BindingDB BDBM81395 APO-866::US20240300968, Example Comparative FK8661::US20240327418, Example FK866

BDBM81395 APO-866::US20240300968, Example Comparative FK8661::US20240327418, Example FK866

SMILES c1ccc(cc1)C(=O)N2CCC(CC2)CCCCNC(=O)/C=C/c3cccnc3

InChI Key InChIKey=KPBNHDGDUADAGP-UHFFFAOYSA-N

Data 2 KI 30 IC50 1 Kd

PDB links: 4 PDB IDs match this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 33 hits for monomerid = 81395

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 0.150nMAssay Description:Inhibition of recombinant human NAMPT preincubated for 5 mins followed by NAM addition measured for 15 mins by fluorescence based assayMore data for this Ligand-Target Pair

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Date in BDB:
12/18/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 9nMAssay Description:Inhibition of NAMPT (unknown origin) using NAM as substrate incubated for 5 mins followed by substrate addition measured after 15 mins by fluorometri...More data for this Ligand-Target Pair

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Date in BDB:
7/19/2020
Entry Details Article
PubMed PDB

3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 5nMAssay Description:Inhibition of human full length C-terminal flag/His-tagged NAMPT (1 to 491 residues) expressed in HEK293-6E cells by TR-FRET assayMore data for this Ligand-Target Pair

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Date in BDB:
8/15/2020
Entry Details Article
PubMed PDB

3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 6.80nMAssay Description:Inhibition of recombinant NAMPT (unknown origin) using NAM and PRPP as substrates incubated for 60 mins in presence of NMNAT1 measured at 5 mins inte...More data for this Ligand-Target Pair

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Date in BDB:
2/24/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Mouse)
University of Pavia

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 2.70nMAssay Description:Inhibition of recombinant mouse wild-type NAMPT expressed in bacterial expression system using PRPP as substrate in presence of mouse NMNAT-3 measure...More data for this Ligand-Target Pair

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Date in BDB:
2/21/2021
Entry Details Article
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 32nMAssay Description:Inhibition of recombinant NAMPT (unknown origin) using nicotinamide as substrate measured every 5 mins for 30 mins in presence of recombinant NMNAT1More data for this Ligand-Target Pair

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Date in BDB:
2/27/2021
Entry Details Article
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

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Date in BDB:
2/27/2021
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 21nMAssay Description:Inhibition of recombinant NAMPT (unknown origin) using nicotinamide and pyrophosphate as substrate incubated for 60 mins and measured for 30 mins at ...More data for this Ligand-Target Pair

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Date in BDB:
8/20/2022
Entry Details Article
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 35nMAssay Description:Inhibition of recombinant human NAMPT incubated for 60 mins by colorimetric assayMore data for this Ligand-Target Pair

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Date in BDB:
6/25/2023
Entry Details
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 9nMAssay Description:Inhibition of human recombinant NAMPT using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluores...More data for this Ligand-Target Pair

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Date in BDB:
10/9/2019
Entry Details Article
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 3.30nMAssay Description:Inhibition of full-length recombinant human NAMPT (2 to 491 residues) expressed in Escherichia coli using NAM as substrate preincubated for 5 mins fo...More data for this Ligand-Target Pair

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Date in BDB:
12/15/2024
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 96.1nMAssay Description:a) Formulation of 100% solution: 50 μL of HDAC buffer was mixed with 10 μL of enzyme solution, 40 μL of substrate was added after 5 mi...More data for this Ligand-Target Pair

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Date in BDB:
2/3/2025
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 1.60E+3nMAssay Description:In a 96-well opaque black plate, NAMPT (30 nM all concentrations provided as final), PRPP (50 μM) and ATP (2 mM) with or without test compounds ...More data for this Ligand-Target Pair

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Date in BDB:
1/8/2025
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 0.560nMAssay Description:Inhibition of NAMPT (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
12/19/2024
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

Kd: 10nMAssay Description:Displacement of FP-probe ZN-2-102 from C-terminal His6-tagged wild type human NAMPT rear channel assessed as dissociation constant by fluorescence po...More data for this Ligand-Target Pair

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Date in BDB:
12/21/2024
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 12nMAssay Description:Inhibition of NAMPT (unknown origin) using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins in presence...More data for this Ligand-Target Pair

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Date in BDB:
12/13/2024
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 34nMAssay Description:Inhibition of recombinant NAMPT (unknown origin) incubated for 60 mins by SpectraMax microplate reader analysisMore data for this Ligand-Target Pair

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Date in BDB:
12/13/2024
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 3nMAssay Description:Inhibition of C-terminal His-tagged NAMPT (unknown origin) expressed in Escherichia coli BL21 using nicotinamide as substrate preincubated for 15 min...More data for this Ligand-Target Pair

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Date in BDB:
4/13/2014
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Mouse)
University of Pavia

