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Target
High affinity nerve growth factor receptor
Ligand
BDBM356133
Substrate
n/a
Meas. Tech.
Functional Activity Assay
IC50
4.60±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:
BDBM356133
Synonyms:
N-(4-(3-acetamidophenyl)-2- methylpyrimidin-5-yl)-2-fluoro- 5-(1-methyl-1H-pyrazol-3-yl)-4- (trifluoromethyl)benzamide | US9815846, Compound 133
Type:
Small organic molecule
Emp. Form.:
C25H20F4N6O2
Mol. Mass.:
512.4589
SMILES:
CC(=O)Nc1cccc(c1)-c1nc(C)ncc1NC(=O)c1cc(-c2ccn(C)n2)c(cc1F)C(F)(F)F
Structure:
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