[3H]strychnine [Ligand Id: 2360] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL227934 (Strychnine)
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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]
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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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  • Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
  • Glycine Receptor (All subtypes) in Rat [GtoPdb: 428]
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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]
Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
GtoPdb - - 8.5 pKd - - - Nature (1987) 328: 215-20 [PMID:3037383];
Neuron (1992) 9: 491-6 [PMID:1326295]
Glycine Receptor (All subtypes) in Rat [GtoPdb: 428]
GtoPdb - - 8.5 pKd - - - Neuron (1992) 9: 491-6 [PMID:1326295]

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]