Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
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) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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] |
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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]