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ChEMBL ligand: CHEMBL573 (Acidum nicotinicum, Niacin, Niacin extended release, Niacin Td, Niacor, Niaspan, Niaspan Er, Niaspan titration starter pack, Nicangin, Nicolar, Nicotinate, Nicotinic acid, NSC-169454, Simcor, Vitamin b3, Wampocap) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Amyloid-beta 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] |
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4] | ||||||||
GtoPdb | - | - | 7.3 | pKd | 50.1 | nM | Kd |
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 | 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 GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127105-127105 [PMID:32199732] |
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 | Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127105-127105 [PMID:32199732] |
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 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 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 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]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 | J Med Chem (2007) 50: 6303-6306 [PMID:17994679] |
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 GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis | F | 5.3 | pEC50 | 5000 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127105-127105 [PMID:32199732] |
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 | 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 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 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 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 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 | 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 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] |
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 GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay | F | 7.75 | pEC50 | 17.6 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
ChEMBL | Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes | B | 7.84 | pEC50 | 14.5 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
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 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]