cannabichromene [Ligand Id: 11093] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL422704 (Cannabichromene)
  • 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]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • L-lactate dehydrogenase A chain in Human [ChEMBL: CHEMBL4835] [UniProtKB: P00338]
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  • N-Acylethanolamine acid amidase/N-acylsphingosine-amidohydrolase in Human [ChEMBL: CHEMBL4349] [GtoPdb: 1402] [UniProtKB: Q02083]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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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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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 pIC50 >100000 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 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 6.15 pKi 714 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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 6.59 pKi 257 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
L-lactate dehydrogenase A chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4835] [UniProtKB: P00338]
ChEMBL Non-competitive inhibition of human LDHA assessed as reduction in lactate production using pyruvate as substrate in presence of NADH by Lineweaver-Burk plot analysis B 5.07 pKi 8500 nM Ki J Nat Prod (2021) 84: 1469-1477 [PMID:33887133]
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]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Agonist activity at GAL4-tagged PPARgamma (unknown origin) transiently expressed in HEK293T cells co-transfected with GAL4-tagged luc incubated for 6 hrs by dual luciferase reporter gene assay B 4.6 pEC50 >25000 nM EC50 J Nat Prod (2020) 83: 1711-1715 [PMID:32315173]
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 TRPA1 channel in rat DRG neurons assessed as increase in intracellular calcium influx F 4.46 pEC50 34300 nM EC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
GtoPdb Measuring increase in intracellular calcium influx in HEK293 cells expressing rat TRPA1. - 7.22 pEC50 60 nM EC50 J Med Chem (2010) 53: 5085-107 [PMID:20356305]
ChEMBL Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx F 7.22 pEC50 60 nM EC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]