compound 11 [PMID: 20638279] [Ligand Id: 6235] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1209431 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 6.11 | pIC50 | 775.2 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
| ChEMBL | Agonist activity at human mGluR4 expressed in CHO-K1 cells | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
| GtoPdb | - | - | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4901-5 [PMID:20638279] |
| ChEMBL | Positive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assay | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
| ChEMBL | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2011) 54: 5070-5081 [PMID:21688779] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Positive allosteric modulation of rat mGluR4 expressed in CHO-K1 cells | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Negative allosteric modulation of human mGluR5 expressed in CHO-K1 cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
| ChEMBL | Positive allosteric modulation of human mGluR5 expressed in CHO-K1 cells | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
| ChEMBL | Agonist activity at human mGluR5 expressed in CHO-K1 cells in absence of glutamate | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| ChEMBL | Negative allosteric modulation of rat mGluR5 expressed in CHO-K1 cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4901-4905 [PMID:20638279] |
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]
