DGIdb - CNR1 Gene Record

CNR1 1268 Druggable Genome

Alternate Names:

1268
CANNABINOID RECEPTOR 1
CNR1
CANN6
CB-R
CB1
CB1A
CB1K5
CB1R
CNR
114610
2159
ENSG00000118432
OTTHUMG00000015184
P21554
CNR1_HUMAN
PA26681
CANNABINOID RECEPTOR 1 (CB1) (CB-R) (CANN6). [SOURCE:UNIPROT/SWISSPROT;ACC:P21554]
BE0000061
56
NP_057167
NM_016083
CB<sub>1</sub> receptor
T76685

Gene Info:

Interpro Acc	IPR000276
Interpro Name	GPCR, rhodopsin-like, 7TM
Human Readable Name	DRUGGABLE GENOME
Uniprot Status	Swiss-Prot
Interpro Type	Family
Interpro Short Name	7TM_GPCR_Rhodpsn
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
Target Main Class	Receptors
Transmembrane Helix Count	7
GuideToPharmacology Gene Category Name	Cannabinoid receptors
GuideToPharmacology Gene Category ID	13
Gene Biotype	PROTEIN_CODING

(12 More Sources)

Gene Categories: Category Details

CELL SURFACE
KINASE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME
ENZYME

Publications:

Darmani, 2001, The cannabinoid CB1 receptor antagonist SR 141716A reverses the antiemetic and motor depressant actions of WIN 55, 212-2., Eur. J. Pharmacol.
Hirst et al., 1996, Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist., Neurosci. Lett.
Pertwee, 1999, Cannabis and cannabinoids: pharmacology and rationale for clinical use., Forsch Komplementarmed
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Pertwee et al., 1996, Evidence for the presence of cannabinoid CB1 receptors in mouse urinary bladder., Br. J. Pharmacol.
Davis et al., 2007, The emerging role of cannabinoid neuromodulators in symptom management., Support Care Cancer
Heimann AS et al., 2007, Hemopressin is an inverse agonist of CB1 cannabinoid receptors., Proc Natl Acad Sci U S A
Yan L et al., 2010, Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity., J Med Chem
Lambeng N et al., 2007, Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies., Bioorg Med Chem Lett
Laprairie RB et al., 2015, Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor., Br J Pharmacol
Nurmi EL et al., 2013, Moderation of antipsychotic-induced weight gain by energy balance gene variants in the RUPP autism network risperidone studies., Transl Psychiatry
Tiwari AK et al., 2010, A common polymorphism in the cannabinoid receptor 1 (CNR1) gene is associated with antipsychotic-induced weight gain in Schizophrenia., Neuropsychopharmacology
Monteleone P et al., 2010, Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain., J Clin Psychopharmacol
Urbani P et al., 2008, Novel sterically hindered cannabinoid CB1 receptor ligands., Bioorg Med Chem
Suhara Y et al., 2007, Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand., Bioorg Med Chem
Manca I et al., 2013, Novel pyrazole derivatives as neutral CB₁ antagonists with significant activity towards food intake., Eur J Med Chem
Shire et al., 1996, Structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A., J. Biol. Chem.
Tseng SL et al., 2008, Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists., J Med Chem
Wu CH et al., 2009, Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice., J Med Chem
Kumar Srivastava B et al., 2008, Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist., Bioorg Med Chem Lett
Cawston EE et al., 2015, Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors., J Med Chem
Pryce et al., 2003, Mifepristone or inhibition of 11beta-hydroxylase activity potentiates the sedating effects of the cannabinoid receptor-1 agonist Delta(9)-tetrahydrocannabinol in mice., Neurosci. Lett.
Tsai et al., 2000, Association study of a cannabinoid receptor gene (CNR1) polymorphism and schizophrenia., Psychiatr. Genet.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Gorriti et al., 2005, Acute delta9-tetrahydrocannabinol exposure facilitates quinpirole-induced hyperlocomotion., Pharmacol. Biochem. Behav.
Zamponi GW et al., 2009, Scaffold-based design and synthesis of potent N-type calcium channel blockers., Bioorg Med Chem Lett
Morales P et al., 2017, Molecular Targets of the Phytocannabinoids: A Complex Picture., Prog Chem Org Nat Prod
Appendino G et al., 2006, First "hybrid" ligands of vanilloid TRPV1 and cannabinoid CB2 receptors and non-polyunsaturated fatty acid-derived CB2-selective ligands., FEBS Lett

