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

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ChEMBL ligand: CHEMBL227934 (Strychnine)
  • glycine receptor α1 subunit/glycine receptor β subunit/glycine receptor α2 subunit/glycine receptor α3 subunit/Glycine receptor in Rat [ChEMBL: CHEMBL3392921] [GtoPdb: 423427424425] [UniProtKB: P07727P20781P22771P24524]
  • This target only has 1 pki data point
1 CHEMBL227934_lig_chart_1 Glycine receptor Rat
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  • glycine receptor α1 subunit/glycine receptor β subunit/Glycine receptor (alpha-1/beta) in Human [ChEMBL: CHEMBL2363052] [GtoPdb: 423427] [UniProtKB: P23415P48167]
  • This target only has 0 pki data point
2 CHEMBL227934_lig_chart_2 Glycine receptor (alpha-1/beta) Human
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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]
3 CHEMBL227934_lig_chart_3 Glycine receptor subunit alpha-1 HumanRat
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  • M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
  • This target only has 0 pki data point
4 CHEMBL227934_lig_chart_4 M1 receptor Human
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 0 pki data point
5 CHEMBL227934_lig_chart_5 M2 receptor Human
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 0 pki data point
6 CHEMBL227934_lig_chart_6 M3 receptor Human
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 0 pki data point
7 CHEMBL227934_lig_chart_7 M4 receptor Human
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
  • This target only has 0 pki data point
8 CHEMBL227934_lig_chart_8 M5 receptor Human
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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: 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 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]
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 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 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]
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]
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 27:

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]