(S)-5-iodowillardiine [Ligand Id: 4071] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL121915 ((S)-5-Iodowillardiine)
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
  • 7.08
1 CHEMBL121915_lig_chart_1 Glutamate receptor ionotropic, AMPA 1 HumanRat
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
  • 6.98
2 CHEMBL121915_lig_chart_2 Glutamate receptor ionotropic, AMPA 2 HumanRat
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  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492]
  • This target only has 1 pki data point
  • 6.01
3 CHEMBL121915_lig_chart_3 Glutamate receptor ionotropic, AMPA 3 Rat
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  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
  • 6.13
4 CHEMBL121915_lig_chart_4 Glutamate receptor ionotropic, AMPA 4 HumanRat
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
  • This target only has 1 pki data point
  • 8.62
5 CHEMBL121915_lig_chart_5 Glutamate receptor ionotropic kainate 1 Rat
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Rat [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
  • This target only has 1 pki data point
  • 4
6 CHEMBL121915_lig_chart_6 Glutamate receptor ionotropic kainate 2 Rat
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  • GluK3/Glutamate receptor ionotropic kainate 3 in Rat [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
  • This target only has 0 pki data point
  • 0
7 CHEMBL121915_lig_chart_7 Glutamate receptor ionotropic kainate 3 Rat
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  • GluK5/Glutamate receptor ionotropic kainate 5 in Human [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478]
  • This target only has 1 pki data point
  • 9.62
8 CHEMBL121915_lig_chart_8 Glutamate receptor ionotropic kainate 5 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]