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Report error Found 18 Enz. Inhib. hit(s) for PDB: 3TKM

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

Kd: 0.400nMAssay Description:Binding affinity to human PPARdelta (unknown origin) by competitive TR-FRET assayMore data for this Ligand-Target Pair

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Date in BDB:
9/24/2013
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 1nMAssay Description:Agonist activity at PPARdelta (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
8/18/2020
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

IC50: 1nMAssay Description:Binding affinity for human PPAR delta receptorMore data for this Ligand-Target Pair

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Date in BDB:
11/10/2009
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 1nMAssay Description:Maximum transcriptional activation of human PPAR delta receptorMore data for this Ligand-Target Pair

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Date in BDB:
11/10/2009
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 1.90nMAssay Description:Agonist activity at human PPARdelta expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 ...More data for this Ligand-Target Pair

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Date in BDB:
2/20/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 2nMAssay Description:Agonist activity at human PPARdelta after 22 to 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair

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Date in BDB:
8/17/2020
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 2.90nMAssay Description:Displacement of pan-PPAR fluormone from PPARdelta LBD by TR-FRET based LanthaScreen assayMore data for this Ligand-Target Pair

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Date in BDB:
2/8/2013
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 3.5nMAssay Description:Agonist activity at human PPARdelta expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assayMore data for this Ligand-Target Pair

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Date in BDB:
6/24/2023
Entry Details
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 4nMAssay Description:Agonist activity at human PPAR-deltaMore data for this Ligand-Target Pair

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Date in BDB:
3/23/2022
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 10nMAssay Description:Agonist activity at pBIND tagged human PPARdelta expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assayMore data for this Ligand-Target Pair

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Date in BDB:
6/24/2023
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 13nMAssay Description:Agonist activity at human PPARdelta measured by dual luciferase reporter gene assayMore data for this Ligand-Target Pair

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Date in BDB:
6/24/2023
Entry Details
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 13nMAssay Description:Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair

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Date in BDB:
8/18/2020
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 13nMAssay Description:Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair

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Date in BDB:
2/26/2021
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 18nMAssay Description:Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assayMore data for this Ligand-Target Pair

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Date in BDB:
8/23/2022
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 27nMAssay Description:Agonist activity at human PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactiv...More data for this Ligand-Target Pair

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Date in BDB:
3/5/2023
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Mouse)
Glaxosmithkline

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 30nMAssay Description:Activity against murine PPAR delta receptorMore data for this Ligand-Target Pair

PDB KEGG
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Date in BDB:
11/10/2009
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 67nMAssay Description:Activation of PPARbeta-LBD (unknown origin) assessed as fluorescein-labeled coactivator C33 recruitment by TR-FRET assayMore data for this Ligand-Target Pair

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Date in BDB:
10/6/2017
Entry Details Article
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3D Structure (crystal)

Peroxisome proliferator-activated receptor delta(Human)
Helmholtz Centre For Infection Research

Curated by ChEMBL

BDBM50127222({4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl...)

EC50: 300nMAssay Description:Agonist activity at human PPARdelta LBD by cell based luciferase reporter gene assayMore data for this Ligand-Target Pair

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Date in BDB:
1/5/2013
Entry Details Article
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3D Structure (crystal)

Filter my 18 hits

Targets 1▿
- Peroxisome proliferator-activated receptor delta 18
Publications 15▿
- Bioorg Med Chem Lett 13: 1517-21 (2003) 3
- Eur J Med Chem 159: 267-276 (2018) 2
- Bioorg Med Chem 56: (2022) 1
- Eur J Med Chem 229: (2022) 1
- J Med Chem 54: 788-808 (2012) 1
- J Med Chem 64: 6996-7032 (2021) 1
- Bioorg Med Chem Lett 28: 2717-2722 (2018) 1
- Eur J Med Chem 164: 352-365 (2019) 1
- J Med Chem 56: 1535-43 (2013) 1
- J Med Chem 63: 2854-2876 (2020) 1
- Bioorg Med Chem Lett 26: 3978-83 (2016) 1
- J Med Chem 55: 4978-89 (2012) 1
- Eur J Med Chem 225: (2021) 1
- J Med Chem 65: 1961-1978 (2022) 1
- J Med Chem 59: 9201-9214 (2016) 1
Institutions 10▿
- Guangdong Pharmaceutical University 6
- Glaxosmithkline 3
- University of Oklahoma 2
- Korea University 1
- University of Toledo College of Pharmacy and Pharmaceutical Sciences 1
- Trinity College 1
- Tes Pharma 1
- Johnson & Johnson Pharmaceutical Research and Development 1
- Helmholtz Centre For Infection Research 1
- University of Toronto 1
Affinity: 0.40 to 3.0E+2 nM▿
- IC50 1
- Kd 1
- EC50 16
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1