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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| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
