cannabidiol [Ligand Id: 4150] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL190461 (BTX-1204, BTX-1503, (-)-cannabidiol, Cannabidiol, Cannabidiol solution, Cardiolrx, (-)-cbd, CBD, .delta.1(2)-trans-cannabidiol, Epidiolex, Epidyolex, GWP-42003, GWP42003, GWP-42003-P, GWP42003-P, (-)-trans-cannabidiol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | B | 4.77 | pIC50 | 17070 | nM | IC50 | Eur J Med Chem (2021) 223: 113735-113735 [PMID:34371367] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | Inhibition of alpha2B receptor (unknown origin) | B | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Inhibition of alpha2C receptor (unknown origin) | B | 5.43 | pKi | 3700 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 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-55,940 from human CB1 receptor expressed in CHO cells incubated for 1 hr by liquid scintillation spectrometry | B | 5.36 | pKi | 4350 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 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 | Displacement of [3H]CP55940 from rat brain membrane CB1 receptor assessed as inhibition constant incubated for 90 mins | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2020) 192: 112163-112163 [PMID:32109623] |
| 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]CP-55,940 from human CB2 receptor expressed in CHO cells incubated for 1 hr by liquid scintillation spectrometry | B | 5.54 | pKi | 2860 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 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] |
| ChEMBL | Partial agonist activity at wild type CB2 receptor (unknown origin) expressed in HEK293T assessed as increase in picometer shifts of reflected light wavelengths in presence of JWH-133 by DMR assay | F | 6.2 | pEC50 | 630.96 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V361.35M mutant (unknown origin) expressed in HEK293T assessed as increase in picometer shifts of reflected light wavelengths in presence of JWH-133 by DMR assay | F | 6.2 | pEC50 | 630.96 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V1133.32M mutant (unknown origin) expressed in HEK293T assessed as increase in picometer shifts of reflected light wavelengths by DMR assay | F | 6.2 | pEC50 | 630.96 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at wild type CB2 receptor (unknown origin) expressed in HEK293T assessed as increase in picometer shifts of reflected light wavelengths by DMR assay | F | 6.3 | pEC50 | 501.19 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V1133.32M mutant (unknown origin) expressed in HEK293T assessed as increase in picometer shifts of reflected light wavelengths in presence of JWH-133 by DMR assay | F | 6.4 | pEC50 | 398.11 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Positive allosteric modulation of JWH-133-induced agonist activity at wild type CB2 receptor (unknown origin) stably expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP levels preincubated for 15 mins followed by forskolin addition incubated for 15 mins by HTRF assay | F | 6.6 | pEC50 | 251.19 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at wild type CB2 receptor (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins by HTRF assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at wild type CB2 receptor (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins in presence of JWH-133 by HTRF assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V361.35M mutant (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins in presence of JWH-133 by AlphaScreenSureFire method | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 S2857.39L mutant (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins in presence of JWH-133 by HTRF assay | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V1133.32M mutant (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins in presence of JWH-133 by AlphaScreenSureFire method | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V1133.32M mutant (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins by HTRF assay | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 S2857.39L mutant (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins in presence of JWH-133 by AlphaScreenSureFire method | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V1133.32M mutant (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins in presence of JWH-133 by HTRF assay | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V361.35M mutant (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins in presence of JWH-133 by HTRF assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at wild type CB2 receptor (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins by AlphaScreenSureFire method | F | 7.9 | pEC50 | 12.59 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 V1133.32M mutant (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins by AlphaScreenSureFire method | F | 7.9 | pEC50 | 12.59 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 A2827.36M mutant (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins in presence of JWH-133 by AlphaScreenSureFire method | F | 7.9 | pEC50 | 12.59 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at CBR2 A2827.36M mutant (unknown origin) stably expressed in HEK293T assessed as decrease in forskolin induced cAMP level preincubated for 15 mins followed by forskolin addition incubated for 15 mins in presence of JWH-133 by HTRF assay | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| ChEMBL | Partial agonist activity at wild type CB2 receptor (unknown origin) expressed in HEK293T assessed as increase in ERK1/2 phosphorylation incubated for 7 mins in presence of JWH-133 by AlphaScreenSureFire method | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2021) 64: 9354-9364 [PMID:34161090] |
| 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] |
| Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466] | ||||||||
| ChEMBL | Binding affinity to recombinant human caspase-1 assessed as dissociation constant measured after 90 sec by SPR method | B | 7.73 | pKd | 18.8 | nM | Kd | J Nat Prod (2021) 84: 1563-1572 [PMID:33955754] |
| Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
| ChEMBL | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | B | 6.17 | pIC50 | 670 | nM | IC50 | Eur J Med Chem (2021) 223: 113735-113735 [PMID:34371367] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Inhibition of delta-type opioid receptor receptor (unknown origin) | B | 5.19 | pKi | 6400 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Inhibition of D1 dopamine receptor (unknown origin) | B | 5.57 | pKi | 2700 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 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] |
