arcaine [Ligand Id: 4137] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL102740 (1-(4-Guanidinobutyl)Guanidine, Arcaine)
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  • ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5]
ChEMBL Ability to inhibit MK-801 binding to NMDA receptor in the presence of 100 uM of spermidine was determined B 4.1 pIC50 79980 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 3459-3464 [PMID:9934452]
ChEMBL Ability to inhibit MK-801 binding to the NMDA receptor was determined B 5.04 pIC50 9130 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 3459-3464 [PMID:9934452]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL Displacement of [3H]-ifenprodil from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine B 4.61 pIC50 24400 nM IC50 Bioorg. Med. Chem. (2015) 23: 4489-4500 [PMID:26117647]
ChEMBL Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis B 5.19 pIC50 6390 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 4131-4135 [PMID:26296478]
ChEMBL Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine B 5.34 pIC50 4600 nM IC50 Bioorg. Med. Chem. (2015) 23: 4489-4500 [PMID:26117647]
ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
GtoPdb - - 2.9 pEC50 ~1200000 nM EC50 Mol Pain (2010) 6: 88 [PMID:21143836]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]