SIB-1893 [Ligand Id: 1432] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL88612 (SIB-1893)
  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • Luciferin 4-monooxygenase in Photinus pyralis [ChEMBL: CHEMBL5567] [UniProtKB: P08659]
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
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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 6.46 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]