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Found 309 with Last Name = 'michel' and Initial = 'k'
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataKi:  0.170nMAssay Description:Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatumMore data for this Ligand-Target Pair
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50304496(3-Benzo[1,3]dioxol-5-yl-4-[3-(2-fluoroethoxy)-4,5-...)
Affinity DataKi:  1.10nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50365964(CHEMBL1956235 | CHEMBL2070530)
Affinity DataKi:  1.18nMAssay Description:Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatumMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336694(3-Benzo[1,3]dioxol-5-yl-4-{3-(2-(2-(2-(2-fluoroeth...)
Affinity DataKi:  1.40nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336695(3-Benzo[1,3]dioxol-5-yl-4-{3-[1-(2-{2-[2-(2-fluoro...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336697(3-Benzo[1,3]dioxol-5-yl-4-[3-(2-{2-[2-(2-{4-[4-(2-...)
Affinity DataKi:  3.5nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336699(CHEMBL1672884 | N-[1-(2-{2-[2-(2-{5-[4-Benzo[1,3]d...)
Affinity DataKi:  3.90nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336696(3-Benzo[1,3]dioxol-5-yl-4-[3-(2-{2-[2-(2-{1-[2-(2-...)
Affinity DataKi:  4.40nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336698(CHEMBL1672885 | N-[1-(2-{2-[2-(2-{5-[4-Benzo[1,3]d...)
Affinity DataKi:  7.30nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin-1 receptor(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336700(3-Benzo[1,3]dioxol-5-yl-4-{3-[2-(2-{2-[2-(4-fluoro...)
Affinity DataKi:  7.90nMAssay Description:Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336697(3-Benzo[1,3]dioxol-5-yl-4-[3-(2-{2-[2-(2-{4-[4-(2-...)
Affinity DataKi:  37nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50304496(3-Benzo[1,3]dioxol-5-yl-4-[3-(2-fluoroethoxy)-4,5-...)
Affinity DataKi:  240nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336699(CHEMBL1672884 | N-[1-(2-{2-[2-(2-{5-[4-Benzo[1,3]d...)
Affinity DataKi:  288nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336694(3-Benzo[1,3]dioxol-5-yl-4-{3-(2-(2-(2-(2-fluoroeth...)
Affinity DataKi:  418nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336698(CHEMBL1672885 | N-[1-(2-{2-[2-(2-{5-[4-Benzo[1,3]d...)
Affinity DataKi:  893nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336696(3-Benzo[1,3]dioxol-5-yl-4-[3-(2-{2-[2-(2-{1-[2-(2-...)
Affinity DataKi:  5.34E+3nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336700(3-Benzo[1,3]dioxol-5-yl-4-{3-[2-(2-{2-[2-(4-fluoro...)
Affinity DataKi:  6.45E+3nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelin receptor type B(Mus musculus)
University Hospital Mu£Nster

Curated by ChEMBL
LigandPNGBDBM50336695(3-Benzo[1,3]dioxol-5-yl-4-{3-[1-(2-{2-[2-(2-fluoro...)
Affinity DataKi:  8.45E+3nMAssay Description:Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.5nMAssay Description:Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatumMore data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351929(CHEMBL1821820)
Affinity DataIC50:  0.650nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351935(CHEMBL1821728)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
LigandPNGBDBM50389801(CHEMBL2070528)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human recombinant PDE10A using cAMP as substrate incubated for 30 mins prior to substrate addition measured after 3 hrs to overnight by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50365964(CHEMBL1956235 | CHEMBL2070530)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of human recombinant PDE10A using cAMP as substrate incubated for 30 mins prior to substrate addition measured after 3 hrs to overnight by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447276(CHEMBL3113985)
Affinity DataIC50:  2nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351924(CHEMBL1821815)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50365964(CHEMBL1956235 | CHEMBL2070530)
Affinity DataIC50:  3.47nMAssay Description:Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatumMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351923(CHEMBL1821814)
Affinity DataIC50:  3.70nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50500213(CHEMBL3746243)
Affinity DataIC50:  3.80nMAssay Description:Binding affinity to human biotinylated AviTag GKRP assessed as inhibition of protein interaction with fluorescein tagged human glucokinase by AlphaSc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447275(CHEMBL3114185)
Affinity DataIC50:  4nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50389800(CHEMBL2070529)
Affinity DataIC50:  5.70nMAssay Description:Inhibition of human recombinant PDE10A using cAMP as substrate incubated for 30 mins prior to substrate addition measured after 3 hrs to overnight by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447273(CHEMBL3114186)
Affinity DataIC50:  6nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50500210(CHEMBL3745887)
Affinity DataIC50:  6nMAssay Description:Binding affinity to human biotinylated AviTag GKRP assessed as inhibition of protein interaction with fluorescein tagged human glucokinase by AlphaSc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447274(CHEMBL3114183)
Affinity DataIC50:  6nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447272(CHEMBL3113980)
Affinity DataIC50:  7nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447271(CHEMBL3114187)
Affinity DataIC50:  9nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50448558(CHEMBL3127349)
Affinity DataIC50:  9.70nMAssay Description:Inhibition of biotin-tagged human GKRP-fluorescein-tagged human GK interaction preincubated for 20 mins followed by fluorescein-tagged human GK addit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351934(CHEMBL1821825)
Affinity DataIC50:  10nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351928(CHEMBL1821819)
Affinity DataIC50:  11nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50500200(CHEMBL3746444)
Affinity DataIC50:  11nMAssay Description:Binding affinity to human biotinylated AviTag GKRP assessed as inhibition of protein interaction with fluorescein tagged human glucokinase by AlphaSc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351937(CHEMBL1821827)
Affinity DataIC50:  11nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50448559(CHEMBL3127352)
Affinity DataIC50:  12nMAssay Description:Inhibition of biotin-tagged human GKRP-fluorescein-tagged human GK interaction preincubated for 20 mins followed by fluorescein-tagged human GK addit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447270(CHEMBL3113988)
Affinity DataIC50:  14nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351940(CHEMBL1821830)
Affinity DataIC50:  15nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHexokinase-4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50447269(CHEMBL3113989)
Affinity DataIC50:  16nMAssay Description:Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP incubated for 20 mins prior to addition of fluorescein-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351926(CHEMBL1821817)
Affinity DataIC50:  16nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351936(CHEMBL1821826)
Affinity DataIC50:  16nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50500205(CHEMBL3746456)
Affinity DataIC50:  17nMAssay Description:Binding affinity to human biotinylated AviTag GKRP assessed as inhibition of protein interaction with fluorescein tagged human glucokinase by AlphaSc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetGlucokinase regulatory protein(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50500201(CHEMBL3746034)
Affinity DataIC50:  18nMAssay Description:Binding affinity to human biotinylated AviTag GKRP assessed as inhibition of protein interaction with fluorescein tagged human glucokinase by AlphaSc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351935(CHEMBL1821728)
Affinity DataIC50:  18nMAssay Description:Inhibition of BACE1 in human HEK293 cells expressing APP with Swedish mutation assessed as amyloidbeta 40 level by sandwich ELISAMore data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50351930(CHEMBL1821821)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant BACE1 after 60 mins by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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