strychnine [Ligand Id: 347] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL227934 (NSC-5365, Strychnidin-10-one, Strychnine, Strychninum) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| glycine receptor α1 subunit/glycine receptor β subunit/glycine receptor α2 subunit/glycine receptor α3 subunit/Glycine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL3392921] [GtoPdb: 423, 427, 424, 425] [UniProtKB: P07727, P20781, P22771, P24524] | ||||||||
| ChEMBL | DRUGMATRIX: Glycine, Strychnine-Sensitive radioligand binding (ligand: [3H] Strychnine) | B | 8.33 | pKi | 4.69 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Glycine, Strychnine-Sensitive radioligand binding (ligand: [3H] Strychnine) | B | 8.08 | pIC50 | 8.29 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| glycine receptor α1 subunit/glycine receptor β subunit/Glycine receptor (alpha-1/beta) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2363052] [GtoPdb: 423, 427] [UniProtKB: P23415, P48167] | ||||||||
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response by fluorescence-based FLIPR membrane potential blue assay | B | 6.29 | pIC50 | 512.86 | nM | IC50 | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay | B | 6.29 | pIC50 | 512.86 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay | B | 6.29 | pIC50 | 510 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response by fluorescence-based FLIPR membrane potential blue assay | B | 6.29 | pIC50 | 510 | nM | IC50 | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Antagonist activity at recombinant human glycine receptor alpha 1 beta expressed in human tsA201 cells assessed as inhibition of glycine-induced receptor activation after 30 mins by FLIPR membrane potential blue assay | B | 6.74 | pIC50 | 181.97 | nM | IC50 | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| ChEMBL | Antagonist activity at recombinant human glycine receptor alpha 1 beta expressed in human tsA201 cells assessed as inhibition of glycine-induced receptor activation after 30 mins by FLIPR membrane potential blue assay | B | 6.74 | pIC50 | 180 | nM | IC50 | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1beta expressed in HEK293 cells assessed as reduction in glycine-induced currents by whole-cell patch-clamp assay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1beta expressed in HEK293 cells assessed as reduction in glycine-induced whole cell currents by patch-clamp technique | B | 7.24 | pIC50 | 58 | nM | IC50 | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Antagonist activity at recombinant human glycine receptor alpha 1 beta expressed in HEK293 cells assessed as inhibition of glycine-induced current at -50mV holding potential by whole cell patch-clamp method | B | 7.24 | pIC50 | 58 | nM | IC50 | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415] | ||||||||
| ChEMBL | Displacement of [3H]strychnine from human glycine receptor subunit alpha-1 expressed in HEK293 cell membranes | B | 6.91 | pKi | 123 | nM | Ki | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Displacement of [3H]strychnine from recombinant human glycine receptor alpha 1 expressed in HEK293 cell membranes after 30 mins by liquid scintillation counting method | B | 7.64 | pKi | 23 | nM | Ki | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| ChEMBL | Displacement of [3H]strychnine from human glycine receptor subunit alpha-1 expressed in HEK293 cell membranes preincubated for 30 mins followed by [3H]strychnine addition and measured after 30 mins by liquid scintillation counting method | B | 8.3 | pKi | 5 | nM | Ki | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay | B | 6.82 | pIC50 | 151.36 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 expressed in human tsA201 cells assessed as reduction in glycine-induced response by fluorescence-based FLIPR membrane potential blue assay | B | 6.82 | pIC50 | 151.36 | nM | IC50 | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 expressed in human tsA201 cells assessed as reduction in glycine-induced response by fluorescence-based FLIPR membrane potential blue assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 assessed as inhibition of glycine-induced current measured at the onset of compound application by patch-clamp assay | B | 6.87 | pIC50 | 134 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at recombinant human glycine receptor alpha 1 expressed in human tsA201 cells assessed as inhibition of glycine-induced receptor activation after 30 mins by FLIPR membrane potential blue assay | B | 7.03 | pIC50 | 93.33 | nM | IC50 | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| ChEMBL | Antagonist activity at recombinant human glycine receptor alpha 1 expressed in human tsA201 cells assessed as inhibition of glycine-induced receptor activation after 30 mins by FLIPR membrane potential blue assay | B | 7.03 | pIC50 | 93 | nM | IC50 | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 expressed in HEK293 cells assessed as reduction in glycine-induced whole cell currents by patch-clamp technique | B | 7.29 | pIC50 | 51 | nM | IC50 | J Nat Prod (2019) 82: 2332-2336 [PMID:31385511] |
| ChEMBL | Antagonist activity at recombinant human glycine receptor alpha 1 expressed in HEK293 cells assessed as inhibition of glycine-induced current at -50 mV holding potential by whole cell patch-clamp method | B | 7.29 | pIC50 | 51 | nM | IC50 | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 expressed in HEK293 cells assessed as reduction in glycine-induced currents by whole-cell patch-clamp assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| ChEMBL | Antagonist activity at human glycine receptor subunit alpha-1 assessed as inhibition of glycine-induced current measured at the later state of compound application by patch-clamp assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Nat Prod (2021) 84: 382-394 [PMID:33596384] |
| glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3246] [GtoPdb: 423] [UniProtKB: P07727] | ||||||||
| ChEMBL | Displacement of [3H]strychnine from glycine receptor alpha 1 in rat brain synaptic membranes | B | 7.92 | pKi | 12 | nM | Ki | J Nat Prod (2016) 79: 2997-3005 [PMID:27966945] |
| TAS2R10/Taste receptor type 2 member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559704] [GtoPdb: 666] [UniProtKB: Q9NYW0] | ||||||||
| ChEMBL | Activity at human TAS2R10 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay | F | 4.4 | pEC50 | 40000 | nM | EC50 | EP-2267129-B1. Bitter taste receptors (2015) |
| GtoPdb | - | - | 4.48 | pEC50 | 33400 | nM | EC50 | Chem Senses (2010) 35: 157-70 [PMID:20022913] |
| ChEMBL | Activity at human TAS2R10 expressed in HEK293/15 cells assessed as effect on calcium response by FLIPR assay | F | 5.3 | pEC50 | 5000 | nM | EC50 | EP-2267129-B1. Bitter taste receptors (2015) |
| TAS2R46/Taste receptor type 2 member 46 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523253] [GtoPdb: 679] [UniProtKB: P59540] | ||||||||
| ChEMBL | Agonist activity at human TAS2R46 stably expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4-AM dye based FLIPR assay | F | 6.16 | pEC50 | 690 | nM | EC50 | US-8603762-B2. Methods to identify modulators of the interaction between dextromethorphan and the bitter taste receptor TAS2R46 (2013) |
| GtoPdb | - | - | 6.37 | pEC50 | 430 | nM | EC50 | J Agric Food Chem (2007) 55: 6236-43 [PMID:17595105] |
| M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| GtoPdb | - | - | 4.9 | pKd | - | - | - | Mol Pharmacol (1995) 48: 362-78 [PMID:7651370] |
| GtoPdb | - | - | 5 | pKd | - | - | - |
Mol Pharmacol (1995) 48: 362-78 [PMID:7651370]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
| M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| GtoPdb | - | - | 5 | pKd | - | - | - |
Mol Pharmacol (1995) 48: 362-78 [PMID:7651370]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]; Mol Pharmacol (2003) 64: 180-90 [PMID:12815174] |
| M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 5.7 | pKd | - | - | - |
Mol Pharmacol (1995) 48: 362-78 [PMID:7651370]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
| M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| GtoPdb | - | - | 5 | pKd | - | - | - |
Mol Pharmacol (1995) 48: 362-78 [PMID:7651370]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
| M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| GtoPdb | - | - | 3.6 | pKd | - | - | - | Mol Pharmacol (1995) 48: 362-78 [PMID:7651370] |
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]
