BDBM50236225 CHEMBL4074744::US11186582, Example 269::US11419874, DNS-8254

SMILES Cc1cc([C@@H]2CN(CC(F)(F)C2)C(=O)c2ccc(F)c(Br)c2)n2ncnc2n1

InChI Key InChIKey=TTWAYHJJEHLVNR-UHFFFAOYSA-N

Data  14 IC50  1 EC50

PDB links: 2 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 15 hits for monomerid = 50236225   

TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE4D3 (unknown origin) using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured after 30 mi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of PDE10A1 (unknown origin) using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured after 30 m...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human full length N-terminal GST-tagged PDE9A2 expressed in Baculovirus infected Sf9 insect cells using cGMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human full length N-terminal GST-tagged PDE11A4 expressed in Baculovirus infected Sf9 insect cells using cAMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Rat)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataEC50:  670nMAssay Description:Inhibition of PDE2a in rat primary cortical neurons assessed as increase in Bay 41-8543-stimulated intracellular cGMP level preincubated for 30 mins ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 8nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human full length N-terminal GST-tagged PDE8A1 expressed in Baculovirus infected Sf9 insect cells using cAMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE7A (unknown origin) using fluorescently labeled cAMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE6C (unknown origin) expressed in Baculovirus infected Sf9 insect cells using cGMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE5A1 (unknown origin) expressed in Baculovirus infected Sf9 insect cells using fluorescently labeled cGMP as substrate by fluorescenc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE1B (unknown origin) using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured after 30 min...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PDE3A (unknown origin) using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured after 30 min...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 100nMAssay Description:An IMAP TR-FRET-based phosphodiesterase assay was developed using the PDE2A isoform. IMAP technology is based on high-affinity binding of phosphate b...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Human)
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 8nMAssay Description:Isolated cardiomyocytes were washed twice in PBS at room temperature, transferred to 4% paraformaldehyde (PFA) and gently shaken for 30 min, then was...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
LigandPNGBDBM50236225(CHEMBL4074744 | US11186582, Example 269 | US114198...)
Affinity DataIC50: 1.70E+3nMAssay Description:Isolated cardiomyocytes were washed twice in PBS at room temperature, transferred to 4% paraformaldehyde (PFA) and gently shaken for 30 min, then was...More data for this Ligand-Target Pair
In DepthDetails
US Patent