cannabidiol [Ligand Id: 4150] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL190461 (CBD, Cannabidiol, BTX-1503, Epidiolex, GWP42003-P, GWP-42003, GWP42003, GWP-42003-P)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
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  • N-Acylethanolamine acid amidase/N-acylsphingosine-amidohydrolase in Human [ChEMBL: CHEMBL4349] [GtoPdb: 1402] [UniProtKB: Q02083]
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  • Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • GPR18 in Human [GtoPdb: 89] [UniProtKB: Q14330]
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  • TRPV2 in Human [GtoPdb: 508] [UniProtKB: Q9Y5S1]
  • TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • TRPV3 in Rat [GtoPdb: 509]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL Inhibition of FAAH in rat brain membranes using [14C]-AEA as substrate measured after 30 mins by scintillation counting method B 4.27 pIC50 53200 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Binding affinity towards cloned human Cannabinoid receptor 1 B 3.64 pKi 3.64 nM Log Ki J. Med. Chem. (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL Binding affinity to human CB1 receptor B 5.36 pKi 4350 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Displacement of [3H]CP-55940 from human cannabinoid CB1 receptor expressed in CHO cells B 5.62 pKi 2400 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]-CP55940 from recombinant human CB1 receptor expressed in Sf9 cell membranes co-expressing Galphai3beta1gamma2 measured after 90 mins by scintillation counting method B 5.84 pKi 1459 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]HU243 from CB1 receptor in Sabra rat brain B 5 pKi >10000 nM Ki J. Med. Chem. (2006) 49: 1113-1117 [PMID:16451075]
ChEMBL Displacement of [3H]-HU-243 from CB1 receptor in Sabra rat brain synaptosomes after 90 mins B 5 pKi >10000 nM Ki ACS Med. Chem. Lett. (2016) 7: 424-428 [PMID:27096053]
ChEMBL Binding affinity for Cannabinoid receptor 1 by the ability to displace radiolabeled CP-55940 from purified rat forebrain synaptosomes B 5.9 pKi 1265 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 3583-3586 [PMID:12443781]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity towards cloned human cannabinoid receptor 2 B 3.46 pKi 3.46 nM Log Ki J. Med. Chem. (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL Displacement of [3H]CP-55940 from human cannabinoid CB2 receptor expressed in CHO cells B 5 pKi 10000 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Binding affinity to human CB2 receptor B 5.54 pKi 2860 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Displacement of [3H]-CP55940 from recombinant human CB2 receptor expressed in Sf9 cell membranes co-expressing Galphai3beta1gamma2 measured after 90 mins by scintillation counting method B 6.43 pKi 372 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Binding affinity for Cannabinoid receptor 2 by the ability to displace radiolabeled CP-55940 from mouse spleen synaptosomes B 6.64 pKi 230 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 3583-3586 [PMID:12443781]
GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6]
GtoPdb - - 6.46 pIC50 350 nM IC50 Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302];
Pharmacol Rev (2010) 62: 588-631 [PMID:21079038]
ChEMBL Binding affinity to GPR55 B 6.35 pEC50 445 nM EC50 J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
N-Acylethanolamine acid amidase/N-acylsphingosine-amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4349] [GtoPdb: 1402] [UniProtKB: Q02083]
ChEMBL Inhibition of recombinant human NAAA expressed in HEK293 cells using [14C]-N-palmitoylethanolamine as substrate measured after 30 mins by beta-counting method B 4 pIC50 >100000 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
ChEMBL Inhibition of recombinant human DAGLalpha expressed in COS7 cells using [14C]-oleoyl-2-arachidonoyl-glycerol as substrate measured after 20 mins by beta-counting method B 4 pIC50 >100000 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
ChEMBL Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx F 7.02 pEC50 96 nM EC50 J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in rat ventricular myocytes F 7 pIC50 100 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles
GPR18 in Human [GtoPdb: 89] [UniProtKB: Q14330]
GtoPdb - - 4.29 pEC50 51100 nM EC50 Br J Pharmacol (2012) 165: 2414-24 [PMID:21595653]
TRPV2 in Human [GtoPdb: 508] [UniProtKB: Q9Y5S1]
GtoPdb - - 4.5 pEC50 31700 nM EC50 J Neurosci (2008) 28: 6231-8 [PMID:18550765]
TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2]
GtoPdb - - 5.43 pEC50 3700 nM EC50 J Neurosci (2008) 28: 6231-8 [PMID:18550765]
TRPV3 in Rat [GtoPdb: 509]
GtoPdb Calcium imaging - 5.43 pEC50 3700 nM EC50 Acta Physiol (Oxf) (2012) 204: 255-66 [PMID:21726418]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]