Reaction Details Report a problem with these data
Target
Mast/stem cell growth factor receptor Kit [V559D,T670I]
Ligand
BDBM504400
Substrate
n/a
Meas. Tech.
Biochemical Activity Assay
IC50
5.5±n/a nM
Citation
 Hodous, BL; Kim, JL; Wilson, KJ Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR US Patent  US11040979 Publication Date 6/22/2021 
Target
Name:
Mast/stem cell growth factor receptor Kit [V559D,T670I]
Synonyms:
CD117 antigen | KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (V559D/T670I) | Mast/stem cell growth factor receptor precursor | Proto-oncogene tyrosine-protein kinase Kit | SCFR | Tyrosine Kinase c-Kit Mutant (V559D/T670I)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
109896.38
Organism:
Homo sapiens (Human)
Description:
P10721[V559D,T670I]
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKDVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVIIEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
  
Inhibitor
Name:
BDBM504400
Synonyms:
(S)-4-(4-(5-(1-amino-1-(4-fluorophenyl)ethyl)pyrimidin-2-yl)piperazin-1-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[1,2-b]pyridazine-3-carbonitrile | US11040979, Compound 4
Type:
Small organic molecule
Emp. Form.:
C28H27FN10
Mol. Mass.:
522.5794
SMILES:
Cn1cc(cn1)-c1cc2c(N3CCN(CC3)c3ncc(cn3)[C@@](C)(N)c3ccc(F)cc3)c(cnn2c1)C#N |r|
Structure:
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