BDBM375513 (4-(3-(4-chlorophenyl)imidazo[1,2-b]pyridazin-6-yl)phenyl)(4-methylpiperazin-1-yl)methanone::US9908886, Example 54

SMILES CN1CCN(CC1)C(=O)c1ccc(cc1)-c1ccc2ncc(-c3ccc(cc3)C#N)n2n1

InChI Key InChIKey=PEHQJHHHTXOGJK-UHFFFAOYSA-N

Data  9 IC50

  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 9 hits for monomerid = 375513   

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Agency For Science, Technology and Research

US Patent
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 100nMAssay Description:MNK1 and MNK2 inhibitor activity was determined using recombinant kinase domains expressed in E. coli. MNK1 and MNK2 were expressed as GST fusion pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/27/2020
Entry Details
Go to US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Agency For Science, Technology and Research

US Patent
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 100nMAssay Description:MNK1 and MNK2 inhibitor activity was determined using recombinant kinase domains expressed in E. coli. MNK1 and MNK2 were expressed as GST fusion pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/27/2020
Entry Details
Go to US Patent

TargetCytochrome P450 3A4(Human)
Agency For Science, Technology and Research (A*Star)

Curated by ChEMBL
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Agency For Science, Technology and Research

US Patent
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 20nMAssay Description:Inhibition of GST-tagged MNK1 (37 to 341 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using JH3 peptide as substrate preincubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Agency For Science, Technology and Research

US Patent
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 25nMAssay Description:Inhibition of GST-tagged MNK2 (72 to 385 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using JH3 peptide as substrate preincubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Agency For Science, Technology and Research (A*Star)

Curated by ChEMBL
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate preincubated for 5 mins followed by NADPH addition by LC-MS/MS ana...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Agency For Science, Technology and Research (A*Star)

Curated by ChEMBL
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 326nMAssay Description:Inhibition of MNK1/2 in human HeLa cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Agency For Science, Technology and Research

US Patent
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 20nMAssay Description:Inhibition of MNK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2024
Entry Details
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Agency For Science, Technology and Research

US Patent
LigandPNGBDBM375513(US9908886, Example 54 | (4-(3-(4-chlorophenyl)imid...)
Affinity DataIC50: 30nMAssay Description:Inhibition of MNK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2024
Entry Details
PubMed