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Found 3235 with Last Name = 'chappie' and Initial = 'ta'
LigandPNGBDBM50398003(CHEMBL2180402)
Affinity DataKi:  0.100nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50398003(CHEMBL2180402)
Affinity DataKi:  0.100nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
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
LigandPNGBDBM50398012(CHEMBL2180422 | US8492392, 1-17)
Affinity DataKi:  0.630nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore 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
TargetD(2) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM21398(4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1...)
Affinity DataKi:  0.840nMAssay Description:In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]-spiperone displacement.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

LigandPNGBDBM50398013(CHEMBL2180421 | US8492392, K-2)
Affinity DataKi:  0.900nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore 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
LigandPNGBDBM50398011(CHEMBL2180423 | US8492392, O-2)
Affinity DataKi:  0.920nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50398004(CHEMBL2180401)
Affinity DataKi:  0.950nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore 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
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
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
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069035((7R,9aS)-7-Phenoxymethyl-2-phenyl-octahydro-pyrido...)
Affinity DataKi:  1.60nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069037((7R,9aS)-7-Phenoxymethyl-2-pyridin-2-yl-octahydro-...)
Affinity DataKi:  1.70nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069036((7S,9aS)-7-Phenoxymethyl-2-pyrimidin-2-yl-octahydr...)
Affinity DataKi:  1.70nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069036((7S,9aS)-7-Phenoxymethyl-2-pyrimidin-2-yl-octahydr...)
Affinity DataKi:  1.70nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More 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
LigandPNGBDBM50398008(CHEMBL2180426)
Affinity DataKi:  2nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069039((7S,9aS)-7-(4-Fluoro-phenoxymethyl)-2-(5-fluoro-py...)
Affinity DataKi:  2nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM119778(CHEMBL2180429 | US8691827, I-9)
Affinity DataKi:  2.20nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore 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
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069048((7R,9aS)-7-(4-Fluoro-phenoxymethyl)-2-pyrimidin-2-...)
Affinity DataKi:  2.80nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069034((7R,9aS)-2-(5-Chloro-pyridin-2-yl)-7-(4-fluoro-phe...)
Affinity DataKi:  3.20nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM21398(4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1...)
Affinity DataKi:  3.30nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069041((7R,9aS)-7-(4-Fluoro-phenoxymethyl)-2-(5-fluoro-py...)
Affinity DataKi:  3.40nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069047((7R,9aS)-7-Phenoxymethyl-2-pyrimidin-2-yl-octahydr...)
Affinity DataKi:  3.5nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069038(7-Phenoxymethyl-2-pyrimidin-2-yl-octahydro-pyrido[...)
Affinity DataKi:  3.80nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More 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
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
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069042((7R,9aS)-7-(4-Fluoro-phenoxymethyl)-2-(4-fluoro-ph...)
Affinity DataKi:  5.30nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.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
LigandPNGBDBM50398005(CHEMBL2180430 | US8691827, I-8)
Affinity DataKi:  15nMAssay Description:Inhibition of PDE10A by fluorescence polarization assayMore 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
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069043((7R,9aS)-7-(4-Methoxy-phenoxymethyl)-2-pyrimidin-2...)
Affinity DataKi:  18nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.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
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
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
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069049((7R,9aS)-7-(4-tert-Butyl-phenoxymethyl)-2-pyrimidi...)
Affinity DataKi:  20nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.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
TargetD(2) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069036((7S,9aS)-7-Phenoxymethyl-2-pyrimidin-2-yl-octahydr...)
Affinity DataKi:  38nMAssay Description:In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]-spiperone displacement.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069036((7S,9aS)-7-Phenoxymethyl-2-pyrimidin-2-yl-octahydr...)
Affinity DataKi:  38nMAssay Description:In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]-spiperone displacement.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50069044((7R,9aR)-7-(4-Fluoro-phenoxymethyl)-2-(5-fluoro-py...)
Affinity DataKi:  39nMAssay Description:In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]-spiperone displacment.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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