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TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090035(4-(3,4-Difluoro-phenyl)-1-methyl-2-oxo-1,2,3,4-tet...)
Affinity DataKi:  0.0680nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090023(4-(3,4-Difluoro-phenyl)-2-oxo-1,2,3,4-tetrahydro-p...)
Affinity DataKi:  0.0700nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Human)
Glaxosmithkline

LigandPNGBDBM8336(N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-...)
Affinity DataKi:  0.0800nM ΔG°:  -57.1kJ/molepH: 7.0 T: 22°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082825(4-(3,4-Difluoro-phenyl)-3-[5-(4-methoxycarbonyl-4-...)
Affinity DataKi:  0.100nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082792(4-Benzo[1,2,5]oxadiazol-5-yl-3-[3-(4-methoxycarbon...)
Affinity DataKi:  0.100nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082797(4-(3,4-Difluoro-phenyl)-3-[3-(4-methoxycarbonyl-4-...)
Affinity DataKi:  0.100nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082880(6-(3,4-Difluoro-phenyl)-2,4-dimethyl-1-[5-(4-o-tol...)
Affinity DataKi:  0.100nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50434787(CHEMBL2386635 | US10487083, Example C | US10703751...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of recombinant JAK1 (unknown origin) using Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins in presence of ATPMore data for this Ligand-Target Pair
TargetGlycogen synthase kinase-3 alpha(Human)
Glaxosmithkline

LigandPNGBDBM8337(N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-c]pyrida...)
Affinity DataKi:  0.110nM ΔG°:  -56.3kJ/molepH: 7.0 T: 22°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090032((R)-4-(3,4-Difluoro-phenyl)-1-methyl-2-oxo-1,2,3,4...)
Affinity DataKi:  0.120nMAssay Description:Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090010(4-(3,4-Difluoro-phenyl)-1,6-dimethyl-2-oxo-1,2,3,4...)
Affinity DataKi:  0.120nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090018(4-(3,4-Difluoro-phenyl)-2-oxo-1,2,3,4-tetrahydro-p...)
Affinity DataKi:  0.130nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090019(4-(3,4-Difluoro-phenyl)-3,6-dimethyl-2-oxo-1,2,3,4...)
Affinity DataKi:  0.140nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090042(4-(3,4-Difluoro-phenyl)-6-methoxymethyl-2-oxo-1,2,...)
Affinity DataKi:  0.140nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090036(4-(3,4-Difluoro-phenyl)-2-oxo-1,2,3,4-tetrahydro-p...)
Affinity DataKi:  0.160nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090025(4-(3,4-Difluoro-phenyl)-2-oxo-1,2,3,4-tetrahydro-p...)
Affinity DataKi:  0.170nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090031(4-(3,4-Difluoro-phenyl)-2-oxo-1,2,3,4-tetrahydro-p...)
Affinity DataKi:  0.170nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090015(4-(3,4-Difluoro-phenyl)-6-methyl-2-oxo-1,2,3,4-tet...)
Affinity DataKi:  0.170nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090016(4-(3,4-Difluoro-phenyl)-1-methyl-2-oxo-1,2,3,4-tet...)
Affinity DataKi:  0.180nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090017((R)-4-(3,4-Difluoro-phenyl)-1,6-dimethyl-2-oxo-1,2...)
Affinity DataKi:  0.180nMAssay Description:Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090027((R)-4-(3,4-Difluoro-phenyl)-1,3,6-trimethyl-2-oxo-...)
Affinity DataKi:  0.180nMAssay Description:Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082790(1-(3-{[5-Carbamoyl-4-ethyl-6-(4-nitro-phenyl)-2-ox...)
Affinity DataKi:  0.190nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of humanMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Human)
Glaxosmithkline

