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ChEMBL ligand: CHEMBL1086310 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy | B | 4.74 | pIC50 | 18000 | nM | IC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy | B | 4.75 | pIC50 | 17782.79 | nM | IC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 797-800 [PMID:22222037] |
ChEMBL | Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx by FLIPR | F | 5.12 | pIC50 | 7500 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
GtoPdb | Calcium imaging | - | 5.2 | pIC50 | - | - | - | Proc Natl Acad Sci USA (2007) 104: 13525-30 [PMID:17686976] |
ChEMBL | Antagonist activity at human TRPA1 channel assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx | F | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Inhibition of human TRPA1 expressed in HEK293 cells after 10 mins by FLIPR assay | B | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
ChEMBL | Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced increase in calcium influx by fluorescence analysis in presence of 5 uM AITC | B | 5.21 | pIC50 | 6200 | nM | IC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Antagonist activity at human TRPA1 channel assessed as inhibition of formalin-induced intracellular calcium influx | F | 5.28 | pIC50 | 5300 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx by FLIPR | F | 5.31 | pIC50 | 4900 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Antagonist activity at TRPA1 (unknown origin) | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2014) 57: 5129-5140 [PMID:24884675] |
ChEMBL | Antagonist activity at human TRPA1 channel assessed as inhibition of nifedipine-induced intracellular calcium influx | F | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis | F | 5.74 | pIC50 | 1800 | nM | IC50 | Bioorg Med Chem (2012) 20: 1690-1698 [PMID:22325155] |
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 BITC-induced increase in intracellular calcium concentration by Fluo4-AM based fluorometric assay | F | 5.25 | pIC50 | 5600 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 797-800 [PMID:22222037] |
ChEMBL | Antagonist activity at Sprague-Dawley rat TRPA1 expressed in rat DRG neurons assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis | F | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem (2012) 20: 1690-1698 [PMID:22325155] |
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 human TRPM8 channel | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8] | ||||||||
ChEMBL | Antagonist activity at human TRPV3 channel | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0] | ||||||||
ChEMBL | Antagonist activity at human TRPV4 channel | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
ChEMBL | Antagonist activity at human TRPV1 channel | F | 4.7 | pIC50 | >20000 | nM | IC50 | 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]