Reaction Details Report a problem with these data
Target
Mast/stem cell growth factor receptor Kit
Ligand
BDBM8849
Substrate
biotinylated synthetic peptide
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
IC50
930±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
More Info.:
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:
BDBM8849
Synonyms:
3-[4-amino-5-(4-{[(3-methylphenyl)carbamoyl]amino}phenyl)thieno[2,3-d]pyrimidin-6-yl]-N,N-dimethylpropanamide | 3-{4-Amino-5-[4-(3-m-tolylureido)phenyl]thieno[2,3-d]-pyrimidin-6-yl}-N,N-dimethylpropionamide | Thienopyrimidine deriv. 53
Type:
Small organic molecule
Emp. Form.:
C25H26N6O2S
Mol. Mass.:
474.578
SMILES:
CN(C)C(=O)CCc1sc2ncnc(N)c2c1-c1ccc(NC(=O)Nc2cccc(C)c2)cc1
Substrate
Name:
biotinylated synthetic peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2470.20
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
ITINAHAEEEYFFLFAAMIDE