ChEMBL ligand: CHEMBL566757 (APO 866, APO-866, APO866, Daporinad, FK 866, FK-866, FK866, K 22.175)
histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618] There should be some charts here, you may need to enable JavaScript!
Nicotinamide phosphoribosyltransferase in Human [ChEMBL: CHEMBL1744525] [UniProtKB: P43490] Nicotinamide phosphoribosyltransferase in Mouse [ChEMBL: CHEMBL3259474] [UniProtKB: Q99KQ4] 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
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL	Inhibition of C-terminal 6XHis-tagged/FLAG-tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Boc-Lys-(acetyl)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence analysis	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2024) 266: 116127-116127 [PMID:38224650]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL	Inhibition of C-terminal 6XHis-tagged full length human recombinant HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 cells using Boc-Lys-(acetyl)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence analysis	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2024) 266: 116127-116127 [PMID:38224650]
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618]
ChEMBL	Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489 residues) expressed in baculovirus-infected Sf9 cells using Boc-Lys-(acetyl)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence analysis	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2024) 266: 116127-116127 [PMID:38224650]
Nicotinamide phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744525] [UniProtKB: P43490]
ChEMBL	Displacement of FP-probe ZN-2-102 from C-terminal His6-tagged wild type human NAMPT rear channel assessed as dissociation constant by fluorescence polarization assay	B	8	pKd	10	nM	Kd	J Med Chem (2023) 66: 16704-16727 [PMID:38096366]
ChEMBL	Displacement of fluorescent labelled OG488 from human full length FLAG-tagged NAMPT (1 to 491 residues) expressed in HEK293-6E cells in absence of PRPP by TR-FRET assay	B	8.22	pKi	6	nM	Ki	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Inhibition of C-terminal His-tagged human recombinant NAMPT using FK866 or isoindoline urea-based Oregon green (488) probe incubated for 3 hrs by TR-FRET assay	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2017) 27: 3317-3325 [PMID:28610984]
ChEMBL	Noncompetitive inhibition of NAMPT (unknown origin)	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2013) 56: 6279-6296 [PMID:23679915]
ChEMBL	Inhibition of NAMPT (unknown origin) assessed as inhibition constant	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2024) 67: 8099-8121 [PMID:38722799]
ChEMBL	Binding affinity to NAMPT (unknown origin) assessed as inhibition constant	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2024) 67: 5999-6026 [PMID:38580317]
ChEMBL	Displacement of fluorescent labelled OG488 from human full length FLAG-tagged NAMPT (1 to 491 residues) expressed in HEK293-6E cells in presence of PRPP by TR-FRET assay	B	9.7	pKi	0.2	nM	Ki	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Inhibition of human NAmPRTase by spectrophotometric analysis	B	4.83	pIC50	14800	nM	IC50	Eur J Med Chem (2011) 46: 1153-1164 [PMID:21330015]
ChEMBL	Inhibition of N-terminal GST-tagged human recombinant NAMPT (2 to 491 residues) expressed in Escherichia coli expression system incubated for 30 mins by fluorescence based analysis	B	7.38	pIC50	41.5	nM	IC50	Eur J Med Chem (2024) 266: 116127-116127 [PMID:38224650]
ChEMBL	Inhibition of recombinant human NAMPT incubated for 60 mins by colorimetric assay	B	7.46	pIC50	35	nM	IC50	J Med Chem (2022) 65: 7746-7769 [PMID:35640078]
ChEMBL	Inhibition of recombinant NAMPT (unknown origin) incubated for 60 mins by SpectraMax microplate reader analysis	B	7.47	pIC50	33.7	nM	IC50	J Med Chem (2023) 66: 1027-1047 [PMID:36595482]
ChEMBL	Inhibition of recombinant NAMPT (unknown origin) using nicotinamide as substrate measured every 5 mins for 30 mins in presence of recombinant NMNAT1	B	7.49	pIC50	32	nM	IC50	J Med Chem (2016) 59: 5766-5779 [PMID:27224875]
ChEMBL	Inhibition of NAMPT (unknown origin)	B	7.59	pIC50	25.9	nM	IC50	J Med Chem (2024) 67: 8667-8692 [PMID:38651495]
ChEMBL	Inhibition of recombinant NAMPT (unknown origin) using nicotinamide and pyrophosphate as substrate incubated for 60 mins and measured for 30 mins at 5 mins interval by colorimetric assay	B	7.68	pIC50	20.7	nM	IC50	Eur J Med Chem (2021) 211: 113022-113022 [PMID:33239261]
ChEMBL	Inhibition of recombinant NAMPT (unknown origin) by fluorescence based assay	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2024) 271: 116444-116444 [PMID:38691889]
ChEMBL	Inhibition of NAMPT (unknown origin) using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins in presence of ATP by fluorescence based microplate reader analysis	B	7.92	pIC50	12	nM	IC50	J Med Chem (2023) 66: 1048-1062 [PMID:36563407]
ChEMBL	Inhibition of human recombinant NAMPT using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence assay	B	8.05	pIC50	9	nM	IC50	J Med Chem (2017) 60: 7965-7983 [PMID:28885834]
ChEMBL	Inhibition of NAMPT (unknown origin) using NAM as substrate incubated for 5 mins followed by substrate addition measured after 15 mins by fluorometric method	B	8.05	pIC50	9	nM	IC50	ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808]
ChEMBL	Inhibition of recombinant NAMPT (unknown origin) using NAM and PRPP as substrates incubated for 60 mins in presence of NMNAT1 measured at 5 mins interval for 30 mins by WST1 assay	B	8.17	pIC50	6.8	nM	IC50	Bioorg Med Chem Lett (2019) 29: 1502-1506 [PMID:30992165]
ChEMBL	Inhibition of human full length C-terminal flag/His-tagged NAMPT (1 to 491 residues) expressed in HEK293-6E cells by TR-FRET assay	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2018) 28: 437-440 [PMID:29287958]
ChEMBL	Inhibition of full-length recombinant human NAMPT (2 to 491 residues) expressed in Escherichia coli using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence based assay	B	8.49	pIC50	3.27	nM	IC50	Eur J Med Chem (2023) 250: 115170-115170 [PMID:36787658]
ChEMBL	Inhibition of Nampt (unknown origin) using NAM/PRPP as substrate preincubated for 15 mins measured after 30 mins	B	8.52	pIC50	3	nM	IC50	J Med Chem (2013) 56: 4921-4937 [PMID:23617784]
ChEMBL	Inhibition of C-terminal His-tagged human full-length NAMPT expressed in Escherichia coli Rosetta DE3 using nicotinamide as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins in presence of PRPP	B	8.52	pIC50	3	nM	IC50	J Med Chem (2014) 57: 770-792 [PMID:24405419]
ChEMBL	Inhibition of C-terminal His-tagged NAMPT (unknown origin) expressed in Escherichia coli BL21 using nicotinamide as substrate preincubated for 15 mins before substrate addition measured after 30 mins by mass spectrometry-based assay	B	8.52	pIC50	3	nM	IC50	J Med Chem (2013) 56: 6413-6433 [PMID:23859118]
ChEMBL	Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP	B	8.52	pIC50	3	nM	IC50	J Med Chem (2016) 59: 8345-8368 [PMID:27541271]
ChEMBL	Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (2013) 56: 9071-9088 [PMID:24164086]
ChEMBL	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	B	9	pIC50	1	nM	IC50	J Med Chem (2016) 59: 8345-8368 [PMID:27541271]
ChEMBL	Inhibition of NAMPT (unknown origin)	B	9.25	pIC50	0.56	nM	IC50	Bioorg Med Chem Lett (2023) 92: 129393-129393 [PMID:37369332]
ChEMBL	Inhibition of recombinant human NAMPT preincubated for 5 mins followed by NAM addition measured for 15 mins by fluorescence based assay	B	9.82	pIC50	0.15	nM	IC50	J Med Chem (2023) 66: 16694-16703 [PMID:38060985]
ChEMBL	Inhibition of NAMPT in human SH-SY5Y cells assessed as NAD depletion incubated for 16 hrs	B	10.52	pIC50	0.03	nM	IC50	Medchemcomm (2015) 6: 1891-1897
Nicotinamide phosphoribosyltransferase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259474] [UniProtKB: Q99KQ4]
ChEMBL	Inhibition of recombinant mouse NAMPT expressed in bacteria assessed as reduction in NADH formation using [14C]NAM as substrate measured for 1 hr by coupled enzymatic assay	B	7.21	pIC50	61	nM	IC50	Medchemcomm (2015) 6: 1891-1897
ChEMBL	Inhibition of recombinant mouse NAMPT expressed in bacterial expression system using nicotinamide as substrate after 1 hr by fluorescence based NMNAT-3 enzyme coupled assay	B	8.31	pIC50	4.9	nM	IC50	J Med Chem (2017) 60: 1768-1792 [PMID:28165742]
ChEMBL	Inhibition of recombinant mouse wild-type NAMPT expressed in bacterial expression system using PRPP as substrate in presence of mouse NMNAT-3 measured for 1 hr by fluorescence assay	B	8.57	pIC50	2.7	nM	IC50	Eur J Med Chem (2019) 181: 111576-111576 [PMID:31400709]

ChEMBL data shown on this page come from version 36:

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]