Reaction Details Report a problem with these data
Target
Mast/stem cell growth factor receptor Kit
Ligand
BDBM8863
Substrate
biotinylated synthetic peptide
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
IC50
200±n/a nM
Citation
 Dai, Y; Guo, Y; Frey, RR; Ji, Z; Curtin, ML; Ahmed, AA; Albert, DH; Arnold, L; Arries, SS; Barlozzari, T; Bauch, JL; Bouska, JJ; Bousquet, PF; Cunha, GA; Glaser, KB; Guo, J; Li, J; Marcotte, PA; Marsh, KC; Moskey, MD; Pease, LJ; Stewart, KD; Stoll, VS; Tapang, P; Wishart, N; Davidsen, SK; Michaelides, MR Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. J Med Chem 48:6066-83 (2005) [PubMed]  Article 
Target
Name:
Mast/stem cell growth factor receptor Kit
Synonyms:
CD117 antigen | CD_antigen=CD117 | KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (cKIT) | Proto-oncogene c-Kit | Proto-oncogene tyrosine-protein kinase Kit | SCFR | Stem cell growth factor receptor | Tyrosine Kinase c-Kit | Tyrosine-protein kinase Kit | Tyrosine-protein kinase Kit (c-Kit) | c-kit | p-145 c-kit | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Type:
Protein
Mol. Mass.:
109869.37
Organism:
Homo sapiens (Human)
Description:
P10721
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM8863
Synonyms:
3-(4-{4-aminothieno[2,3-d]pyrimidin-5-yl}-3-chlorophenyl)-1-(3-methylphenyl)urea | N-[4-(4-Aminothieno[2,3-d]pyrimidin-5-yl)-3-chloro-phenyl]-N -(3-methylphenyl)urea | Thienopyrimidine deriv. 89
Type:
Small organic molecule
Emp. Form.:
C20H16ClN5OS
Mol. Mass.:
409.892
SMILES:
Cc1cccc(NC(=O)Nc2ccc(-c3csc4ncnc(N)c34)c(Cl)c2)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated synthetic peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2470.20
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
ITINAHAEEEYFFLFAAMIDE