strychnine [Ligand Id: 347] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL227934 (Strychnine)
There should be some charts here, you may need to enable JavaScript!
  • glycine receptor α1 subunit/glycine receptor β subunit/Glycine receptor (alpha-1/beta) in Human [ChEMBL: CHEMBL2363052] [GtoPdb: 423427] [UniProtKB: P23415P48167]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
There should be some charts here, you may need to enable JavaScript!
  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
There should be some charts here, you may need to enable JavaScript!
  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
There should be some charts here, you may need to enable JavaScript!
  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
There should be some charts here, you may need to enable JavaScript!
  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
There should be some charts here, you may need to enable JavaScript!
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: 423427424425] [UniProtKB: P07727P20781P22771P24524]
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: 423427] [UniProtKB: P23415P48167]
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 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 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]
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]
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 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 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 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 whole cell currents by patch-clamp technique B 7.29 pIC50 51 nM IC50 J Nat Prod (2019) 82: 2332-2336 [PMID:31385511]
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 B 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 B 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]