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ChEMBL ligand: CHEMBL121915 ((S)-5-Iodowillardiine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 1 expressed in HEK293 cells | B | 6.79 | pKi | 163 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flop iGluR1 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 4.47 | pEC50 | 33600 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
ChEMBL | Potency on Ionotropic glutamate receptor AMPA in hippocampal neurons | F | 4.72 | pEC50 | 19200 | nM | EC50 | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 2 expressed in HEK293 cells | B | 6.75 | pKi | 176 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491] | ||||||||
ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR2(R) expressed in Sf9 cells | B | 6.98 | pKi | 105 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492] | ||||||||
ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 expressed in Sf9 cells | B | 6.01 | pKi | 976 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells | B | 6.01 | pKi | 972 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493] | ||||||||
ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR4 expressed in Sf9 cells | B | 6.13 | pKi | 738 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756] | ||||||||
ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260] | ||||||||
ChEMBL | Displacement of [3H]kainic acid from rat recombinant iGluR6(V,C,R) receptor expressed in Sf9 cells | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264] | ||||||||
ChEMBL | Potency on Ionotropic glutamate receptor kainate in dorsal root ganglion cells | F | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
GluK5/Glutamate receptor ionotropic kainate 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478] | ||||||||
ChEMBL | Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 expressed in HEK293 cells | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
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]