Reaxys
PubChem
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Bioactivities (61)
SigmaAldrich
Reactions (1)
Substances (1)
Structure
Targets (12)
Citations (25)
Structure/Compound Data Chemical Name: 1-pentyl-2-methyl-3-(1-naphthoyl)indole Reaxys Registry Number: 8350109
Type of Substance: heterocyclic Molecular Formula: C25H25NO Linear Structure Formula: C25H25NO Molecular Weight: 355.48 InChI Key: IBBNKINXTRKICJ-UHFFFAOYSA-N
1
N° of preparations All Preps | All Reactions
Available Data
Target
N° of ref.
0 prep out of 1 reactions.
Druglikeness
Bioactivity
Identification
Show Targets
25
Highest Clinical Phase: Preclinical
Synthesize | Hide Details Find similar Chemical Names and Synonyms 1-pentyl-2-methyl-3-(1-naphthoyl)indole Druglikeness Bioactivity In vitro: Efficacy (56) Quantitative Results pX
Parameter
8.01
Ki
Value (qual)
Value (quant)
Unit
9.8
nM
Action on Target
Target Cannabinoid
Tissue/Organ
Cell
Bioassay
Dose
CHO
Binding
1.00000E-
Effect
Reference (expand all/collapse all) Journal of Pharmacology ...
receptor 1 [human]:Wild
cell line
11 M
Title/Abstract Full Text View citing articles Show Details
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
8.51
Ki
3.1
nM
Cannabinoid receptor 2 [human]:Wild
CHO cell line
Binding
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
CHO cell line
Binding
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
CHO cell line
cAMP production
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
CHO cell line
cAMP production
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
CHO cell line
cAMP production
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
CHO cell line
cAMP production
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
8.85
Ki
1.4
nM
Cannabinoid receptor 1 [human]:Mutated
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
7.83
EC50
14.7
nM
Agonist
Cannabinoid receptor 1 [human]:Wild
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
Emax(%)
79
%
Agonist
Cannabinoid receptor 1 [human]:Wild
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
8.33
EC50
4.7
nM
Agonist
Cannabinoid receptor 1 [human]:Mutated
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
Emax(%)
70
%
Agonist
Cannabinoid receptor 1 [human]:Mutated
Chin, Chen-Ni; Murphy, James W.; Huffman, John W.; Kendall, Debra A.
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 2 p. 837 - 844 Title/Abstract Full Text View citing articles Show Details
8.59
IC50
2.56
nM
Agonist
cannabinoid receptor [Mus musculus]:Wild
vas deferens
Organ contraction
brain cortex
Binding
European Journal of Phar...
Title/Abstract Full Text Show Details
Pertwee; Griffin; Lainton; Huffman
European Journal of Pharmacology, 1995 , vol. 284, # 3 p. 241 - 247 Title/Abstract Full Text Show Details
8.02
Ki
9.5
nM
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
0.100000 nM
Drug and Alcohol Depende...
Title/Abstract Full Text View citing articles Show Details
Aung, Mie Mie; Griffin, Graeme; Huffman, John W.; Wu, Ming-Jung; Keel, Cheryl; Yang, Bin; Showalter, Vincent M.; Abood, Mary E.; Martin, Billy R.
Drug and Alcohol Dependence, 2000 , vol. 60, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
8.53
Ki
2.94
nM
Cannabinoid receptor 2 [human]:Wild
CHO cell line
Binding
0.100000 nM
Drug and Alcohol Depende...
Title/Abstract Full Text View citing articles Show Details
Aung, Mie Mie; Griffin, Graeme; Huffman, John W.; Wu, Ming-Jung; Keel, Cheryl; Yang, Bin; Showalter, Vincent M.; Abood, Mary E.; Martin, Billy R.
Drug and Alcohol Dependence, 2000 , vol. 60, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
9.5
nM
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
brain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Wiley, Jenny L.; Compton, David R.; Dai, Dong; Lainton, Julia A. H.; Phillips, Michelle; Huffman, John W.; Martin, Billy R.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 285, # 3 p. 995 - 1004 Title/Abstract Full Text View citing articles Show Details
8.53
Ki
2.94
nM
Cannabinoid receptor 2 [human]:Wild
CHO cell line
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
brain cortex
Binding
Bioorganic and Medicinal...