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 4.90nMAssay Description:Inhibition of recombinant mouse NAMPT expressed in bacterial expression system using nicotinamide as substrate after 1 hr by fluorescence based NMNAT...More data for this Ligand-Target Pair

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Date in BDB:
7/15/2019
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 3nMAssay Description:Inhibition of Nampt (unknown origin) using NAM/PRPP as substrate preincubated for 15 mins measured after 30 minsMore data for this Ligand-Target Pair

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Date in BDB:
4/13/2014
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 2.20nMAssay Description:Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after ...More data for this Ligand-Target Pair

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Date in BDB:
7/25/2014
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 3nMAssay Description:Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incuba...More data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
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3D Structure (crystal)

Cytochrome P450 2D6(Human)
Genentech

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 1.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
Entry Details Article
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Cytochrome P450 2C9(Human)
Genentech

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 3.60E+3nMAssay Description:Reversible inhibition of CYP2C9 in human liver microsomes using (S)-warfarin as substrate in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
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Cytochrome P450 3A4(Human)
Genentech

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 1.50E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
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Cytochrome P450 2C19(Human)
Genentech

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 1.00E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
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Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 1nMAssay Description:Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assayMore data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
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3D Structure (crystal)

Cytochrome P450 3A4(Human)
Genentech

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 540nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair

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Date in BDB:
8/5/2018
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Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 3nMAssay Description:Inhibition of C-terminal His-tagged human full-length NAMPT expressed in Escherichia coli Rosetta DE3 using nicotinamide as substrate preincubated fo...More data for this Ligand-Target Pair

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Date in BDB:
7/26/2014
Entry Details Article
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 1.48E+4nMAssay Description:Inhibition of human NAmPRTase by spectrophotometric analysisMore data for this Ligand-Target Pair

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Date in BDB:
12/2/2011
Entry Details Article
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

IC50: 0.140nMAssay Description:In vitro inhibition assay using human nampt, NMN adenylytransferase (nmant1)and UDP-glucose dehdryogenase (ugdh) genes.More data for this Ligand-Target Pair

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Date in BDB:
9/6/2011
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

Ki: 0.300nMAssay Description:Noncompetitive inhibition of NAMPT (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
4/13/2014
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3D Structure (crystal)

Nicotinamide phosphoribosyltransferase(Human)
Nanchang University

Curated by ChEMBL

BDBM81395(APO-866 | US20240327418, Example FK866 | US2024030...)

Ki: 3nMAssay Description: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-...More data for this Ligand-Target Pair

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Date in BDB:
12/9/2019
Entry Details Article
PubMed PDB

3D Structure (crystal)

Filter my 33 hits

Targets 5▿
- Nicotinamide phosphoribosyltransferase 28
- Cytochrome P450 3A4 2
- Cytochrome P450 2C9 1
- Cytochrome P450 2C19 1
- Cytochrome P450 2D6 1
Publications 25▿
- J Med Chem 59: 8345-68 (2016) 7
- J Med Chem 59: 5766-79 (2016) 2
- J Med Chem 56: 9071-88 (2013) 1
- Eur J Med Chem 181: (2019) 1
- Eur J Med Chem 46: 1153-64 (2011) 1
- Eur J Med Chem 250: (2023) 1
- J Med Chem 56: 6413-33 (2013) 1
- Bioorg Med Chem Lett 29: 1502-1506 (2019) 1
- J Med Chem 66: 1048-1062 (2023) 1
- J Med Chem 57: 770-92 (2014) 1
- J Med Chem 66: 16704-16727 (2023) 1
- Bioorg Med Chem Lett 27: 3317-3325 (2017) 1
- J Med Chem 66: 1027-1047 (2023) 1
- J Med Chem 66: 16694-16703 (2023) 1
- ACS Med Chem Lett 9: 34-38 (2018) 1
- Bioorg Med Chem Lett 92: (2023) 1
- J Med Chem 60: 7965-7983 (2017) 1
- US Patent US20240327418 (2024) 1
- Chem Biol 17: 659-64 (2010) 1
- Eur J Med Chem 211: (2021) 1
- J Med Chem 65: 7746-7769 (2022) 1
- US Patent US20240300968 (2024) 1
- J Med Chem 56: 6279-96 (2013) 1
- J Med Chem 56: 4921-37 (2013) 1
- J Med Chem 60: 1768-1792 (2017) 1
Institutions 17▿
- Genentech 8
- Chinese Academy of Sciences 3
- China Pharmaceutical University 3
- Second Military Medical University 3
- Forma Therapeutics 2
- University of Eastern Piedmont 2
- Topotarget 1
- Universidad De Sevilla 1
- School of Life Science 1
- Ocean University of China 1
- University of Manchester 1
- Changzhou University 1
- Kyowa Hakko Kogyo 1
- University of Arizona 1
- University of Pavia 1
- Nanchang University 1
- Abbvie 1
Affinity: 0.14 to 1.5E+4 nM▿
- Ki 2
- IC50 30
- Kd 1
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1