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)
Beta amyloid A4 protein in Human [ChEMBL: CHEMBL2487] [UniProtKB: P05067] There should be some charts here, you may need to enable JavaScript!
HCA3 receptor/HM74 nicotinic acid GPCR in Human [ChEMBL: CHEMBL4421] [GtoPdb: 313] [UniProtKB: P49019] There should be some charts here, you may need to enable JavaScript!
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] 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]