Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetMast/stem cell growth factor receptor Kit
LigandBDBM50533694
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1926540 (CHEMBL4429612)
EC50<100±n/a nM
Citation Li, BWang, ALiu, JQi, ZLiu, XYu, KWu, HChen, CHu, CWang, WWu, JHu, ZYe, LZou, FLiu, FWang, BWang, LRen, TZhang, SBai, MZhang, SLiu, JLiu, Q Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase. J Med Chem59:8456-72 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mast/stem cell growth factor receptor Kit
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:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50533694
n/a
NameBDBM50533694
Synonyms:CHEMBL4445808
TypeSmall organic molecule
Emp. Form.C34H36F3N5O5
Mol. Mass.651.6753
SMILESCCC(=O)NCC1CCN(CC1)c1ccc(NC(=O)Nc2cccc(Oc3ccnc4cc(OC)c(OC)cc34)c2)cc1C(F)(F)F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: