Compile Data Set for Download or QSAR
Report error Found 7898 Enz. Inhib. hit(s) with Target = 'Glucocorticoid receptor'
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataIC50: 0.00800nMAssay Description:Inhibition of CHO-K1 cells expressing glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250114(CHEMBL4104286)
Affinity DataIC50: 0.0200nMAssay Description:Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50266693(CHEBI:5391 | Glucagen Hypokit | Glucagon | Glucago...)
Affinity DataEC50:  0.0200nMAssay Description:Activation of human GCCR expressed in human CHO-K1 cell lines assessed as intracellular cAMP generation incubated for 30 mins measured by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250125(CHEMBL4061359)
Affinity DataIC50: 0.0290nMAssay Description:Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50206900(CHEMBL3895181)
Affinity DataIC50: 0.0300nMAssay Description:Antagonist activity at GR in human HepG2 cells assessed as inhibition of protein mediated-transcriptional activity by MMTV-promoter driven luciferase...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50266693(CHEBI:5391 | Glucagen Hypokit | Glucagon | Glucago...)
Affinity DataEC50:  0.0300nMAssay Description:Activation of human GCCR expressed in human HEK293 cells assessed as luminescence signal incubated for 16 hrs at 37C measured by CRE-driven luciferas...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203432(CHEMBL3911831)
Affinity DataIC50: 0.0300nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250115(CHEMBL4086388)
Affinity DataIC50: 0.0320nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM141378(US8916600, 12 | US9738632, Example 12)
Affinity DataIC50: 0.0370nMAssay Description:Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50354851(Veramyst | FLUTICASONE FUROATE)
Affinity DataIC50: 0.0398nMAssay Description:Agonist activity at GR in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203418(CHEMBL3902818)
Affinity DataIC50: 0.0400nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50354849(Flovent hfa | Cutivate | Flovent | Flovent diskus ...)
Affinity DataIC50: 0.0400nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203441(CHEMBL3973775)
Affinity DataIC50: 0.0400nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50206899(CHEMBL3964460)
Affinity DataEC50:  0.0400nMAssay Description:Agonist activity at GR in human HepG2 cells assessed as protein mediated-transcriptional activity by MMTV-promoter driven luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50587188(CHEMBL5080959)
Affinity DataEC50:  0.0400nMAssay Description:Activation of human GCCR expressed in human CHO-K1 cell lines assessed as intracellular cAMP generation incubated for 30 mins measured by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50354849(Flovent hfa | Cutivate | Flovent | Flovent diskus ...)
Affinity DataIC50: 0.0440nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250112(CHEMBL4072756)
Affinity DataIC50: 0.0490nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50206940(CHEMBL3981243)
Affinity DataEC50:  0.0500nMAssay Description:Agonist activity at GR in human HepG2 cells assessed as protein mediated-transcriptional activity by MMTV-promoter driven luciferase reporter gene as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203413(CHEMBL3920760)
Affinity DataIC50: 0.0500nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM141371(US8916600, 5 | US9738632, Example 5)
Affinity DataIC50: 0.0510nMAssay Description:Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM141372(US8916600, 6 | US9738632, Example 6)
Affinity DataIC50: 0.0560nMAssay Description:Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM141379(US8916600, 13 | US9738632, Example 13)
Affinity DataIC50: 0.0620nMAssay Description:Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250126(CHEMBL4094154)
Affinity DataIC50: 0.0660nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50206950(CHEMBL3933702)
Affinity DataIC50: 0.0700nMAssay Description:Antagonist activity at GR in human HepG2 cells assessed as inhibition of protein mediated-transcriptional activity by MMTV-promoter driven luciferase...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250125(CHEMBL4061359)
Affinity DataIC50: 0.0730nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50354849(Flovent hfa | Cutivate | Flovent | Flovent diskus ...)
