BindingDB BDBM50185140 AP-26113::Brigatinib::US11248003, Example Brigatinib::US20230322822, Compound Brigatinib::US20240409609, Compound Ref. 1

BDBM50185140 AP-26113::Brigatinib::US11248003, Example Brigatinib::US20230322822, Compound Brigatinib::US20240409609, Compound Ref. 1

SMILES CN1CCN(CC1)C2CCN(CC2)c3ccc(c(c3)OC)Nc4ncc(c(n4)Nc5ccccc5P(=O)(C)C)Cl

InChI Key InChIKey=AILRADAXUVEEIR-UHFFFAOYSA-N

Data 237 IC50

PDB links: 4 PDB IDs match this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 237 hits for monomerid = 50185140

Receptor-type tyrosine-protein kinase FLT3(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
10/3/2017
Entry Details Article
PubMed

Proto-oncogene tyrosine-protein kinase ROS(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
10/3/2017
Entry Details Article
PubMed

Insulin receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 196nMAssay Description:Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair

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Date in BDB:
10/3/2017
Entry Details Article
PubMed

Insulin-like growth factor 1 receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 25nMAssay Description:Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair

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Date in BDB:
10/3/2017
Entry Details Article
PubMed

ALK tyrosine kinase receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
10/3/2017
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
8/18/2020
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
8/18/2020
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
2/23/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
2/23/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
2/26/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

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Date in BDB:
2/26/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
2/26/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

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Date in BDB:
2/26/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
2/26/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

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Date in BDB:
2/26/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 48nMAssay Description:Inhibition of wild type EGFR (unknown origin) by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
8/13/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 1.5nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
8/13/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 2.5nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
8/13/2021
Entry Details Article
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3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 1.5nMAssay Description:Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
8/13/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

ALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
3/21/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

ALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
3/21/2022
Entry Details Article
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3D Structure (crystal)

ALK tyrosine kinase receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
3/21/2022
Entry Details Article
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3D Structure (crystal)

ALK tyrosine kinase receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
3/21/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 19nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR...More data for this Ligand-Target Pair

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Date in BDB:
8/23/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 13nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme...More data for this Ligand-Target Pair

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Date in BDB:
8/23/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 261nMAssay Description:Inhibition of wild type EGFR (unknown origin) measured by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
3/5/2023
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 38nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISAMore data for this Ligand-Target Pair

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Date in BDB:
3/5/2023
Entry Details Article
PubMed PDB

3D Structure (crystal)

ALK tyrosine kinase receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 1.20nMAssay Description:Binding affinity to ALK (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
3/5/2023
Entry Details Article
PubMed PDB

3D Structure (crystal)

ALK tyrosine kinase receptor(Human)
Ariad Pharmaceuticals

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 4.10nMAssay Description:Binding affinity to ALK G1202R mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
3/5/2023
Entry Details Article
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3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 21nMAssay Description:Inhibition of Wild type EGFR (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
3/4/2023
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 203nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as protein phosphorylation measured after 2 hrs by...More data for this Ligand-Target Pair

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Date in BDB:
3/4/2023
Entry Details Article
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor [1-18,20-1210,T790M,C797S](Human)
Oncobix

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
6/13/2022
Entry Details
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PDB

3D Structure (crystal)

Hepatocyte growth factor receptor(Human)
Oncobix

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 70nMAssay 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

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Date in BDB:
6/13/2022
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Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
6/20/2023
Entry Details
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
6/20/2023
Entry Details
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3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 53nMAssay Description:Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assayMore data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
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3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 75nMAssay Description:Inhibition of wild type EGFR (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 28nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
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3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 11nMAssay Description:Inhibition of EGFR del19 mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 0.700nMAssay Description:Inhibition of EGFR del19/T790M mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
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3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 4.90nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
PubMed PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 3.90nMAssay Description:Inhibition of EGFR del19/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/20/2023
Entry Details
PubMed PDB

3D Structure (crystal)

NUAK family SNF1-like kinase 1(Human)
University of Science and Technology (Ust)

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 47nMAssay Description:Inhibition of NUAK1 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
6/18/2023
Entry Details
PubMed

Epidermal growth factor receptor [1-18,20-1210,T790M](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
11/22/2023
Entry Details
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3D Structure (crystal)

Epidermal growth factor receptor [1-18,20-1210,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
11/22/2023
Entry Details
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3D Structure (crystal)

