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ChEMBL ligand: CHEMBL605836 (GSK1331258) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 5.3 | pKi | 5011.87 | 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 | 5.3 | pKi | 5011.87 | 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 | 6.2 | pKi | 630.96 | 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 | 5.7 | pEC50 | 1995.26 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
GtoPdb | - | - | 7.1 | pEC50 | 80 | 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 | 7.1 | pEC50 | 79.43 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096] |
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]