Reaction Details Report a problem with these data
Target
BDNF/NT-3 growth factors receptor
Ligand
BDBM50565738
Substrate
n/a
Meas. Tech.
ChEMBL_2093489 (CHEMBL4774752)
EC50
69±n/a nM
Citation
 Wang, B; Zhang, W; Liu, X; Zou, F; Wang, J; Liu, Q; Wang, A; Hu, Z; Chen, Y; Qi, S; Jiang, Z; Chen, C; Hu, C; Wang, L; Wang, W; Liu, Q; Liu, J Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants. Eur J Med Chem 207:0 (2020) [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:
BDBM50565738
Synonyms:
CHEMBL4794404
Type:
Small organic molecule
Emp. Form.:
C25H27N7OS
Mol. Mass.:
473.593
SMILES:
CN1CCN(CC(=O)Nc2nc(C)c(s2)-c2ccc3c(\C=C\c4ccccn4)n[nH]c3c2)CC1
Structure:
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