Target
Mast/stem cell growth factor receptor Kit [D816V]
Ligand
BDBM472794
Substrate
n/a
Meas. Tech.
Biochemical Enzymatic Activity
IC50
<0.30±n/a nM
Citation
 Dineen, TA Compositions and methods for treating KIT- and PDGFRA-mediated diseases US Patent  US10829493 Publication Date 11/10/2020 
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:
BDBM472794
Synonyms:
US10829493, Example 20
Type:
Small organic molecule
Emp. Form.:
C29H31FN10O2
Mol. Mass.:
570.6206
SMILES:
C[C@](N)(c1ccc(F)cc1)c1cnc(nc1)N1CCN(CC1)c1ncnn2cc(cc12)-c1cnn(c1)[C@H]1COC[C@H]1O |r|
Structure:
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