Reaction Details Report a problem with these data
Target
High affinity nerve growth factor receptor
Ligand
BDBM24917
Substrate
PGT
Meas. Tech.
TrkA Enzyme Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
84±n/a nM
Citation
 Lippa, B; Morris, J; Corbett, M; Kwan, TA; Noe, MC; Snow, SL; Gant, TG; Mangiaracina, M; Coffey, HA; Foster, B; Knauth, EA; Wessel, MD Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists. Bioorg Med Chem Lett 16:3444-8 (2006) [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 | 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:
BDBM24917
Synonyms:
3-{[(4-chlorophenyl)methyl]sulfanyl}-5-[(6-oxo-1,6-dihydropyridin-3-yl)amino]-1,2-thiazole-4-carboxamide | isothiazole, 10g
Type:
Small organic molecule
Emp. Form.:
C16H13ClN4O2S2
Mol. Mass.:
392.883
SMILES:
NC(=O)c1c(SCc2ccc(Cl)cc2)nsc1Nc1ccc(=O)[nH]c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PGT
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
Synthetic tyrosine residues within a generic polypeptide substrate.
Residue:
3
Sequence:
NA