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ChEMBL ligand: CHEMBL3613642 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 receptor expressed in HEK293 cells assessed as inhibition of menthol-stimulated calcium flux after 10 mins | B | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
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 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-stimulated calcium flux after 10 mins | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0] | ||||||||
GtoPdb | - | - | 6.2 | pIC50 | - | - | - | Bioorg Med Chem Lett (2015) 25: 4011-5 [PMID:26235950] |
ChEMBL | Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 20% hypotonic solution-induced Ca2+ influx | B | 6.24 | pIC50 | 570 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
ChEMBL | Antagonist activity at human TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8] | ||||||||
ChEMBL | Antagonist activity at mouse TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins | B | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
GtoPdb | - | - | 6.5 | pIC50 | - | - | - | Bioorg Med Chem Lett (2015) 25: 4011-5 [PMID:26235950] |
ChEMBL | Antagonist activity at mouse TRPV4 receptor expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-stimulated calcium flux after 10 mins | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
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 20% hypotonic solution-induced Ca2+ influx | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
ChEMBL | Antagonist activity at rat TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins | B | 6.18 | pIC50 | 660 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
ChEMBL | Antagonist activity at rat TRPV4 receptor expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-stimulated calcium flux after 10 mins | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
ChEMBL | Antagonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-stimulated calcium flux after 10 mins | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950] |
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]