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TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266556(US10323016, Example 5 | CHEMBL4073081)
Affinity DataEC50:  44nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetInsulin-degrading enzyme(Human)
Univ. Lille

Curated by ChEMBL
LigandPNGBDBM50602608(CHEMBL5191945)
Affinity DataEC50:  2.69E+4nMAssay Description:Activation of human recombinant IDE using ATTO 655-Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-trp as substrate incubated for 10 mins followed by substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetPeroxisome proliferator-activated receptor delta(Human)
University of Valencia

Curated by ChEMBL
LigandPNGBDBM50645466(CHEMBL5202264)
Affinity DataEC50:  2.20nMMore data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266567(US10323016, Example 21 | CHEMBL4090147)
Affinity DataEC50:  2nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

LigandPNGBDBM50189965(methyl 2-(4-(3-(2-propyl-4-(trifluoromethyl)phenox...)
Affinity DataEC50:  1.19E+3nMAssay Description:Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetRetinoic acid receptor beta(Human)
University of Lille

Curated by ChEMBL
LigandPNGBDBM50265921(3-(4-((5,5,8,8-tetramethyl-5,6,7,8-tetrahydronapht...)
Affinity DataEC50:  26nMAssay Description:Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandPNGBDBM50294690((S)-2-ethoxy-3-(4-(2-(6-((methoxyimino)(phenyl)met...)
Affinity DataEC50:  114nMAssay Description:Agonist activity at human PPARalpha by Gal4 transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Human)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266574(US10323016, Example 2 | CHEMBL4081298)
Affinity DataEC50:  299nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetG-protein coupled bile acid receptor 1(Human)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266575(US10323016, Example 14 | CHEMBL4085777)
Affinity DataEC50:  7.75E+3nMAssay Description:Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
TargetPeroxisome proliferator-activated receptor delta(Human)
University of Valencia

Curated by ChEMBL
LigandPNGBDBM50189967(2-(2-methyl-4-(3-(4-propyl-6-(trifluoromethyl)pyri...)
Affinity DataEC50:  15nMAssay Description:Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin-degrading enzyme(Human)
Univ. Lille

Curated by ChEMBL
LigandPNGBDBM50602618(CHEMBL5198912)
Affinity DataEC50:  8.13E+3nMAssay Description:Activation of human recombinant IDE using ATTO 655-Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-trp as substrate incubated for 10 mins followed by substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
LigandPNGBDBM50234372((R)-2-ethoxy-3-(4-(2-(6-((methoxyimino)(phenyl)met...)
Affinity DataEC50:  65nMAssay Description:Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
TargetRetinoic acid receptor beta(Human)
University of Lille

Curated by ChEMBL
LigandPNGBDBM50265949(3-(3-((5,5,8,8-tetramethyl-5,6,7,8-tetrahydronapht...)
Affinity DataEC50: >1.00E+3nMAssay Description:Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266537(US10323016, Example 3 | CHEMBL4075688)
Affinity DataEC50:  12nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
TargetPeroxisome proliferator-activated receptor delta(Human)
University of Valencia

Curated by ChEMBL
LigandPNGBDBM50189965(methyl 2-(4-(3-(2-propyl-4-(trifluoromethyl)phenox...)
Affinity DataEC50:  98nMAssay Description:Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50234372((R)-2-ethoxy-3-(4-(2-(6-((methoxyimino)(phenyl)met...)
Affinity DataEC50:  194nMAssay Description:Agonist activity at human PPARalpha by GAL4 transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
LigandPNGBDBM50282748(CHEMBL4164063)
Affinity DataEC50:  1.00E+4nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
LigandPNGBDBM50234374((S)-ethyl 2-ethoxy-3-(4-(2-(6-((methoxyimino)(phen...)
Affinity DataEC50:  14nMAssay Description:Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266565(US10323016, Example 17 | CHEMBL4091702)
Affinity DataEC50:  140nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266536(US10323016, Example 1 | CHEMBL4085664)
Affinity DataEC50:  68nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
TargetRetinoic acid receptor beta(Human)
University of Lille

Curated by ChEMBL
LigandPNGBDBM31883(ALL-TRANS-RETINOIC ACID | SMR000058245 | cid_44479...)
Affinity DataEC50:  12nMAssay Description:Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetInsulin-degrading enzyme(Human)
Univ. Lille

