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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  • glycine receptor α1 subunit/glycine receptor β subunit/Glycine receptor (alpha-1/beta) in Human [ChEMBL: CHEMBL2363052] [GtoPdb: 423, 427] [UniProtKB: P23415, P48167]
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  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Rat [ChEMBL: CHEMBL3246] [GtoPdb: 423] [UniProtKB: P07727]
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  • M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
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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 (null)
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 (null)
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 (null)
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]