nicotinic acid [Ligand Id: 1588] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL573 (NSC-169454, Niacor, Nicolar, Niaspan Titration Starter Pack, Nicotinic Acid, Niacin Td, Niacin, Niaspan, Niaspan Er, Nicangin, Simcor, Wampocap, Nicotinate)
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  • HCA3 receptor/HM74 nicotinic acid GPCR in Human [ChEMBL: CHEMBL4421] [GtoPdb: 313] [UniProtKB: P49019]
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  • HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
  • HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Mouse [ChEMBL: CHEMBL4420] [GtoPdb: 312] [UniProtKB: Q9EP66]
  • HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Rat [ChEMBL: CHEMBL4731] [GtoPdb: 312] [UniProtKB: Q80Z39]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Beta amyloid A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
ChEMBL Inhibition of amyloid beta aggregation (unknown origin) after 4 hrs by thioflavin S assay in presence of Zn2+ B 4.36 pIC50 43700 nM IC50 J. Med. Chem. (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL Inhibition of amyloid beta aggregation (unknown origin) after 4 hrs by thioflavin S assay in absence of Zn2+ B 4.88 pIC50 13100 nM IC50 J. Med. Chem. (2013) 56: 6775-6791 [PMID:23905680]
HCA3 receptor/HM74 nicotinic acid GPCR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4421] [GtoPdb: 313] [UniProtKB: P49019]
ChEMBL Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay F 4.12 pEC50 75857.76 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 5620-5623 [PMID:17804224]
ChEMBL Agonist activity at human GPR109b F 5 pEC50 >10000 nM EC50 ACS Med. Chem. Lett. (2011) 2: 171-176 [PMID:24900295]
ChEMBL Agonist activity at human GPR109b F 5 pEC50 >10000 nM EC50 ACS Med. Chem. Lett. (2012) 3: 63-68 [PMID:24900372]
GtoPdb - - 6.52 pEC50 - - - J. Biol. Chem. (2003) 278: 9869-74 [PMID:12522134]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
ChEMBL Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin B 6.98 pKi 104 nM Ki J. Med. Chem. (2010) 53: 2666-2670 [PMID:20184326]
ChEMBL Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry B 7.09 pKi 82 nM Ki J. Med. Chem. (2010) 53: 2666-2670 [PMID:20184326]
ChEMBL Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2008) 51: 5101-5108 [PMID:18665582]
ChEMBL Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay F 4.17 pIC50 67300 nM IC50 J. Biol. Chem. (2007) 282: 18028-18036 [PMID:17452318]
ChEMBL Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis B 6.6 pIC50 249 nM IC50 Bioorg. Med. Chem. (2015) 23: 4013-4025 [PMID:25737085]
ChEMBL Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells B 6.82 pIC50 150 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4948-4951 [PMID:18752940]
ChEMBL Displacement of [3H]niacin from human GPR109A B 6.85 pIC50 140 nM IC50 J. Med. Chem. (2007) 50: 6303-6306 [PMID:17994679]
ChEMBL Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4768-4772 [PMID:19592242]
ChEMBL Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4768-4772 [PMID:19592242]
ChEMBL Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3426-3430 [PMID:20444602]
ChEMBL Displacement of [3H]niacin from GRP109A receptor B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3372-3375 [PMID:20452209]
ChEMBL Displacement of [3H]nicotinic acid from human GPR10a receptor B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 4472-4474 [PMID:20615702]
ChEMBL Displacement of [3H]niacin from human GPR109A expressed in CHO cells B 6.85 pIC50 140 nM IC50 J. Med. Chem. (2009) 52: 2587-2602 [PMID:19309152]
ChEMBL Displacement of [3H]niacin from human GPR109A B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6723-6728 [PMID:18029181]
ChEMBL Displacement of [3H]nicotinic acid from human GPR109a receptor B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2121-2124 [PMID:19307116]
ChEMBL Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells B 6.89 pIC50 130 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4963-4967 [PMID:18760600]
ChEMBL Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay F 5.56 pEC50 2754.23 nM EC50 Eur J Med Chem (2018) 152: 208-222 [PMID:29709786]
ChEMBL Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay F 5.56 pEC50 2727 nM EC50 Eur J Med Chem (2018) 152: 208-222 [PMID:29709786]
ChEMBL Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay F 5.85 pEC50 1400 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 4963-4967 [PMID:18760600]
ChEMBL Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serum B 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 3372-3375 [PMID:20452209]
ChEMBL Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 4768-4772 [PMID:19592242]
ChEMBL Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 3426-3430 [PMID:20444602]
ChEMBL Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 4948-4951 [PMID:18752940]
ChEMBL Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay F 6 pEC50 1000 nM EC50 J. Med. Chem. (2009) 52: 2587-2602 [PMID:19309152]
ChEMBL Agonist activity at human GPR106A by [35S]GTPgammaS binding assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 6723-6728 [PMID:18029181]
ChEMBL Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay F 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 5620-5623 [PMID:17804224]
ChEMBL Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay F 6 pEC50 1000 nM EC50 J. Med. Chem. (2007) 50: 6303-6306 [PMID:17994679]
ChEMBL Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay F 6.11 pEC50 780 nM EC50 ACS Med. Chem. Lett. (2012) 3: 637-639 [PMID:24900524]
ChEMBL Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA B 6.24 pEC50 580 nM EC50 J. Biol. Chem. (2007) 282: 18028-18036 [PMID:17452318]
ChEMBL Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay F 6.28 pEC50 527 nM EC50 J. Med. Chem. (2010) 53: 2666-2670 [PMID:20184326]
ChEMBL Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation F 6.92 pEC50 120 nM EC50 J. Med. Chem. (2007) 50: 1445-1448 [PMID:17358052]
ChEMBL Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test F 6.92 pEC50 120 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4914-4919 [PMID:17588745]
ChEMBL Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation F 7 pEC50 100 nM EC50 ACS Med. Chem. Lett. (2011) 2: 171-176 [PMID:24900295]
ChEMBL Agonist activity at human HM74A F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 854-858 [PMID:22209457]
ChEMBL Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation F 7 pEC50 99 nM EC50 ACS Med. Chem. Lett. (2012) 3: 63-68 [PMID:24900372]
GtoPdb - - 7.2 pEC50 63.1 nM EC50 J. Biol. Chem. (2003) 278: 9869-74 [PMID:12522134];
Nat. Med. (2003) 9: 352-5 [PMID:12563315];
Biochem. Biophys. Res. Commun. (2003) 303: 364-9 [PMID:12646212]
ChEMBL Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay F 7.29 pEC50 51 nM EC50 J. Med. Chem. (2012) 55: 3644-3666 [PMID:22435740]
ChEMBL Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA B 7.33 pEC50 47 nM EC50 Bioorg. Med. Chem. (2015) 23: 4013-4025 [PMID:25737085]
ChEMBL Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay F 7.57 pEC50 27 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2797-2800 [PMID:20363624]
ChEMBL Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay F 7.57 pEC50 26.92 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 4207-4209 [PMID:19524438]
ChEMBL Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay F 7.68 pEC50 20.75 nM EC50 Eur J Med Chem (2018) 152: 208-222 [PMID:29709786]
ChEMBL Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay F 7.68 pEC50 20.7 nM EC50 Eur J Med Chem (2018) 152: 208-222 [PMID:29709786]
ChEMBL Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay F 8.06 pEC50 8.71 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 5620-5623 [PMID:17804224]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4420] [GtoPdb: 312] [UniProtKB: Q9EP66]
ChEMBL Displacement of [3H]niacin from mouse GPR109A B 6.85 pIC50 140 nM IC50 J. Med. Chem. (2007) 50: 6303-6306 [PMID:17994679]
ChEMBL Displacement of [3H]nicotinic acid from mouse GPR109a receptor B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2121-2124 [PMID:19307116]
ChEMBL Displacement of [3H]nicotinic acid from mouse GPR10a receptor B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 4472-4474 [PMID:20615702]
ChEMBL Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay F 6.57 pEC50 270 nM EC50 J. Med. Chem. (2007) 50: 6303-6306 [PMID:17994679]
ChEMBL Agonist activity at mouse GPR109a F 7.54 pEC50 29 nM EC50 ACS Med. Chem. Lett. (2011) 2: 171-176 [PMID:24900295]
ChEMBL Agonist activity at mouse GPR109a F 7.54 pEC50 29 nM EC50 ACS Med. Chem. Lett. (2012) 3: 63-68 [PMID:24900372]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4731] [GtoPdb: 312] [UniProtKB: Q80Z39]
ChEMBL Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane. B 7.48 pKi 33 nM Ki J. Med. Chem. (2003) 46: 3945-3951 [PMID:12930155]
ChEMBL Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay F 6.17 pEC50 670 nM EC50 J. Med. Chem. (2009) 52: 2587-2602 [PMID:19309152]
ChEMBL Agonist activity at rat GPR109a F 7.41 pEC50 39 nM EC50 ACS Med. Chem. Lett. (2011) 2: 171-176 [PMID:24900295]
ChEMBL Agonist activity at rat GPR109a F 7.41 pEC50 39 nM EC50 ACS Med. Chem. Lett. (2012) 3: 63-68 [PMID:24900372]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]