BCTC [Ligand Id: 2460] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL441472 |
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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-mediated hydrolysis of [3H]AEA in rat brain membrane | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6806-6809 [PMID:19875281] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
| ChEMBL | Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as decrease in intracellular calcium level | F | 5.35 | pEC50 | 4500 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 6806-6809 [PMID:19875281] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Inhibition of TRPM8 (unknown origin) | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem (2013) 21: 6542-6553 [PMID:24055075] |
| ChEMBL | Antagonist activity at TRPM8 (unknown origin) assessed as reduction in menthol-induced calcium influx | B | 6.32 | pIC50 | 475 | nM | IC50 | J Med Chem (2018) 61: 6140-6152 [PMID:29939028] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108632] [GtoPdb: 500] [UniProtKB: Q8R4D5] | ||||||||
| GtoPdb | Whole-cell voltage-clamp recordings or Ca2+-microfluorimetry in heterologous cells (HEK, CHO, and Xenopus oocytes) expressing TRPM8 | - | 6.1 | pIC50 | 800 | nM | IC50 | Br J Pharmacol (2004) 141: 737-45 [PMID:14757700] |
| ChEMBL | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx by fluorescence-based assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2014) 77: 285-297 [PMID:24484240] |
| ChEMBL | Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of icilin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to icilin stimulation by Fluo-4 AM dye based fluorescence assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2014) 77: 1831-1838 [PMID:25052206] |
| ChEMBL | Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of menthol-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to menthol stimulation by Fluo-4 AM dye based fluorescence assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2014) 77: 1831-1838 [PMID:25052206] |
| ChEMBL | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of menthol-induced intracellular Ca2+ influx by fluorescence-based assay | B | 6.46 | pIC50 | 350 | nM | IC50 | J Nat Prod (2014) 77: 285-297 [PMID:24484240] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455] | ||||||||
| ChEMBL | Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at +80 mV holding potential by whole cell patch-clamp assay | B | 6.32 | pIC50 | 475 | nM | IC50 | J Med Chem (2016) 59: 2179-2191 [PMID:26847872] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Displacement of [3H]MPOU from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method | B | 7.98 | pKi | 10.5 | nM | Ki | J Med Chem (2017) 60: 8246-8252 [PMID:28892388] |
| ChEMBL | Displacement of [3H]RTX from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method | B | 8.36 | pKi | 4.32 | nM | Ki | J Med Chem (2017) 60: 8246-8252 [PMID:28892388] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK cells assessed as inhibition of 10 nM capsaicin-induced calcium uptake by FLIPR assay | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2021) 64: 370-384 [PMID:33385210] |
| ChEMBL | Inhibition of TRPV1 (unknown origin) | B | 7.46 | pIC50 | 34.9 | nM | IC50 | Bioorg Med Chem (2013) 21: 6542-6553 [PMID:24055075] |
| ChEMBL | Inhibition of human vanilloid receptor 1 in HEK293 cells in capsaicin-induced FLIPR assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5513-5519 [PMID:15482915] |
| GtoPdb | - | - | 7.5 | pIC50 | 34.9 | nM | IC50 | Bioorg Med Chem (2013) 21: 6542-53 [PMID:24055075] |
| ChEMBL | Inhibition of human vanilloid receptor 1 in HEK293 cells in pH 5.5-induced FLIPR assay | B | 7.53 | pIC50 | 29.8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5513-5519 [PMID:15482915] |
| ChEMBL | Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced channel activation | B | 7.62 | pIC50 | 24 | nM | IC50 | Eur J Med Chem (2020) 194: 112236-112236 [PMID:32217416] |
| ChEMBL | Antagonist activity at capsaicin-stimulated human TRPV1 receptor in aequorin expressing cells preincubated for 2.5 mins followed by capsaicin addition | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2016) 24: 849-857 [PMID:26795113] |
| ChEMBL | Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence of ATP followed by capsaicin addition by luminescence assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2019) 178: 433-445 [PMID:31202991] |
| ChEMBL | Inhibition of human TRPV1 expressed in HEK293 cells assessed as reduction in capsaicin-induced activity pretreated for 2.5 mins followed by capsaicin addition measured immediately in presence of coelenterazine h | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2018) 26: 4567-4573 [PMID:30093345] |
| ChEMBL | Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced intracellular calcium level preincubated for 2.5 mins followed by capsaicin addition measured for 5 mins by aequorin dye based assay | B | 8.02 | pIC50 | 9.6 | nM | IC50 | Bioorg Med Chem (2018) 26: 845-854 [PMID:29317149] |
| ChEMBL | Displacement of [3H]RTX from human TRPV1 expressed in HEK293 cell membranes after 60 mins by scintillation counting method | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem (2018) 26: 3716-3726 [PMID:29887511] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as decrease in intracellular calcium level | F | 8.17 | pIC50 | 6.7 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6806-6809 [PMID:19875281] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at human recombinant TRPV1 expressed in human 1321N1 cells assessed as inhibition of capsaicin-induced calcium influx by FLIPR assay | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2008) 16: 8516-8525 [PMID:18722778] |
| ChEMBL | Antagonist activity at recombinant human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced activation | B | 8.74 | pIC50 | 1.83 | nM | IC50 | Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay | F | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay | F | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay | F | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to capsaicin stimulation by Fluo-4 AM dye based fluorescence assay | B | 9.74 | pIC50 | 0.18 | nM | IC50 | J Nat Prod (2014) 77: 1831-1838 [PMID:25052206] |
| ChEMBL | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay | B | 9.82 | pIC50 | 0.15 | nM | IC50 | J Nat Prod (2014) 77: 285-297 [PMID:24484240] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line | F | 7.46 | pIC50 | 34.9 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3611-3616 [PMID:14505681] |
| GtoPdb | - | - | 7.5 | pIC50 | - | - | - | J Pharmacol Exp Ther (2003) 306: 377-86 [PMID:12721338] |
| ChEMBL | Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay | B | 8.31 | pIC50 | 4.86 | nM | IC50 | Eur J Med Chem (2013) 66: 193-203 [PMID:23796768] |
| ChEMBL | Vanilloid receptor subtype 1 antagonist activity based on its ability to block low pH-induced activation of the rat VR1 channel in a HEK293 cell line | F | 8.32 | pIC50 | 4.8 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3611-3616 [PMID:14505681] |
| ChEMBL | Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay | B | 8.67 | pIC50 | 2.12 | nM | IC50 | Eur J Med Chem (2013) 66: 193-203 [PMID:23796768] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay | F | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay | F | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay | F | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay | F | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Antagonist activity against acid-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 at pH5 | F | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2006) 49: 3719-3742 [PMID:16759115] |
| ChEMBL | Antagonist activity against capsaicin-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 | F | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2006) 49: 3719-3742 [PMID:16759115] |
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]
