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TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50000727((R)-3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-di...)
Affinity DataEC50:  0.0350nMAssay Description:Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1/2(Rat)
Hebrew University

Curated by ChEMBL
LigandPNGBDBM50229577(CHEMBL63818)
Affinity DataKi:  0.0450nMAssay Description:Compound was evaluated for the competitive inhibition of [3H]3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2019
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50061108(3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-dimeth...)
Affinity DataEC50:  0.0560nMAssay Description:Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50532778(CHEMBL4465566 | US10882838, Example 3.6)
Affinity DataKi:  0.100nMAssay Description:All the cannabinoids discussed in this invention are tested for their ability to bind to CB1 and CB2 receptors using membranes from rat brain or HEK2...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2021
Entry Details
US Patent

TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50061108(3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-dimeth...)
Affinity DataKi:  0.100nMAssay Description:Binding to Cannabinoid receptor 1 using African green monkey (COS-7) cells transfected with the cDNA of rat CB1.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50532778(CHEMBL4465566 | US10882838, Example 3.6)
Affinity DataKi:  0.100nMAssay Description:Displacement of [3H]CP55940 from CB1 receptor in rat brain membranes by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50350429(CHEMBL1814154)
Affinity DataIC50: 0.100nMpH: 7.4Assay Description:Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50532778(CHEMBL4465566 | US10882838, Example 3.6)
Affinity DataKi:  0.100nMAssay Description:Displacement of [3H]CP55940 from CB1 receptor in rat brain membranes by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50350447(CHEMBL1814329)
Affinity DataIC50: 0.100nMpH: 7.4Assay Description:Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50350458(CHEMBL1814333)
Affinity DataIC50: 0.100nMpH: 7.4Assay Description:Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50000727((R)-3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-di...)
Affinity DataKi:  0.100nMAssay Description:Binding to Cannabinoid receptor 1 using African green monkey (COS-7) cells transfected with the cDNA of rat CB1.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50067497(CP-55244 | CHEMBL131627 | (2S,4S,4aS,6R,8aR)-4-[4-...)
Affinity DataKi:  0.110nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/2/2012
Entry Details
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50067497(CP-55244 | CHEMBL131627 | (2S,4S,4aS,6R,8aR)-4-[4-...)
Affinity DataKi:  0.110nMAssay Description:Displacement of [3H]CP-55940 binding to Cannabinoid receptor 1 in rat brain membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM21281(WIN55212-2 | CHEMBL188 | (2,3-dihydro-5-methyl-3-(...)
Affinity DataKi:  0.140nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/25/2012
Entry Details
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM227552(US9339486, CP55,940)
Affinity DataEC50:  0.140nMAssay Description:The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/15/2017
Entry Details
US Patent

TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50328671((6aR,9R,10aR)-3-(1-hexylcyclobutyl)-6,6-dimethyl-6...)
Affinity DataKi:  0.160nMAssay Description:Displacement of [3H]CP55940 from rat brain CB1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2011
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50072775(ChEMBL_75020 | 5-(1,1-Dimethyl-heptyl)-2-[(1R,2R,5...)
Affinity DataEC50:  0.160nMAssay Description:Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50328671((6aR,9R,10aR)-3-(1-hexylcyclobutyl)-6,6-dimethyl-6...)
Affinity DataKi:  0.160nMAssay Description:Displacement of [3H]-CP-55,940 from CB1R in rat brain membranes measured by radioligand based competition binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM21278(SR141716 | 5-(4-chlorophenyl)-1-(2,4-dichloropheny...)
Affinity DataEC50:  0.170nMAssay Description:Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50061113(3-(1',1'-dimethylheptyl)-6,6,9-trimethyl-6H-benzo[...)
Affinity DataEC50:  0.180nMAssay Description:Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1/2(Rat)
Hebrew University

Curated by ChEMBL
LigandPNGBDBM50000727((R)-3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-di...)
Affinity DataKi:  0.181nMAssay Description:Compound was evaluated for the competitive inhibition of [3H]3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2019
Entry Details Article
PubMed
TargetCannabinoid receptor 1/2(Rat)
Hebrew University

