ChEMBL ligand: CHEMBL420311
CD38/Lymphocyte differentiation antigen CD38 in Human [ChEMBL: CHEMBL4660] [GtoPdb: 2766] [UniProtKB: P28907] There should be some charts here, you may need to enable JavaScript!
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6] There should be some charts here, you may need to enable JavaScript!
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] There should be some charts here, you may need to enable JavaScript!
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7] 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
CD38/Lymphocyte differentiation antigen CD38 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4660] [GtoPdb: 2766] [UniProtKB: P28907]
ChEMBL	Inhibitory activity against pig brain NAD glycohydrolase (NADase) by radiochemical Nicotinamide release assay	B	4	pIC50	>100000	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
ChEMBL	Uncompetitive inhibition of His6-tagged SIRT1 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant measured every 2 mins for 30 mins in presence of NAD+ and ATP by FLucK549Ac based Michaelis-Menten analysis	B	6.94	pKi	114	nM	Ki	J Med Chem (2021) 64: 5838-5849 [PMID:33876629]
ChEMBL	Inhibitory activity against recombinant human SIRT1 expressed in Escherichia coli by fluorimetric assay	B	4	pIC50	>100000	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
ChEMBL	Inhibition of recombinant human N-tagged GST-SIRT1 fusion protein using fluorescent ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay	B	4.01	pIC50	98000	nM	IC50	Medchemcomm (2012) 3: 373-378 [PMID:24340169]
ChEMBL	Inhibition of SIRT1 by high throughput screening assay	B	5.82	pIC50	1500	nM	IC50	J Med Chem (2011) 54: 417-432 [PMID:21080630]
ChEMBL	Inhibition of SIRT1 using p53-based 18mer as substrate	B	5.89	pIC50	1300	nM	IC50	J Med Chem (2011) 54: 417-432 [PMID:21080630]
ChEMBL	Inhibitory activity against human SIRT1 by radiochemical Nicotinamide release assay	B	5.89	pIC50	1290	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
ChEMBL	Inhibition of human recombinant His-tagged full-length Sirt1 expressed in Escherichia coli BL21 DE3 Rosetta2 using acetyl-p53-peptide as substrate by coupled deacetylation assay	B	6	pIC50	1000	nM	IC50	J Med Chem (2018) 61: 10922-10928 [PMID:30395713]
ChEMBL	Inhibition of recombinant human SIRT1 (193 to 741 residues) expressed in Escherichia coli expression system using RHKK(Ac)W-NH2 as substrate measured after 2 hrs by HPLC method	B	6.16	pIC50	690	nM	IC50	Eur J Med Chem (2020) 202: 112561-112561 [PMID:32711231]
ChEMBL	Inhibition of His-tagged human recombinant SIRT1 expressed in Escherichia coli using Cbz-Lys(Ac)-AMC as substrate by fluorescence assay	B	6.3	pIC50	500	nM	IC50	Bioorg Med Chem Lett (2015) 25: 2514-2518 [PMID:25971769]
ChEMBL	Inhibition of human recombinant SIRT1 assessed as deacetylation of N-acetyl lysine residue in p53 (317 to 320) after 30 mins by luciferase-mediated luminescence assay	B	6.48	pIC50	330	nM	IC50	Eur J Med Chem (2015) 92: 145-155 [PMID:25549554]
ChEMBL	Inhibition of human recombinant SIRT1 using p53 (379 to 382 residues) conjugated to AMC as substrate incubated for 45 mins in presence of NAD+ by fluorescence assay	B	6.52	pIC50	300	nM	IC50	Medchemcomm (2019) 10: 2140-2145 [PMID:32904142]
ChEMBL	Inhibition of human recombinant SIRT1 using AMC-p53 (379 to 382 residues) as substrate incubated for 45 mins followed by NAD+ addition measured after 30 mins by fluorescence assay	B	6.52	pIC50	300	nM	IC50	Medchemcomm (2016) 7: 2094-2099
ChEMBL	Inhibition of SIRT1	B	6.55	pIC50	280	nM	IC50	Bioorg Med Chem Lett (2007) 17: 2448-2451 [PMID:17329104]
ChEMBL	Inhibition of recombinant SIRT1 preincubated for 5 mins before addition of substrate measured after 1 hr by fluorescence-based assay	B	6.55	pIC50	280	nM	IC50	J Med Chem (2009) 52: 2153-2156 [PMID:19296597]
ChEMBL	Inhibition of His-tagged SIRT1 (1 to 747) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after 30 mins by mass spectrophotometric analysis	B	6.59	pIC50	260	nM	IC50	J Med Chem (2013) 56: 3666-3679 [PMID:23570514]
ChEMBL	Inhibition of recombinant human N-terminal GST-tagged SIRT1 (193 to 741 residues) using human p53 derived peptides as substrate incubated for 45 mins by fluorescence assay	B	6.6	pIC50	250	nM	IC50	Medchemcomm (2015) 6: 1857-1863
ChEMBL	Inhibition of full length human SIRT1 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay	B	6.68	pIC50	210	nM	IC50	J Med Chem (2014) 57: 8340-8357 [PMID:25275824]
ChEMBL	Inhibition of human recombinant SIRT1 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay	B	6.8	pIC50	160	nM	IC50	J Med Chem (2012) 55: 8193-8197 [PMID:22931526]
ChEMBL	Inhibition of human N-terminal His-tagged SIRT1 (183 to 664 residues) expressed in Escherichia coli using Ac-Tyr-Lys-Leu-Lys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins in presence of NAD+ by fluorescence assay	B	6.85	pIC50	140	nM	IC50	Eur J Med Chem (2020) 192: 112201-112201 [PMID:32163813]
ChEMBL	Inhibition of SIRT1 (unknown origin)	B	6.89	pIC50	130	nM	IC50	Eur J Med Chem (2017) 134: 230-241 [PMID:28415012]
ChEMBL	Inhibitory activity against recombinant human SIRT1 expressed in Escherichia coli by fluorimetric assay	B	6.91	pIC50	123	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
ChEMBL	Inhibition of N-terminal His-tagged recombinant human SIRT-1 expressed in Escherichia coli using Fluor-de-Lys-SIRT1 as substrate after 15 mins by fluorescence assay	B	7	pIC50	100	nM	IC50	J Med Chem (2017) 60: 4714-4733 [PMID:28475330]
ChEMBL	Inhibition of SIRT1 using Ac-His-Arg-Lys-Lys(Ac)-AMC as substrate	B	7	pIC50	100	nM	IC50	J Med Chem (2011) 54: 417-432 [PMID:21080630]
ChEMBL	Inhibition of recombinant SIRT1 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay	B	7	pIC50	100	nM	IC50	ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL	Inhibitory activity against recombinant human SIRT1 expressed in Escherichia coli by fluorimetric assay	B	7.01	pIC50	98	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
ChEMBL	Inhibition of SIRT1	B	7.01	pIC50	98	nM	IC50	J Med Chem (2011) 54: 417-432 [PMID:21080630]
ChEMBL	Inhibition of human SIRT1 deacetylase activity using acetylated H3K9 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 mins by UV-HPLC analysis	B	7.07	pIC50	85	nM	IC50	J Med Chem (2019) 62: 4131-4141 [PMID:30986062]
ChEMBL	Inhibition of His6-tagged SIRT1 (unknown origin) expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by NAD+ addition and measured after 30 mins by FLucK529Ac based luminescence assay	B	7.32	pIC50	48	nM	IC50	J Med Chem (2021) 64: 5838-5849 [PMID:33876629]
GtoPdb	-	-	7.42	pIC50	38	nM	IC50	Mol Cell Biol (2006) 26: 28-38 [PMID:16354677]
ChEMBL	Inhibition of human recombinant GST-tagged SIRT1 expressed in 293T cells by Fluor de Lys fluorescence assay	B	7.42	pIC50	38	nM	IC50	Bioorg Med Chem (2011) 19: 3616-3624 [PMID:21306906]
ChEMBL	Inhibition of human N-terminal His-tagged SIRT1 (183 to 664 residues) expressed in Escherichia coli using Ac-Arg-Leu-Ile-Lys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins in presence of NAD+ by fluorescence assay	B	8.22	pIC50	6	nM	IC50	Eur J Med Chem (2020) 192: 112201-112201 [PMID:32163813]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL	Inhibition of human recombinant SIRT2 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay	B	4.31	pIC50	48500	nM	IC50	J Med Chem (2012) 55: 8193-8197 [PMID:22931526]
ChEMBL	Inhibition of recombinant human C-terminal His-tagged SIRT2 (13 to 319 residues) using human p53 derived peptides as substrate incubated for 45 mins by fluorescence assay	B	4.36	pIC50	43700	nM	IC50	Medchemcomm (2015) 6: 1857-1863
ChEMBL	Inhibition of N-terminal His-tagged recombinant human SIRT-2 expressed in Escherichia coli using Fluor-de-Lys-SIRT1 as substrate after 15 mins by fluorescence assay	B	4.7	pIC50	20100	nM	IC50	J Med Chem (2017) 60: 4714-4733 [PMID:28475330]
ChEMBL	Inhibition of recombinant SIRT2 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay	B	4.7	pIC50	20000	nM	IC50	ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL	Inhibition of SIRT2	B	4.7	pIC50	20000	nM	IC50	J Med Chem (2011) 54: 417-432 [PMID:21080630]
ChEMBL	Inhibition of recombinant human full length SIRT2 using fluorescent ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay	B	4.71	pIC50	19600	nM	IC50	Medchemcomm (2012) 3: 373-378 [PMID:24340169]
ChEMBL	Inhibitory activity against recombinant human SIRT2 expressed in Escherichia coli by fluorimetric assay	B	4.71	pIC50	19600	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
ChEMBL	Inhibition of human recombinant GST-tagged SIRT2 by Fluor de Lys fluorescence assay	B	4.71	pIC50	19600	nM	IC50	Bioorg Med Chem (2011) 19: 3616-3624 [PMID:21306906]
ChEMBL	Inhibition of SIRT2	B	4.85	pIC50	14000	nM	IC50	Bioorg Med Chem Lett (2007) 17: 2448-2451 [PMID:17329104]
ChEMBL	Inhibition of recombinant SIRT2 preincubated for 5 mins before addition of substrate measured after 3 hrs by fluorescence-based assay	B	4.85	pIC50	14000	nM	IC50	J Med Chem (2009) 52: 2153-2156 [PMID:19296597]
ChEMBL	Inhibition of His-tagged human recombinant SIRT2 expressed in Escherichia coli using Cbz-Lys(Ac)-AMC as substrate by fluorescence assay	B	5.19	pIC50	6500	nM	IC50	Bioorg Med Chem Lett (2015) 25: 2514-2518 [PMID:25971769]
ChEMBL	Inhibition of human N-terminal His-tagged SIRT2 (56 to 356 residues) expressed in Escherichia coli using Ac-Ser-Ser-Ile-Lys(De)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins in presence of NAD+ by fluorescence assay	B	5.28	pIC50	5240	nM	IC50	Eur J Med Chem (2020) 192: 112201-112201 [PMID:32163813]
ChEMBL	Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrate addition measured after 30 mins by mass spectrophotometric analysis	B	5.54	pIC50	2900	nM	IC50	J Med Chem (2013) 56: 3666-3679 [PMID:23570514]
ChEMBL	Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay	B	5.71	pIC50	1940	nM	IC50	J Med Chem (2014) 57: 8340-8357 [PMID:25275824]
ChEMBL	Inhibition of recombinant human N-terminal His6-tagged/SUMO-fused SIRT2 (38 to 356 residues) expressed in Escherichia coli BL21 assessed as reduction in deacetylase activity using acetylated H3K9 as substrate preincubated for 15 mins followed by substrate addition and measured after 6 mins by UV-HPLC analysis	B	5.74	pIC50	1800	nM	IC50	J Med Chem (2019) 62: 4131-4141 [PMID:30986062]
ChEMBL	Inhibition of recombinant human SIRT2 expressed in baculovirus infected SF9 cells expression system using RHKK(Ac)W-NH2 as substrate measured after 20 mins by HPLC method	B	5.82	pIC50	1500	nM	IC50	Eur J Med Chem (2020) 202: 112561-112561 [PMID:32711231]
ChEMBL	Inhibition of human N-terminal His-tagged SIRT2 (56 to 356 residues) expressed in Escherichia coli using Ac-Arg-Leu-Ile-Lys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins in presence of NAD+ by fluorescence assay	B	5.85	pIC50	1420	nM	IC50	Eur J Med Chem (2020) 192: 112201-112201 [PMID:32163813]
ChEMBL	Inhibition of SIRT-2 in human NCI-H460 cells assessed as inhibition of p53 deacetylation after 6 hrs by immunoprecipitation/immunoblotting analysis	B	6	pIC50	1000	nM	IC50	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of His6-tagged/TEV fused SIRT2 (unknown origin) expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by NAD+ addition and measured after 30 mins by FLucK529Ac based luminescence assay	B	6.3	pIC50	500	nM	IC50	J Med Chem (2021) 64: 5838-5849 [PMID:33876629]
ChEMBL	Inhibition of recombinant human N-terminal His6-tagged SIRT-2 expressed in Escherichia coli using p53-K382-(Ac) as substrate after 45 mins by fluorimetric analysis	B	7.01	pIC50	98	nM	IC50	Medchemcomm (2012) 3: 135-161
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
ChEMBL	Inhibition of catalytically active human SIRT3 (102 to 399 amino acids) expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay	B	3.89	pIC50	128000	nM	IC50	J Med Chem (2014) 57: 8340-8357 [PMID:25275824]
ChEMBL	Inhibition of human N-terminal His-tagged SIRT3 (122 to 391 residues) expressed in Escherichia coli using Ac-Arg-Leu-Ile-Lys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins in presence of NAD+ by fluorescence assay	B	4.09	pIC50	82100	nM	IC50	Eur J Med Chem (2020) 192: 112201-112201 [PMID:32163813]
ChEMBL	Inhibition of human His-tagged SIRT3 (102 to 399) expressed in Escherichia coli BL21(DE3) assessed as inhibition of deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after 30 mins by mass spectrophotometric analysis	B	4.3	pIC50	>50000	nM	IC50	J Med Chem (2013) 56: 3666-3679 [PMID:23570514]
ChEMBL	Inhibition of recombinant SIRT3 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay	B	4.31	pIC50	49000	nM	IC50	ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL	Inhibitory activity against recombinant human SIRT3 expressed in Escherichia coli by fluorimetric assay	B	4.31	pIC50	48700	nM	IC50	J Med Chem (2005) 48: 8045-8054 [PMID:16335928]
ChEMBL	Inhibition of human N-terminal His-tagged SIRT3 (122 to 391 residues) expressed in Escherichia coli using Ac-Tyr-Lys-Leu-Lys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins in presence of NAD+ by fluorescence assay	B	4.6	pIC50	25400	nM	IC50	Eur J Med Chem (2020) 192: 112201-112201 [PMID:32163813]
ChEMBL	Inhibition of His6-tagged/TEV fused SIRT3 (unknown origin) expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by NAD+ addition and measured after 30 mins by FLucK529Ac based luminescence assay	B	5.19	pIC50	6400	nM	IC50	J Med Chem (2021) 64: 5838-5849 [PMID:33876629]

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]