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  65 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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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 69 hits for monomerid = 14774   

TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of PDE4D2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of PDE4D (unknown origin) using cAMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of PDE4D (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of PDE4B (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of PDE4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.490nMAssay Description:Inhibition of recombinant human PDE4B using cAMP as substrate after 30 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Human)
Kyorin Pharmaceutical

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

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of core catalytic domains PDE4B (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of recombinant human PDE4B1 expressed in African green monkey COS7 cells using cAMP as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.560nMAssay Description:Inhibition of human PDE4D by ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of human PDE4B by ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of PDE4D (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.840nMAssay Description:Inhibition of PDE4B (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of PDE4D (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant PDE4CMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of human recombinant PDE4BMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of human recombinant PDE4AMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human recombinant PDE4DMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of PDE4D2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.840nMAssay Description:Inhibition of human recombinant PDE4B by liquid scintillation counter methodMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of human recombinant PDE4D using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured af...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human recombinant PDE4C using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured af...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.150nMAssay Description:Inhibition of human recombinant PDE4B using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured af...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.210nMAssay Description:Inhibition of human recombinant PDE4A using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured af...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of human PDE4D by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.840nMAssay Description:Inhibition of human PDE4B by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 2.00E+5nMpH: 7.5 T: 2°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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 2.00E+5nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of human phosphodiesterase 4More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Sun Yat-Sen University

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Human)
Vrije Universiteit Amsterdam

Curated by ChEMBL
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14774(DAXAS | 3-(cyclopropylmethoxy)-N-(3,5-dichloropyri...)
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 Article
PubMed
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