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Target
High affinity nerve growth factor receptor
Ligand
BDBM226350
Substrate
n/a
Meas. Tech.
ChEMBL_1809731 (CHEMBL4309191)
IC50
5.0±n/a nM
Citation
 Bagal, SK; Omoto, K; Blakemore, DC; Bungay, PJ; Bilsland, JG; Clarke, PJ; Corbett, MS; Cronin, CN; Cui, JJ; Dias, R; Flanagan, NJ; Greasley, SE; Grimley, R; Johnson, E; Fengas, D; Kitching, L; Kraus, ML; McAlpine, I; Nagata, A; Waldron, GJ; Warmus, JS Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors. J Med Chem 62:247-265 (2019) [PubMed]  Article
Target
Name:
High affinity nerve growth factor receptor
Synonyms:
2.7.10.1 | MTC | NTRK1 | NTRK1/NTRK2 | NTRK1_HUMAN | Nerve growth factor receptor Trk-A | Neurotrophic tyrosine kinase receptor type 1 | Neurotrophic tyrosine kinase receptor type 1 (TrkA) | Synonyms=MTC | TRK | TRK1-transforming tyrosine kinase protein | TRKA | TRKA GN | TRKA GN | Trk-A | Tropomyosin alpha-3 chain/High affinity nerve growth factor receptor | Tropomyosin-related kinase A | Tropomyosin-related kinase A (TrkA) | Tyrosine kinase receptor | Tyrosine kinase receptor (Trk) | Tyrosine kinase receptor A | Tyrosine kinase receptor A (Trk A) | Tyrosine kinase receptor A (Trk-A) | Tyrosine kinase receptor A (TrkA) | gp140trk | p140-TrkA
Type:
n/a
Mol. Mass.:
87498.18
Organism:
Homo sapiens (Human)
Description:
P04629
Residue:
796
Sequence:
MLRGGRRGQLGWHSWAAGPGSLLAWLILASAGAAPCPDACCPHGSSGLRCTRDGALDSLHHLPGAENLTELYIENQQHLQHLELRDLRGLGELRNLTIVKSGLRFVAPDAFHFTPRLSRLNLSFNALESLSWKTVQGLSLQELVLSGNPLHCSCALRWLQRWEEEGLGGVPEQKLQCHGQGPLAHMPNASCGVPTLKVQVPNASVDVGDDVLLRCQVEGRGLEQAGWILTELEQSATVMKSGGLPSLGLTLANVTSDLNRKNVTCWAENDVGRAEVSVQVNVSFPASVQLHTAVEMHHWCIPFSVDGQPAPSLRWLFNGSVLNETSFIFTEFLEPAANETVRHGCLRLNQPTHVNNGNYTLLAANPFGQASASIMAAFMDNPFEFNPEDPIPVSFSPVDTNSTSGDPVEKKDETPFGVSVAVGLAVFACLFLSTLLLVLNKCGRRNKFGINRPAVLAPEDGLAMSLHFMTLGGSSLSPTEGKGSGLQGHIIENPQYFSDACVHHIKRRDIVLKWELGEGAFGKVFLAECHNLLPEQDKMLVAVKALKEASESARQDFQREAELLTMLQHQHIVRFFGVCTEGRPLLMVFEYMRHGDLNRFLRSHGPDAKLLAGGEDVAPGPLGLGQLLAVASQVAAGMVYLAGLHFVHRDLATRNCLVGQGLVVKIGDFGMSRDIYSTDYYRVGGRTMLPIRWMPPESILYRKFTTESDVWSFGVVLWEIFTYGKQPWYQLSNTEAIDCITQGRELERPRACPPEVYAIMRGCWQREPQQRHSIKDVHARLQALAQAPPVYLDVLG
  
Inhibitor
Name:
BDBM226350
Synonyms:
US9328096, 43
Type:
Small organic molecule
Emp. Form.:
C24H18Cl2FN5O3
Mol. Mass.:
514.336
SMILES:
OCCNC(=O)c1cc(NC(=O)c2cc(c(Cl)cc2Cl)-c2ncccc2F)n(n1)-c1ccccc1
Structure:
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