Curated by ChEMBL
LigandPNGBDBM50602609(CHEMBL5179418)
Affinity DataEC50:  1.32E+4nMAssay Description:Activation of human recombinant IDE using ATTO 655-Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-trp as substrate incubated for 10 mins followed by substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266559(CHEMBL4067717)
Affinity DataEC50:  40nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
LigandPNGBDBM50643354(CHEMBL5589777)
Affinity DataEC50:  226nMMore data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
LigandPNGBDBM50282751(CHEMBL4163242)
Affinity DataEC50:  50nMAssay Description:Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266580(CHEMBL4087611)
Affinity DataEC50:  0.300nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
LigandPNGBDBM50282751(CHEMBL4163242)
Affinity DataEC50:  1.00E+4nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
TargetRetinoic acid receptor alpha(Human)
University of Lille

Curated by ChEMBL
LigandPNGBDBM50265949(3-(3-((5,5,8,8-tetramethyl-5,6,7,8-tetrahydronapht...)
Affinity DataEC50: >1.00E+3nMAssay Description:Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandPNGBDBM50294691((S)-2-(2-benzoylphenylamino)-3-(4-(2-(6-((methoxyi...)
Affinity DataEC50:  14nMAssay Description:Agonist activity at human PPARgamma by Gal4 transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM398271(US10323016, Example 8)
Affinity DataEC50:  17nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetInsulin-degrading enzyme(Human)
Univ. Lille

Curated by ChEMBL
LigandPNGBDBM50602615(CHEMBL5185924)
Affinity DataEC50:  2.69E+4nMAssay Description:Activation of human recombinant IDE using ATTO 655-Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-trp as substrate incubated for 10 mins followed by substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
LigandPNGBDBM50282761(CHEMBL4167789)
Affinity DataEC50:  1.00E+3nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
LigandPNGBDBM50234378(ethyl 2-ethoxy-3-(4-(2-(6-((methoxyimino)(phenyl)m...)
Affinity DataEC50:  30nMAssay Description:Agonist activity at human PPARalpha by GAL4 transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266579(CHEMBL4074376)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266566(US10323016, Example 19 | CHEMBL4068227)
Affinity DataEC50:  4.80nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetG-protein coupled bile acid receptor 1(Human)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM398271(US10323016, Example 8)
Affinity DataEC50:  260nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266572(US10323016, Example 15 | CHEMBL4060122)
Affinity DataEC50:  366nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
LigandPNGBDBM50282749(CHEMBL4159869)
Affinity DataEC50:  1.00E+4nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266541(CHEMBL4069569)
Affinity DataEC50:  82nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
LigandPNGBDBM50282760(CHEMBL4174996)
Affinity DataEC50:  300nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
LigandPNGBDBM50234375((S)-2-ethoxy-3-(4-(2-(6-((methoxyimino)(phenyl)met...)
Affinity DataEC50:  114nMAssay Description:Agonist activity at human PPARalpha by GAL4 transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Mouse)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266562(CHEMBL4068186)
Affinity DataEC50:  254nMAssay Description:Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Human)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266558(US10323016, Example 18 | CHEMBL4088938)
Affinity DataEC50:  750nMAssay Description:In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
Go to US Patent

TargetRetinoic acid receptor beta(Human)
University of Lille

Curated by ChEMBL
LigandPNGBDBM50265919(3-(3-((4-tert-butylphenyl)ethynyl)phenyl)-1,2,4-ox...)
Affinity DataEC50: >1.00E+3nMAssay Description:Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetG-protein coupled bile acid receptor 1(Human)
Universite De Lille 2 Droit Et Sante

US Patent
LigandPNGBDBM50266566(US10323016, Example 19 | CHEMBL4068227)
Affinity DataEC50:  47nMAssay Description:Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2020
Entry Details Article
PubMed
LigandPNGBDBM24566(JMC515449 Compound 1 | Wyeth 14,643 | 2-({4-chloro...)
Affinity DataEC50:  1.00E+4nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM28681(cid_5281055 | [3H]rosiglitazone | CHEMBL121 | ROSI...)
Affinity DataEC50:  4nMAssay Description:Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
LigandPNGBDBM50282755(CHEMBL4160661)
Affinity DataEC50:  1.00E+4nMAssay Description:Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2020
Entry Details Article
PubMed
LigandPNGBDBM50189967(2-(2-methyl-4-(3-(4-propyl-6-(trifluoromethyl)pyri...)
Affinity DataEC50:  1.33E+3nMAssay Description:Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetRetinoic acid receptor alpha(Human)
University of Lille

Curated by ChEMBL
LigandPNGBDBM50265917(4-((4-tert-butylphenyl)ethynyl)benzoic acid | CHEM...)
Affinity DataEC50: >1.00E+3nMAssay Description:Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
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