Title/Abstract Full Text Show Details
CHO cell line
Binding
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Showalter, Vincent M.; Compton, David R.; Martin, Billy R.; Abood, Mary E.
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 3 p. 989 - 999 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
9.5
nM
cannabinoid receptor [Rattus norvegicus]:Wild
Huffman; Dai
Bioorganic and Medicinal Chemistry Letters, 1994 , vol. 4, # 4 p. 563 - 566 Title/Abstract Full Text Show Details
8.7
pKi
8.7
Cannabinoid receptor 1 [human]:Wild
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5086 - 5098 Title/Abstract Full Text View citing articles Show Details
8.2
pKi
8.2
Cannabinoid receptor 2 [human]:Wild
CHO cell line
Binding
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5086 - 5098 Title/Abstract Full Text View citing articles Show Details
8.3
pEC50
8.3
Agonist
Cannabinoid receptor 1 [human]:Wild
CHO cell line
Flux release
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5086 - 5098 Title/Abstract Full Text View citing articles Show Details
8.3
pEC50
8.3
Inverse agonist
Cannabinoid receptor 2 [human]:Wild
CHO cell line
cAMP production
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5086 - 5098 Title/Abstract Full Text View citing articles Show Details
6.55
IC50
0.28
µM
Blocker
Cannabinoid receptor 2 [Rattus norvegicus]:Wild +
prefrontal cortex
Electrophysiology
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5086 - 5098 Title/Abstract Full Text View citing articles Show Details
Emax(%)
73.5
%
Blocker
Cannabinoid receptor 2 [Rattus norvegicus]:Wild + Cannabinoid receptor 1 [Rattus norvegicus]:Wild
prefrontal cortex
Electrophysiology
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.
European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5086 - 5098 Title/Abstract Full Text View citing articles Show Details
8.1
EC50
8
nM
Agonist
Cannabinoid receptor 1 [Mus musculus]:Wild
brain
cells
GTPgammaS
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Brents, Lisa K.; Gallus-Zawada, Anna; Radominska-Pandya, Anna; Vasiljevik, Tamara; Prisinzano, Thomas E.; Fantegrossi, William E.; Moran, Jeffery H.; Prather, Paul L.
Biochemical Pharmacology, 2012 , vol. 83, # 7 p. 952 - 961 Title/Abstract Full Text View citing articles Show Details
pX
Parameter
Value (qual)
Value (quant)
Unit
8
Ki
=
10
nM
Action on Target Radioligand (/ligand)
Target
Tissue/Organ
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Cell
Bioassay
brain cell
Dose
Effect
Reference (expand all/collapse all) Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Padgett, Lea W.; Isherwood, Matthew L.; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 20 p. 5432 - 5435 Title/Abstract Full Text View citing articles Show Details
8.54
Ki
=
2.9
nM
Radioligand (/ligand)
Cannabinoid receptor 2:Wild
British Journal of Pharm...
Title/Abstract Full Text View citing articles Show Details
Poso; Huffman
British Journal of Pharmacology, 2008 , vol. 153, # 2 p. 335 - 346 Title/Abstract Full Text View citing articles Show Details
Activity
=
0.7
µM/kg
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 2 p. 439 - 447 Title/Abstract Full Text View citing articles Show Details
Activity
=
4.3
µM/kg
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 2 p. 439 - 447 Title/Abstract Full Text View citing articles Show Details
=
0.98
nm
Cannabinoid receptor 1:Wild
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Fichera, Maria; Cruciani, Gabriele; Bianchi, Alfredo; Musumarra, Giuseppe
Journal of Medicinal Chemistry, 2000 , vol. 43, # 12 p. 2300 - 2309 Title/Abstract Full Text View citing articles Show Details
ED50
=
0.25
µM/kg
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 2 p. 439 - 447 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
=
9.5
nM
Radioligand (/ligand)
Cannabinoid receptor 1 [Mus musculus]:Wild
brain cell
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 2 p. 439 - 447 Title/Abstract Full Text View citing articles Show Details
=
0.47
nm
Inhibitor
Cannabinoid receptor 2:Wild
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Fichera, Maria; Cruciani, Gabriele; Bianchi, Alfredo; Musumarra, Giuseppe
Journal of Medicinal Chemistry, 2000 , vol. 43, # 12 p. 2300 - 2309 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
=
9.5
nM
Radioligand (/ligand)
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Mabon, Ross; Wu, Ming-Jung; Lu, Jianzhong; Hart, Richard; Hurst, Dow P.; Reggio, Patricia H.; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 4 p. 539 - 549 Title/Abstract Full Text View citing articles Show Details
ED50
=
2.62
µM/kg
Bioorganic & medicinal c...
Title/Abstract Full Text Show Details
Bioorganic & medicinal c...
Title/Abstract Full Text Show Details
CHO cell line
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
John W. Huffman; Dong Dai; Billy R. Martin; David R. Compton
Bioorganic & medicinal chemistry letters, 1994 , vol. 4, # 4 p. 563 - 566 Title/Abstract Full Text Show Details
8.02
Ki
=
9.5
nM
Inhibitor
cannabinoid receptor:Wild
John W. Huffman; Dong Dai; Billy R. Martin; David R. Compton
Bioorganic & medicinal chemistry letters, 1994 , vol. 4, # 4 p. 563 - 566 Title/Abstract Full Text Show Details
8.54
Ki
=
2.9
nM
Radioligand (/ligand)
Cannabinoid receptor 2 [human]:Wild
Huffman, John W.; Zengin, Gulay; Wu, Ming-Jung; Lu, Jianzhong; Hynd, George; Bushell, Kristen; Thompson, Alicia L.S.; Bushell, Simon; Tartal, Cindy; Hurst, Dow P.; Reggio, Patricia H.; Selley, Dana E.; Cassidy, Michael P.; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 1 p. 89 - 112 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
=
9.5
nM
Radioligand (/ligand)
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Zengin, Gulay; Wu, Ming-Jung; Lu, Jianzhong; Hynd, George; Bushell, Kristen; Thompson, Alicia L.S.; Bushell, Simon; Tartal, Cindy; Hurst, Dow P.; Reggio, Patricia H.; Selley, Dana E.; Cassidy, Michael P.; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 1 p. 89 - 112 Title/Abstract Full Text View citing articles Show Details
Ratio
3.3
Radioligand (/ligand)
Cannabinoid receptor 2 [human]:Wild
CHO cell line
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Huffman, John W.; Zengin, Gulay; Wu, Ming-Jung; Lu, Jianzhong; Hynd, George; Bushell, Kristen; Thompson, Alicia L.S.; Bushell, Simon; Tartal, Cindy; Hurst, Dow P.; Reggio, Patricia H.; Selley, Dana E.; Cassidy, Michael P.; Wiley, Jenny L.; Martin, Billy R.
Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 1 p. 89 - 112 Title/Abstract Full Text View citing articles Show Details
ED50
=
0.7
µM/kg
Current pharmaceutical d...
Title/Abstract Full Text Show Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Current pharmaceutical d...
Title/Abstract Full Text Show Details
Current pharmaceutical d...
Title/Abstract Full Text Show Details
Huffman
Current pharmaceutical design, 2000 , vol. 6, # 13 p. 1323 - 1337 Title/Abstract Full Text Show Details
8.02
Ki
=
9.5
nM
Inhibitor
Huffman
Current pharmaceutical design, 2000 , vol. 6, # 13 p. 1323 - 1337 Title/Abstract Full Text Show Details
ED50
=
4.3
µM/kg
Huffman
Current pharmaceutical design, 2000 , vol. 6, # 13 p. 1323 - 1337 Title/Abstract Full Text Show Details
ED50
=
0.25
µM/kg
Current pharmaceutical d...
Title/Abstract Full Text Show Details
Cannabinoid receptor 2 [human]:Wild
Current pharmaceutical d...
