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Found 477 with Last Name = 'humphrey' and Initial = 'j'
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM29568(CHEMBL2 | PRAZOSIN | PRAZOSIN HYDROCHLORIDE | [3H]...)
Affinity DataKi:  0.160nMAssay Description:Compound was tested for the inhibition of [3H]prazosin binding Alpha-1 adrenergic receptor of crude rat brain membrane.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361649(CHEMBL1938415)
Affinity DataKi:  0.600nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361648(CHEMBL1940246)
Affinity DataKi:  0.600nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361642(CHEMBL1940251)
Affinity DataKi:  0.700nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361641(CHEMBL1940247)
Affinity DataKi:  0.900nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361652(CHEMBL1940250)
Affinity DataKi:  1nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361650(CHEMBL1940248)
Affinity DataKi:  1.30nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361644(CHEMBL1940253)
Affinity DataKi:  1.40nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361643(CHEMBL1940252)
Affinity DataKi:  1.40nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50016897(2-(2,6-dichloroanilino)-1,3-diazacyclopentene-(2) ...)
Affinity DataKi:  1.70nMAssay Description:Compound was tested for the inhibition of [3H]clonidine binding Alpha-2 adrenergic receptor of crude rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361653(CHEMBL1940245)
Affinity DataKi:  2nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361651(CHEMBL1940249)
Affinity DataKi:  2.5nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14768((R)-6,7-Dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrol...)
Affinity DataKi:  4nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50026847(1-[2-(6,7-Dimethoxy-isochroman-1-yl)-ethyl]-4-(4-f...)
Affinity DataKi:  4nMAssay Description:Compound was tested for the inhibition of [3H]prazosin binding alpha-1-adrenergic receptor of crude rat brain membrane.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50223655(CHEMBL160763)
Affinity DataKi:  4nMAssay Description:Compound was tested for the inhibition of [3H]prazosin binding Alpha-2 adrenergic receptor of crude rat brain membrane.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Rattus norvegicus)
Pfizer

Curated by ChEMBL
LigandPNGBDBM107767(US11419874, PF-05180999 | US8598155, 2)
Affinity DataKi:  4.20nMAssay Description:Displacement of radiolabeled 4-(azetidin-1-yl)-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-1-(tritritiomethyl)pyrazolo[3,4-d]pyrimidine from PD...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM31046(3-[4,5-dihydro-1H-imidazol-2-ylmethyl-(4-methylphe...)
Affinity DataKi:  9.30nMAssay Description:Compound was tested for the inhibition of [3H]clonidine binding Alpha-2 adrenergic receptor of crude rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlpha-1A/Alpha-1B/Alpha-1D adrenergic receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM31046(3-[4,5-dihydro-1H-imidazol-2-ylmethyl-(4-methylphe...)
Affinity DataKi:  9.80nMAssay Description:Compound was tested for the inhibition of [3H]prazosin binding Alpha-1 adrenergic receptor of crude rat brain membrane.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361651(CHEMBL1940249)
Affinity DataKi:  10nMAssay Description:Inhibition of His-tagged AKT1 using 5FAM-GRPRTSSFAEGCONH2 as substrate by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14760((R)-6,7-Dimethoxy-4-[3-(naphthalen-2-yloxy)-pyrrol...)
Affinity DataKi:  12nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
LigandPNGBDBM14764((R)-6,7-Dimethoxy-4-[3-(quinolin-6-yloxy)-pyrrolid...)
Affinity DataKi:  12nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14766((R)-6,7-Dimethoxy-4-[3-(quinolin-7-yloxy)-pyrrolid...)
Affinity DataKi:  12nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14763((R)-6,7-Dimethoxy-4-[3-(7-methoxy-naphthalen-2-ylo...)
Affinity DataKi:  17nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14754(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)
Affinity DataKi:  17nM ΔG°:  -43.9kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
LigandPNGBDBM14762((R)-6,7-Dimethoxy-4-[3-(6-methoxy-naphthalen-2-ylo...)
Affinity DataKi:  18nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14765((R)-6,7-Dimethoxy-4-[3-(2-methyl-quinolin-6-yloxy)...)
Affinity DataKi:  18nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14767((R)-4-[3-(Isoquinolin-3-yloxy)-pyrrolidin-1-yl]-6,...)
Affinity DataKi:  19nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14755(6,7-dimethoxy-4-[8-(4-methylpiperazin-1-yl)sulfony...)
Affinity DataKi:  25nM ΔG°:  -43.0kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361647(CHEMBL1940244)
Affinity DataKi:  35nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
LigandPNGBDBM14756((R)-4-[3-(5-Chloro-pyrimidin-2-yloxy)-pyrrolidin-1...)
Affinity DataKi:  44nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14761((R)-6,7-Dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrol...)
Affinity DataKi:  48nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14748((R)-4-[3-(4-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi:  54nM ΔG°:  -41.1kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14745((R)-4-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidi...)
Affinity DataKi:  56nM ΔG°:  -41.0kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3B(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14761((R)-6,7-Dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrol...)
Affinity DataKi:  56nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14751((R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi:  61nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50026847(1-[2-(6,7-Dimethoxy-isochroman-1-yl)-ethyl]-4-(4-f...)
Affinity DataKi:  62nMAssay Description:Compound was tested for the inhibition of [3H]clonidine binding Alpha-2 adrenergic receptor of crude rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14753((R)-4-[3-(3,4-Dimethoxy-phenoxy)-pyrrolidin-1-yl]-...)
Affinity DataKi:  67nM ΔG°:  -40.5kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14752((R)-4-[3-(Indan-5-yloxy)-pyrrolidin-1-yl]-6,7-dime...)
Affinity DataKi:  68nM ΔG°:  -40.5kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14757((R)-6,7-Dimethoxy-4-[3-(pyridin-2-yloxy)-pyrrolidi...)
Affinity DataKi:  77nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3B(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14751((R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi:  88nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14751((R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi:  94nM ΔG°:  -39.7kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14741((R)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrroli...)
Affinity DataKi: <100nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361646(CHEMBL1940243)
Affinity DataKi:  100nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361652(CHEMBL1940250)
Affinity DataKi:  100nMAssay Description:Inhibition of His-tagged AKT1 using 5FAM-GRPRTSSFAEGCONH2 as substrate by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14747((R)-4-[3-(4-tert-Butyl-phenoxy)-pyrrolidin-1-yl]-6...)
Affinity DataKi:  100nM ΔG°:  -39.6kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14739((R)-6,7-Dimethoxy-4-[3-(2-trifluoromethyl-phenoxy)...)
Affinity DataKi: <100nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14740((R)-6,7-Dimethoxy-4-(3-o-tolyloxy-pyrrolidin-1-yl)...)
Affinity DataKi: <100nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14742((S)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrroli...)
Affinity DataKi: >100nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14743((R)-4-[3-(2-Chloro-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi: <100nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14744((R)-2-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidi...)
Affinity DataKi: <100nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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