NABILONE CNR1

Interaction Score: 7.93

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
11698062 8981483 10575283 11752352 8864542 17139494

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
MARINOL CNR1

Interaction Score: 3.96

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TEND TdgClinicalTrial TTD
OTENABANT CNR1

Interaction Score: 3.96

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology ChemblInteractions
DRINABANT CNR1

Interaction Score: 3.96

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank ChemblInteractions

TARANABANT CNR1

Interaction Score: 3.3

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

Details of the Assay for Interaction Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting.

PMIDs:
20423086

Sources:
DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions

CHEMBL498746 CNR1

Interaction Score: 2.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19530697

Sources:
DTC
CHEMBL146346 CNR1

Interaction Score: 2.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17110113

Sources:
DTC

SURINABANT CNR1

Interaction Score: 2.64

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Direct Interaction yes

Details of the Assay for Interaction Inhibition of [3H]CP-55940 binding to human cannabinoid receptor 1 expressed in CHO cells

PMIDs:
None found

Sources:
TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

HEMOPRESSIN CNR1

Interaction Score: 2.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18077343

Sources:
DTC
RIMONABANT CNR1

Interaction Score: 1.98

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Rimonabant

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
23357307 8636122 18712856 19530697 11752352 18585913 26203658

Sources:
TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology
DRONABINOL CNR1

Interaction Score: 1.65

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Sativex

Novel drug target Established target

Mechanism of Interaction Cannabinoid CB1 receptor agonist

PMIDs:
12686391 11204352 11752352 17139284 17016423 15894066

Sources:
NCI TdgClinicalTrial DrugBank ChemblInteractions
AMAUROMINE CNR1

Interaction Score: 1.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AZD2207 CNR1

Interaction Score: 1.32

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

IBIPINABANT CNR1

Interaction Score: 1.32

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Direct Interaction yes

Details of the Assay for Interaction Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

TEBIPENEM CNR1

Interaction Score: 1.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
N-[6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-YL]-4,4,4-TRIFLUORO-3-HYDROXYBUTANAMIDE (DIASTEREOMERIC MIX) CNR1

Interaction Score: 1.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20423086

Sources:
DTC
CHEMBL3186422 CNR1

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16406364

Sources:
DrugBank
Z160 CNR1

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19815411

Sources:
DTC
SAD448 CNR1

Interaction Score: 0.66

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL561013 CNR1

Interaction Score: 0.66

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL1354658 CNR1

Interaction Score: 0.66

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology
NONABINE CNR1

Interaction Score: 0.66

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OLORINAB CNR1

Interaction Score: 0.66

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Details of the Assay for Interaction In a DiscoverX PathHunter β-arrestin recruitment assay.

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
LENABASUM CNR1

Interaction Score: 0.44

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
2-ARACHIDONOYLGLYCEROL CNR1

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17110113

Sources:
DTC
CANNABINOL CNR1

Interaction Score: 0.44

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
TETRAHYDROCANNABIVARIN CNR1

Interaction Score: 0.38

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
28120232

Sources:
DrugBank
PROPACETAMOL CNR1

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
CONATUMUMAB CNR1

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CP-55940 CNR1

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17027269

Sources:
DTC
WIN-552122 CNR1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18579386 17027269

Sources:
DTC
ORLISTAT CNR1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CANNABIDIOL CNR1

Interaction Score: 0.12

Interaction Types & Directionality:

allosteric modulator

antagonist (inhibitory)

modulator

Interaction Info:

Specific Action of the Ligand Negative

Endogenous Drug? False

Direct Interaction? False

PMIDs:
26218440

Sources:
DrugBank GuideToPharmacology ChemblInteractions
QUETIAPINE CNR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23799528 20107430 20631561

Sources:
PharmGKB
ARIPIPRAZOLE CNR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23799528 20107430 20631561

Sources:
PharmGKB
DEXANABINOL CNR1

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
ANANDAMIDE CNR1

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? True

PMIDs:
None found

Sources:
GuideToPharmacology
RISPERIDONE CNR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23799528 20107430 20631561

