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ChEMBL ligand: CHEMBL88612 (SIB-1893) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 6.46 | pIC50 | 344.4 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
Luciferin 4-monooxygenase in Photinus pyralis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5567] [UniProtKB: P08659] | ||||||||
ChEMBL | Inhibition of Photinus pyralis luciferase by Steady-Glo reporter gene assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 2372-2386 [PMID:18363348] |
ChEMBL | Inhibition of Photinus pyralis luciferase by BrightGlo reporter gene assay | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2008) 51: 2372-2386 [PMID:18363348] |
ChEMBL | Inhibition of Photinus pyralis luciferase by PK-Light assay | B | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (2008) 51: 2372-2386 [PMID:18363348] |
ChEMBL | Inhibition of Photinus pyralis luciferase by Easy lite assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2008) 51: 2372-2386 [PMID:18363348] |
ChEMBL | Inhibition of Photinus pyralis luciferase | B | 5.37 | pIC50 | 4300 | nM | IC50 | J Med Chem (2008) 51: 2372-2386 [PMID:18363348] |
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
ChEMBL | Agonist potency against cloned human metabotropic glutamate receptor 1 | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
ChEMBL | Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor. | F | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 5390-5401 [PMID:10639281] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
ChEMBL | Antagonist potency against cloned Metabotropic glutamate receptor 2 | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
ChEMBL | Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) | F | 4.59 | pKi | 26000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
GtoPdb | - | - | 6.8 | pEC50 | 150 | nM | EC50 | Br J Pharmacol (2003) 138: 1026-30 [PMID:12684257] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
ChEMBL | Agonist potency against cloned metabotropic glutamate receptor 5 | F | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
ChEMBL | In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated phosphoinositide (PI) hydrolysis | F | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 407-409 [PMID:11814808] |
ChEMBL | Tested in vitro binding affinity for displacement of [3H]M-MPEP from membrane of L(-tk) cells expressing the Metabotropic glutamate receptor 5, activity expressed as IC50 | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 407-409 [PMID:11814808] |
GtoPdb | - | - | 6.5 | pIC50 | - | - | - |
Bioorg Med Chem Lett (2002) 12: 407-9 [PMID:11814808]; J Pharmacol Exp Ther (1999) 290: 170-81 [PMID:10381773] |
ChEMBL | Compound was tested for it's antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5) | F | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (1999) 42: 5390-5401 [PMID:10639281] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
ChEMBL | Inhibition of [3H]MPEP binding to mGluR5 in rat brain membrane | B | 5.97 | pIC50 | 1080 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3371-3375 [PMID:16678408] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6). | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7). | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
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]