LigandPNGBDBM8339(N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-c]pyrida...)
Affinity DataKi:  0.190nM ΔG°:  -54.9kJ/molepH: 7.0 T: 22°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082790(1-(3-{[5-Carbamoyl-4-ethyl-6-(4-nitro-phenyl)-2-ox...)
Affinity DataKi:  0.200nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082784(1-(3-{[5-Carbamoyl-6-(3,4-difluoro-phenyl)-4-ethyl...)
Affinity DataKi:  0.200nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082784(1-(3-{[5-Carbamoyl-6-(3,4-difluoro-phenyl)-4-ethyl...)
Affinity DataKi:  0.200nMAssay Description:In vitro binding affinity radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50366618(CHEMBL448620 | SNAP-5089)
Affinity DataKi:  0.200nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082798(4-(2,4-Difluoro-phenyl)-3-[3-(4-methoxycarbonyl-4-...)
Affinity DataKi:  0.200nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082794(1-(3-{[5-Carbamoyl-6-(2,4-difluoro-phenyl)-4-ethyl...)
Affinity DataKi:  0.200nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082790(1-(3-{[5-Carbamoyl-4-ethyl-6-(4-nitro-phenyl)-2-ox...)
Affinity DataKi:  0.200nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082784(1-(3-{[5-Carbamoyl-6-(3,4-difluoro-phenyl)-4-ethyl...)
Affinity DataKi:  0.210nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of humanMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090043(4-(3,4-Difluoro-phenyl)-6-methoxymethyl-2-oxo-1,2,...)
Affinity DataKi:  0.240nMAssay Description:Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090014(4-(3,4-Difluoro-phenyl)-6-methyl-2-oxo-1,2,3,4-tet...)
Affinity DataKi:  0.25nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50341447(4-[(4-Chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(h...)
Affinity DataKi:  0.251nMAssay Description:Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082872(6-(3,4-Difluoro-phenyl)-1-{5-[4-(2-methoxy-phenyl)...)
Affinity DataKi:  0.300nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082801(3-[3-(4-Methoxycarbonyl-4-phenyl-piperidin-1-yl)-p...)
Affinity DataKi:  0.300nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50434786(CHEMBL2386636)
Affinity DataKi:  0.300nMAssay Description:Inhibition of recombinant JAK1 (unknown origin) using Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins in presence of ATPMore data for this Ligand-Target Pair
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090012(4-(3,4-Difluoro-phenyl)-1,3-dimethyl-2-oxo-1,2,3,4...)
Affinity DataKi:  0.300nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50205359(CHEMBL3917428)
Affinity DataKi:  0.316nMAssay Description:Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082865(6-(3,4-Difluoro-phenyl)-1-[5-(4,4-diphenyl-piperid...)
Affinity DataKi:  0.330nMAssay Description:Binding affinity against isolated human prostate using [3H]- prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090029(4-(3,4-Difluoro-phenyl)-1,6-dimethyl-2-oxo-1,2,3,4...)
Affinity DataKi:  0.390nMAssay Description:Evaluated for the ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50090020(4-(3,4-Difluoro-phenyl)-6-methyl-2-oxo-1,2,3,4-tet...)
Affinity DataKi:  0.390nMAssay Description:Ability to displace [125I]- HEAT from human cloned Alpha-1A adrenergic receptor stably expressed in CHO cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50205360(CHEMBL3921827)
Affinity DataKi:  0.398nMAssay Description:Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082870(6-(3,4-Difluoro-phenyl)-2,4-dimethyl-1-[5-(4-pheny...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082865(6-(3,4-Difluoro-phenyl)-1-[5-(4,4-diphenyl-piperid...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataKi:  0.400nMAssay Description:Inhibition of JAK3 (unknown origin) using Leu-Pro-Leu-Asp-Lys-Asp-Tyr-Tyr-Val-Val-Arg as substrate after 30 mins in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082875(1-[5-(4-Cyano-4-phenyl-piperidin-1-yl)-pentyl]-6-(...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082873(6-(3,4-Difluoro-phenyl)-1-{5-[4-(2-methoxy-phenyl)...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50082879(1-[5-(4-Cyano-4-phenyl-piperidin-1-yl)-pentyl]-6-(...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity against Alpha-1A adrenergic receptor (recombinant human receptor) using [3H]prazosin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A adrenergic receptor(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50366618(CHEMBL448620 | SNAP-5089)
Affinity DataKi:  0.400nMAssay Description:In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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