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Target Report Card

Target Name and Classification

Target ID CHEMBL218
Preferred Name Cannabinoid CB1 receptor
Synonyms CANN6 | CB-R | CB1 | CNR | CNR1 | Cannabinoid receptor 1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > lipid-like ligand receptor (family a gpcr) > cannabinoid receptor

Target Components

Component Description Relationship Accession
Cannabinoid receptor 1 SINGLE PROTEIN P21554

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3301387 Cannabinoid CB1 receptor/orexin receptor 1 complex PROTEIN COMPLEX
CHEMBL3885538 Cannabinoid receptor 1/Mu-type opioid receptor PROTEIN COMPLEX
CHEMBL2096981 Cannabinoid receptor PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL465 DRONABINOL Cannabinoid CB1 receptor agonist 4 DailyMed PubMed
CHEMBL111 RIMONABANT Cannabinoid CB1 receptor antagonist 4 PubMed PubMed PubMed
CHEMBL2218896 NABILONE Cannabinoid CB1 receptor agonist 4 DailyMed
CHEMBL190461 CANNABIDIOL Cannabinoid CB1 receptor negative allosteric modulator 3 PubMed
CHEMBL220360 TARANABANT Cannabinoid CB1 receptor inverse agonist 3 PubMed
CHEMBL562668 OTENABANT Cannabinoid CB1 receptor antagonist 3 PubMed
CHEMBL189676 SURINABANT Cannabinoid CB1 receptor antagonist 2 PubMed
CHEMBL412262 IBIPINABANT Cannabinoid CB1 receptor antagonist 2 PubMed
CHEMBL2106841 NONABINE Cannabinoid CB1 receptor agonist 2 PubMed
CHEMBL3545166 DRINABANT Cannabinoid CB1 receptor antagonist 2 PubMed PubMed
CHEMBL3545289 AZD2207 Cannabinoid CB1 receptor antagonist 2 Other
CHEMBL3545387 SAD448 Cannabinoid CB1 receptor agonist 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000118432
Ensembl ENSG00000118432
GO Cellular Component GO:0005739 (mitochondrion)
GO:0005741 (mitochondrial outer membrane)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030424 (axon)
GO:0030426 (growth cone)
GO:0042734 (presynaptic membrane)
GO:0042995 (cell projection)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0045121 (membrane raft)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004949 (cannabinoid receptor activity)
GO:0005515 (protein binding)
GO:0008144 (drug binding)
GO Biological Process GO:0002866 (positive regulation of acute inflammatory response to antigenic stimulus)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007187 (G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger)
GO:0007188 (adenylate cyclase-modulating G-protein coupled receptor signaling pathway)
GO:0007283 (spermatogenesis)
GO:0007413 (axonal fasciculation)
GO:0007568 (aging)
GO:0007584 (response to nutrient)
GO:0007611 (learning or memory)
GO:0007613 (memory)
GO:0010976 (positive regulation of neuron projection development)
GO:0019216 (regulation of lipid metabolic process)
GO:0019233 (sensory perception of pain)
GO:0031622 (positive regulation of fever generation)
GO:0031999 (negative regulation of fatty acid beta-oxidation)
GO:0032228 (regulation of synaptic transmission, GABAergic)
GO:0032496 (response to lipopolysaccharide)
GO:0033004 (negative regulation of mast cell activation)
GO:0033602 (negative regulation of dopamine secretion)
GO:0035094 (response to nicotine)
GO:0038171 (cannabinoid signaling pathway)
GO:0042220 (response to cocaine)
GO:0042593 (glucose homeostasis)
GO:0043065 (positive regulation of apoptotic process)
GO:0043271 (negative regulation of ion transport)
GO:0043278 (response to morphine)
GO:0045471 (response to ethanol)
GO:0045759 (negative regulation of action potential)
GO:0045776 (negative regulation of blood pressure)
GO:0045777 (positive regulation of blood pressure)
GO:0050796 (regulation of insulin secretion)
GO:0051001 (negative regulation of nitric-oxide synthase activity)
GO:0051966 (regulation of synaptic transmission, glutamatergic)
GO:0060135 (maternal process involved in female pregnancy)
GO:0060259 (regulation of feeding behavior)
GO:0060405 (regulation of penile erection)
GO:0099553 (trans-synaptic signaling by endocannabinoid, modulating synaptic transmission)
Wikipedia Cannabinoid_receptor_type_1

Target Cross References - Protein

canSAR P21554
Human Protein Atlas ENSG00000118432
IntAct P21554
Guide to Pharmacology 56
MICAD NBK23326 (Cannabinoid CB1 receptor)
NBK24613 (Cannabinoid CB1receptors)
NBK47107 (Cannabinoid CB1 receptors)
NBK47334 (Cannabinoid CB1 receptors)
Open Targets ENSG00000118432
PharmGKB PA26681
Pharos P21554 (Tclin)
Reactome R-HSA-373076 (Class A/1 (Rhodopsin-like receptors).)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt B2R9T4 E1P512 P21554 Q13949 Q495Z0 Q4PLI4 Q4VBM6 Q5JVL5 Q5UB37 Q9UNN0

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000810 (Canbinoid_rcpt_1.)
IPR002230 (Cnbnoid_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)

Target Cross References - Structure

PDBe 5TGZ 5U09 5XR8 5XRA