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Target
Mast/stem cell growth factor receptor Kit [D816V]
Ligand
BDBM369363
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:
BDBM369363
Synonyms:
4-[6-(4,4-difluoro-1-piperidyl)thieno[3,2- d]pyrimidin-4-yl]-N-[(1S)-1-(3- methoxyphenyl)ethyl]-2,2-dimethyl- piperazine-1-carboxamide | US10227357, Compound P-0680
Type:
Small organic molecule
Emp. Form.:
C27H34F2N6O2S
Mol. Mass.:
544.66
SMILES:
COc1cccc(c1)[C@H](C)NC(=O)N1CCN(CC1(C)C)c1ncnc2cc(sc12)N1CCC(F)(F)CC1 |r|
Structure:
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