(-)-methadone [Ligand Id: 1605] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL159659 (Levothyl, Levomethadone, L-polamivet, (-)-methadone, Levometadona, L-methadone, Methadone, l-, (6r)-methadone, D-(-)-methadone, (r)-methadone, Polamivet, Levadone, R-(-)-methadone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Antagonist activity at GluN1/GluN2A receptor (unknown origin) overexpressed in CHO cells assessed as inhibition of Ca2+ flux incubated for 24 hrs in presence of glycine/L-glutamate by FLIPR assay | B | 4.7 | pIC50 | 19952.62 | nM | IC50 | J Med Chem (2025) 68: 5455-5470 [PMID:39999356] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Antagonist activity at GluN1/GluN2B receptor (unknown origin) overexpressed in CHO cells assessed as inhibition of Ca2+ flux incubated for 24 hrs in presence of glycine/L-glutamate by FLIPR assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2025) 68: 5455-5470 [PMID:39999356] |
| GluN1/GluN2C/Ionotropic glutamate receptor NMDA 1/2C in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038504] [GtoPdb: 455, 458] [UniProtKB: Q05586, Q14957] | ||||||||
| ChEMBL | Antagonist activity at GluN1/GluN2C receptor (unknown origin) overexpressed in CHO cells assessed as inhibition of Ca2+ flux incubated for 24 hrs in presence of glycine/L-glutamate by FLIPR assay | B | 5.1 | pIC50 | 7943.28 | nM | IC50 | J Med Chem (2025) 68: 5455-5470 [PMID:39999356] |
| GluN2D/GluN1/Ionotropic glutamate receptor NMDA 1/2D in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038505] [GtoPdb: 459, 455] [UniProtKB: O15399, Q05586] | ||||||||
| ChEMBL | Antagonist activity at GluN1/GluN2D receptor (unknown origin) overexpressed in CHO cells assessed as inhibition of Ca2+ flux incubated for 24 hrs in presence of glycine/L-glutamate by FLIPR assay | B | 4.9 | pIC50 | 12589.25 | nM | IC50 | J Med Chem (2025) 68: 5455-5470 [PMID:39999356] |
| δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 9.2 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL data shown on this page come from version 37:
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]
