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Target
Mast/stem cell growth factor receptor Kit [D816V]
Ligand
BDBM368962
Substrate
n/a
Meas. Tech.
Cell-Based Assays of c-Kit Mutant Kinase Activity
Ki
500±n/a nM
Citation
 Lin, J; Buell, J; Chan, K; Ewing, T; Ibrahim, P; Nespi, M; Pham, P; Shi, S; Spevak, W; Wu, G; Zhang, J; Zhang, Y Compounds and methods for kinase modulation, and indications therefor US Patent  US10227357 Publication Date 3/12/2019 
Target
Name:
Mast/stem cell growth factor receptor Kit [D816V]
Synonyms:
KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (D816V) | Mast/stem cell growth factor receptor Kit 1 (D816V) | SCFR | Tyrosine-protein kinase Kit (Kit)(D816V)
Type:
Protein
Mol. Mass.:
109854.42
Organism:
Homo sapiens (Human)
Description:
Human Kit D816V mutant
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARVIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM368962
Synonyms:
4-[6-(3-pyridyl)-7H-pyrrolo[2,3-d]pyrimidin-4- yl]-N-[3-(trifluoromethyl)phenyl]piperazine- 1-carboxamide | US10227357, Compound P-0223
Type:
Small organic molecule
Emp. Form.:
C23H20F3N7O2
Mol. Mass.:
483.4458
SMILES:
FC(F)(F)Oc1ccc(NC(=O)N2CCN(CC2)c2ncnc3[nH]c(cc23)-c2cccnc2)cc1
Structure:
Search PDB for entries with ligand similarity: