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 (2020) |
| 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 (2020) |
| 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 (2020) |
| 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 (2020) |
| 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 (2020) |
| 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 (2020) |
| 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 (2020) |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
