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 | 35 | nM | IC50 | Bioorg Med Chem Lett (2023) 80: 129101-129101 [PMID:36481449] |
| 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] |
| ChEMBL | Inhibition of human TRPV1 | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649] |
| 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-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 | 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 | 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 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]
