VU0361737 [Ligand Id: 3956] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL562551 |
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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 | 6.39 | pIC50 | 406.3 | 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 | Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method | B | 8.29 | pIC50 | 5.13 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3956-3960 [PMID:26231155] |
| ChEMBL | Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method | B | 8.29 | pIC50 | 5.1 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3956-3960 [PMID:26231155] |
| GtoPdb | - | - | 6.6 | pEC50 | 240 | nM | EC50 | J Med Chem (2009) 52: 4115-8 [PMID:19469556] |
| ChEMBL | Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization | F | 6.62 | pEC50 | 240 | nM | EC50 | J Med Chem (2009) 52: 4115-4118 [PMID:19469556] |
| 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 | 6.62 | pEC50 | 240 | 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 | Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis | B | 7.89 | pIC50 | 12.88 | nM | IC50 | J Med Chem (2014) 57: 9130-9138 [PMID:25330258] |
| ChEMBL | Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis | B | 7.89 | pIC50 | 12.8 | nM | IC50 | J Med Chem (2014) 57: 9130-9138 [PMID:25330258] |
| ChEMBL | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux | B | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2009) 52: 4115-4118 [PMID:19469556] |
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]
