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Target
BDNF/NT-3 growth factors receptor
Ligand
BDBM374727
Substrate
n/a
Meas. Tech.
ChEMBL_2150839 (CHEMBL5035301)
IC50
0.050000±n/a nM
Citation
 Liu, Z; Yu, P; Dong, L; Wang, W; Duan, S; Wang, B; Gong, X; Ye, L; Wang, H; Tian, J Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer. J Med Chem 64:10286-10296 (2021) [PubMed]  Article 
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:
BDBM374727
Synonyms:
(7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14- tetrahydro-1,15-ethenopyrazolo[4,3- f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)- one | US10246466, Example 93 | US10618912, Example 93 | US11291667, Compound 1
Type:
Small organic molecule
Emp. Form.:
C18H18FN5O2
Mol. Mass.:
355.3662
SMILES:
C[C@H]1CNC(=O)c2cnn3ccc(N[C@H](C)c4cc(F)ccc4O1)nc23 |r|
Structure:
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