BDBM14777 (2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione::(6R,12aR)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1,2,1,6]pyrido[3,4-b]indole-1,4-dione::CHEMBL779::Cialis::GF 196960::Tadalafil

SMILES [H][C@]12Cc3c([nH]c4ccccc34)[C@H](N1C(=O)CN(C)C2=O)c1ccc2OCOc2c1

InChI Key InChIKey=WOXKDUGGOYFFRN-IIBYNOLFSA-N

Data  4 KI  89 IC50  1 Kd  3 EC50

PDB links: 2 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 97 hits for monomerid = 14777   

TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Rattus norvegicus)
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataKi:  5nMAssay Description:Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cellsMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataKi:  5.20nMAssay Description:Inhibition of PDE5 (unknown origin)More data for this Ligand-Target Pair
TargetGlycerophosphocholine phosphodiesterase GPCPD1(RAT)
Medical College Of Georgia

Curated by PDSP Ki Database
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataKi:  9.77nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataKi:  10nMAssay Description:Inhibition of human phosphodiesterase 5More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.00E+5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  5.00E+4nMpH: 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 ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase [574-941](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.30E+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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  2.80E+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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  9.20E+3nMAssay 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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.90E+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
TargetcGMP-specific 3',5'-cyclic phosphodiesterase [531-875](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.20nMAssay 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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  7.40E+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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.50E+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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.90E+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
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  10nMAssay 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
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  6.70nMAssay Description:Inhibitory activity against phosphodiesterase 5 (PDE5) obtained from human corpus cavernosum tissueMore data for this Ligand-Target Pair
TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  37nMAssay Description:Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expressionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  33nMAssay Description:Inhibition of human phosphodiesterase 11More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human phosphodiesterase 5More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of Phosphodiesterase 5 from human plateletsMore data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of Human recombinant PDE4 (Phosphodiesterase 4)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  5nMAssay Description:In vitro inhibitory activity against bovine phosphodiesterase 5More data for this Ligand-Target Pair
TargetP04972/P11541/P16586/P22571/P23439/Q95142(Bos taurus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  5.10E+3nMAssay Description:Inhibition of bovine retina PDE6 (Phosphodiesterase 6)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of bovine aorta PDE1 (Phosphodiesterase 1)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  290nMAssay Description:Inhibition of human recombinant PDE11More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  300nMAssay Description:Inhibition of human recombinant PDE11A-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3B(Homo sapiens (Human))
German University In Cairo

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of human recombinant PDE3B-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  50nMAssay Description:Inhibition of human recombinant PDE11A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant PDE5A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant PDE5 after 1.5 hrs by fluorescent polarization assayMore data for this Ligand-Target Pair
TargetO43924/P16499/P18545/P35913/P51160/Q13956(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of human phosphodiesterase 6More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  5nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Shandong University

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of PDE5 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  5nMAssay Description:In vitro inhibitory activity against bovine phosphodiesterase 5More data for this Ligand-Target Pair
TargetPhosphodiesterase(Bos taurus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of bovine aorta PDE3 (Phosphodiesterase 3)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of Human recombinant PDE2 (Phosphodiesterase 2)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of Phosphodiesterase 9More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human phosphodiesterase 2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibitory concentration against human phosphodiesterase 10More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.26E+5nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  3.98E+5nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of bovine PDE5 after 24 hrs by HTRFMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.00E+5nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  7.94E+4nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using I...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily E/KQT member 1(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.58E+5nMAssay Description:Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using Ion...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.26E+5nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonW...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily E/KQT member 1(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  2.51E+5nMAssay Description:Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.58E+5nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  12nMAssay Description:Inhibition of bovine PDE5More data for this Ligand-Target Pair
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