Reaction Details Report a problem with these data
Target
Mast/stem cell growth factor receptor Kit [D816V]
Ligand
BDBM369349
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:
BDBM369349
Synonyms:
5-ethyl-N-[1-[6-(1-methylpyrazol-4-yl)- 7H-pyrrolo[2,3-d]pyrimidin-4-yl]-4- piperidyl]thiophene-2-sulfonamide | US10227357, Compound P-0665
Type:
Small organic molecule
Emp. Form.:
C21H25N7O2S2
Mol. Mass.:
471.599
SMILES:
CCc1ccc(s1)S(=O)(=O)NC1CCN(CC1)c1ncnc2[nH]c(cc12)-c1cnn(C)c1
Structure:
Search PDB for entries with ligand similarity: