Reaction Details |
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Target | Ephrin type-B receptor 4 |
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Ligand | BDBM50198782 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_437765 (CHEMBL905854) |
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Ki | 63.8±n/a nM |
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Citation | Noronha, G; Barrett, K; Boccia, A; Brodhag, T; Cao, J; Chow, CP; Dneprovskaia, E; Doukas, J; Fine, R; Gong, X; Gritzen, C; Gu, H; Hanna, E; Hood, JD; Hu, S; Kang, X; Key, J; Klebansky, B; Kousba, A; Li, G; Lohse, D; Mak, CC; McPherson, A; Palanki, MS; Pathak, VP; Renick, J; Shi, F; Soll, R; Splittgerber, U; Stoughton, S; Tang, S; Yee, S; Zeng, B; Zhao, N; Zhu, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Ephrin type-B receptor 4 |
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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
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BDBM50198782 |
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n/a |
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Name | BDBM50198782 |
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 |
Type | Small organic molecule |
Emp. Form. | C26H25Cl2N5O |
Mol. Mass. | 494.416 |
SMILES | Cc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1c(Cl)cccc1Cl |
Structure |
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