Sources:
PharmGKB
OLANZAPINE CNR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23799528 20107430 20631561

Sources:
PharmGKB
HALOPERIDOL CNR1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23799528 20107430 20631561

Sources:
PharmGKB
CLOZAPINE CNR1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23799528 20107430 20631561

Sources:
PharmGKB
NABIXIMOLS CNR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26218440

Sources:
DrugBank
COCAINE CNR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

Ensembl: ENSG00000118432
- Version: 101_38
Alternate Names:

CNR1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P21554
- Version: 11-September-2012
Alternate Names:

CNR1 Uniprot Gene Name

1268 Entrez Gene Id

ENSG00000118432 Ensembl Gene Id

Gene Info:

Interpro Acc IPR000276

Interpro Name GPCR, rhodopsin-like, 7TM

Human Readable Name DRUGGABLE GENOME

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P21554
- Version: 01-August-2011
Alternate Names:

1268 Entrez Gene Id

ENSG00000118432 Ensembl Gene Id

CNR1_HUMAN Uniprot Id

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
RussLampel: ENSG00000118432
- Version: 26-July-2011
Alternate Names:

CNR1 Display Id

ENSG00000118432 Ensembl Gene Id

CANNABINOID RECEPTOR 1 (CB1) (CB-R) (CANN6). [SOURCE:UNIPROT/SWISSPROT;ACC:P21554] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P21554
- Version: January-2014
Alternate Names:

CNR1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
GuideToPharmacology: 1268
- Version: 29-September-2020
Alternate Names:

2159 HUGO Gene ID

2159 HUGO Gene Symbol

cannabinoid receptor 1 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Cannabinoid receptors

GuideToPharmacology Gene Category ID 13

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

PharmGKB: CNR1

Version: 18-August-2020

Alternate Names:

PA26681 PharmGKB ID

Gene Info:

Publications:

Nurmi EL et al., 2013, Moderation of antipsychotic-induced weight gain by energy balance gene variants in the RUPP autism network risperidone studies., Transl Psychiatry

Tiwari AK et al., 2010, A common polymorphism in the cannabinoid receptor 1 (CNR1) gene is associated with antipsychotic-induced weight gain in Schizophrenia., Neuropsychopharmacology

Monteleone P et al., 2010, Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain., J Clin Psychopharmacol

DrugBank: BE0000061

Version: 5.1.7

Alternate Names:

CNR1 DrugBank Gene Name

P21554 UniProt Accession

1268 Entrez Gene Id

Gene Info:

Publications:

Pryce et al., 2003, Mifepristone or inhibition of 11beta-hydroxylase activity potentiates the sedating effects of the cannabinoid receptor-1 agonist Delta(9)-tetrahydrocannabinol in mice., Neurosci. Lett.

Tsai et al., 2000, Association study of a cannabinoid receptor gene (CNR1) polymorphism and schizophrenia., Psychiatr. Genet.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

NCI: CNR1
- Version: 14-September-2017
Alternate Names:

Gene Info:

Publications:

Gorriti et al., 2005, Acute delta9-tetrahydrocannabinol exposure facilitates quinpirole-induced hyperlocomotion., Pharmacol. Biochem. Behav.

DTC: CNR1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Heimann AS et al., 2007, Hemopressin is an inverse agonist of CB1 cannabinoid receptors., Proc Natl Acad Sci U S A

Yan L et al., 2010, Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity., J Med Chem

Wu CH et al., 2009, Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice., J Med Chem

HingoraniCasas: ENSG00000118432
- Version: 31-May-2017
Alternate Names:

ENSG00000118432 Gene Symbol

CNR1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: CNR
- Version: chembl_23
Alternate Names:

CNR GENE_SYMBOL

CNR1 GENE_SYMBOL

Cannabinoid receptor 1 UNIPROT

Gene Info:

Publications:
Pharos: CNR1
- Version: 03-September-2020
Alternate Names:

Cannabinoid receptor 1 Gene Name

P21554 UniProt ID

Gene Info:

Gene Categories:

KINASE, ENZYME

Publications:
GO: CNR1
- Version: 05-September-2020
Alternate Names:

