Reaction Details |
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Target | Focal adhesion kinase 1 |
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Ligand | BDBM50018830 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1363665 (CHEMBL3293407) |
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IC50 | 17±n/a nM |
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Citation | Johnson, TW; Richardson, PF; Bailey, S; Brooun, A; Burke, BJ; Collins, MR; Cui, JJ; Deal, JG; Deng, YL; Dinh, D; Engstrom, LD; He, M; Hoffman, J; Hoffman, RL; Huang, Q; Kania, RS; Kath, JC; Lam, H; Lam, JL; Le, PT; Lingardo, L; Liu, W; McTigue, M; Palmer, CL; Sach, NW; Smeal, T; Smith, GL; Stewart, AE; Timofeevski, S; Zhu, H; Zhu, J; Zou, HY; Edwards, MP Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo J Med Chem57:4720-44 (2014) [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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BDBM50018830 |
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n/a |
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Name | BDBM50018830 |
Synonyms: | CHEMBL3286830 | US10543199, Compound PF-06463922 | US10780082, Compound PF-06463922 | US11517561, Compound PF-06463922 |
Type | Small organic molecule |
Emp. Form. | C21H19FN6O2 |
Mol. Mass. | 406.413 |
SMILES | C[C@H]1Oc2cc(cnc2N)-c2c(CN(C)C(=O)c3ccc(F)cc13)nn(C)c2C#N |r| |
Structure |
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