RN-9893 [Ligand Id: 10304] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3613642
  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
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  • TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8]
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  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8]
  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Rat [ChEMBL: CHEMBL2775] [GtoPdb: 510] [UniProtKB: Q9ERZ8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]