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ChEMBL ligand: CHEMBL173031 (LY-233053, LY-235723) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | Tested in vitro for the affinity against NMDA receptor in a cortical wedge assay | B | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 43-48 |
ChEMBL | Tested in vitro for the affinity against NMDA receptor by examining its ability to inhibit [3H]-CGS-19,755 binding | B | 6.97 | pIC50 | 107 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 43-48 |
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 | Compound was tested for the antagonistic activity against depolarizations due to NMDA using rat cortical slice preparation | F | 4.38 | pIC50 | 42000 | nM | IC50 | J Med Chem (1992) 35: 3111-3115 [PMID:1387167] |
ChEMBL | Compound was tested for the antagonistic activity against depolarizations due to NMDA using rat cortical slice preparation | F | 4.41 | pIC50 | 39100 | nM | IC50 | J Med Chem (1992) 35: 3111-3115 [PMID:1387167] |
ChEMBL | Compound was evaluated in vitro in a cortical-wedge preparation for the antagonism of N-methyl-D-aspartate-induced responses | F | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (1991) 34: 90-97 [PMID:1825117] |
ChEMBL | Compound was tested in vitro for its ability to inhibit depolarizations induced by 40 uM NMDA in a cortical slice (NMDA antagonist) | F | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 389-394 [PMID:9871691] |
ChEMBL | Ability to inhibit [3H]-CGS- 19755 binding to NMDA receptor | B | 5.62 | pIC50 | 2393 | nM | IC50 | J Med Chem (1992) 35: 3111-3115 [PMID:1387167] |
ChEMBL | Compound was tested for the antagonistic activity against depolarizations due to NMDA using rat cortical slice preparation | F | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1992) 35: 3111-3115 [PMID:1387167] |
ChEMBL | Ability to inhibit [3H]-CGS- 19755 binding to NMDA receptor | B | 6.97 | pIC50 | 107 | nM | IC50 | J Med Chem (1992) 35: 3111-3115 [PMID:1387167] |
ChEMBL | In vitro binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]CGS-19,755 ligand | B | 6.97 | pIC50 | 107 | nM | IC50 | J Med Chem (1991) 34: 90-97 [PMID:1825117] |
ChEMBL | In vitro compound's ability to displace [3H]-CGS-19,755 binding as a measure of its affinity for the glutamate recognition site on the NMDA receptor complex. | B | 6.97 | pIC50 | 107 | nM | IC50 | J Med Chem (1992) 35: 3547-3560 [PMID:1404235] |
ChEMBL | Ability to inhibit [3H]-CGS- 19755 binding to NMDA receptor | B | 7.17 | pIC50 | 67 | nM | IC50 | J Med Chem (1992) 35: 3111-3115 [PMID:1387167] |
ChEMBL | Compound was tested in vitro for inhibition of binding of [3H]-CGS- 19755 radioligand to NMDA receptor in rat brain membranes | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 389-394 [PMID:9871691] |
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]