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Target
High affinity nerve growth factor receptor
Ligand
BDBM356059
Substrate
n/a
Meas. Tech.
Functional Activity Assay
IC50
0.230±n/a nM
Citation
 Mitchell, H; Fraley, ME; Cooke, AJ; Stump, CA; Chen, Y; Zhang, X; McComas, CC; Schirripa, K; McWherter, M; Mercer, SP; Babaoglu, K; Meng, D; Wu, J; Liu, P; Wood, HB; Bao, J; Li, CS; Mao, Q; Qi, Z TrkA kinase inhibitors, compositions and methods thereof US Patent  US9815846 Publication Date 11/14/2017 
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 | 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:
BDBM356059
Synonyms:
2-fluoro-5-(1-methyl-1H- pyrazol-3-yl)-N-(6-((2- (methylsulfonyl)acetamido)methyl)- 2-phenylpyridin-3-yl)-4- (trifluoromethyl)benzamide | US9815846, Compound 59
Type:
Small organic molecule
Emp. Form.:
C27H23F4N5O4S
Mol. Mass.:
589.561
SMILES:
Cn1ccc(n1)-c1cc(C(=O)Nc2ccc(CNC(=O)CS(C)(=O)=O)nc2-c2ccccc2)c(F)cc1C(F)(F)F
Structure:
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