Reaction Details |
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Target | Mast/stem cell growth factor receptor Kit [V559D,T670I] |
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Ligand | BDBM504399 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Biochemical Activity Assay |
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IC50 | 5.5±n/a nM |
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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 |
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More Info.: | Get all data from this article, Assay Method |
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Mast/stem cell growth factor receptor Kit [V559D,T670I] |
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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: | MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKDVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVIIEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV
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BDBM504399 |
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n/a |
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Name | BDBM504399 |
Synonyms: | (S)-1-(2-(4-(3-chloro-6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[1,2-b]pyridazin-4-yl)piperazin-1-yl)pyrimidin-5-yl)-1-(4-fluorophenyl)ethanamine | US11040979, Compound 3 |
Type | Small organic molecule |
Emp. Form. | C27H27ClFN9 |
Mol. Mass. | 532.015 |
SMILES | Cn1cc(cn1)-c1cc2c(N3CCN(CC3)c3ncc(cn3)[C@@](C)(N)c3ccc(F)cc3)c(Cl)cnn2c1 |r| |
Structure |
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