Curated by ChEMBL
LigandPNGBDBM50229579(CHEMBL65475)
Affinity DataKi:  0.190nMAssay Description:Compound was evaluated for the competitive inhibition of [3H]3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2019
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50000727((R)-3-(1,1-Dimethyl-heptyl)-9-hydroxymethyl-6,6-di...)
Affinity DataKi:  0.190nMAssay Description:Binding affinity for Cannabinoid receptor 1 using African green monkey (COS-7) cells transfected with the cDNA of rat brain synaptosomal membrane pre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50323009(1'-(5-(4-chlorophenyl)-4-(2,4-dichlorophenyl)-1-me...)
Affinity DataIC50: 0.200nMAssay Description:Binding affinity to CB1 receptor in rat brain synaptosomal membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2011
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50267545((4-(3-cyclopropyl-5-(trifluoromethyl)phenylsulfony...)
Affinity DataIC50: 0.200nMAssay Description:Displacement of [3H] SR-141716 from rat recombinant CB1R expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50067499((6aR,10aR)-3-(1,1-dimethyl-heptyl)-9-hydroxymethyl...)
Affinity DataKi:  0.230nMAssay Description:Displacement of [3H]CP-55940 binding to Cannabinoid receptor 1 in rat brain membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50061111((R)-3-(1,1-Dimethyl-heptyl)-6,6,9-trimethyl-6a,7,8...)
Affinity DataKi:  0.241nMAssay Description:Binding to Cannabinoid receptor 1 using African green monkey (COS-7) cells transfected with the cDNA of rat CB1.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50463772(CHEMBL4239190)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]CP-55,940 from rat brain Cb1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50200841(CHEMBL220360 | N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-...)
Affinity DataIC50: 0.300nMpH: 7.4Assay Description:Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50582411(CHEMBL5084325)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]CP55940 from rat brain membrane CB1 receptor assessed as inhibition constant incubated for 1 hr by TopCount scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50233599(CHEMBL3104360)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]CP-55,940 from CB1 receptor in rat brain by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50233619(CHEMBL4085404 | US10882838, Example 1.18)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]CP-55,940 from CB1 receptor in rat brain membranes by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/5/2019
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50459322(CHEMBL4215369)
Affinity DataEC50:  0.300nMAssay Description:Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50233599(CHEMBL3104360)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]CP-55,940 from CB1 receptor in rat brain membranes by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/5/2019
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50233619(CHEMBL4085404 | US10882838, Example 1.18)
Affinity DataKi:  0.300nMAssay Description:All the cannabinoids discussed in this invention are tested for their ability to bind to CB1 and CB2 receptors using membranes from rat brain or HEK2...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2021
Entry Details
US Patent

TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50463775(CHEMBL4240671)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]CP-55,940 from rat brain Cb1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM21278(SR141716 | 5-(4-chlorophenyl)-1-(2,4-dichloropheny...)
Affinity DataKi:  0.310nMAssay Description:Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS bindingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50063885((6aR,10aR)-3-(2-Hexyl-[1,3]dithiolan-2-yl)-6,6,9-t...)
Affinity DataKi:  0.320nMAssay Description:Binding affinity against rat brain Cannabinoid receptor 1 using [3H]CP-55940More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50063885((6aR,10aR)-3-(2-Hexyl-[1,3]dithiolan-2-yl)-6,6,9-t...)
Affinity DataKi:  0.320nMAssay Description:The compound was evaluated for its affinity towards cannabinoid receptor 1 (CB1) in rat brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50063885((6aR,10aR)-3-(2-Hexyl-[1,3]dithiolan-2-yl)-6,6,9-t...)
Affinity DataKi:  0.320nMAssay Description:Binding affinity for Cannabinoid receptor 1 by the ability to displace radiolabeled CP-55940 from purified rat forebrain synaptosomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50242451(hemopressin | CHEMBL510801)
Affinity DataEC50:  0.350nMAssay Description:Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50603275(CHEMBL5187249)
Affinity DataKi:  0.380nMAssay Description:Displacement of [3H]-CP-55,940 from CB1R in rat brain membranes measured by radioligand based competition binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50582403(CHEMBL5085420)
Affinity DataKi:  0.390nMAssay Description:Displacement of [3H]CP55940 from rat brain membrane CB1 receptor assessed as inhibition constant incubated for 1 hr by TopCount scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50350449(CHEMBL1814331)
Affinity DataIC50: 0.400nMpH: 7.4Assay Description:Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50582412(CHEMBL5087407)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]CP55940 from rat brain membrane CB1 receptor assessed as inhibition constant incubated for 1 hr by TopCount scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50582400(CHEMBL5077315)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]CP55940 from rat brain membrane CB1 receptor assessed as inhibition constant incubated for 1 hr by TopCount scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50323003(1'-(5-(4-chlorophenyl)-4-(2,4-dichlorophenyl)-1-(2...)
Affinity DataIC50: 0.400nMAssay Description:Binding affinity to CB1 receptor in rat brain synaptosomal membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2011
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50463775(CHEMBL4240671)
Affinity DataEC50:  0.400nMAssay Description:Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50233605(CHEMBL3104362 | US10882838, Example 1.20)
Affinity DataEC50:  0.400nMAssay Description:Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetCannabinoid receptor 1(Rat)
Institute of Science

Curated by ChEMBL
LigandPNGBDBM50582405(CHEMBL5074603)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]CP55940 from rat brain membrane CB1 receptor assessed as inhibition constant incubated for 1 hr by TopCount scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
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