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Target5-hydroxytryptamine receptor 3A(Guinea pig)
European Research Centre For Drug Discovery and Development (Natsyndrugs)

Curated by ChEMBL
LigandPNGBDBM50081970(6-(4-Methyl-piperazin-1-yl)-pyrido[2,3-e]pyrrolo[1...)
Affinity DataEC50:  340nMAssay Description:Intrinsic activity at 5HT3 receptor in voltage-stimulated guinea pig left atrium assessed as positive inotropic potency relative to serotoninMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 3A(Guinea pig)
European Research Centre For Drug Discovery and Development (Natsyndrugs)

Curated by ChEMBL
LigandPNGBDBM50060688(7-Fluoro-4-(4-methyl-piperazin-1-yl)-pyrrolo[1,2-a...)
Affinity DataEC50:  160nMAssay Description:Agonist activity at 5HT3 receptor in voltage-stimulated guinea pig left atrium assessed as positive inotropic potencyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 3A(Guinea pig)
European Research Centre For Drug Discovery and Development (Natsyndrugs)

Curated by ChEMBL
LigandPNGBDBM50060685(9-fluoro-4-(4-methylpiperazin-1-yl)pyrrolo[1,2-a]q...)
Affinity DataKd:  64.6nMAssay Description:Antagonist activity at 5HT3 receptor in spontaneously beating guinea pig right atrium assessed as inhibition of serotonin-induced maximum response by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 3A(Guinea pig)
European Research Centre For Drug Discovery and Development (Natsyndrugs)

Curated by ChEMBL
LigandPNGBDBM50081969(9-Methyl-4-(4-methyl-piperazin-1-yl)-pyrrolo[1,2-a...)
Affinity DataKd:  955nMAssay Description:Antagonist activity at 5HT3 receptor in spontaneously beating guinea pig right atrium assessed as inhibition of serotonin-induced maximum response by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392637(CHEMBL215421)
Affinity DataKd:  0.324nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392639(CHEMBL2153551)
Affinity DataKd:  50.1nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392641(CHEMBL2153553)
Affinity DataKd:  2.82nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392643(CHEMBL2153555)
Affinity DataKd:  0.912nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392645(CHEMBL2153557)
Affinity DataKd:  1.20nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392647(CHEMBL2153559)
Affinity DataKd:  39.8nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392637(CHEMBL215421)
Affinity DataKd:  0.105nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392639(CHEMBL2153551)
Affinity DataKd:  166nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392641(CHEMBL2153553)
Affinity DataKd:  1.70nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392643(CHEMBL2153555)
Affinity DataKd:  0.275nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392645(CHEMBL2153557)
Affinity DataKd:  28.8nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392647(CHEMBL2153559)
Affinity DataKd:  53.7nMAssay Description:Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1B adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392637(CHEMBL215421)
Affinity DataKd:  0.676nMAssay Description:Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1B adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392639(CHEMBL2153551)
Affinity DataKd:  15.8nMAssay Description:Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1B adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392641(CHEMBL2153553)
Affinity DataKd:  0.263nMAssay Description:Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1B adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392643(CHEMBL2153555)
Affinity DataKd:  8.91nMAssay Description:Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1B adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392645(CHEMBL2153557)
Affinity DataKd:  2.75nMAssay Description:Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1B adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392647(CHEMBL2153559)
Affinity DataKd:  16.6nMAssay Description:Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-induced contractions after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1D adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392637(CHEMBL215421)
Affinity DataKd:  0.631nMAssay Description:Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions after 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1D adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392639(CHEMBL2153551)
Affinity DataKd:  51.3nMAssay Description:Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions after 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1D adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392641(CHEMBL2153553)
Affinity DataKd:  11.8nMAssay Description:Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions after 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1D adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392643(CHEMBL2153555)
Affinity DataKd:  3.02nMAssay Description:Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions after 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1D adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392645(CHEMBL2153557)
Affinity DataKd:  9.33nMAssay Description:Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions after 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetAlpha-1D adrenergic receptor(Rat)
University of Milan

Curated by ChEMBL
LigandPNGBDBM50392647(CHEMBL2153559)
Affinity DataKd:  5.75nMAssay Description:Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions after 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
University of Perugia

Curated by ChEMBL
LigandPNGBDBM8610(24F2-1,25(OH)D3 | Ketoconazole (k) | KTZ | 1-[4-(4...)
Affinity DataIC50: 1nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 5 mins by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM81939(NSC_62969 | VERAPAMIL | CAS_52-53-9)
Affinity DataIC50: 1.40nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22032(PK 11195 | PK11195 | RP 52028 | N-(butan-2-yl)-1-(...)
Affinity DataIC50: 2nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCytochrome P450 3A4(Human)
University of Perugia

Curated by ChEMBL
LigandPNGBDBM8610(24F2-1,25(OH)D3 | Ketoconazole (k) | KTZ | 1-[4-(4...)
Affinity DataIC50: 4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 4 mins by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 3A(Rat)
European Research Centre For Drug Discovery and Development (Natsyndrugs)

Curated by ChEMBL
LigandPNGBDBM50081981(4-(4-Benzyl-piperazin-1-yl)-9-methyl-pyrrolo[1,2-a...)
Affinity DataIC50: 8.80nMAssay Description:Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041505(Dimethyl-carbamic acid 5-(4-methoxy-phenyl)-6-thia...)
Affinity DataIC50: 9nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
University of Perugia

Curated by ChEMBL
LigandPNGBDBM50121975((6-Methoxy-quinolin-4-yl)-(5-vinyl-1-aza-bicyclo[2...)
Affinity DataIC50: 9nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 10 mins by LC-MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50052311(Acetic acid (4R,5R)-7-chloro-1-dimethylaminomethyl...)
Affinity DataIC50: 12nMAssay Description:Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 3A(Rat)
European Research Centre For Drug Discovery and Development (Natsyndrugs)

Curated by ChEMBL
LigandPNGBDBM50081974(4-(4-Benzyl-piperazin-1-yl)-7-fluoro-pyrrolo[1,2-a...)
Affinity DataIC50: 13nMAssay Description:Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
LigandPNGBDBM50029417([4-(4-Methoxy-phenyl)-4H-benzo[b]pyrrolo[1,2-d][1,...)
Affinity DataIC50: 17nMAssay Description:Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041493(Acetic acid 5-phenyl-6-thia-10b-aza-benzo[e]azulen...)
Affinity DataIC50: 20nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041506(Acetic acid 7-chloro-5-(4-methoxy-phenyl)-6-thia-1...)
Affinity DataIC50: 20nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041504(Butyric acid 5-phenyl-6-thia-10b-aza-benzo[e]azule...)
Affinity DataIC50: 22nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041513(Hexanoic acid 5-phenyl-6-thia-10b-aza-benzo[e]azul...)
Affinity DataIC50: 23nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041496(Butyric acid 5-(4-methoxy-phenyl)-6-thia-10b-aza-b...)
Affinity DataIC50: 28nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041502(Acetic acid 5-(4-methoxy-phenyl)-6-thia-10b-aza-be...)
Affinity DataIC50: 34nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
LigandPNGBDBM81939(NSC_62969 | VERAPAMIL | CAS_52-53-9)
Affinity DataIC50: 39nMAssay Description:Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041508(Pentanoic acid 5-phenyl-6-thia-10b-aza-benzo[e]azu...)
Affinity DataIC50: 48nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
LigandPNGBDBM50004704(Acetic acid 5-(2-dimethylamino-ethyl)-2-(4-methoxy...)
Affinity DataIC50: 54nMAssay Description:Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50052317(Acetic acid (4R,5R)-1-dimethylaminomethyl-5-phenyl...)
Affinity DataIC50: 139nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
LigandPNGBDBM81939(NSC_62969 | VERAPAMIL | CAS_52-53-9)
Affinity DataIC50: 150nMAssay Description:Inhibition of (-)-[3H]- D-888 binding to L-type calcium channels in kitten heart ventricle membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
University of Siena

Curated by ChEMBL
LigandPNGBDBM50041485(Acetic acid 9-chloro-5-phenyl-6-thia-10b-aza-benzo...)
Affinity DataIC50: 150nMAssay Description:Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMed
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