[3H]strychnine [Ligand Id: 2360] 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 (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) |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
