BindingDB BDBM50337134 2-((2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one::CHEMBL1673046::Scaffold, B46::US9266890, IV-6

BDBM50337134 2-((2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one::CHEMBL1673046::Scaffold, B46::US9266890, IV-6

SMILES CCOc1cc(ccc1Nc2ncc3c(n2)N(c4ccccc4C(=O)N3C)C)N5CCC(CC5)O

InChI Key InChIKey=QAPAJIZPZGWAND-UHFFFAOYSA-N

Data 7 IC50 9 Kd

PDB links: 3 PDB IDs match this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 233 hits for monomerid = 50337134

Leucine-rich repeat serine/threonine-protein kinase 2(Human)
Harvard Medical School

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 46nMAssay Description:Inhibition of recombinant human GST-tagged LRRK2 catalytic domain (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as...More data for this Ligand-Target Pair

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Date in BDB:
8/12/2021
Entry Details Article
PubMed

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 52nMAssay Description:Inhibition of ERK5 (unknown origin) by ADP-Glo kinase assayMore data for this Ligand-Target Pair

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Date in BDB:
12/19/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Leucine-rich repeat serine/threonine-protein kinase 2(Human)
Harvard Medical School

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 59nMAssay Description:Inhibition of LRRK2 G2019S mutant (unknown origin) using LRRKtide as substrate incubated for 1 hrs in presence of ATP by Adapta TR-FRET assayMore data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 80nMAssay Description:Binding affinity to ERK5 (unknown origin) assessed as dissociation constant by ATP-competition binding assayMore data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed PDB

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 80nMAssay Description:In vitro Erk5 binding assay: Ambit Kd values in nanomolar. Kd values generated by Ambit binding assay over a concentration range of the compound.More data for this Ligand-Target Pair

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Date in BDB:
1/23/2017
Entry Details
US Patent
PDB

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 80nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair

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Date in BDB:
10/3/2011
Entry Details Article
PubMed PDB

3D Structure (crystal)

Serine/threonine-protein kinase DCLK2(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 190nMAssay Description:Binding affinity to DCAMKL2 (unknown origin) assessed as dissociation constant by ATP-competition binding assayMore data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 200nMAssay Description:Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin...More data for this Ligand-Target Pair

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Date in BDB:
2/19/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Bromodomain-containing protein 4(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 205nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assayMore data for this Ligand-Target Pair

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

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

EC50: 240nMAssay Description:Inhibition of EGF-stimulated ERK5 autophosphorylation in human HeLa cells preincubated with compound for 1 hrs followed by EGF stimulation for 17 min...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed PDB

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 240nMAssay Description:Inhibition of ERK5 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
12/16/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 240nMAssay Description:Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysisMore data for this Ligand-Target Pair

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Date in BDB:
1/5/2013
Entry Details Article
PubMed PDB

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 300nMAssay Description:Inhibition of ERK5 in human HeLa cells incubated for 15 mins prior to ATP addition by KiNativ profiling methodMore data for this Ligand-Target Pair

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Date in BDB:
2/22/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 364nMAssay Description:Inhibition of N-terminal 6His-tagged human ERK5 expressed in baculovirus infected Sf21 cells co-expressing HA-tagged human MEK5-DD using ARKKRRHPSGPP...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed PDB

3D Structure (crystal)

Serine/threonine-protein kinase PLK4(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 600nMAssay Description:Binding affinity to PLK4 (unknown origin) assessed as dissociation constant by ATP-competition binding assayMore data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Bromodomain testis-specific protein(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 675nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assayMore data for this Ligand-Target Pair

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

Serine/threonine-protein kinase DCLK1(Human)
Harvard Medical School

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 716nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged DCLK1 (G351 to H689 residues) expressed in Escherichia coli BL21 DE3 using 5-FAM-KKLRRTLSVA-CO...More data for this Ligand-Target Pair

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Date in BDB:
8/12/2021
Entry Details Article
PubMed

Bromodomain-containing protein 4(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 735nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysisMore data for this Ligand-Target Pair

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

3D Structure (crystal)

Bromodomain-containing protein 4(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 800nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assayMore data for this Ligand-Target Pair

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Date in BDB:
3/4/2023
Entry Details Article
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3D Structure (crystal)

