Target
Mast/stem cell growth factor receptor Kit [V559D,T670I]
Ligand
BDBM504398
Substrate
n/a
Meas. Tech.
Biochemical Activity Assay
IC50
5.5±n/a nM
Citation
 Hodous, BLKim, JLWilson, 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:
BDBM504398
Synonyms:
(S)-1-(2-(4-(3-fluoro-6-(1-methyl-11H-pyrazol-4-yl)pyrrolo[1,2-b]pyridazin-4-yl)piperazin-1-yl)pyrimidin-5-yl)-1-(4-fluorophenyl)ethanamine | US11040979, Compound 2
Type:
Small organic molecule
Emp. Form.:
C27H27F2N9
Mol. Mass.:
515.5604
SMILES:
Cn1cc(cn1)-c1cc2c(N3CCN(CC3)c3ncc(cn3)[C@@](C)(N)c3ccc(F)cc3)c(F)cnn2c1 |r|
Structure:
Search PDB for entries with ligand similarity: