Query Query
1. Query N
O
Results
Date
1 substances in Reaxys
2018-03-27 16h:18m:02s (EST)
Search as: As drawn
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Reaxys ID 8350109 View in Reaxys
N
1/1 Chemical Name: 1-pentyl-2-methyl-3-(1-naphthoyl)indole Linear Structure Formula: C25H25NO Molecular Formula: C25H25NO Molecular Weight: 355.48 Type of Substance: heterocyclic InChI Key: IBBNKINXTRKICJ-UHFFFAOYSA-N Note:
O
Substance Label (2) Label References 17
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; vol. 11; nb. 4; (2003); p. 539 - 549, View in Reaxys
JWH-018
Showalter, Vincent M.; Compton, David R.; Martin, Billy R.; Abood, Mary E.; Journal of Pharmacology and Experimental Therapeutics; vol. 278; nb. 3; (1996); p. 989 - 999, View in Reaxys
Druglikeness (1) 1 of 1
LogP
7.372
H Bond Donors
0
H Bond Acceptors
2
Rotatable Bonds
6
TPSA
22
Lipinski Number
3
Veber Number
2
Highest Clinical Phase (1) Highest Clinical Phase Preclinical Medchem (61) 1 of 61
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
Ki
Unit
nM
Quantitative value
9.8
Deviation
2.80000
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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2 of 61
Measurement pX
8.01
Concomitants: Compound RN
24140639; 24140641; 2835835; 6659789; 6659789
Concomitants: Compound name
Leupeptine; Pepstatin; Pefabloc; CP 55940; [3H]-CP 55940
Concomitants: Compound role
COM; COM; COM; NSB; RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human]
3 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
Ki
Unit
nM
Quantitative value
3.1
Deviation
0.300000
Measurement pX
8.51
Concomitants: Compound RN
24140639; 24140641; 2835835; 6659789; 6659789
Concomitants: Compound name
Leupeptine; Pepstatin; Pefabloc; CP 55940; [3H]-CP 55940
Concomitants: Compound role
COM; COM; COM; NSB; RAD
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Mutated:Substitution,1,Phenylalanine,191,Leucine,Substitution,2,Leucine,193,Isoleucine,Substitution,3,Glycine,195,Serine,Substitution,4,Alanine,198,Methionine,Substitution,5,Serine,199,Threonine,Substitution,6,Phenylalanine, 208,Leucine
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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4 of 61
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
Ki
Unit
nM
Quantitative value
1.4
Deviation
0.200000
Measurement pX
8.85
Concomitants: Compound RN
24140639; 24140641; 2835835; 6659789; 6659789
Concomitants: Compound name
Leupeptine; Pepstatin; Pefabloc; CP 55940; [3H]-CP 55940
Concomitants: Compound role
COM; COM; COM; NSB; RAD
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human]
5 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
cAMP production
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
EC50
Unit
nM
Quantitative value
14.7
Deviation
3.90000
Measurement pX
7.83
Concomitants: Compound RN
4300863; 52645
Concomitants: Compound name
Forskolin; [3H]-cAMP
Concomitants: Compound role
IND; MAR
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human]
6 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
cAMP production
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
Emax(%)
Unit
%
Quantitative value
79
Concomitants: Compound RN
4300863; 52645
Concomitants: Compound name
Forskolin; [3H]-cAMP
Concomitants: Compound role
IND; MAR
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Mutated:Substitution,1,Phenylalanine,191,Leucine,Substitution,2,Leucine,193,Isoleucine,Substitution,3,Glycine,195,Serine,Substitution,4,Alanine,198,Methionine,Substitution,5,Serine,199,Threonine,Substitution,6,Phenylalanine, 208,Leucine
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
cAMP production
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
EC50
Unit
nM
Quantitative value
4.7
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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7 of 61
Deviation
0.800000
Measurement pX
8.33
Concomitants: Compound RN
4300863; 52645
Concomitants: Compound name
Forskolin; [3H]-cAMP
Concomitants: Compound role
IND; MAR
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1 [human]
8 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Mutated:Substitution,1,Phenylalanine,191,Leucine,Substitution,2,Leucine,193,Isoleucine,Substitution,3,Glycine,195,Serine,Substitution,4,Alanine,198,Methionine,Substitution,5,Serine,199,Threonine,Substitution,6,Phenylalanine, 208,Leucine
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
cAMP production
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
JWH 018
Substance Dose
1.00000E-11 M
Measurement Parameter
Emax(%)
Unit
%
Quantitative value
70
Concomitants: Compound RN
4300863; 52645
Concomitants: Compound name
Forskolin; [3H]-cAMP
Concomitants: Compound role
IND; MAR
Target Name
cannabinoid receptor [Mus musculus]
Target Synonyms
cannabinoid receptor
Target, Subunit, Species cannabinoid receptor [Mus musculus] Target Mutant/Chimera Details
cannabinoid receptor [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Bioassay Name
Organ contraction
Biological Species/NCBI MF1 mouse ID
9 of 61
Organs/Tissues
vas deferens
Substance RN
8350109View in Reaxys
Substance Name
1-pentyl-2-methyl-3-(1-naphthoyl)indole
Measurement Parameter
IC50
Unit
nM
Quantitative value
2.56
Measurement pX
8.59
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI Sprague Dawley rat ID
10 of 61
Organs/Tissues
brain cortex
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
7
Substance Dose
0.100000 nM
Measurement Parameter
Ki
Unit
nM
Quantitative value
9.5
Deviation
4.50000
Measurement pX
8.02
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940
Concomitants: Compound role
NSB; RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human]
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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11 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
7
Substance Dose
0.100000 nM
Measurement Parameter
Ki
Unit
nM
Quantitative value
2.94
Deviation
2.60000
Measurement pX
8.53
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940
Concomitants: Compound role
NSB; RAD
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI Sprague Dawley rat ID Organs/Tissues
brain
Cell Fraction
Cytoplasmic membrane
Substance RN
8350109View in Reaxys
Substance Name
7
Measurement Parameter
Ki
Unit
nM
Quantitative value
9.5
Deviation
4.50000
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement pX
8.02
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940; Tris EDTA
Concomitants: Compound role
NSB; RAD; COM
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Spontaneous activity
Biological Species/NCBI Institute for Cancer Research mouse ID Substance RN
8350109View in Reaxys
Substance Name
7
Substance Route of Adm.
intravenous administration
Substance Dosing Regi- Single men
13 of 61
Measurement Parameter
ED50
Unit
µmol/kg
Quantitative value
0.7
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI Institute for Cancer Research mouse ID Substance RN
8350109View in Reaxys
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Substance Name
7
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
max effect
Quantitative value
0.25
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Spontaneous activity
Biological Species/NCBI Institute for Cancer Research mouse ID
15 of 61
Substance RN
8350109View in Reaxys
Substance Name
7
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
max effect
Quantitative value
4.3
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Spontaneous activity
Biological Species/NCBI Institute for Cancer Research mouse ID Substance RN
8350109View in Reaxys
Substance Name
7
Measurement Parameter
ED50
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Unit
µmol/kg
Measurement Object
max effect
Quantitative value
1.9
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI Sprague Dawley rat ID Substance RN
8350109View in Reaxys
Substance Name
7
Substance Route of Adm.
oral administration
Substance Dosing Regi- Repeated men
17 of 61
Measurement Parameter
ED50
Unit
µmol/kg
Qualitative value
<
Quantitative value
8.5
Concomitants: Compound RN
6659789; 4354308
Concomitants: Compound name
CP 55940; Delta9-THC
Concomitants: Compound role
TRA; TRA
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
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Cell Fraction
Cytoplasmic membrane
Substance RN
8350109View in Reaxys
Substance Name
JWH-018
Measurement Parameter
Ki
Unit
nM
Quantitative value
2.94
Deviation
2.65000
Measurement pX
8.53
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940
Concomitants: Compound role
NSB; RAD
Showalter, Vincent M.; Compton, David R.; Martin, Billy R.; Abood, Mary E.; Journal of Pharmacology and Experimental Therapeutics; vol. 278; nb. 3; (1996); p. 989 - 999, View in Reaxys 18 of 61
Target Name
cannabinoid receptor [Rattus norvegicus]
Target Synonyms
cannabinoid receptor
Target, Subunit, Species cannabinoid receptor [Rattus norvegicus] Target Mutant/Chimera Details
cannabinoid receptor [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI Sprague Dawley rat ID
19 of 61
Organs/Tissues
brain cortex
Cell Fraction
Cytoplasmic membrane
Substance RN
8350109View in Reaxys
Substance Name
n-pentyl
Measurement Parameter
Ki
Unit
nM
Quantitative value
9.5
Measurement pX
8.02
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940
Concomitants: Compound role
NSB; RAD
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
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Target, Subunit, Species Cannabinoid receptor 1 [human]
20 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
Cpd 10
Measurement Parameter
pKi
Quantitative value
8.7
Deviation
0.100000
Measurement pX
8.7
Concomitants: Compound RN
6659789
Concomitants: Compound name
[3H]-CP 55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO cell line
Cell Fraction
Membrane
Substance RN
8350109View in Reaxys
Substance Name
Cpd 10
Measurement Parameter
pKi
Quantitative value
8.2
Deviation
0.100000
Measurement pX
8.2
Concomitants: Compound RN
6659789
Concomitants: Compound name
[3H]-CP 55940
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21 of 61
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human]
22 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux release
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Substance Name
Cpd 10
Measurement Parameter
pEC50
Quantitative value
8.3
Deviation
0.200000
Measurement pX
8.3
Concomitants: Compound RN
1913991; 1913991
Concomitants: Compound name
[3H]-Arachidonic acid; [3H]-Arachidonic acid; BSA
Concomitants: Compound role
MAR; SUB; COM
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Inverse agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
cAMP production
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Substance Name
Cpd 10
Measurement Parameter
pEC50
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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23 of 61
Quantitative value
8.3
Deviation
0.300000
Measurement pX
8.3
Concomitants: Compound RN
4300863; 3555164
Concomitants: Compound name
Forskolin; IBMX
Concomitants: Compound role
IND; COM
Target Name
Cannabinoid receptor 2 [Rattus norvegicus]; Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cnr2; rcb2 + brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
q9qzn9 + p20272
Target, Subunit, Species Cannabinoid receptor 2 [Rattus norvegicus]; Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 2 [Rattus norvegicus]:Wild; Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus; Rattus norvegicus
Target Transfection
Non Transfected; Non Transfected
Substance Action on Target
Blocker
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI Wistar rat ID
24 of 61
Organs/Tissues
prefrontal cortex
Substance RN
8350109View in Reaxys
Substance Name
Cpd 10
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.28
Measurement pX
6.55
Target Name
Cannabinoid receptor 2 [Rattus norvegicus]; Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cnr2; rcb2 + brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
q9qzn9 + p20272
Target, Subunit, Species Cannabinoid receptor 2 [Rattus norvegicus]; Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 2 [Rattus norvegicus]:Wild; Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus; Rattus norvegicus
Target Transfection
Non Transfected; Non Transfected
Substance Action on Target
Blocker
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Biological Species/NCBI Wistar rat ID
25 of 61
Organs/Tissues
prefrontal cortex
Substance RN
8350109View in Reaxys
Substance Name
Cpd 10
Measurement Parameter
Emax(%)
Unit
%
Quantitative value
73.5
Deviation
10.8000
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
GTPgammaS
Biological Species/NCBI Mus musculus ID
26 of 61
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
Homogenate
Substance RN
8350109View in Reaxys
Substance Name
JWH-018
Measurement Parameter
EC50
Unit
nM
Quantitative value
8
Measurement pX
8.1
Concomitants: Compound RN
93029; 9743845; 10309076
Concomitants: Compound name
Adenosine; [35S]-GTPgS; GDP; BSA
Concomitants: Compound role
COM; MAR; COM; COM
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus]
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Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards Cannabinoid receptor 1 from rat brain using [3H]CP-55,940 as radioligand
Biological Species/NCBI Rattus norvegicus ID
27 of 61
Cells/Cell Lines
brain cell
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
10
Deviation
4
Measurement pX
8
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 2
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2 (cannabinoid receptor 2); cx5; hcb2; mcb2; rcb2
Target, Subunit, Species Cannabinoid receptor 2
28 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 2:Wild
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards CB2 receptor
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
3
Measurement pX
8.54
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo spontaneous activity of the compound was determined in mice
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
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Measurement Parameter
Activity
Unit
µM/kg
Measurement Object
SA
Qualitative value
=
Quantitative value
0.7
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.; Bioorganic and Medicinal Chemistry; vol. 8; nb. 2; (2000); p. 439 - 447, View in Reaxys 29 of 61
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Cannabimimetic activity was determined in mouse by measuring rectal temperature
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Activity
Unit
µM/kg
Measurement Object
Retention time
Qualitative value
=
Quantitative value
4.3
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.; Bioorganic and Medicinal Chemistry; vol. 8; nb. 2; (2000); p. 439 - 447, View in Reaxys 30 of 61
Target Name
Cannabinoid receptor 1
Target Synonyms
brain-type cannabinoid receptor; cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1); skr6 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1
31 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 1:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibition constant (LogKi) of the compound against Cannabinoid receptor 1
Substance RN
8350109View in Reaxys
Unit
nm
Qualitative value
=
Quantitative value
0.98
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo antinociceptive activity of the compound was determined in mouse by tail flick method
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Antinociceptive activity
Qualitative value
=
Quantitative value
0.25
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.; Bioorganic and Medicinal Chemistry; vol. 8; nb. 2; (2000); p. 439 - 447, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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32 of 61
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro binding affinity of the compound towards cannabinoid receptor 1 using [3H]CP-55940 as radioligand in mouse brain
Biological Species/NCBI Mus musculus ID Cells/Cell Lines
brain cell
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman, John W.; Lu, Jianzhong; Dai, Dong; Kitaygorodskiy, Aleksandr; Wiley, Jenny L.; Martin, Billy R.; Bioorganic and Medicinal Chemistry; vol. 8; nb. 2; (2000); p. 439 - 447, View in Reaxys 33 of 61
Target Name
Cannabinoid receptor 2
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2 (cannabinoid receptor 2); cx5; hcb2; mcb2; rcb2
Target, Subunit, Species Cannabinoid receptor 2
34 of 61
Target Mutant/Chimera Details
Cannabinoid receptor 2:Wild
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibition constant (LogKi) of the compound against Cannabinoid receptor 2
Substance RN
8350109View in Reaxys
Unit
nm
Qualitative value
=
Quantitative value
0.47
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro binding affinity of the compound towards cannabinoid receptor 1 of rat whole brain membrane using 1 nM [3H]CP-55940 as radioligand
Biological Species/NCBI Rattus norvegicus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
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; vol. 11; nb. 4; (2003); p. 539 - 549, View in Reaxys 35 of 61
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Average of the effective dose required to produce spontaneous activity, antinociception, hypothermia, and catalepsy in a mouse model of cannabimimetic activity
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Average of the effective dose required
Qualitative value
=
Quantitative value
2.62
John W. Huffman; Dong Dai; Billy R. Martin; David R. Compton; Bioorganic & medicinal chemistry letters; vol. 4; nb. 4; (1994); p. 563 - 566, View in Reaxys 36 of 61
Target Name
cannabinoid receptor
Target Synonyms
cannabinoid receptor; cannaboid receptor
Target, Subunit, Species cannabinoid receptor Target Mutant/Chimera Details
cannabinoid receptor:Wild
Substance Action on Target
Inhibitor
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Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro Inhibition constant of compound to displace [3H]CP-55940 from cannabinoid receptor
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
John W. Huffman; Dong Dai; Billy R. Martin; David R. Compton; Bioorganic & medicinal chemistry letters; vol. 4; nb. 4; (1994); p. 563 - 566, View in Reaxys 37 of 61
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards human cannabinoid receptor 2 expressed in CHO cells using [3H]CP 55,940 as radioligand upon incubation at 30 degree C for 1 h
Biological Species/NCBI human ID
38 of 61
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards cannabinoid receptor 1 using [3H]CP 55,940 as radioligand in rat brain membranes
Biological Species/NCBI Rattus norvegicus ID
39 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity of human cannabinoid receptor 2 expressed in CHO cells to that of rat cannabinoid receptor 1
Biological Species/NCBI human ID
40 of 61
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Measurement Parameter
Ratio
Quantitative value
3.3
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose of the compound measured spontaneous activity(SA) in mouse
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Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Spontaneous activity
Qualitative value
=
Quantitative value
0.7
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 41 of 61
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory constant of the compound against cannabinoid receptor 1 using [3H] CP-55,940 as radioligand in rat brain membrane
Biological Species/NCBI Rattus norvegicus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 42 of 61
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose of the compound measured hypothermia (as decrease in rectal temperature, RT) in mouse
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
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Measurement Object
Hypothermia
Qualitative value
=
Quantitative value
4.3
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 43 of 61
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose of the compound measured antinociception (as tail flick, TF) in mouse
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Antinociception
Qualitative value
=
Quantitative value
0.25
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 44 of 61
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory constant of the compound against cannabinoid receptor 2 using [3H] WIN-55,212 as radioligand in human spleen membrane
Biological Species/NCBI human ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]WIN 55212-2
Concomitants: Compound role
RAD
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 45 of 61
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
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Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards human Cannabinoid receptor 2 using [3H](-)CP55940 as radioligand
Biological Species/NCBI human ID
46 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
13.8
Measurement pX
7.86
Concomitants: Compound name
[3H](-)CP-55940
Concomitants: Compound role
RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose required for spontaneous activity was determined in mouse
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Qualitative value
=
Quantitative value
0.7
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 47 of 61
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effect on hypothermia was determined in mouse by measuring the decrease in rectal temperature
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Activity
Measurement Object
Decrease in rectal temperature
Quantitative value
4.3
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 48 of 61
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
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Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards Cannabinoid receptor 1 (40 ug) from rat forebrain synaptosomal membranes using 0.76 nM [3H]CP-55,940 as radioligand upon incubation for 1 h at 30 degree C
Biological Species/NCBI Rattus norvegicus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 49 of 61
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo antinociceptive activity was determined in mouse using tail flick method
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Activity
Unit
µM/kg
Measurement Object
Antinociceptive activity
Qualitative value
=
Quantitative value
0.25
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 50 of 61
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
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Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity towards human Cannabinoid receptor 1 to that of human Cannabinoid receptor 2
Biological Species/NCBI human ID
51 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
Ratio
Quantitative value
24.3
Target Name
Cannabinoid receptor 2 [Mus musculus]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cnr2; mcb2
Target Uniprot ID
p47936
Target, Subunit, Species Cannabinoid receptor 2 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 2 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards Cannabinoid receptor 2 (40 ug) from mouse spleen membranes using 0.76 nM [3H]CP-55,940 as radioligand upon incubation for 1 h at 30 degree C
Biological Species/NCBI Mus musculus ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 52 of 61
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
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Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards rat cannabinoid receptor 1 in brain homogenates
Biological Species/NCBI Rattus norvegicus ID
53 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
pKi
Quantitative value
8.022
Measurement pX
8.02
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity of the compound towards rat brain homogenate cannabinoid receptor 1 to that of cloned human cannabinoid receptor 2
Biological Species/NCBI Rattus norvegicus ID
54 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
Ratio
Quantitative value
0.94
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards cloned human cannabinoid receptor 2 was determined
Biological Species/NCBI human ID Substance RN
8350109View in Reaxys
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55 of 61
Measurement Parameter
pKi
Quantitative value
8.538
Measurement pX
8.54
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
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
Biological Species/NCBI human ID
56 of 61
Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
Qualitative Results
Ki not calculated
Measurement Parameter
Qualitative
Measurement Object
Ki
Concomitants: Compound name
[3H]CP 55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Negative logarithm of 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
Biological Species/NCBI human ID Cells/Cell Lines
CHO cell line
Substance RN
8350109View in Reaxys
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57 of 61
Measurement Parameter
pKi
Quantitative value
8.537
Measurement pX
8.54
Concomitants: Compound name
[3H]CP 55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards human cannabinoid receptor 1
Biological Species/NCBI human ID
58 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards human cannabinoid receptor 2
Biological Species/NCBI human ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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59 of 61
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards rat brain cannabinoid receptor 1 using [3H] CP 55,940 upon incubation in 50 mM Tris-HCl, pH 7.4 at 30 degree C for 1 hour
Biological Species/NCBI Rattus norvegicus ID
60 of 61
Organs/Tissues
brain
Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity towards rat brain cannabinoid receptor 1 to that of human cannabinoid receptor 2
Biological Species/NCBI Rattus norvegicus ID Organs/Tissues
brain
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61 of 61
Substance RN
8350109View in Reaxys
Measurement Parameter
Ratio
Measurement Object
Ratio
Quantitative value
3.3
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards human cannabinoid receptor 2 using [3H] CP 55,940 upon incubation in 50 mM Tris-HCl, pH 7.4 at 30 degree C for 1 hour
Biological Species/NCBI human ID Substance RN
8350109View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2
Deviation
2.6
Measurement pX
8.7
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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