VU0364770 [Ligand Id: 6234] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL556667 (N-(3-Chlorophenyl)Picolinamide) |
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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 | 6.48 | pIC50 | 333.2 | 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 | Positive allosteric modulator activity at human mGlu4 receptor | B | 5.92 | pEC50 | 1196 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 3956-3960 [PMID:26231155] |
| ChEMBL | Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization | F | 5.96 | pEC50 | 1100 | nM | EC50 | J Med Chem (2009) 52: 4115-4118 [PMID:19469556] |
| ChEMBL | Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay | F | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2641-2646 [PMID:29958762] |
| ChEMBL | Agonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysis | F | 5.96 | pEC50 | 1100 | nM | EC50 | Eur J Med Chem (2022) 237: 114378-114378 [PMID:35462165] |
| GtoPdb | - | - | 6 | pEC50 | 1100 | nM | EC50 | J Pharmacol Exp Ther (2012) 340: 404-21 [PMID:22088953] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Positive allosteric modulator activity at rat mGlu4 receptor | B | 6.48 | pEC50 | 330 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 3956-3960 [PMID:26231155] |
| GtoPdb | - | - | 6.5 | pEC50 | 290 | nM | EC50 | J Pharmacol Exp Ther (2012) 340: 404-21 [PMID:22088953] |
| ChEMBL | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux | B | 6.54 | pEC50 | 290 | 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]
