BDBM50004205 MK-045::MK-0457::TOZASERTIB::US9249124, VX680::VX-68::VX-680
SMILES CN1CCN(CC1)c1cc(Nc2cc(C)[nH]n2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1
InChI Key InChIKey=GCIKSSRWRFVXBI-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 70 hits for monomerid = 50004205
Affinity DataKi: 0.370nMAssay Description:Inhibition of Aurora A (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 0.600nMAssay Description:Inhibition of recombinant N-terminal His6-tagged Aurora A (62 to 344 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 0.600nMAssay Description:Inhibition of N-terminal His-6-tagged recombinant Aurora 1 (62 to 344) (unknown origin) expressed in baculovirus expression system by radiometric ass...More data for this Ligand-Target Pair
Affinity DataKi: 0.650nMAssay Description:Inhibition of Aurora A (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 0.700nMAssay Description:Inhibition of recombinant N-terminal His6-tagged Aurora A (1 to 403 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 2nMAssay Description:Inhibition of recombinant Aurora A kinase derived from human Hela cells using kemptide as substrate in presence of [c-32P]ATPMore data for this Ligand-Target Pair
Affinity DataKi: 3.40nMAssay Description:Inhibition of Aurora B (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 4.60nMAssay Description:Inhibition of N-terminal His-6-tagged recombinant Aurora 3 (1 to 309) (unknown origin) expressed in baculovirus expression system by radiometric assa...More data for this Ligand-Target Pair
Affinity DataKi: 4.60nMAssay Description:Inhibition of recombinant N-terminal His6-tagged Aurora C (1 to 309 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 4.60nMAssay Description:Inhibition of N-terminal His6-tagged Aurora C (1 to 309 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 4.60nMAssay Description:Inhibition of recombinant N-terminal His6-tagged Aurora C (1 to 309 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 4.60nMAssay Description:Inhibition of Aurora C (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataKi: 7.70nMAssay Description:Inhibition of PLK4 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataKi: 11nMAssay Description:Inhibition of PLK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 18nMAssay Description:Inhibition of N-terminal His6-tagged Aurora B (1 to 403 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 18nMAssay Description:Inhibition of recombinant N-terminal His6-tagged Aurora B (1 to 403 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 18nMAssay Description:Inhibition of recombinant N-terminal His6-tagged Aurora B (62 to 344 residues) (unknown origin) expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataKi: 18nMAssay Description:Inhibition of N-terminal His-6-tagged recombinant Aurora 2 (1 to 403) (unknown origin) expressed in baculovirus expression system by radiometric assa...More data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Hangzhou Medical College
Curated by ChEMBL
Hangzhou Medical College
Curated by ChEMBL
Affinity DataKi: 30nMAssay Description:Binding affinity to FLT3 (unknown origin)More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Homo sapiens (Human))
Hangzhou Medical College
Curated by ChEMBL
Hangzhou Medical College
Curated by ChEMBL
Affinity DataKi: 30nMAssay Description:Binding affinity to wild type BCR-ABL (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 36nMAssay Description:Inhibition of DLK (unknown origin)More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Homo sapiens (Human))
Hangzhou Medical College
Curated by ChEMBL
Hangzhou Medical College
Curated by ChEMBL
Affinity DataKi: 42nMAssay Description:Binding affinity to wild type BCR-ABL T315I mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 6.22E+3nMAssay Description:IC50 determinations for TBK1 were performed with the KinEASE-STK assay from Cisbio according to the manufacturer's instructions. A biotinylated s...More data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMpH: 7.4 T: 2°CAssay Description:Aurora A was exchanged into 50 mM phosphate buffer (pH 7.4) including 1 mM DTT via PD-10 columns and was concentrated to 20 mg mL-1 using Amicon Ultr...More data for this Ligand-Target Pair
Affinity DataIC50: 2.80nM Kd: 17nMpH: 7.4Assay Description:The binding of inhibitors to Aurora A kinase was analyzed with a MicroCal iTC200 titration calorimeter (GE Healthcare, Piscataway, N.J.). The protein...More data for this Ligand-Target Pair
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Technical University Of Dortmund
Curated by ChEMBL
Technical University Of Dortmund
Curated by ChEMBL
Affinity DataIC50: 241nMAssay Description:Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assayMore data for this Ligand-Target Pair
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Technical University Of Dortmund
Curated by ChEMBL
Technical University Of Dortmund
Curated by ChEMBL
Affinity DataKd: 230nMAssay Description:Binding affinity to wild type DDR2 (unknown origin) by FLiK assayMore data for this Ligand-Target Pair
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Technical University Of Dortmund
Curated by ChEMBL
Technical University Of Dortmund
Curated by ChEMBL
Affinity DataKd: >2.50E+3nMAssay Description:Binding affinity to human acrylodan-labeled N-terminal His-tagged DDR2 (558 to 855 aa) by FLiK assayMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Inhibition of aurora B (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of aurora A (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.60nMAssay Description:Inhibition of aurora C (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 261nMAssay Description:Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 453nMAssay Description:Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 68nMAssay Description:Inhibition of human recombinant AurKB after 4 hrs by ADP-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Inhibition of human recombinant AurKA after 4 hrs by ADP-Glo assayMore data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Mus musculus)
University Of Antwerp
Curated by ChEMBL
University Of Antwerp
Curated by ChEMBL
Affinity DataIC50: 1.02E+3nMAssay Description:Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 24 hrs followed...More data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
University Of Antwerp
Curated by ChEMBL
University Of Antwerp
Curated by ChEMBL
Affinity DataKd: 20nMAssay Description:Binding affinity to RIPK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 0.501nMAssay Description:Binding affinity to DNA-tagged human partial length AURKA expressed in mammalian expression system by qPCR methodMore data for this Ligand-Target Pair
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Heidelberg University
Curated by ChEMBL
Heidelberg University
Curated by ChEMBL
Affinity DataKd: 3.20nMAssay Description:Binding affinity to DNA-tagged human partial length TrkA expressed in mammalian expression system by qPCR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Inhibition of recombinant aurora B (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of Aurora A kinase (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.60nMAssay Description:Inhibition of Aurora C kinase (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 127nMAssay Description:Inhibition of recombinant Aurora A (unknown origin) using TAMRA-PKAtide as substrate after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of recombinant Aurora B (unknown origin) using TAMRA-PKAtide as substrate after 1 hr by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Mus musculus)
University Of Antwerp
Curated by ChEMBL
University Of Antwerp
Curated by ChEMBL
Affinity DataIC50: 980nMAssay Description:Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 0.5 hrs followe...More data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
University Of Antwerp
Curated by ChEMBL
University Of Antwerp
Curated by ChEMBL
Affinity DataIC50: 208nMAssay Description:Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 24 hrs followed...More data for this Ligand-Target Pair
Affinity DataIC50: 23nMAssay Description:Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrateMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.950nMAssay Description:Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence methodMore data for this Ligand-Target Pair
Affinity DataIC50: 15nMAssay Description:Inhibition of Aurora B (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence methodMore data for this Ligand-Target Pair