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Target
Focal adhesion kinase 1
Ligand
BDBM50246140
Substrate
n/a
Meas. Tech.
ChEMBL_558213 (CHEMBL962347)
IC50
1.9±n/a nM
Citation
 Walker, DP; Bi, FC; Kalgutkar, AS; Bauman, JN; Zhao, SX; Soglia, JR; Aspnes, GE; Kung, DW; Klug-McLeod, J; Zawistoski, MP; McGlynn, MA; Oliver, R; Dunn, M; Li, JC; Richter, DT; Cooper, BA; Kath, JC; Hulford, CA; Autry, CL; Luzzio, MJ; Ung, EJ; Roberts, WG; Bonnette, PC; Buckbinder, L; Mistry, A; Griffor, MC; Han, S; Guzman-Perez, A Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation. Bioorg Med Chem Lett 18:6071-7 (2008) [PubMed]  Article 
Target
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:
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFIIRPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRERIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDHPHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESKRFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFTSASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWAYDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGYPSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQEIAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLSRGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNEGVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLALRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQMLTAAHALAVDAKNLLDVIDQARLKMLGQTRPH
  
Inhibitor
Name:
BDBM50246140
Synonyms:
CHEMBL513744 | D3RKN_5 | N-methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide
Type:
Small organic molecule
Emp. Form.:
C22H21F3N6O3S
Mol. Mass.:
506.501
SMILES:
CN(c1cccc(CNc2nc(Nc3ccc4NC(=O)Cc4c3)ncc2C(F)(F)F)c1)S(C)(=O)=O
Structure:
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