYSLLGLKDQVNTVGIPI
  
Inhibitor
Name:
BDBM50021626
Synonyms:
CHEMBL3298400
Type:
Small organic molecule
Emp. Form.:
C18H23N3O2S
Mol. Mass.:
345.459
SMILES:
CC(C)(C)CNC(=O)CC1CNC(=O)c2cc(cn12)-c1ccsc1
Structure:
Search PDB for entries with ligand similarity: