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Target
Focal adhesion kinase 1
Ligand
BDBM50246060
Substrate
n/a
Meas. Tech.
ChEMBL_2511105
IC50
2.0±n/a nM
Citation
 Han, S; Mistry, A; Chang, JS; Cunningham, D; Griffor, M; Bonnette, PC; Wang, H; Chrunyk, BA; Aspnes, GE; Walker, DP; Brosius, AD; Buckbinder, L Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. J Biol Chem 284:13193-201[PubMed] 
Target
Name:
Focal adhesion kinase 1
Synonyms:
FRNK | Focal adhesion kinase (FAK) | Focal adhesion kinase (PTK2) | Focal adhesion kinase 1 (FAK) | Focal adhesion kinase-related nonkinase | Protein phosphatase 1 regulatory subunit 71 | FADK 1 | FLT4 | PPP1R71 | Protein-tyrosine kinase 2 | p125FAK | pp125FAK | FAK1_HUMAN | PTK2 | FAK | FAK1 | VHL/Focal adhesion kinase 1 | Focal adhesion kinase 1/vascular endothelial growth factor receptor 3
Type:
Tyrosine-protein kinase
Mol. Mass.:
119233.17
Organism:
Human
Description:
Q05397
Residue:
1052
Sequence:
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFIIRPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRERIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDHPHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESKRFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFTSASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWAYDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGYPSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQEIAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLSRGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNEGVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLALRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQMLTAAHALAVDAKNLLDVIDQARLKMLGQTRPH
  
Inhibitor
Name:
BDBM50246060
Synonyms:
CHEMBL472212 | N-methyl-N-(2-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide | N-methyl-N-{2-[({2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl}amino)methyl]phenyl}methanesulfonamide | CHEMBL541649 | PF-431396 | D3RKN_6
Type:
Small organic molecule
Emp. Form.:
C22H21F3N6O3S
Mol. Mass.:
506.13
SMILES:
CN(c1ccccc1CNc2c(cnc(n2)Nc3ccc4c(c3)CC(=O)N4)C(F)(F)F)S(=O)(=O)C
Structure:
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