CNR GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, G PROTEIN COUPLED RECEPTOR

Publications:
dGene: CNR1
- Version: 27-Jun-2013
Alternate Names:

1268 Gene ID

CANN6 dGene Synonym

CB-R dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Cannabinoid receptor 1
- Version: 2020.06.01
Alternate Names:

CB1 TTD Gene Abbreviation

T76685 TTD Target ID

Gene Info:

Publications:

Specific Action of the Ligand	Agonist
Endogenous Drug?	False
Direct Interaction?	False

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inverse agonist

Direct Interaction	yes
Mechanism of Interaction	Cannabinoid CB1 receptor antagonist
Novel drug target	Established target

Trial Name	Rimonabant
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Trial Name	Sativex
Novel drug target	Established target
Mechanism of Interaction	Cannabinoid CB1 receptor agonist

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False
Direct Interaction?	False

Details of the Assay for Interaction	In a DiscoverX PathHunter β-arrestin recruitment assay.
Specific Action of the Ligand	Agonist
Endogenous Drug?	False

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False
Direct Interaction?	False

Specific Action of the Ligand	Negative
Endogenous Drug?	False
Direct Interaction?	False

CNR1	Uniprot Gene Name
1268	Entrez Gene Id
ENSG00000118432	Ensembl Gene Id

partial agonist (activating)
agonist (activating)

CNR1	Display Id
ENSG00000118432	Ensembl Gene Id
CANNABINOID RECEPTOR 1 (CB1) (CB-R) (CANN6). [SOURCE:UNIPROT/SWISSPROT;ACC:P21554]	Description

2159	HUGO Gene ID
2159	HUGO Gene Symbol
cannabinoid receptor 1	HUGO Gene Name

CNR1	DrugBank Gene Name
P21554	UniProt Accession
1268	Entrez Gene Id

CNR1 Gene Record

CNR1 1268 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Specific Action of the Ligand Agonist Endogenous Drug? False Direct Interaction? False

PMIDs: 11698062 8981483 10575283 11752352 8864542 17139494

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: None found

Sources: TEND TdgClinicalTrial TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inverse agonist

PMIDs: None found

Sources: DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cannabinoid CB1 receptor antagonist Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality: inverse agonist (inhibitory) antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Inverse agonist Details of the Assay for Interaction Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting.

PMIDs: 20423086

Sources: DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19530697

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17110113

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Cannabinoid CB1 receptor antagonist Direct Interaction yes Details of the Assay for Interaction Inhibition of [3H]CP-55940 binding to human cannabinoid receptor 1 expressed in CHO cells

PMIDs: None found

Sources: TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18077343

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Rimonabant Novel drug target Established target Specific Action of the Ligand Antagonist

PMIDs: 23357307 8636122 18712856 19530697 11752352 18585913 26203658

Sources: TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name Sativex Novel drug target Established target Mechanism of Interaction Cannabinoid CB1 receptor agonist

PMIDs: 12686391 11204352 11752352 17139284 17016423 15894066

Sources: NCI TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Cannabinoid CB1 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Cannabinoid CB1 receptor antagonist Direct Interaction yes Details of the Assay for Interaction Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20423086

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16406364

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19815411

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Cannabinoid CB1 receptor agonist Direct Interaction yes

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
11698062 8981483 10575283 11752352 8864542 17139494

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TEND TdgClinicalTrial TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

Details of the Assay for Interaction Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting.

PMIDs:
20423086

Sources:
DTC TdgClinicalTrial GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
19530697

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17110113

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Direct Interaction yes

Details of the Assay for Interaction Inhibition of [3H]CP-55940 binding to human cannabinoid receptor 1 expressed in CHO cells

PMIDs:
None found

Sources:
TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
18077343

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Rimonabant

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
23357307 8636122 18712856 19530697 11752352 18585913 26203658

Sources:
TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Sativex

Novel drug target Established target

Mechanism of Interaction Cannabinoid CB1 receptor agonist

PMIDs:
12686391 11204352 11752352 17139284 17016423 15894066

Sources:
NCI TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor antagonist

Direct Interaction yes

Details of the Assay for Interaction Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
20423086

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
16406364

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
19815411

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Cannabinoid CB1 receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions