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Found 578 with Last Name = 'brugel' and Initial = 'ta'
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50130561((R)-N-((S)-1-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dime...)
Affinity DataKi:  0.300nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327257(3-(1-(cyclopropylmethyl)piperidin-4-yloxy)-N-(3-(3...)
Affinity DataKi:  0.5nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM82551(C18130 | CAS_105618-26-6 | NOR-BNI (HCI)2 | NORBNI)
Affinity DataKi:  0.900nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50325855(CHEMBL1223951 | exo-3-((1R,3s,5S)-8-benzyl-8-azabi...)
Affinity DataKi:  40nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327259(3-(1-benzylpiperidin-4-yloxy)benzamide | CHEMBL125...)
Affinity DataKi:  75nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327258(3-(1-(cyclopropylmethyl)piperidin-4-yloxy)benzamid...)
Affinity DataKi:  146nMAssay Description:Binding affinity to kappa opioid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50156071(3-Cyano-N-(2,5-diphenyl-2H-pyrazol-3-yl)-benzamide...)
Affinity DataKi:  250nMAssay Description:Displacement of [3H]-MPEP from human mGluR5More data for this Ligand-Target Pair
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50331975(1-(4-(2-chloro-4-fluorophenyl)piperazin-1-yl)-2-(p...)
Affinity DataKi:  2.37E+3nMAssay Description:Displacement of [3H]-MPEP from human mGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327248(CHEMBL1257821 | endo-3-(8-(4-methylbenzyl)-8-azabi...)
Affinity DataIC50:  0.140nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327247(CHEMBL1257820 | endo-3-(8-(3-phenylpropyl)-8-azabi...)
Affinity DataIC50:  0.25nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327244(3-Endo-(8-((5-methylthiophen-2-yl)methyl)-8-azabic...)
Affinity DataIC50:  0.260nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327246(CHEMBL1257698 | endo-3-(8-phenethyl-8-azabicyclo[3...)
Affinity DataIC50:  0.380nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Procter and Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50474810(CHEMBL92082)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of LPS-stimulated p38-related TNF-alpha production in human peripheral blood mononuclear cells (PBMC)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327243(CHEMBL1257577 | endo-3-(8-(thiophen-2-ylmethyl)-8-...)
Affinity DataIC50:  0.430nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50130561((R)-N-((S)-1-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dime...)
Affinity DataIC50:  0.5nMAssay Description:Antagonist activity at human kappa opioid receptor assessed as inhibition of dynorphin A-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327249(CHEMBL1257937 | endo-3-(8-(3-methylbenzyl)-8-azabi...)
Affinity DataIC50:  0.520nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50325855(CHEMBL1223951 | exo-3-((1R,3s,5S)-8-benzyl-8-azabi...)
Affinity DataIC50:  0.610nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327250(CHEMBL1257938 | endo-3-(8-(2-methylbenzyl)-8-azabi...)
Affinity DataIC50:  0.620nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327256(CHEMBL1258280 | endo-3-(8-(benzo[d][1,3]dioxol-5-y...)
Affinity DataIC50:  0.620nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327264(CHEMBL1258503 | endo-3-(8-(2-oxo-2-(phenylamino)et...)
Affinity DataIC50:  0.720nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Procter and Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50474810(CHEMBL92082)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of LPS-stimulated p38-related IL1-beta production in human peripheral blood mononuclear cells (PBMC)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM158387(US9029381, 29)
Affinity DataIC50:  0.834nMAssay Description:The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327268(CHEMBL1258725 | endo-3-(8-(1,2,3,4-tetrahydronapht...)
Affinity DataIC50:  0.950nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460344(CHEMBL4228859)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460371(CHEMBL4228975)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460368(CHEMBL4226039)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460377(CHEMBL4225587)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460356(CHEMBL4224734)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460357(CHEMBL4226364)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM158386(US9029381, 28)
Affinity DataIC50:  1.37nMAssay Description:The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327251(CHEMBL1258047 | endo-3-(8-(pyridin-4-ylmethyl)-8-a...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327266(CHEMBL1258616 | endo-3-(8-(1-(5-methylthiophen-2-y...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM158358(US9029381, 10 | US9029381, 11 | US9029381, 12)
Affinity DataIC50:  1.63nMAssay Description:The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327274(CHEMBL1257227 | endo-3-(8-((S)-1-phenylethyl)-8-az...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327253(CHEMBL1258164 | endo-3-(8-(pyridin-2-ylmethyl)-8-a...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Procter and Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50474826(CHEMBL330282)
Affinity DataIC50:  2nMAssay Description:Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327255(CHEMBL1258279 | endo-3-(8-(cyclohexylmethyl)-8-aza...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460353(CHEMBL4225116)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Procter And Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50188343(4-(2,6-dichloro-phenyl)-8-[4-(2-diethylamino-ethox...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant Lck in presence of 10 mM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM82551(C18130 | CAS_105618-26-6 | NOR-BNI (HCI)2 | NORBNI)
Affinity DataIC50:  2.10nMAssay Description:Antagonist activity at human kappa opioid receptor assessed as inhibition of dynorphin A-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM82551(C18130 | CAS_105618-26-6 | NOR-BNI (HCI)2 | NORBNI)
Affinity DataIC50:  2.10nMAssay Description:Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327245(CHEMBL1255595 | endo-3-(8-((5-methylfuran-2-yl)met...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50327275(CHEMBL1257347 | endo-3-(8-((R)-1-(5-methylthiophen...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Procter And Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50195334(3-(2-(1H-benzo[d]imidazol-1-yl)-6-(2-(diethylamino...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant Lck by ProFlour assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460375(CHEMBL4225641)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Procter And Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50195351(1-(3-(2,5-dimethylbenzyl)-5-(3-cyclohexylpropyl)ph...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant Lck by ProFlour assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Procter And Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50195345(3-(2-(1H-benzo[d]imidazol-1-yl)-6-(4-methylpiperaz...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant Lck by ProFlour assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460355(CHEMBL4225853)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent glycine transporter 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50460354(CHEMBL4228817)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glyci...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Procter and Gamble Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50474810(CHEMBL92082)
Affinity DataIC50:  3nMAssay Description:Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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