| Heat sensitive channel TRPV3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879847] [UniProtKB: Q4QYD9] | ||||||||
| ChEMBL | Antagonist activity at rat TRPV3 expressed in HEK293 cells assessed as inhibition of thymol-induced Ca2+ response preincubated for 5 mins followed by thymol addition by Fluo-4AM dye based fluorescence assay | B | 6.12 | pIC50 | 750 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| ChEMBL | Agonist activity at rat TRPV3 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method | B | 6.29 | pEC50 | 510 | nM | EC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| Hemozoin in Plasmodium falciparum (target type: MACROMOLECULE) [ChEMBL: CHEMBL613898] | ||||||||
| ChEMBL | Inhibition of Beta-hematin in Plasmodium falciparum cells assessed as hemozoin formation after 32 hrs by NP40 detergent-mediated assay | B | 4.29 | pIC50 | 51100 | nM | IC50 | Bioorg Med Chem Lett (2021) 54: 128442-128442 [PMID:34763083] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Inhibition of histamine H3 receptor (unknown origin) | B | 5.51 | pKi | 3100 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Inhibition of kappa-type opioid receptor (unknown origin) | B | 5.64 | pKi | 2300 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 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 | 4.62 | pKi | 24000 | nM | Ki | J Nat Prod (2021) 84: 1469-1477 [PMID:33887133] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Inhibition of mu-type opioid receptor (unknown origin) | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| ChEMBL | Negative allosteric modulation of human mu opioid receptor expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of fentanyl | F | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2023) 66: 9466-9494 [PMID:37437224] |
| ChEMBL | Negative allosteric modulation of human mu opioid receptor expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 15 mins in presence of DAMGO | F | 6.51 | pIC50 | 311 | nM | IC50 | J Med Chem (2023) 66: 9466-9494 [PMID:37437224] |
| ChEMBL | Negative allosteric modulation of mu opioid receptor (unknown origin) | B | 4.38 | pEC50 | 41700 | nM | EC50 | J Med Chem (2023) 66: 9466-9494 [PMID:37437224] |
| 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] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 | F | 5.39 | pIC50 | 4100 | nM | IC50 | Bioorg Med Chem Lett (2021) 54: 128442-128442 [PMID:34763083] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1a receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method | B | 5.1 | pEC50 | 8000 | nM | EC50 | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Displacement of [3H] ketanserin from rat 5-HT2aR expressed in mouse NIH/3T3 cells incubated for 30 mins by liquid scintillation counting method | B | 4.49 | pEC50 | 32000 | nM | EC50 | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibition of 5-HT2C (unknown origin) | B | 5.96 | pKi | 1100 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | Inhibition of sigma2 receptor (unknown origin) | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2020) 63: 12137-12155 [PMID:32804502] |
| 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 | Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of allylisothiocyanate-induced Ca2+ response preincubated for 5 mins followed by allylisothiocyanate addition by Fluo-4AM dye based fluorescence assay | B | 6.35 | pIC50 | 450 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| ChEMBL | Agonist activity at rat TRPA1 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of allylisothiocyanate by Fluo-4-AM dye based spectrofluorimetric method | B | 6.32 | pEC50 | 480 | nM | EC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| GtoPdb | - | - | 6.32 | pEC50 | 480 | nM | EC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| 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] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Antagonist activity at TRPM8 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455] | ||||||||
| GtoPdb | - | - | 5.55 | pIC50 | 2800 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| ChEMBL | Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced Ca2+ response preincubated for 5 mins followed by icilin addition by Fluo-4AM dye based fluorescence assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| TRPV2 in Human [GtoPdb: 508] [UniProtKB: Q9Y5S1] | ||||||||
| GtoPdb | - | - | 4.5 | pEC50 | 31700 | nM | EC50 | J Neurosci (2008) 28: 6231-8 [PMID:18550765] |
| TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2] | ||||||||
| ChEMBL | Antagonist activity at rat TRPV2 expressed in HEK293 cells assessed as inhibition of LPC-induced Ca2+ response preincubated for 5 mins followed by LPC addition by Fluo-4AM dye based fluorescence assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| GtoPdb | - | - | 5.43 | pEC50 | 3700 | nM | EC50 | J Neurosci (2008) 28: 6231-8 [PMID:18550765] |
| ChEMBL | Agonist activity at rat TRPV2 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method | B | 5.92 | pEC50 | 1200 | nM | EC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| TRPV4/Transient receptor potential cation channel subfamily V member 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2775] [GtoPdb: 510] [UniProtKB: Q9ERZ8] | ||||||||
| ChEMBL | Antagonist activity at rat TRPV4 expressed in HEK293 cells assessed as inhibition of GSK1016790A-induced Ca2+ response preincubated for 5 mins followed by GSK1016790A addition by Fluo-4AM dye based fluorescence assay | B | 5.23 | pIC50 | 5900 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| ChEMBL | Agonist activity at rat TRPV4 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method | B | 6.05 | pEC50 | 900 | nM | EC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ response preincubated for 5 mins followed by capsaicin addition by Fluo-4AM dye based fluorescence assay | B | 5.43 | pIC50 | 3700 | nM | IC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| ChEMBL | Agonist activity at human TRPV1 overexpressed in HEK293 cells incubated for 1 hr by Fluo-4 AM dye based microscopic analysis | B | 4.41 | pEC50 | 38530 | nM | EC50 | Bioorg Med Chem (2023) 90: 117379-117379 [PMID:37336082] |
| ChEMBL | Agonist activity at human TRPV1 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method | B | 5.39 | pEC50 | 4100 | nM | EC50 | J Nat Prod (2020) 83: 2727-2736 [PMID:32880179] |
| 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] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
