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TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531567(CHEMBL4557032)
Affinity DataEC50: <1.00E+4nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM238159(US9394291, 4a | US10017502, Example 4b)
Affinity DataEC50:  13nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50318300(CHEMBL1095097 | SC-66110 | EPLERENONE)
Affinity DataEC50:  100nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531586(CHEMBL4462110)
Affinity DataEC50: <1.00E+4nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531569(CHEMBL4532472)
Affinity DataEC50:  0.0501nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531568(CHEMBL4455600)
Affinity DataEC50:  13nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM404273(US10017502, Example 6b)
Affinity DataEC50:  1nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as induction of nuclear translocation of mineralocorticoid r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531563(CHEMBL4463240)
Affinity DataIC50: 0.794nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
LigandPNGBDBM50365480(CHEMBL1957366)
Affinity DataIC50: 1nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365495(CHEMBL1957460)
Affinity DataIC50: 1nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365481(CHEMBL1957367)
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531587(CHEMBL4471322)
Affinity DataIC50: 2.5nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531598(CHEMBL4572476)
Affinity DataIC50: 2.5nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
LigandPNGBDBM50365487(CHEMBL1957375)
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365484(CHEMBL1955881)
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Rat)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531569(CHEMBL4532472)
Affinity DataIC50: 7.90nMAssay Description:Antagonist activity at gal4-fused rat mineralocorticoid receptor LBD in expressed in human U2OS cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50209531((R)-2-[3-cyano-2-(2'-ethoxy-biphenyl-4-yl)-6-fluor...)
Affinity DataIC50: 8nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365483(CHEMBL1957369)
Affinity DataIC50: 8nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365486(CHEMBL1957374)
Affinity DataIC50: 9nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Rat)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM404273(US10017502, Example 6b)
Affinity DataIC50: 10nMAssay Description:Antagonist activity at gal4-fused rat mineralocorticoid receptor LBD in expressed in human U2OS cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
LigandPNGBDBM50365476(CHEMBL1957361)
Affinity DataIC50: 12nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365479(CHEMBL1957364)
Affinity DataIC50: 13nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365500(CHEMBL1957462)
Affinity DataIC50: 13nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetAMP deaminase 2(Human)
Astrazeneca R&D

LigandPNGBDBM154583(6-[4-({[(1S)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 16nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531593(CHEMBL4555842)
Affinity DataIC50: 20nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAMP deaminase 1(Rat)
Astrazeneca R&D

LigandPNGBDBM154584(4-[4-({[(1R)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 20nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
TargetAMP deaminase 1(Mouse)
Astrazeneca R&D

LigandPNGBDBM154584(4-[4-({[(1R)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 20nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
LigandPNGBDBM50365485(CHEMBL1957373)
Affinity DataIC50: 21nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365482(CHEMBL1957368)
Affinity DataIC50: 22nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetAMP deaminase 1(Human)
Astrazeneca R&D

LigandPNGBDBM154584(4-[4-({[(1R)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 24nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
TargetAMP deaminase 1(Mouse)
Astrazeneca R&D

LigandPNGBDBM154583(6-[4-({[(1S)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 24nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531569(CHEMBL4532472)
Affinity DataIC50: 25nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAMP deaminase 1(Rat)
Astrazeneca R&D

LigandPNGBDBM154583(6-[4-({[(1S)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 27nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
LigandPNGBDBM50365494(CHEMBL1957381)
Affinity DataIC50: 27nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50365496(CHEMBL1957370)
Affinity DataIC50: 31nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531569(CHEMBL4532472)
Affinity DataIC50: 32nMAssay Description:Antagonist activity at full length human mineralocorticoid receptor expressed in human U2OS cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM404273(US10017502, Example 6b)
Affinity DataIC50: 32nMAssay Description:Antagonist activity at full length human mineralocorticoid receptor expressed in human U2OS cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
LigandPNGBDBM31589(triaryl imidazole, 1)
Affinity DataIC50: 35nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
LigandPNGBDBM14754(CHEMBL19224 | 1-[(3,4-dimethoxyphenyl)methyl]-6,7-...)
Affinity DataIC50: 36nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAMP deaminase 1(Human)
Astrazeneca R&D

LigandPNGBDBM154583(6-[4-({[(1S)-1-(isoquinolin-8-yl)ethyl]amino}methy...)
Affinity DataIC50: 38nMpH: 7.4Assay Description:AMPD1 was added to buffer A (50 mM HEPES, 150 mM KCl, 5 mM MgCl2, and 0.5 mMglutathione [pH 7.4]) to a concentration of 10 nM. A substrate mix consis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2015
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Rat)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50318300(CHEMBL1095097 | SC-66110 | EPLERENONE)
Affinity DataIC50: 40nMAssay Description:Antagonist activity at gal4-fused rat mineralocorticoid receptor LBD in expressed in human U2OS cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50235933(CHEMBL3775714)
Affinity DataIC50: 50nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM238161(US9394291, 5a | US10017502, Example 5a)
Affinity DataIC50: 50nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM404276(US10017502, Example 8a)
Affinity DataIC50: 50nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50228080(Spiranolactone | S-(2'R,7R,8R,9S,10R,13S,14S)-10,1...)
Affinity DataIC50: 50nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
LigandPNGBDBM50365492(CHEMBL1957379)
Affinity DataIC50: 52nMAssay Description:Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531570(CHEMBL4556735)
Affinity DataIC50: 63nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50318300(CHEMBL1095097 | SC-66110 | EPLERENONE)
Affinity DataIC50: 63nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as blocking of nuclear translocation of mineralocorticoid re...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531589(CHEMBL4468672)
Affinity DataIC50: 63nMAssay Description:Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMineralocorticoid receptor(Human)
Pharmaron-Beijing

Curated by ChEMBL
LigandPNGBDBM50531567(CHEMBL4557032)
Affinity DataIC50: 63nMAssay Description:Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as blocking of nuclear translocation of mineralocorticoid re...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
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