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  54 IC50

PDB links: 4 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 8 hits for monomerid = 50185140   

TargetEpidermal growth factor receptor(Homo sapiens (Human))
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50:  38nMAssay Description:Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant using poly (Glu,Tyr)...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50:  51nMAssay Description:Inhibition of recombinant human EGFR T790M/L858R double mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50:  77nMAssay Description:Inhibition of wild-type EGFR (unknown origin) using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
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
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50:  184nMAssay Description:Inhibition of EML4/ALK G1202R 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
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Jinan University

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
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