Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL173031 (LY-233053, LY-235723) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]