Reaction Details |
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Target | Mast/stem cell growth factor receptor Kit |
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Ligand | BDBM50238268 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1662941 (CHEMBL4012622) |
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IC50 | 1.9±n/a nM |
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Citation | Lu, Y; Mao, F; Li, X; Zheng, X; Wang, M; Xu, Q; Zhu, J; Li, J Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). J Med Chem60:5099-5119 (2017) [PubMed] Article |
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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 |
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Name: | Mast/stem cell growth factor receptor Kit |
Synonyms: | CD117 antigen | CD_antigen=CD117 | KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (cKIT) | Proto-oncogene c-Kit | Proto-oncogene tyrosine-protein kinase Kit | SCFR | Stem cell growth factor receptor | Tyrosine Kinase c-Kit | Tyrosine-protein kinase Kit | Tyrosine-protein kinase Kit (c-Kit) | c-kit | p-145 c-kit | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog |
Type: | Protein |
Mol. Mass.: | 109869.37 |
Organism: | Homo sapiens (Human) |
Description: | P10721 |
Residue: | 976 |
Sequence: | MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV
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BDBM50238268 |
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n/a |
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Name | BDBM50238268 |
Synonyms: | CHEMBL4091975 |
Type | Small organic molecule |
Emp. Form. | C23H18N6O |
Mol. Mass. | 394.4286 |
SMILES | Cc1n[nH]c2nccc(-c3ccc(NC(=O)Nc4cnc5ccccc5c4)cc3)c12 |
Structure |
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