Non-receptor tyrosine-protein kinase TNK1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 890nMAssay Description:Binding affinity to TNK1 (unknown origin) assessed as dissociation constant by ATP-competition binding assayMore data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Mitogen-activated protein kinase 7(Human)
Peking University

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 1.50E+3nMAssay Description:Inhibition of ERK5 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed PDB

3D Structure (crystal)

Bromodomain-containing protein 4(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 1.60E+3nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
2/22/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Bromodomain testis-specific protein(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 3.50E+3nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assayMore data for this Ligand-Target Pair

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

Bromodomain testis-specific protein(Human)
Moffitt Cancer Center

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

Kd: 4.20E+3nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysisMore data for this Ligand-Target Pair

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

Non-receptor tyrosine-protein kinase TNK1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 1.00E+4nMAssay Description:Inhibition of TNK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Activated CDC42 kinase 1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 1.80E+4nMAssay Description:Inhibition of ACK1 in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Ribosomal protein S6 kinase alpha-1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 2.60E+4nMAssay Description:Inhibition of RSK1 domain 2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 ...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Ribosomal protein S6 kinase alpha-1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 2.90E+4nMAssay Description:Inhibition of RSK1 domain 2 K1 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured a...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Ribosomal protein S6 kinase alpha-1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 3.10E+4nMAssay Description:Inhibition of RSK1 domain 2 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured a...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Phosphatidylinositol 4-kinase beta(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 3.40E+4nMAssay Description:Inhibition of PIK4CB in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Phosphatidylinositol 4-kinase alpha(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 3.60E+4nMAssay Description:Inhibition of PIK4CA in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Focal adhesion kinase 1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 3.90E+4nMAssay Description:Inhibition of FAK in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured after 10 mins by LC...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Ribosomal protein S6 kinase alpha-3(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 4.70E+4nMAssay Description:Inhibition of RSK2 domain 2 K2 site in human HeLa cells lysate pre incubated for 15 mins followed by ADP acyl phosphate probe addition and measured a...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Ribosomal protein S6 kinase alpha-3(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 4.90E+4nMAssay Description:Inhibition of RSK2 domain 2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 ...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

RAC-alpha serine/threonine-protein kinase(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of AKT1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Platelet-derived growth factor receptor alpha/beta(Mouse)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of ABL1/2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Acylglycerol kinase, mitochondrial(Homo sapiens)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of AGK in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Aurora kinase A(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of AURA in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Serine/threonine-protein kinase ATR(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of ATR in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by LC...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Serine/threonine-protein kinase A-Raf(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of ARAF in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Platelet-derived growth factor receptor alpha/beta(Mouse)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of AMPKalpha1/2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 m...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Calcium/calmodulin-dependent protein kinase type II subunit delta(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of CAMK2d in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Calcium/calmodulin-dependent protein kinase type 1D(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of CAMK1d in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by...More data for this Ligand-Target Pair

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Date in BDB:
10/13/2025
Entry Details
PubMed

Serine/threonine-protein kinase B-raf(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of BRAF in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Date in BDB:
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Platelet-derived growth factor receptor alpha/beta(Mouse)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of AURA/AURB/AURC in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 4(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of ERK4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of ERK2 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 3(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of ERK1 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by L...More data for this Ligand-Target Pair

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Ephrin type-B receptor 4(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of EphB4 in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by ...More data for this Ligand-Target Pair

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Glycogen synthase kinase-3 alpha(Human)
The Scripps Research Institute

Curated by ChEMBL

BDBM50337134(US9266890, IV-6 | Scaffold, B46 | CHEMBL1673046 | ...)

IC50: 5.00E+4nMAssay Description:Inhibition of GSK3A in human HeLa cells lysate pre incubated for 15 mins followed by ATP acyl phosphate probe addition and measured after 10 mins by ...More data for this Ligand-Target Pair

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Displayed 1 to 50 (of 233 total ) | Next | Last >>

