BDBM14774 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide::CHEMBL193240::DAXAS::ROF::Roflumilast

SMILES FC(F)Oc1ccc(cc1OCC1CC1)C(=O)Nc1c(Cl)cncc1Cl

InChI Key InChIKey=MNDBXUUTURYVHR-UHFFFAOYSA-N

Data  4 KI  62 IC50

PDB links: 3 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 62 hits for monomerid = 14774   

LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMpH: 7.5 T: 30°CAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.840nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.680nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  1.70E+4nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  2.50E+4nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Human)
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human phosphodiesterase 4More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of human recombinant PDE4B1 activity assessed as residual cAMP concentration by HTRF assayMore data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of human recombinant PDE4D2 activity assessed as residual cAMP concentration by HTRF assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.690nMAssay Description:Inhibition of human PDE4B1 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A(Human)
RhôNe-Poulenc Rorer

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.590nMAssay Description:Inhibition of human PDE4A4 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.270nMAssay Description:Inhibition of human PDE4D3 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.840nMAssay Description:Inhibition of the human PDE4B catalytic domain after 30 mins in presence of [3H]cAMP/[3H]cGMP by scintillation countingMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human recombinant PDE4B2 assessed as decrease in cAMP hydrolysis preincubated with substrate prior to enzyme addition measured after 30...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.840nMAssay Description:Inhibition of human PDE4BMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.398nMAssay Description:Inhibition of human recombinant PDE4B by scintillation proximity assayMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.398nMAssay Description:Inhibition of human recombinant PDE4B by scintillation proximity assayMore data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  460nMAssay Description:Inhibition of human PDE4D2 catalytic domain (86 to 413) expressed in Escherichia coli BL21 using [3H]-cAMP/[3H]-cGMP after 15 mins by liquid scintill...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  670nMAssay Description:Inhibition of human PDE4B2 catalytic domain and UCR2 (92 to 521) expressed in Escherichia coli BL21 using [3H]-cAMP/[3H]-cGMP after 15 mins by liquid...More data for this Ligand-Target Pair
TargetAdenosine receptor A1(Human)
RhôNe-Poulenc Rorer

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >1.00E+3nMAssay Description:Antagonist activity at adenosine A1 receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.690nMAssay Description:Inhibition of human recombinant PDE4B1 assessed as reduction in [3H]cAMP hydrolysis to [3H]AMP incubated for 60 mins by PDE-SPA assayMore data for this Ligand-Target Pair
TargetAdenosine receptor A2a(Human)
RhôNe-Poulenc Rorer

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >1.00E+3nMAssay Description:Antagonist activity at adenosine A2a receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2b(Human)
RhôNe-Poulenc Rorer

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >1.00E+3nMAssay Description:Antagonist activity at adenosine A2b receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of recombinant human PDE4B1 using [3H]-cAMP as substrate preincubated for 15 mins followed substrate addition measured after 60 mins by sc...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.890nMAssay Description:Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of human PDE4B by ELISAMore data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.560nMAssay Description:Inhibition of human PDE4D by ELISAMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of core catalytic domains PDE4B (unknown origin)More data for this Ligand-Target Pair
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of core catalytic domains PDE3A (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.490nMAssay Description:Inhibition of recombinant human PDE4B using cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.490nMAssay Description:Inhibition of human recombinant PDE4B (152 to 564 amino acids) using cAMP as substrate after 30 mins by plate reader analysisMore data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  480nMAssay Description:Inhibition of human PDE4D2 (86 to 413 residues) catalytic domain using [3H]-cAMP as substrate after 15 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of PDE4B (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of PDE4D (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of PDE4D (unknown origin) using cAMP as substrateMore data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.680nMAssay Description:Inhibition of human His-tagged PDE4D catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  84nMAssay Description:Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  84nMAssay Description:Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate...More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.680nMAssay Description:Inhibition of human His-tagged PDE4D catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate...More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of PDE4D2 (unknown origin)More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Human)
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of PDE4 (unknown origin)More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of human PDE4B using [3H]cAMP as substrate incubated for 5 mins followed by substrate addition and measured after 10 mins by scintillation...More data for this Ligand-Target Pair