suvecaltamide [Ligand Id: 12648] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1684950 (Cx-8998, CX-8998, JZP-385, JZP385, Mk-8998, MK-8998, Suvecaltamide) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Inhibition of CB2 receptor (unknown origin) | B | 5.27 | pIC50 | 5340 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| Cav3.1/Voltage-gated T-type calcium channel alpha-1G subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4641] [GtoPdb: 535] [UniProtKB: O43497] | ||||||||
| ChEMBL | Inhibition of Cav3.1 (unknown origin) at holding potential (Vh) -80 mV and measured by whole-cell voltage-camp assay | B | 7.16 | pIC50 | 69 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| GtoPdb | - | - | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2016) 59: 8398-411 [PMID:27579577] |
| ChEMBL | Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2016) 59: 8398-8411 [PMID:27579577] |
| ChEMBL | Inhibition of CaV 3.1 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2016) 59: 10661-10675 [PMID:27933950] |
| Cav3.2/Voltage-gated T-type calcium channel alpha-1H subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1859] [GtoPdb: 536] [UniProtKB: O95180] | ||||||||
| ChEMBL | Inhibition of Cav3.2 (unknown origin) at holding potential (Vh) -80 mV and measured by whole-cell voltage-camp assay | B | 7.02 | pIC50 | 96 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| ChEMBL | Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay | B | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (2016) 59: 8398-8411 [PMID:27579577] |
| ChEMBL | Inhibition of CaV 3.2 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay | B | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (2016) 59: 10661-10675 [PMID:27933950] |
| GtoPdb | - | - | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (2016) 59: 8398-411 [PMID:27579577] |
| Cav3.3/Voltage-gated T-type calcium channel alpha-1I subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5558] [GtoPdb: 537] [UniProtKB: Q9P0X4] | ||||||||
| ChEMBL | Inhibition of Cav3.3 (unknown origin) at holding potential (Vh) -100 mV and measured by whole-cell voltage-camp assay | B | 5.62 | pIC50 | 2400 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| ChEMBL | Inhibition of Cav3.3 in human HEK293 cells measured under hyperpolarizing conditions by FLIPR assay | B | 6.79 | pIC50 | 161 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| ChEMBL | Inhibition of Cav3.3 (unknown origin) at holding potential (Vh) -80 mV and measured by whole-cell voltage-camp assay | B | 7.08 | pIC50 | 84 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| ChEMBL | Inhibition of Cav3.3 in human HEK293 cells measured by FLIPR assay | B | 8.44 | pIC50 | 3.6 | nM | IC50 | WO-2020072773-A1. Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide (null) |
| GtoPdb | - | - | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2016) 59: 8398-411 [PMID:27579577] |
| ChEMBL | Inhibition of T-type calcium channel Cav3.3 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2016) 59: 8398-8411 [PMID:27579577] |
| ChEMBL | Inhibition of CaV 3.3 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2016) 59: 10661-10675 [PMID:27933950] |
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]
