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: CHEMBL566757 (APO 866, APO-866, APO866, Daporinad, FK 866, FK-866, K 22.175) |
---|
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 |
---|---|---|---|---|---|---|---|---|
Nicotinamide phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744525] [UniProtKB: P43490] | ||||||||
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 | 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 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 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 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 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 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 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 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 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 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]