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| ChEMBL ligand: CHEMBL381055 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| caseinolytic mitochondrial matrix peptidase proteolytic subunit/ATP-dependent Clp protease proteolytic subunit, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523305] [GtoPdb: 3273] [UniProtKB: Q16740] | ||||||||
| ChEMBL | Agonist activity at N-terminal SUMO tagged human ClpP transfected in Escherichia coli assessed as induction of alpha-casein degradation preincubated for 10 mins followed by alpha-casein addition and measured after 2 hrs by brilliant blue staining based SDS-PAGE analysis | B | 4.53 | pEC50 | 29710 | nM | EC50 | J Med Chem (2024) 67: 10622-10642 [PMID:38905539] |
| ChEMBL | Agonist activity at human ClpP using Ac-WLA-AMC as substrate assessed as induction of substrate degradation | B | 5.92 | pEC50 | 1200 | nM | EC50 | J Med Chem (2024) 67: 10622-10642 [PMID:38905539] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | F | 6.7 | pEC50 | 199.53 | nM | EC50 | J Med Chem (2013) 56: 7243-7259 [PMID:23947773] |
| ChEMBL | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | F | 6.7 | pEC50 | 199 | nM | EC50 | J Med Chem (2013) 56: 7243-7259 [PMID:23947773] |
| GtoPdb | - | - | 6.8 | pEC50 | 157 | nM | EC50 | Neuropharmacology (2013) 64: 224-39 [PMID:22884720] |
| ChEMBL | Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay | F | 6.8 | pEC50 | 157 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| GtoPdb | - | - | 5.44 | pKi | 3650 | nM | Ki | Neuropharmacology (2013) 64: 224-39 [PMID:22884720] |
| GtoPdb | - | - | 6.5 | pIC50 | - | - | - | Neuropharmacology (2005) 49 (S1): 252- |
| ChEMBL | Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes | F | 6.77 | pEC50 | 170 | nM | EC50 | J Med Chem (2006) 49: 3332-3344 [PMID:16722652] |
| ChEMBL | Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
| GtoPdb | - | - | 7.26 | pEC50 | 55 | nM | EC50 | Neuropharmacology (2013) 64: 224-39 [PMID:22884720] |
ChEMBL data shown on this page come from version 36:
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]