Reaction Details |
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Target | Focal adhesion kinase 1 |
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Ligand | BDBM158154 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1577153 (CHEMBL3807415) |
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IC50 | 140±n/a nM |
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Citation | Menichincheri, M; Ardini, E; Magnaghi, P; Avanzi, N; Banfi, P; Bossi, R; Buffa, L; Canevari, G; Ceriani, L; Colombo, M; Corti, L; Donati, D; Fasolini, M; Felder, E; Fiorelli, C; Fiorentini, F; Galvani, A; Isacchi, A; Borgia, AL; Marchionni, C; Nesi, M; Orrenius, C; Panzeri, A; Pesenti, E; Rusconi, L; Saccardo, MB; Vanotti, E; Perrone, E; Orsini, P Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. J Med Chem59:3392-408 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Focal adhesion kinase 1 |
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Name: | Focal adhesion kinase 1 |
Synonyms: | FADK 1 | FAK | FAK1 | FAK1_HUMAN | FLT4 | FRNK | Focal adhesion kinase (FAK) | Focal adhesion kinase (PTK2) | Focal adhesion kinase 1 (FAK) | Focal adhesion kinase 1/vascular endothelial growth factor receptor 3 | Focal adhesion kinase-related nonkinase | PPP1R71 | PTK2 | Protein phosphatase 1 regulatory subunit 71 | Protein-tyrosine kinase 2 | VHL/Focal adhesion kinase 1 | p125FAK | pp125FAK |
Type: | Tyrosine-protein kinase |
Mol. Mass.: | 119233.17 |
Organism: | Homo sapiens (Human) |
Description: | Q05397 |
Residue: | 1052 |
Sequence: | MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGD
ATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEW
KYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSY
WEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESI
LKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQ
TIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFII
RPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRE
RIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDH
PHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESK
RFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFT
SASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWA
YDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGY
PSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQE
IAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLS
RGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNE
GVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLA
LRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQM
LTAAHALAVDAKNLLDVIDQARLKMLGQTRPH
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BDBM158154 |
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n/a |
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Name | BDBM158154 |
Synonyms: | US10081622, Compound 11 | US10370379, Entrectinib | US11059827, Compound Entrectinib | US11267806, Compound T-12 | US9029356, 11 | US9255087, 11 | US9616059, 11 |
Type | Small organic molecule |
Emp. Form. | C31H34F2N6O2 |
Mol. Mass. | 560.6375 |
SMILES | CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1 |
Structure |
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