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ChEMBL ligand: CHEMBL2133556 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871] |
ChEMBL | Antagonist activity at human recombinant TRPV4 expressed in CHO-K1 cells assessed as blockade of 1000 nM 4alphaPDD-induced calcium mobilization by FLIPR assay | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4930-4935 [PMID:27637151] |
ChEMBL | Antagonist activity at human TRPV4 assessed as inhibition of 4alpha-PDD-induced activation | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4936-4941 [PMID:27634196] |
GtoPdb | - | - | 7.3 | pIC50 | 48 | nM | IC50 | Proc Natl Acad Sci USA (2010) 107: 19084-9 [PMID:20956320] |
ChEMBL | Antagonist activity at TRPV4 (unknown origin) | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127022-127022 [PMID:32063431] |
ChEMBL | Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method | B | 7.32 | pIC50 | 48 | nM | IC50 | ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109] |
ChEMBL | Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of hypotonicity-induced activation pretreated for 5 mins followed by hypotonic solution addition measured for 5 mins by FLIPR assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871] |
ChEMBL | Antagonist activity at human TRPV4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264] |
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 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method | B | 7.77 | pIC50 | 17 | nM | IC50 | ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109] |
ChEMBL | Antagonist activity at mouse TRPV4 | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264] |
GtoPdb | - | - | 7.8 | pIC50 | - | - | - | Proc Natl Acad Sci USA (2010) 107: 19084-9 [PMID:20956320] |
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 recombinant rat TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871] |
ChEMBL | Antagonist activity at rat TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method | B | 6.88 | pIC50 | 133 | nM | IC50 | ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109] |
ChEMBL | Antagonist activity at rat TRPV4 | B | 6.88 | pIC50 | 133 | nM | IC50 | Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264] |
GtoPdb | - | - | 6.9 | pIC50 | - | - | - | Proc Natl Acad Sci USA (2010) 107: 19084-9 [PMID:20956320] |
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]