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Targets 148▿
- Platelet-derived growth factor receptor alpha/beta 16
- Mitogen-activated protein kinase 7 11
- Cyclin-dependent kinase 2 4
- Bromodomain-containing protein 4 4
- Serine/threonine-protein kinase PLK1 4
- Ribosomal protein S6 kinase alpha-3 4
- Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha 4
- Ribosomal protein S6 kinase alpha-1 4
- Bromodomain testis-specific protein 3
- Serine/threonine-protein kinase Sgk3 3
- Ribosomal protein S6 kinase alpha-5 3
- Mitogen-activated protein kinase 3 2
- Serine/threonine-protein kinase 4 2
- Calcium/calmodulin-dependent protein kinase type II subunit delta 2
- DNA-dependent protein kinase catalytic subunit 2
- Cyclin-dependent kinase 9 2
- Tyrosine-protein kinase JAK1 2
- Cyclin-dependent kinase 5 2
- Calcium/calmodulin-dependent protein kinase type II subunit gamma 2
- Epidermal growth factor receptor 2
- Non-receptor tyrosine-protein kinase TNK1 2
- Interferon-induced, double-stranded RNA-activated protein kinase 2
- Phosphorylase b kinase gamma catalytic chain, liver/testis isoform 2
- Calcium/calmodulin-dependent protein kinase type 1D 2
- STE20-like serine/threonine-protein kinase 2
- EKC/KEOPS complex subunit TP53RK 2
- Mitogen-activated protein kinase 14 2
- Serine/threonine-protein kinase B-raf 2
- Serine/threonine-protein kinase Nek9 2
- Cyclin-dependent kinase 13 2
- Serine/threonine-protein kinase Nek7 2
- Glycogen synthase kinase-3 beta 2
- Interleukin-1 receptor-associated kinase 4 2
- Tyrosine-protein kinase CSK 2
- Mixed lineage kinase domain-like protein 2
- MAP/microtubule affinity-regulating kinase 3 2
- Serine/threonine-protein kinase 24 2
- Dual specificity mitogen-activated protein kinase kinase 3 2
- Ephrin type-B receptor 4 2
- Dual specificity mitogen-activated protein kinase kinase 1 2
- Serine/threonine-protein kinase 10 2
- Serine/threonine-protein kinase Chk1 2
- Dual specificity mitogen-activated protein kinase kinase 6 2
- Dual specificity mitogen-activated protein kinase kinase 4 2
- Leucine-rich repeat serine/threonine-protein kinase 2 2
- Phosphatidylinositol 4-kinase beta 2
- Serine/threonine-protein kinase ULK3 2
- Peripheral plasma membrane protein CASK 1
- Cyclin-dependent kinase 11B 1
- Hepatocyte growth factor receptor 1
- Serine/threonine-protein kinase Nek8 1
- Glycogen synthase kinase-3 alpha 1
- Protein kinase C iota type 1
- Serine-protein kinase ATM 1
- Serine/threonine-protein kinase Nek4 1
- Serine/threonine-protein kinase Nek3 1
- Serine/threonine-protein kinase Nek1 1
- Macrophage-stimulating protein receptor 1
- Protein kinase C theta type 1
- Phosphatidylinositol 5-phosphate 4-kinase type-2 beta 1
- Serine/threonine-protein kinase tousled-like 2 1
- Serine/threonine-protein kinase tousled-like 1 1
- Dual specificity mitogen-activated protein kinase kinase 7 1
- Dual specificity mitogen-activated protein kinase kinase 5 1
- Serine/threonine-protein kinase Sgk1 1
- Serine/threonine-protein kinase 38-like 1
- Ephrin type-A receptor 2 1
- Serine/threonine-protein kinase SMG1 1
- Serine/threonine-protein kinase mTOR 1
- Eukaryotic translation initiation factor 2-alpha kinase 3 1
- Tyrosine-protein kinase receptor UFO 1
- Insulin-like growth factor 1 receptor 1
- Transcription intermediary factor 1-beta 1
- Serine/threonine-protein kinase 16 1
- Ribosomal protein S6 kinase beta-2 1
- Ribosomal protein S6 kinase beta-1 1
- STE20-related kinase adapter protein beta 1
- Integrin-linked protein kinase 1
- Phosphatidylinositol 3-kinase catalytic subunit type 3 1
- Wee1-like protein kinase 1
- Serine/threonine-protein kinase/endoribonuclease IRE1 1
