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TargetEphrin type-B receptor 4
LigandBDBM50198782
Substrate/Competitorn/a
Meas. Tech.ChEMBL_437765 (CHEMBL905854)
Ki 63.8±n/a nM
Citation Noronha, GBarrett, KBoccia, ABrodhag, TCao, JChow, CPDneprovskaia, EDoukas, JFine, RGong, XGritzen, CGu, HHanna, EHood, JDHu, SKang, XKey, JKlebansky, BKousba, ALi, GLohse, DMak, CCMcPherson, APalanki, MSPathak, VPRenick, JShi, FSoll, RSplittgerber, UStoughton, STang, SYee, SZeng, BZhao, NZhu, H Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. Bioorg Med Chem Lett17:602-8 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Ephrin type-B receptor 4
Name:Ephrin type-B receptor 4
Synonyms:EPHB4 | EPHB4_HUMAN | Ephrin receptor | Ephrin type-B receptor 4 precursor (Tyrosine-protein kinase receptor HTK). | HTK | Hepatoma transmembrane kinase | MYK1 | TYRO11 | Tyrosine-protein kinase TYRO11 | VHL/Ephrin type-B receptor 4
Type:Enzyme
Mol. Mass.:108273.51
Organism:Homo sapiens (Human)
Description:P54760
Residue:987
Sequence:
MELRVLLCWASLAAALEETLLNTKLETADLKWVTFPQVDGQWEELSGLDEEQHSVRTYEV
CDVQRAPGQAHWLRTGWVPRRGAVHVYATLRFTMLECLSLPRAGRSCKETFTVFYYESDA
DTATALTPAWMENPYIKVDTVAAEHLTRKRPGAEATGKVNVKTLRLGPLSKAGFYLAFQD
QGACMALLSLHLFYKKCAQLTVNLTRFPETVPRELVVPVAGSCVVDAVPAPGPSPSLYCR
EDGQWAEQPVTGCSCAPGFEAAEGNTKCRACAQGTFKPLSGEGSCQPCPANSHSNTIGSA
VCQCRVGYFRARTDPRGAPCTTPPSAPRSVVSRLNGSSLHLEWSAPLESGGREDLTYALR
CRECRPGGSCAPCGGDLTFDPGPRDLVEPWVVVRGLRPDFTYTFEVTALNGVSSLATGPV
PFEPVNVTTDREVPPAVSDIRVTRSSPSSLSLAWAVPRAPSGAVLDYEVKYHEKGAEGPS
SVRFLKTSENRAELRGLKRGASYLVQVRARSEAGYGPFGQEHHSQTQLDESEGWREQLAL
IAGTAVVGVVLVLVVIVVAVLCLRKQSNGREAEYSDKHGQYLIGHGTKVYIDPFTYEDPN
EAVREFAKEIDVSYVKIEEVIGAGEFGEVCRGRLKAPGKKESCVAIKTLKGGYTERQRRE
FLSEASIMGQFEHPNIIRLEGVVTNSMPVMILTEFMENGALDSFLRLNDGQFTVIQLVGM
LRGIASGMRYLAEMSYVHRDLAARNILVNSNLVCKVSDFGLSRFLEENSSDPTYTSSLGG
KIPIRWTAPEAIAFRKFTSASDAWSYGIVMWEVMSFGERPYWDMSNQDVINAIEQDYRLP
PPPDCPTSLHQLMLDCWQKDRNARPRFPQVVSALDKMIRNPASLKIVARENGGASHPLLD
QRQPHYSAFGSVGEWLRAIKMGRYEESFAAAGFGSFELVSQISAEDLLRIGVTLAGHQKK
ILASVQHMKSQAKPGTPGGTGGPAPQY
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50198782
n/a
NameBDBM50198782
Synonyms:([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) | 7-(2,6-dichlorophenyl)-5-methyl-N-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)benzo[e][1,2,4]triazin-3-amine | 7-(2,6-dichlorophenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)-phenyl]-1,2,4-benzotriazin-3-amine | CHEMBL230686 | TG-100435 | US8481536, 367 | US8481536, 575
TypeSmall organic molecule
Emp. Form.C26H25Cl2N5O
Mol. Mass.494.416
SMILESCc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1c(Cl)cccc1Cl
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: