BDBM50185140 AP-26113::Brigatinib::US11248003, Example Brigatinib::US20230322822, Compound Brigatinib
SMILES CN1CCN(CC1)C2CCN(CC2)c3ccc(c(c3)OC)Nc4ncc(c(n4)Nc5ccccc5P(=O)(C)C)Cl
InChI Key InChIKey=AILRADAXUVEEIR-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 237 hits for monomerid = 50185140
Affinity DataIC50: 0.370nMAssay Description:Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human ALK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human ALK C1156Y mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of EGFR del19/T790M mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.820nMAssay Description:Inhibition of EGFR Del19/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.820nMAssay Description:Inhibition of EGFR del18/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Bacu...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Bac...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Bacu...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Bac...More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Binding affinity to ALK (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP ad...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human FER using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:Inhibition of human ALK F1174L mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of human EGFR L858R mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of ALK phosphorylation in human SU-DHL-1 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of human FLT3 D835Y mutant using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Inhibition of wild type EGFR (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 25 m...More data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human ALK L1196M mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human ALK L1196M mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of ALK L1196M mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:The inhibitory activity on a C797S-containing epidermal growth factor receptor (EGFR) kinase and an MET kinase was measured for compound 1 obtained i...More data for this Ligand-Target Pair
Affinity DataIC50: 2.10nMAssay Description:Inhibition of human FLT3 using EAIYAAPFAKKK as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 2.10nMAssay Description:Inhibition of ALK phosphorylation in human L-82 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.10nMAssay Description:Inhibition of human FLT3 using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in bacu...More data for this Ligand-Target Pair
Affinity DataIC50: 3.20nMAssay Description:Inhibition of ALK phosphorylation in human KARPAS-299 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3.40nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.40nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.5nMAssay Description:Inhibition of human FES using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.70nMAssay Description:Inhibition of ALK phosphorylation in human NCI-H3122 cells harboring EML4-ALK variant 1 fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3.90nMAssay Description:Inhibition of EGFR del19/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3.90nMAssay Description:Inhibition of human FAK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.10nMAssay Description:Inhibition of human PTK6 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.10nMAssay Description:Binding affinity to ALK G1202R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.40nMAssay Description:Inhibition of EGFR LTCb mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.40nMAssay Description:Inhibition of human TSSK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.40nMAssay Description:Inhibition of EGFR Del19/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substr...More data for this Ligand-Target Pair
Affinity DataIC50: 4.40nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) preincubated for 10 mins followed by ATP and substrate addition and measured afte...More data for this Ligand-Target Pair
Affinity DataIC50: 4.5nMAssay Description:Inhibition of EGFR LTb mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.5nMAssay Description:Inhibition of ALK phosphorylation in human NCI-H2228 cells harboring EML4-ALK variant 3a/3b fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Inhibition of human ALK G1202R mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Inhibition of ALK G1202R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Inhibition of human ALK G1202R mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair

3D Structure (crystal)