Title/Abstract Full Text Show Details
Cannabinoid receptor 2 [human]:Wild
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Huffman
Current pharmaceutical design, 2000 , vol. 6, # 13 p. 1323 - 1337 Title/Abstract Full Text Show Details
8.54
Ki
=
2.9
nM
Inhibitor
Huffman
Current pharmaceutical design, 2000 , vol. 6, # 13 p. 1323 - 1337 Title/Abstract Full Text Show Details
7.86
Ki
=
13.8
nM
Radioligand (/ligand)
Raitio, Katri H.; Salo; Nevalainen; Poso; Jaervinen
Current Medicinal Chemistry, 2005 , vol. 12, # 10 p. 1217 - 1237 Title/Abstract Full Text View citing articles Show Details
ED50
=
0.7
µM/kg
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Huffman; Padgett
Current Medicinal Chemistry, 2005 , vol. 12, # 12 p. 1395 - 1411 Title/Abstract Full Text View citing articles Show Details
Activity
4.3
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Huffman; Padgett
Current Medicinal Chemistry, 2005 , vol. 12, # 12 p. 1395 - 1411 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
=
9.5
nM
Radioligand (/ligand)
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Huffman; Padgett
Current Medicinal Chemistry, 2005 , vol. 12, # 12 p. 1395 - 1411 Title/Abstract Full Text View citing articles Show Details
Activity
=
0.25
µM/kg
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Huffman; Padgett
Current Medicinal Chemistry, 2005 , vol. 12, # 12 p. 1395 - 1411 Title/Abstract Full Text View citing articles Show Details
Ratio
24.3
Radioligand (/ligand)
Cannabinoid receptor 1 [human]:Wild
Cannabinoid receptor 2 [Mus musculus]:Wild
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Raitio, Katri H.; Salo; Nevalainen; Poso; Jaervinen
Current Medicinal Chemistry, 2005 , vol. 12, # 10 p. 1217 - 1237 Title/Abstract Full Text View citing articles Show Details
8.54
Ki
=
2.9
nM
Radioligand (/ligand)
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Huffman; Padgett
Current Medicinal Chemistry, 2005 , vol. 12, # 12 p. 1395 - 1411 Title/Abstract Full Text View citing articles Show Details
8.02
pKi
8.022
Radioligand (/ligand)
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
De Freitas, Guilherme B.L.; da Silva, Leandro L.; Romeiro, Nelilma C.; Fraga, Carlos A.M.
European Journal of Medicinal Chemistry, 2009 , vol. 44, # 6 p. 2482 - 2496 Title/Abstract Full Text View citing articles Show Details
Ratio
0.94
Radioligand (/ligand)
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
De Freitas, Guilherme B.L.; da Silva, Leandro L.; Romeiro, Nelilma C.; Fraga, Carlos A.M.
European Journal of Medicinal Chemistry, 2009 , vol. 44, # 6 p. 2482 - 2496 Title/Abstract Full Text View citing articles Show Details
8.54
pKi
8.538
Radioligand (/ligand)
Cannabinoid receptor 2 [human]:Wild
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
De Freitas, Guilherme B.L.; da Silva, Leandro L.; Romeiro, Nelilma C.; Fraga, Carlos A.M.
European Journal of Medicinal Chemistry, 2009 , vol. 44, # 6 p. 2482 - 2496 Title/Abstract Full Text View citing articles Show Details
8.54
pKi
8.537
Radioligand (/ligand)
Cannabinoid receptor 2 [human]:Wild
CHO cell line
Letters in Drug Design a...
Title/Abstract Full Text View citing articles Show Details
Rituparna; Mahmood; Ravikumar
Letters in Drug Design and Discovery, 2009 , vol. 6, # 8 p. 599 - 619 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
=
9.5
nM
Radioligand (/ligand)
Cannabinoid receptor 1 [human]:Wild
Mini-Reviews in Medicina...
Title/Abstract Full Text View citing articles Show Details
Manera, Clementina; Tuccinardi, Tiziano; Martinelli, Adriano
Mini-Reviews in Medicinal Chemistry, 2008 , vol. 8, # 4 p. 370 - 387 Title/Abstract Full Text View citing articles Show Details
8.54
Ki
=
2.9
nM
Radioligand (/ligand)
Cannabinoid receptor 2 [human]:Wild
Mini-Reviews in Medicina...
