Target
Ephrin type-A receptor 1
Ligand
BDBM50204290
Substrate
n/a
Meas. Tech.
ChEMBL_1627207 (CHEMBL3869728)
IC50
31±n/a nM
Citation
 Lam, BArikawa, YCramlett, JDong, Qde Jong, RFeher, VGrimshaw, CEFarrell, PJHoffman, IDJennings, AJones, BMatuszkiewicz, JMiura, JMiyake, HNatala, SRShi, LTakahashi, MTaylor, EWyrick, CYano, JZalevsky, JNie, Z Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett 26:5947-5950 (2016) [PubMed]  Article 
Target
Name:
Ephrin type-A receptor 1
Synonyms:
EPH | EPH tyrosine kinase | EPH tyrosine kinase 1 | EPHA1 | EPHA1_HUMAN | EPHT | EPHT1 | Ephrin receptor | Ephrin type-A receptor 1 | Ephrin type-A receptor 1 (EPHA1) | Erythropoietin-producing hepatoma receptor | Tyrosine-protein kinase receptor EPH | hEpha1
Type:
Enzyme
Mol. Mass.:
108128.04
Organism:
Homo sapiens (Human)
Description:
P21709
Residue:
976
Sequence:
MERRWPLGLGLVLLLCAPLPPGARAKEVTLMDTSKAQGELGWLLDPPKDGWSEQQQILNGTPLYMYQDCPMQGRRDTDHWLRSNWIYRGEEASRVHVELQFTVRDCKSFPGGAGPLGCKETFNLLYMESDQDVGIQLRRPLFQKVTTVAADQSFTIRDLVSGSVKLNVERCSLGRLTRRGLYLAFHNPGACVALVSVRVFYQRCPETLNGLAQFPDTLPGPAGLVEVAGTCLPHARASPRPSGAPRMHCSPDGEWLVPVGRCHCEPGYEEGGSGEACVACPSGSYRMDMDTPHCLTCPQQSTAESEGATICTCESGHYRAPGEGPQVACTGPPSAPRNLSFSASGTQLSLRWEPPADTGGRQDVRYSVRCSQCQGTAQDGGPCQPCGVGVHFSPGARGLTTPAVHVNGLEPYANYTFNVEAQNGVSGLGSSGHASTSVSISMGHAESLSGLSLRLVKKEPRQLELTWAGSRPRSPGANLTYELHVLNQDEERYQMVLEPRVLLTELQPDTTYIVRVRMLTPLGPGPFSPDHEFRTSPPVSRGLTGGEIVAVIFGLLLGAALLLGILVFRSRRAQRQRQQRQRDRATDVDREDKLWLKPYVDLQAYEDPAQGALDFTRELDPAWLMVDTVIGEGEFGEVYRGTLRLPSQDCKTVAIKTLKDTSPGGQWWNFLREATIMGQFSHPHILHLEGVVTKRKPIMIITEFMENGALDAFLREREDQLVPGQLVAMLQGIASGMNYLSNHNYVHRDLAARNILVNQNLCCKVSDFGLTRLLDDFDGTYETQGGKIPIRWTAPEAIAHRIFTTASDVWSFGIVMWEVLSFGDKPYGEMSNQEVMKSIEDGYRLPPPVDCPAPLYELMKNCWAYDRARRPHFQKLQAHLEQLLANPHSLRTIANFDPRMTLRLPSLSGSDGIPYRTVSEWLESIRMKRYILHFHSAGLDTMECVLELTAEDLTQMGITLPGHQKRILCSIQGFKD
  
Inhibitor
Name:
BDBM50204290
Synonyms:
CHEMBL3979920 | US11077111, Compound IIIa | US20230295171, Example 102
Type:
Small organic molecule
Emp. Form.:
C17H21FN6O
Mol. Mass.:
344.3866
SMILES:
Cn1cc(cn1)-c1nc(N[C@@H]2CCCC[C@@H]2N)c(F)c2CNC(=O)c12 |r|
Structure:
Search PDB for entries with ligand similarity: