daporinad [Ligand Id: 7745] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL566757 (APO 866, APO-866, APO866, Daporinad, FK 866, FK-866, K 22.175)
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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]