Title/Abstract Full Text View citing articles Show Details
Manera, Clementina; Tuccinardi, Tiziano; Martinelli, Adriano
Mini-Reviews in Medicinal Chemistry, 2008 , vol. 8, # 4 p. 370 - 387 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
=
9.5
nM
Radioligand (/ligand)
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
brain
Patent: US2005/9903 A1...
Title/Abstract Full Text Show Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
brain
Patent: US2005/9903 A1...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
Cannabinoid receptor 2 [human]:Wild
Patent: US2005/9903 A1...
Title/Abstract Full Text Show Details
Martin, Billy R.; Huffman, John W.
Patent: US2005/9903 A1, 2005 ; Title/Abstract Full Text Show Details
Ratio
3.3
Martin, Billy R.; Huffman, John W.
Patent: US2005/9903 A1, 2005 ; Title/Abstract Full Text Show Details
8.7
Ki
=
2
nM
Martin, Billy R.; Huffman, John W.
Patent: US2005/9903 A1, 2005 ; Title/Abstract Full Text Show Details
Qualitative Information 1 of 1
Target
Cannabinoid receptor 2 [human]:Wild
Substance action on target
Radioligand (/ligand)
Biological material
human CHO cell line
Assay Description
Binding affinity of the compound towards human cannabinoid receptor 2 expressed in CHO membranes using 102.9 Ci/mmol [3H]CP 55940 as radioligand upon incubation in 50 mM Tris-HCl, pH 7.4 for 1 h at 30 degree C
Results
Ki not calculated
Citation
Rituparna; Mahmood; Ravikumar
Letters in Drug Design and Discovery, 2009 , vol. 6, # 8 p. 599 - 619 Title/Abstract Full Text View citing articles Show Details
In vivo: Animal Model (5) Quantitative Results pX
Parameter
Value (qual)
ED50
Value (quant)
Unit
0.7
µmol/kg
Action on Target
Animal Model
Biological Species
Route of administration
Institute for Cancer Research mouse
intravenous administration
Dose
Dosing regimen Single
Effect
Reference (expand all/collapse all)
Antiinflammatory: non-steroidal
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Analgesic
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Antiinflammatory: non-steroidal
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Antiinflammatory: non-steroidal
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Antiinflammatory: non-steroidal
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Wiley, Jenny L.; Compton, David R.; Dai, Dong; Lainton, Julia A. H.; Phillips, Michelle; Huffman, John W.; Martin, Billy R.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 285, # 3 p. 995 - 1004 Title/Abstract Full Text View citing articles Show Details
ED50
0.25
µmol/kg
tail flick test
Institute for Cancer Research mouse
Wiley, Jenny L.; Compton, David R.; Dai, Dong; Lainton, Julia A. H.; Phillips, Michelle; Huffman, John W.; Martin, Billy R.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 285, # 3 p. 995 - 1004 Title/Abstract Full Text View citing articles Show Details
ED50
4.3
µmol/kg
Institute for Cancer Research mouse
Wiley, Jenny L.; Compton, David R.; Dai, Dong; Lainton, Julia A. H.; Phillips, Michelle; Huffman, John W.; Martin, Billy R.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 285, # 3 p. 995 - 1004 Title/Abstract Full Text View citing articles Show Details
ED50
1.9
µmol/kg
Institute for Cancer Research mouse
Wiley, Jenny L.; Compton, David R.; Dai, Dong; Lainton, Julia A. H.; Phillips, Michelle; Huffman, John W.; Martin, Billy R.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 285, # 3 p. 995 - 1004 Title/Abstract Full Text View citing articles Show Details
ED50
<
8.5
µmol/kg
drug discrimination test
Sprague Dawley rat
oral administration
Repeated
Wiley, Jenny L.; Compton, David R.; Dai, Dong; Lainton, Julia A. H.; Phillips, Michelle; Huffman, John W.; Martin, Billy R.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 285, # 3 p. 995 - 1004 Title/Abstract Full Text View citing articles Show Details
Identification