Target
Ephrin type-A receptor 7
Ligand
BDBM50605159
Substrate
n/a
Meas. Tech.
ChEMBL_2250568 (CHEMBL5164778)
IC50
162±n/a nM
Citation
 Wang, ZWang, JWang, YXiang, SSong, XTu, ZZhou, YZhang, ZMZhang, ZDing, KLu, X Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance. J Med Chem 65:6325-6337 (2022) [PubMed] 
Target
Name:
Ephrin type-A receptor 7
Synonyms:
2.7.10.1 | EHK-3 | EHK3 | EK11 | EPH homology kinase 3 | EPH-like kinase 11 | EPHA7 | EPHA7_HUMAN | Ephrin receptor | HEK11 | Tyrosine Kinase EPHA6 | Tyrosine Kinase EPHA7
Type:
n/a
Mol. Mass.:
112085.32
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
998
Sequence:
MVFQTRYPSWIILCYIWLLRFAHTGEAQAAKEVLLLDSKAQQTELEWISSPPNGWEEISGLDENYTPIRTYQVCQVMEPNQNNWLRTNWISKGNAQRIFVELKFTLRDCNSLPGVLGTCKETFNLYYYETDYDTGRNIRENLYVKIDTIAADESFTQGDLGERKMKLNTEVREIGPLSKKGFYLAFQDVGACIALVSVKVYYKKCWSIIENLAIFPDTVTGSEFSSLVEVRGTCVSSAEEEAENAPRMHCSAEGEWLVPIGKCICKAGYQQKGDTCEPCGRGFYKSSSQDLQCSRCPTHSFSDKEGSSRCECEDGYYRAPSDPPYVACTRPPSAPQNLIFNINQTTVSLEWSPPADNGGRNDVTYRILCKRCSWEQGECVPCGSNIGYMPQQTGLEDNYVTVMDLLAHANYTFEVEAVNGVSDLSRSQRLFAAVSITTGQAAPSQVSGVMKERVLQRSVELSWQEPEHPNGVITEYEIKYYEKDQRERTYSTVKTKSTSASINNLKPGTVYVFQIRAFTAAGYGNYSPRLDVATLEEATGKMFEATAVSSEQNPVIIIAVVAVAGTIILVFMVFGFIIGRRHCGYSKADQEGDEELYFHFKFPGTKTYIDPETYEDPNRAVHQFAKELDASCIKIERVIGAGEFGEVCSGRLKLPGKRDVAVAIKTLKVGYTEKQRRDFLCEASIMGQFDHPNVVHLEGVVTRGKPVMIVIEFMENGALDAFLRKHDGQFTVIQLVGMLRGIAAGMRYLADMGYVHRDLAARNILVNSNLVCKVSDFGLSRVIEDDPEAVYTTTGGKIPVRWTAPEAIQYRKFTSASDVWSYGIVMWEVMSYGERPYWDMSNQDVIKAIEEGYRLPAPMDCPAGLHQLMLDCWQKERAERPKFEQIVGILDKMIRNPNSLKTPLGTCSRPISPLLDQNTPDFTTFCSVGEWLQAIKMERYKDNFTAAGYNSLESVARMTIEDVMSLGITLVGHQKKIMSSIQTMRAQMLHLHGTGIQV
  
Inhibitor
Name:
BDBM50605159
Synonyms:
CHEMBL5195469
Type:
Small organic molecule
Emp. Form.:
C35H33F3N8O3
Mol. Mass.:
670.6835
SMILES:
CN1CCNC(=O)CCCCOc2cc(C#Cc3cnc4ccc1nn34)c(C)c(c2)C(=O)Nc1cc(cc(c1)C(F)(F)F)-n1cnc(C)c1
Structure:
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