spermine [Ligand Id: 710] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL23194 (Spermine, NSC-268508)
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 5A/Carbonic anhydrase VA in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1]
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  • carbonic anhydrase 14/Carbonic anhydrase XIV in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
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  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960]
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  • CaS receptor in Human [GtoPdb: 54] [UniProtKB: P41180]
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  • Kir2.1 in Mouse [GtoPdb: 430] [UniProtKB: P35561]
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  • TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
  • TRPM4 in Mouse [GtoPdb: 496] [UniProtKB: Q7TN37]
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  • TRPM5 in Human [GtoPdb: 497] [UniProtKB: Q9NZQ8]
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  • TRPM7 in Rat [GtoPdb: 499] [UniProtKB: Q925B3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23]
ChEMBL Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration method B 4.13 pKi 74000 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration method B 4.08 pKi 84000 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
ChEMBL Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay B 4.08 pKi 84000 nM Ki Bioorg. Med. Chem. (2011) 19: 1381-1389 [PMID:21282059]
carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
ChEMBL Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration method B 8 pKi 10 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
ChEMBL Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration method B 4.88 pKi 13300 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
ChEMBL Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by CO2 hydration stopped-flow assay B 4.88 pKi 13300 nM Ki Bioorg. Med. Chem. (2011) 19: 1381-1389 [PMID:21282059]
carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
ChEMBL Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration method B 6.08 pKi 840 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0]
ChEMBL Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration method B 6.08 pKi 830 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280]
ChEMBL Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration method B 6 pKi 990 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
ChEMBL Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration method B 6.15 pKi 710 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
ChEMBL Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration method B 4.56 pKi 27600 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
ChEMBL Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by CO2 hydration stopped-flow assay B 4.56 pKi 27600 nM Ki Bioorg. Med. Chem. (2011) 19: 1381-1389 [PMID:21282059]
carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1]
ChEMBL Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration method B 4.65 pKi 22600 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
ChEMBL Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration method B 6.07 pKi 860 nM Ki J. Med. Chem. (2010) 53: 5511-5522 [PMID:20590092]
Caspase 2/Caspase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4884] [GtoPdb: 1618] [UniProtKB: P42575]
ChEMBL Activation of procaspase 2 after 24 hrs B 5.07 pEC50 8500 nM EC50 J. Med. Chem. (2008) 51: 2346-2349 [PMID:18366176]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Ability to enhance [3H]MK-801 binding to NMDA receptors in rat forebrain membranes was calculated with respect to spermine B 5.28 pEC50 5200 nM EC50 J. Med. Chem. (1995) 38: 4891-4896 [PMID:8523402]
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455457] [UniProtKB: P35439Q00960]
ChEMBL Positive allosteric modulation of recombinant rat GluN1/GluN2B receptor expressed in xenopus laevis oocyte assessed as potentiation of glycine-induced current response by whole cell voltage clamp method B 4 pEC50 100000 nM EC50 J Med Chem (2017) 60: 5556-5585 [PMID:28586221]
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960]
ChEMBL Positive allosteric modulation of GluN2B receptor in rat spinal cord neurons assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.09 pEC50 81000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
CaS receptor in Human [GtoPdb: 54] [UniProtKB: P41180]
GtoPdb - - 3.5 pKd - - - Am J Physiol (1997) 273: C1315-23 [PMID:9357776]
Kir2.1 in Mouse [GtoPdb: 430] [UniProtKB: P35561]
GtoPdb - - 9.1 pKd - - - Neuron (1995) 14: 1047-54 [PMID:7748552];
J Physiol (Lond.) (1996) 491 ( Pt 2): 367-81 [PMID:8866861]
TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
GtoPdb - - 4.2 pIC50 61000 nM IC50 Pflugers Arch (2004) 448: 70-5 [PMID:14758478]
TRPM4 in Mouse [GtoPdb: 496] [UniProtKB: Q7TN37]
GtoPdb - - 4.5 pIC50 - - - Cell Calcium (2005) 37: 267-78 [PMID:15670874]
TRPM5 in Human [GtoPdb: 497] [UniProtKB: Q9NZQ8]
GtoPdb - - 4.43 pIC50 37000 nM IC50
TRPM7 in Rat [GtoPdb: 499] [UniProtKB: Q925B3]
GtoPdb - - 5.64 pKi 2300 nM Ki J Gen Physiol (2002) 120: 221-35 [PMID:12149283]

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]