- PAN2-PAN3 deadenylation complex subunit PAN3 1
- Tyrosine-protein kinase Lyn 1
- Focal adhesion kinase 1 1
- Cyclin-dependent kinase 1 1
- Activated CDC42 kinase 1 1
- 1-phosphatidylinositol 3-phosphate 5-kinase 1
- Tyrosine-protein kinase Fer 1
- Serine/threonine-protein kinase D2 1
- 5'-AMP-activated protein kinase catalytic subunit alpha-2 1
- Serine/threonine-protein kinase D3 1
- Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma 1
- Cyclin-dependent kinase 7 1
- Serine/threonine-protein kinase DCLK1 1
- Calcium/calmodulin-dependent protein kinase kinase 1 1
- Serine/threonine-protein kinase 38 1
- Serine/threonine-protein kinase TAO3 1
- Serine/threonine-protein kinase DCLK2 1
- Serine/threonine-protein kinase PRP4 homolog 1
- Serine/threonine-protein kinase TAO2 1
- Cyclin-dependent kinase 16 1
- Mitogen-activated protein kinase kinase kinase kinase 2 1
- Cyclin-dependent kinase 10 1
- Cyclin-dependent kinase 12 1
- Serine/threonine-protein kinase ATR 1
- 5'-AMP-activated protein kinase catalytic subunit alpha-1 1
- Cyclin-dependent kinase 15 1
- Mitogen-activated protein kinase kinase kinase 5 1
- Interleukin-1 receptor-associated kinase 1 1
- Serine/threonine-protein kinase greatwall 1
- Mitogen-activated protein kinase kinase kinase 8 1
- Mitogen-activated protein kinase kinase kinase 7 1
- Mitogen-activated protein kinase kinase kinase 2 1
- Serine/threonine-protein kinase A-Raf 1
- Mitogen-activated protein kinase kinase kinase 1 1
- Mitogen-activated protein kinase kinase kinase 4 1
- RAC-alpha serine/threonine-protein kinase 1
- Microtubule-associated serine/threonine-protein kinase 3 1
- Serine/threonine-protein kinase ULK2 1
- Mitogen-activated protein kinase 1 1
- Serine/threonine-protein kinase 3 1
- 3-phosphoinositide-dependent protein kinase 1 1
- Mitogen-activated protein kinase 4 1
- Dual specificity protein kinase CLK3 1
- Serine/threonine-protein kinase N2 1
- Acylglycerol kinase, mitochondrial 1
- Serine/threonine-protein kinase LATS1 1
- Insulin receptor 1
- Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta 1
- Aurora kinase A 1
- Mitogen-activated protein kinase kinase kinase 20 1
- Inhibitor of nuclear factor kappa-B kinase subunit beta 1
- Serine/threonine-protein kinase PLK4 1
- Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
- Casein kinase I isoform alpha 1
- Serine/threonine-protein kinase LATS2 1
- Tyrosine-protein kinase Fyn 1
- eIF-2-alpha kinase GCN2 1
- Eukaryotic elongation factor 2 kinase 1
- Protein kinase C zeta type 1
- Serine/threonine-protein kinase Chk2 1
- Serine/threonine-protein kinase MARK1 1
- Phosphatidylinositol 4-kinase alpha 1
- Serine/threonine-protein kinase MARK2 1
- SRSF protein kinase 1 1
- Serine/threonine-protein kinase WNK1 1
- Serine/threonine-protein kinase MRCK beta 1
- Mitogen-activated protein kinase kinase kinase 11 1
- ...
Publications 11▿
- Cancer Cell 18: 258-67 214
- J Med Chem 64: 15772-15786 (2021) 6
- Eur J Med Chem 70: 758-67 3
- Eur J Med Chem 178: 530-543 (2019) 2
- J Med Chem 63: 7817-7826 (2020) 2
- US Patent US9266890 (2016) 1
- J Med Chem 66: 4491-4502 (2023) 1
- J Med Chem 66: 13568-13586 (2023) 1
- J Med Chem 62: 928-940 (2019) 1
- ACS Med Chem Lett 2: 195-200 (2011) 1
- Chem Biol 18: 868-79 (2011) 1
Institutions 9▿
- The Scripps Research Institute 214
- Harvard Medical School 6
- Moffitt Cancer Center 6
- Newcastle University 2
- Dana-Farber Cancer Institute 1
- TBA 1
- Newcastle University Centre for Cancer 1
- Peking University 1
- Bayer 1
Affinity: 46 to 5.0E+4 nM▿
- IC50 219
- Kd 13
- EC50 1
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1