Epidermal growth factor receptor [T790M,L858R](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
11/22/2023
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3D Structure (crystal)

Epidermal growth factor receptor [L858R,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
11/22/2023
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3D Structure (crystal)

Epidermal growth factor receptor [L858R,T790M,C797S](Human)
Chengdu Di''Ao Jiuhong Pharmaceutical Factory

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

PDB
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Date in BDB:
11/22/2023
Entry Details
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PDB

3D Structure (crystal)

Epidermal growth factor receptor [1-18,20-1210,T790M,C797S](Human)
Oncobix

US Patent

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

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Date in BDB:
11/22/2023
Entry Details
Go to US Patent
PDB

3D Structure (crystal)

Epidermal growth factor receptor(Human)
Jinan University

Curated by ChEMBL

BDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)

IC50: 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

PDB KEGG
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Date in BDB:
11/22/2023
Entry Details
Go to US Patent
PDB

3D Structure (crystal)

Displayed 1 to 50 (of 237 total ) | Next | Last >>

Filter my 237 hits

Targets 91▿
- Epidermal growth factor receptor 79
- Platelet-derived growth factor receptor alpha/beta 25
- ALK tyrosine kinase receptor 20
- Receptor-type tyrosine-protein kinase FLT3 7
- Mast/stem cell growth factor receptor Kit 3
- Proto-oncogene tyrosine-protein kinase receptor Ret 3
- Epidermal growth factor receptor [1-18,20-1210,T790M,C797S] 3
- Tyrosine-protein kinase ABL1 3
- Insulin-like growth factor 1 receptor 3
- Insulin receptor 3
- Serine/threonine-protein kinase Chk2 2
- ALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4 2
- Proto-oncogene tyrosine-protein kinase ROS 2
- Hepatocyte growth factor receptor 2
- Fibroblast growth factor receptor 1 2
- Fibroblast growth factor receptor 2 2
- NUAK family SNF1-like kinase 1 2
- Tyrosine-protein kinase Fer 1
- Serine/threonine-protein kinase D2 1
- Serine/threonine-protein kinase D3 1
- Calcium/calmodulin-dependent protein kinase type II subunit delta 1
- Serine/threonine-protein kinase D1 1
- Serine/threonine-protein kinase TAO1 1
- Receptor tyrosine-protein kinase erbB-4 1
- Receptor tyrosine-protein kinase erbB-2 1
- Tyrosine-protein kinase FRK 1
- Calcium/calmodulin-dependent protein kinase kinase 2 1
- Angiopoietin-1 receptor 1
- Testis-specific serine/threonine-protein kinase 1 1
- Testis-specific serine/threonine-protein kinase 2 1
- Protein-tyrosine kinase 6 1
- Epidermal growth factor receptor [T790M,C797S,L858R] 1
- Serine/threonine-protein kinase Nek9 1
- Leukocyte tyrosine kinase receptor 1
- Mitogen-activated protein kinase kinase kinase 9 1
- MAP/microtubule affinity-regulating kinase 3 1
- MAP kinase-interacting serine/threonine-protein kinase 1 1
- Tyrosine-protein kinase JAK2 1
- Serine/threonine-protein kinase 10 1
- Epidermal growth factor receptor [L858R,C797S] 1
- cGMP-dependent protein kinase 1 1
- Leucine-rich repeat serine/threonine-protein kinase 2 1
- Proto-oncogene tyrosine-protein kinase Src 1
- Tyrosine-protein kinase Fes/Fps 1
- Serine/threonine-protein kinase SIK2 1
- BDNF/NT-3 growth factors receptor 1
- Ephrin type-A receptor 1 1
- Tyrosine-protein kinase Lck 1
- Serine/threonine-protein kinase 4 1
- Dual specificity protein kinase CLK1 1
