GSK1331268 [Ligand Id: 6253] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL595759 (GSK1331268) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Antagonist activity at human D2 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay | F | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay | F | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay | F | 5.6 | pKi | 2511.89 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Agonist activity at human mGluR2 expressed in CHO cells co-expressing Ga16 G-protein assessed as glutamate-induced response by FLIPR assay | F | 5.9 | pEC50 | 1258.93 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
| GtoPdb | - | - | 6.9 | pEC50 | 125 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 759-62 [PMID:20005096] |
| ChEMBL | Positive modulation of human mGluR2 expressed in CHO cells co-expressing Ga16 G-protein assessed as glutamate-induced response by FLIPR assay | B | 6.9 | pEC50 | 125.89 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
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]
