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Found 1420 with Last Name = 'graham' and Initial = 'th'
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50443348(CHEMBL3086040 | US8669252, 12)
Affinity DataIC50:  0.0790nMAssay Description:Inhibition of recombinant human PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551542(US11312719, Example 88)
Affinity DataIC50:  0.100nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50443348(CHEMBL3086040 | US8669252, 12)
Affinity DataIC50:  0.160nMAssay Description:The potency of compounds of formula I against PrCP was determined by a fluorescence intensity kinetic assay measuring the IC50 values of PrCP inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50443351(CHEMBL3086037 | US8669252, 15)
Affinity DataIC50:  0.180nMAssay Description:The potency of compounds of formula I against PrCP was determined by a fluorescence intensity kinetic assay measuring the IC50 values of PrCP inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM119411(US8669252, 43)
Affinity DataIC50:  0.180nMAssay Description:The potency of compounds of formula I against PrCP was determined by a fluorescence intensity kinetic assay measuring the IC50 values of PrCP inhibit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50443351(CHEMBL3086037 | US8669252, 15)
Affinity DataIC50:  0.180nMAssay Description:Inhibition of recombinant human PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382899(CHEMBL2022787)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551571(US11312719, Example 117)
Affinity DataIC50:  0.200nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551564(1-(4-((2S,5R)-5-(5-amino-8-chloro-9-fluoro-[1,2,4]...)
Affinity DataIC50:  0.200nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50383421(CHEMBL2031595)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of mouse PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551543(US11312719, Example 89)
Affinity DataIC50:  0.200nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382913(CHEMBL2023210)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382904(CHEMBL2022793)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50443348(CHEMBL3086040 | US8669252, 12)
Affinity DataIC50:  0.280nMAssay Description:Inhibition of recombinant mouse PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551504(US11312719, Example 49)
Affinity DataIC50:  0.300nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551476((R)-1-(4-(3-(5-amino-9-fluoro-8-methoxy-[1,2,4]tri...)
Affinity DataIC50:  0.300nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50609742(CHEMBL5286106)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of LRRK2 in human PBMCs assessed as reduction in Ser95 phosphorylationMore data for this Ligand-Target Pair
Ligand Info
In DepthDetails PubMed
LigandPNGBDBM50609742(CHEMBL5286106)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of GST20-tagged LRRK2 in human SH-SY5Y cells assessed as reduction in pSer935 phosphorylation incubated for 90 mins by MSD assayMore data for this Ligand-Target Pair
Ligand Info
In DepthDetails PubMed
LigandPNGBDBM50609728(CHEMBL5267350)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
Ligand Info
In DepthDetails PubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551576(2-(4-((2R or 2S,5R or 5S)-5-(5-amino-9-fluoro-7-me...)
Affinity DataIC50:  0.300nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382906(CHEMBL2023202)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382913(CHEMBL2023210)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of mouse PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382906(CHEMBL2023202)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50361786(CHEMBL1938522)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant human PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by continuous fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551580(US11312719, Example 126 | US11312719, Example 127 ...)
Affinity DataIC50:  0.300nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551576(2-(4-((2R or 2S,5R or 5S)-5-(5-amino-9-fluoro-7-me...)
Affinity DataIC50:  0.300nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551540((S or R)-3-(4-((R)-3-(5-amino-9-fluoro-7-methoxy-[...)
Affinity DataIC50:  0.300nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551485((R)-1-(4-(3-(5-amino-9-fluoro-7-methoxy-[1,2,4]tri...)
Affinity DataIC50:  0.400nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551678((2S,3S or 2R,3R)-3-(4-((3R,5S or 3S,5R)-3-(5-amino...)
Affinity DataIC50:  0.400nMAssay Description:The ability of compounds to antagonize human A2A and A2B adenosine receptors was determined using a kit to measure changes in intracellular cyclic AM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551666((2S,3S or 2R,3R)-3-(4-((3R,5S or 3S,5R)-3-(5-amino...)
Affinity DataIC50:  0.400nMAssay Description:The ability of compounds to antagonize human A2A and A2B adenosine receptors was determined using a kit to measure changes in intracellular cyclic AM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551678((2S,3S or 2R,3R)-3-(4-((3R,5S or 3S,5R)-3-(5-amino...)
Affinity DataIC50:  0.400nMAssay Description:The ability of compounds to antagonize human A2A and A2B adenosine receptors was determined using a kit to measure changes in intracellular cyclic AM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551540((S or R)-3-(4-((R)-3-(5-amino-9-fluoro-7-methoxy-[...)
Affinity DataIC50:  0.400nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382906(CHEMBL2023202)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of mouse PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382905(CHEMBL2022794)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551524(1-(4-((3R,5S or 3S,5R)-3-(5-amino-9-fluoro-7-metho...)
Affinity DataIC50:  0.400nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551566(1-(4-((2S,5R)-5-(5-amino-9-fluoro-8-methyl-[1,2,4]...)
Affinity DataIC50:  0.400nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50383421(CHEMBL2031595)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50361774(CHEMBL1938510)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of recombinant mouse PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by continuous fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50609741(CHEMBL5284341)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of GST20-tagged LRRK2 in human SH-SY5Y cells assessed as reduction in pSer935 phosphorylation incubated for 90 mins by MSD assayMore data for this Ligand-Target Pair
Ligand Info
In DepthDetails PubMed
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50383427(CHEMBL2031588)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of mouse PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382906(CHEMBL2023202)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of mouse PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50383425(CHEMBL2031590)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of mouse PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382912(CHEMBL2023209 | US8569299, 4)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382910(CHEMBL2023207)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human PrCPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM257207(US9493440, 51)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
TargetLysosomal Pro-X carboxypeptidase(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50382912(CHEMBL2023209 | US8569299, 4)
Affinity DataIC50:  0.5nMpH: 5.5 T: 2°CAssay Description:The potency of compounds against PRCP was determined by a fluorescence intensity kinetic assay measuring the IC50 values of PRCP inhibitor test compo...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551643((2S,3S or 2R,3R)-3-(4-((R)-3-(5-amino-9-fluoro-7- ...)
Affinity DataIC50:  0.5nMAssay Description:The ability of compounds to antagonize human A2A and A2B adenosine receptors was determined using a kit to measure changes in intracellular cyclic AM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551666((2S,3S or 2R,3R)-3-(4-((3R,5S or 3S,5R)-3-(5-amino...)
Affinity DataIC50:  0.5nMAssay Description:The ability of compounds to antagonize human A2A and A2B adenosine receptors was determined using a kit to measure changes in intracellular cyclic AM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551464((R)-1-(4-(3-(5-amino-9-fluoro-8-methoxy-[1,2,4]tri...)
Affinity DataIC50:  0.5nMAssay Description:148 μL (5 μg/mL) membranes (Perkin Elmer, Cat. No. RBHA2aM400UA) and 2 μL compounds of the invention to be tested (test compound) were...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAdenosine receptor A2a(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM551674((2S,3S or 2R,3R)-3-(4-((3R,5S or 3S,5R)-3-(5-amino...)
Affinity DataIC50:  0.5nMAssay Description:The ability of compounds to antagonize human A2A and A2B adenosine receptors was determined using a kit to measure changes in intracellular cyclic AM...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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