- Tyrosine-protein kinase BTK 1
- Ephrin type-A receptor 7 1
- Dual specificity protein kinase CLK2 1
- Protein-tyrosine kinase 2-beta 1
- Tyrosine-protein kinase Mer 1
- Tyrosine-protein kinase Blk 1
- Calcium/calmodulin-dependent protein kinase type II subunit gamma 1
- Ribosomal protein S6 kinase alpha-2 1
- Ribosomal protein S6 kinase alpha-3 1
- Ribosomal protein S6 kinase alpha-1 1
- Phosphorylase b kinase gamma catalytic chain, liver/testis isoform 1
- Fibroblast growth factor receptor 4 1
- Epidermal growth factor receptor [L858R,T790M,C797S] 1
- Aurora kinase B 1
- Vascular endothelial growth factor receptor 2 1
- Tyrosine-protein kinase Fgr 1
- Vascular endothelial growth factor receptor 3 1
- Tyrosine-protein kinase HCK 1
- Aurora kinase A 1
- Echinoderm microtubule-associated protein-like 4 1
- Epidermal growth factor receptor [1-18,20-1210,C797S] 1
- Aurora kinase C 1
- Fibroblast growth factor receptor 3 1
- Serine/threonine-protein kinase PLK1 1
- Insulin receptor-related protein 1
- Serine/threonine-protein kinase BRSK1 1
- Tyrosine-protein kinase Fyn 1
- Tyrosine-protein kinase CSK 1
- Macrophage colony-stimulating factor 1 receptor 1
- Tyrosine-protein kinase Lyn 1
- Ribosomal protein S6 kinase alpha-6 1
- Focal adhesion kinase 1 1
- Epidermal growth factor receptor [1-18,20-1210,T790M] 1
- Maternal embryonic leucine zipper kinase 1
- Serine/threonine-protein kinase BRSK2 1
- Serine/threonine-protein kinase MARK1 1
- Serine/threonine-protein kinase MARK2 1
- Ephrin type-B receptor 1 1
- Serine/threonine-protein kinase Chk1 1
- Epidermal growth factor receptor [T790M,L858R] 1
- Tyrosine-protein kinase Yes 1
- ...
Publications 31▿
- Clin Cancer Res 22: 5527-5538 142
- US Patent US20230322822 (2023) 7
- J Med Chem 66: 6849-6868 (2023) 7
- Bioorg Med Chem Lett 72: (2022) 6
- J Nat Prod 82: 3065-3073 (2019) 6
- J Med Chem 66: 14633-14652 (2023) 6
- Eur J Med Chem 261: 5
- J Med Chem 59: 4948-64 (2016) 5
- Bioorg Med Chem Lett 30: (2020) 4
- J Med Chem 63: 10726-10741 (2020) 4
- J Med Chem 65: 6840-6858 (2022) 4
- Bioorg Med Chem 70: (2022) 3
- Eur J Med Chem 261: 3
- Bioorg Med Chem 90: (2023) 3
- US Patent US20240409609 (2024) 3
- ACS Med Chem Lett 14: 591-598 (2023) 3
- J Med Chem 65: 15540-15558 (2022) 2
- ACS Med Chem Lett 9: 1123-1127 (2018) 2
- ACS Med Chem Lett 13: 196-202 (2022) 2
- Eur J Med Chem 225: (2021) 2
- Eur J Med Chem 245: 2
- Eur J Med Chem 275: 2
- Nat Commun 8: 2
- J Med Chem 64: 9152-9165 (2021) 2
- J Med Chem 62: 7302-7308 (2019) 2
- J Med Chem 64: 13704-13718 (2021) 2
- US Patent US11248003 (2022) 2
- Eur J Med Chem 244: (2022) 1
- Bioorg Med Chem Lett 101: (2024) 1
- J Med Chem 64: 2-25 (2021) 1
- J Med Chem 67: 14702-14722 1
Institutions 23▿
- ARIAD Pharmaceuticals, Inc. 142
- Jinan University 17
- China Pharmaceutical University 13
- Chengdu Di''Ao Jiuhong Pharmaceutical Factory 7
- Southeast University 6
- Shanghai Institute of Materia Medica 6
- Soochow University 6
- Sungkyunkwan University 5
- Ariad Pharmaceuticals 5
- East China University of Science & Technology 4
- Terremoto Biosciences 3
- Tu Dortmund University 3
- Xi'an Jiaotong University 3
- Hangzhou Normal University 2
- Shanghaitech University 2
- Astrazeneca 2
- University of Parma 2
- Sun Yat-sen University 2
- Japanese Foundation for Cancer Research 2
- Oncobix 2
- University of Science and Technology (Ust) 1
- East China University of Science and Technology 1
- Jiangnan University 1
Affinity: 0.37 to 9.3E+3 nM▿
- IC50 237
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1