BDBM50185140 AP-26113::Brigatinib::US11248003, Example Brigatinib::US20230322822, Compound Brigatinib

SMILES COc1cc(ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1)N1CCC(CC1)N1CCN(C)CC1

InChI Key InChIKey=AILRADAXUVEEIR-UHFFFAOYSA-N

Data  80 IC50

PDB links: 4 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 80 hits for monomerid = 50185140   

TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 6.60nMAssay Description:Inhibition of EGFR 19 del/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 53nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.90nMAssay Description:Inhibition of ALK G1202R mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of ALK L1196M mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 53nMAssay Description:Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 140nMAssay Description:Inhibition of wild type EGFR (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 17nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 38nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.70E+3nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [1-18,20-1210,T790M,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 194nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [L858R,T790M,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 752nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [L858R,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 548nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M,L858R](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 148nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [1-18,20-1210,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 178nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [1-18,20-1210,T790M](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 164nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetNUAK family SNF1-like kinase 1(Human)
University of Science and Technology (Ust)

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 47nMAssay Description:Inhibition of NUAK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 3.90nMAssay Description:Inhibition of EGFR del19/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 5.40nMAssay Description:Inhibition of EGFR L858R/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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 33.4nMMore data for this Ligand-Target Pair
In DepthDetails
PDB3D3D Structure (crystal)
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [1-18,20-1210,T790M,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 8nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) expressed in Bac-to-Bac baculovirus expression system measured after 2 hrs by ELI...More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.72E+3nMAssay Description:Inhibition of EGFR L858R/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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 5nMAssay Description:Inhibition of EGFR L858R/T790M double mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate ad...More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 109nMAssay Description:Inhibition of wild-type EGFR (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured ...More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 16nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measur...More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.90nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.40nMAssay Description:Inhibition of EGFR LTCb mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 5nMAssay Description:Inhibition of EGFR dTCb mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.5nMAssay Description:Inhibition of EGFR LTb mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 12nMAssay Description:Inhibition of EGFR Del19 mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 14nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 124nMAssay Description:Inhibition of wild type EGFR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 11nMAssay Description:Inhibition of EGFR L858R/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition...More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 41nMAssay Description:Inhibition of EML4/ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as antiproliferative activity after 72 hrs by CellTiter...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 2.5nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 48nMAssay Description:Inhibition of wild type EGFR (unknown origin) by ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 130nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 130nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
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