Affinity DataIC50: 0.0750nMAssay Description:Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-stimulated IL-6 cytokine synthesisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50414604(CHEMBL551816)
Affinity DataIC50: 0.0790nMAssay Description:Agonist activity at GR in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50417875(CHEMBL1668063)
Affinity DataIC50: 0.0794nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50250114(CHEMBL4104286)
Affinity DataIC50: 0.0800nMAssay Description:Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50265728(CHEMBL4081121)
Affinity DataKi:  0.0800nMAssay Description:Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203430(CHEMBL3901719)
Affinity DataIC50: 0.0800nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataKi:  0.0900nMAssay Description:Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203423(CHEMBL3960682)
Affinity DataIC50: 0.0900nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50203435(CHEMBL3940724)
Affinity DataIC50: 0.0900nMAssay Description:Agonist activity at glucocorticoid receptor in human ChaGoK1 cells assessed as inhibition of AP1-mediated transcriptional activity by measuring reduc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/8/2018
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50265798(CHEMBL3736358)
Affinity DataKi:  0.100nMAssay Description:Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50113783(CP-394531 | (2R,4aS,10aR)-4a-benzyl-2-(chloroethyn...)
Affinity DataKi:  0.100nMAssay Description:Displacement of [3H]DEX from human glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50113782((10R,13S,17S)-17-hydroxy-13-methyl-10-(4-methylben...)
Affinity DataKi:  0.100nMAssay Description:Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Rat)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM86689(CAS_84371-65-3 | NSC_55245 | RU-486)
Affinity DataKi:  0.100nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM476583(US10869929, Compound 18 | US11554172, Compound 18)
Affinity DataIC50: 0.100nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen Glucocorticoid Receptor Competitor Ass...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/12/2023
Entry Details
US Patent

TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50214935(5-fluoro-2-((Z)-(9-hydroxy-10-methoxy-2,2,4-trimet...)
Affinity DataIC50: 0.100nMAssay Description:Antagonist activity at GR assessed as inhibition of dexamethasone-induced GRE activationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  0.100nMAssay Description:Agonist activity at recombinant human glucocorticoid receptor expressed in African green monkey CV1 cells by MMTV luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50440220(CHEMBL2426624)
Affinity DataEC50:  0.100nMAssay Description:Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by G...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM18623((18Z)-12-methoxy-18-({3-[(1E)-1-(methoxyimino)ethy...)
Affinity DataKi:  1.10nM ΔG°:  -47.5kJ/mole IC50: 0.200nM EC50:  0.100nMpH: 7.5 T: 2°CAssay Description:Competitive Ligand Binding Assay- The Ki values were determined by the application of the Cheng-Prusoff equation: Ki=IC50/(1+[L]/Kd) where [L] is the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2007
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM18627(Mifeprex | (10S,11S,14S,15S,17R)-17-[4-(dimethylam...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of human glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Rat)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM141379(US8916600, 13 | US9738632, Example 13)
Affinity DataIC50: 0.100nMAssay Description:Transrepression of glucocorticoid receptor in Wistar rat PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins follow...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2019
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50113782((10R,13S,17S)-17-hydroxy-13-methyl-10-(4-methylben...)
Affinity DataKi:  0.100nMAssay Description:Displacement of [3H]DEX from human glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50440220(CHEMBL2426624)
Affinity DataEC50:  0.100nMAssay Description:Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by G...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50195157((8S,11R,13S,14S,17S)-17-hydroxy-11-(4-methoxy-3-me...)
Affinity DataIC50: 0.100nMAssay Description:Binding affinity to human GRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50265798(CHEMBL3736358)
Affinity DataKi:  0.100nMAssay Description:Binding affinity to human recombinant glucocorticoid receptor by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
The Pennsylvania State University

Curated by ChEMBL
LigandPNGBDBM50113783(CP-394531 | (2R,4aS,10aR)-4a-benzyl-2-(chloroethyn...)
Affinity DataKi:  0.100nMAssay Description:Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2012
Entry Details Article
PubMed
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