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Target
BDNF/NT-3 growth factors receptor
Ligand
BDBM134790
Substrate
n/a
Meas. Tech.
ChEMBL_2027227 (CHEMBL4681385)
IC50
5.0±n/a nM
Citation
 Skerratt, SE; Andrews, M; Bagal, SK; Bilsland, J; Brown, D; Bungay, PJ; Cole, S; Gibson, KR; Jones, R; Morao, I; Nedderman, A; Omoto, K; Robinson, C; Ryckmans, T; Skinner, K; Stupple, P; Waldron, G The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain. J Med Chem 59:10084-10099 (2016) [PubMed]
Target
Name:
BDNF/NT-3 growth factors receptor
Synonyms:
GP145-TrkB | NTRK1/NTRK2 | NTRK2 | NTRK2_HUMAN | Neurotrophic tyrosine kinase receptor type 2 | TRKB | Trk-B | TrkB tyrosine kinase | Tropomyosin-related kinase B | Tropomyosin-related kinase B (TRKB) | Tyrosine kinase receptor B (Trk-B)
Type:
Enzyme
Mol. Mass.:
91996.87
Organism:
Homo sapiens (Human)
Description:
Q16620
Residue:
822
Sequence:
MSSWIRWHGPAMARLWGFCWLVVGFWRAAFACPTSCKCSASRIWCSDPSPGIVAFPRLEPNSVDPENITEIFIANQKRLEIINEDDVEAYVGLRNLTIVDSGLKFVAHKAFLKNSNLQHINFTRNKLTSLSRKHFRHLDLSELILVGNPFTCSCDIMWIKTLQEAKSSPDTQDLYCLNESSKNIPLANLQIPNCGLPSANLAAPNLTVEEGKSITLSCSVAGDPVPNMYWDVGNLVSKHMNETSHTQGSLRITNISSDDSGKQISCVAENLVGEDQDSVNLTVHFAPTITFLESPTSDHHWCIPFTVKGNPKPALQWFYNGAILNESKYICTKIHVTNHTEYHGCLQLDNPTHMNNGDYTLIAKNEYGKDEKQISAHFMGWPGIDDGANPNYPDVIYEDYGTAANDIGDTTNRSNEIPSTDVTDKTGREHLSVYAVVVIASVVGFCLLVMLFLLKLARHSKFGMKGPASVISNDDDSASPLHHISNGSNTPSSSEGGPDAVIIGMTKIPVIENPQYFGITNSQLKPDTFVQHIKRHNIVLKRELGEGAFGKVFLAECYNLCPEQDKILVAVKTLKDASDNARKDFHREAELLTNLQHEHIVKFYGVCVEGDPLIMVFEYMKHGDLNKFLRAHGPDAVLMAEGNPPTELTQSQMLHIAQQIAAGMVYLASQHFVHRDLATRNCLVGENLLVKIGDFGMSRDVYSTDYYRVGGHTMLPIRWMPPESIMYRKFTTESDVWSLGVVLWEIFTYGKQPWYQLSNNEVIECITQGRVLQRPRTCPQEVYELMLGCWQREPHMRKNIKGIHTLLQNLAKASPVYLDILG
  
Inhibitor
Name:
BDBM134790
Synonyms:
US8846698, 253
Type:
Small organic molecule
Emp. Form.:
C23H24N8O2
Mol. Mass.:
444.4891
SMILES:
CC(C)n1cc(C(=O)c2cncc(NC(=O)Cn3ccc(n3)C3CC3)c2)c2cnc(N)nc12
Structure:
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