Reaction Details Report a problem with these data
Target
High affinity nerve growth factor receptor [440-796]
Ligand
BDBM27890
Substrate
polyGlu4Tyr
Meas. Tech.
TrkA Enzyme Inhibition Assay
Temperature
298.15±n/a K
IC50
170±n/a nM
Comments
extracted
Citation
 Huang, H; Hutta, DA; Rinker, JM; Hu, H; Parsons, WH; Schubert, C; Desjarlais, RL; Crysler, CS; Chaikin, MA; Donatelli, RR; Chen, Y; Cheng, D; Zhou, Z; Yurkow, E; Manthey, CL; Player, MR Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger). J Med Chem 52:1081-99 (2009) [PubMed]  Article 
Target
Name:
High affinity nerve growth factor receptor [440-796]
Synonyms:
High affinity nerve growth factor receptor | MTC | NTRK1 | NTRK1_HUMAN | Neurotrophic tyrosine kinase receptor type 1 | TRK | TRK1-transforming tyrosine kinase protein | TRKA | Tyrosine Kinase TrkA | p140-TrkA
Type:
Cytoplasmic region
Mol. Mass.:
40053.30
Organism:
Homo sapiens (Human)
Description:
The histidine-tagged recombinant human TrkA cytoplasmic domain (amino acids 440-796) expressed in insect cells was used in enzyme assays.
Residue:
357
Sequence:
NKCGRRNKFGINRPAVLAPEDGLAMSLHFMTLGGSSLSPTEGKGSGLQGHIIENPQYFSDACVHHIKRRDIVLKWELGEGAFGKVFLAECHNLLPEQDKMLVAVKALKEASESARQDFQREAELLTMLQHQHIVRFFGVCTEGRPLLMVFEYMRHGDLNRFLRSHGPDAKLLAGGEDVAPGPLGLGQLLAVASQVAAGMVYLAGLHFVHRDLATRNCLVGQGLVVKIGDFGMSRDIYSTDYYRVGGRTMLPIRWMPPESILYRKFTTESDVWSFGVVLWEIFTYGKQPWYQLSNTEAIDCITQGRELERPRACPPEVYAIMRGCWQREPQQRHSIKDVHARLQALAQAPPVYLDVLG
  
Inhibitor
Name:
BDBM27890
Synonyms:
8-(2,3-dihydro-1H-inden-5-yl)-2-({4-[2-(4-methylpiperazin-1-yl)ethyl]phenyl}amino)-5-oxo-5H,8H-pyrido[2,3-d]pyrimidine-6-carboxamide | Pyrido[2,3-d]pyrimidin-5-one, 17a
Type:
Small organic molecule
Emp. Form.:
C30H33N7O2
Mol. Mass.:
523.6287
SMILES:
CN1CCN(CCc2ccc(Nc3ncc4c(n3)n(cc(C(N)=O)c4=O)-c3ccc4CCCc4c3)cc2)CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
polyGlu4Tyr
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA