Reaction Details |
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Target | Mast/stem cell growth factor receptor Kit [D816V] |
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Ligand | BDBM369254 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Cell-Based Assays of c-Kit Mutant Kinase Activity |
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Ki | 500±n/a nM |
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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 |
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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 [D816V] |
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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: | MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARVIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV
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BDBM369254 |
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n/a |
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Name | BDBM369254 |
Synonyms: | N-[(4-fluorophenyl)methyl]-4-[6-(1- methylsulfonyl-3,6-dihydro-2H-pyridin-4- yl)thieno[3,2-d]pyrimidin-4-yl]piperazine- 1-carboxamide | US10227357, Compound P-0568 |
Type | Small organic molecule |
Emp. Form. | C24H27FN6O3S2 |
Mol. Mass. | 530.638 |
SMILES | CS(=O)(=O)N1CCC(=CC1)c1cc2ncnc(N3CCN(CC3)C(=O)NCc3ccc(F)cc3)c2s1 |c:7| |
Structure |
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