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TargetFocal adhesion kinase 1
LigandBDBM50334594
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1460546
IC50 7.0±n/a nM
Citation Dao, PSmith, NTomkiewicz-Raulet, CYen-Pon, ECamacho-Artacho, MLietha, DHerbeuval, JPCoumoul, XGarbay, CChen, H Design, synthesis, and evaluation of novel imidazo[1,2-a][1,3,5]triazines and their derivatives as focal adhesion kinase inhibitors with antitumor activity. J Med Chem58:237-51 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Focal adhesion kinase 1
Name:VHL/Focal adhesion kinase 1
Synonyms:FADK 1 | FLT4 | FRNK | Focal adhesion kinase (FAK) | Focal adhesion kinase (PTK2) | Focal adhesion kinase 1 (FAK) | Focal adhesion kinase-related nonkinase | PPP1R71 | PTK2 | Protein phosphatase 1 regulatory subunit 71 | Protein-tyrosine kinase 2 | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50334594
NameBDBM50334594
Synonyms:2-(5-chloro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)-N-methylbenzamide | 2-({5-CHLORO-2-[(2-METHOXY-4-MORPHOLIN-4-YLPHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)-N-METHYLBENZAMIDE | 2-[5-chloro-2-[2-methoxy-4-(4-morpholinyl)phenylamino]pyrimidin-4-ylamino]-N-methylbenzamide | CHEMBL458997 | TAE226 | US10266549, Example 12 | US10774092, Example 12
TypeSmall organic molecule
Emp. Form.C23H25ClN6O3
Mol. Mass.468.936
SMILESCNC(=O)c1ccccc1Nc1nc(Nc2ccc(cc2OC)N2CCOCC2)ncc1Cl
Structure
n/a