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Found 138 with Last Name = 'auberson' and Initial = 'y'
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159251(US9034874, 2.2)
Affinity DataKi:  0.5nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159252(US9034874, 2.3)
Affinity DataKi:  0.900nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159248(US9034874, 1.5)
Affinity DataKi:  1.10nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159253(US9034874, 3.1)
Affinity DataKi:  1.20nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159246(US9034874, 1.3)
Affinity DataKi:  1.20nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159244(US9034874, 1.1)
Affinity DataKi:  1.30nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159253(US9034874, 3.1)
Affinity DataKi:  1.60nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50198702((E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-en...)
Affinity DataKi:  1.70nMAssay Description:Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50198702((E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-en...)
Affinity DataKi:  1.80nMAssay Description:Displacement of [3H]ABP688 from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159247(US9034874, 1.4)
Affinity DataKi:  2.30nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159245(US9034874, 1.2)
Affinity DataKi:  2.40nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159249(US9034874, 1.6)
Affinity DataKi:  2.90nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159250(US9034874, 2.1)
Affinity DataKi:  3.10nMAssay Description:The potency of compounds of the invention as H3 receptor antagonists can be assessed by measuring the blockade of (R)-alpha-methylhistamine-mediated ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50198702((E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-en...)
Affinity DataKi:  3.5nMAssay Description:Displacement of [3H]M-MPEP from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159246(US9034874, 1.3)
Affinity DataKi:  10nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50123005(2-(3-Methoxy-phenylethynyl)-6-methyl-pyridine | 2-...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50123005(2-(3-Methoxy-phenylethynyl)-6-methyl-pyridine | 2-...)
Affinity DataKi:  11nMAssay Description:Displacement of [3H]ABP688 from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159252(US9034874, 2.3)
Affinity DataKi:  12nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]ABP688 from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159250(US9034874, 2.1)
Affinity DataKi:  20nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159248(US9034874, 1.5)
Affinity DataKi:  25nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159251(US9034874, 2.2)
Affinity DataKi:  25nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159247(US9034874, 1.4)
Affinity DataKi:  25nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159244(US9034874, 1.1)
Affinity DataKi:  26nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159245(US9034874, 1.2)
Affinity DataKi:  31nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H3 receptor(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM159249(US9034874, 1.6)
Affinity DataKi:  44nMpH: 7.5Assay Description:The affinity of compounds of the invention to the H3 receptor can be assessed by measuring displacement of binding of the radioligand [3H]-N-alpha -M...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50094186((-)1aS,7aS -2-Hydroxyimino-1a,2-dihydro-1H-7-oxa-c...)
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]ABP688 from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50094186((-)1aS,7aS -2-Hydroxyimino-1a,2-dihydro-1H-7-oxa-c...)
Affinity DataKi: >1.00E+5nMAssay Description:Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1/2A(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50451503(CHEMBL12513)
Affinity DataIC50:  0.200nMAssay Description:Inhibitory activity against Xenopus laevis oocyte expressing 1A/2B heteromeric human NMDA (hNMDA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1/2B(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50451505(CHEMBL274422)
Affinity DataIC50:  0.700nMAssay Description:Inhibitory activity against Xenopus laevis oocyte expressing 1A/2B heteromeric human NMDA (hNMDA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1/2A(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50451505(CHEMBL274422)
Affinity DataIC50:  1.10nMAssay Description:Inhibitory activity against Xenopus laevis oocyte expressing 1A/2B heteromeric human NMDA (hNMDA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtaxin-1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM475941(US10865195, Compound 6)
Affinity DataIC50:  1.40nMAssay Description:ATX activity was determined by measurement of released choline in reactions containing ATX (10 nM), choline oxidase (0.1 U/ml), HRP (100 U/ml), ample...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 1/2B(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50451503(CHEMBL12513)
Affinity DataIC50:  1.80nMAssay Description:Inhibitory activity against Xenopus laevis oocyte expressing 1A/2A heteromeric human NMDA (hNMDA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtaxin-1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM475938(US10865195, Compound 4)
Affinity DataIC50:  2nMAssay Description:ATX activity was determined by measurement of released choline in reactions containing ATX (10 nM), choline oxidase (0.1 U/ml), HRP (100 U/ml), ample...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50198702((E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-en...)
Affinity DataIC50:  2.30nMAssay Description:Activity at human recombinant mGluR5 expressed in L(tk-) cells assessed as inhibition of glutamate-induced calcium releaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50198702((E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-en...)
Affinity DataIC50:  2.40nMAssay Description:Activity at human recombinant mGluR5 expressed in L(tk-) cells assessed as inhibition of quisqualate-induced phosphoinositol accumulationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtaxin-1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM418800(US10450298, Compound CHEM-US-00033 | US10450298, C...)
Affinity DataIC50:  3nMAssay Description:ATX activity was determined by measurement of released choline in reactions containing ATX (10 nM), choline oxidase (0.1 U/ml), HRP (100 U/ml), ample...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAtaxin-1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM418917(US10450298, Compound CHEM-US-00035 | US10865195, C...)
Affinity DataIC50:  4nMAssay Description:ATX activity was determined by measurement of released choline in reactions containing ATX (10 nM), choline oxidase (0.1 U/ml), HRP (100 U/ml), ample...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 1/2A(Homo sapiens (Human))
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50451498(CHEMBL536107)
Affinity DataIC50:  4.20nMAssay Description:Inhibitory activity against Xenopus laevis oocyte expressing 1A/2B heteromeric human NMDA (hNMDA) receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtaxin-1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM418916(US10450298, Compound CHEM-US-00034 | US10865195, C...)
Affinity DataIC50:  5nMAssay Description:ATX activity was determined by measurement of released choline in reactions containing ATX (10 nM), choline oxidase (0.1 U/ml), HRP (100 U/ml), ample...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
University Hospital Zurich

Curated by ChEMBL
LigandPNGBDBM50073922(CHEMBL86313 | {(S)-1-[(7-Bromo-2,3-dioxo-1,2,3,4-t...)
Affinity DataIC50:  5nMAssay Description:Compound was evaluated for its binding affinity for the glycine binding site on N-methyl-D-aspartate glutamate receptor by using [3H]-MDL-105,519 bin...More data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
University Hospital Zurich

Curated by ChEMBL
LigandPNGBDBM50084064(CHEMBL167952 | {(S)-1-[(7-Chloro-2,3-dioxo-1,2,3,4...)
Affinity DataIC50:  6nMAssay Description:Compound was evaluated for its binding affinity for the glycine binding site on N-methyl-D-aspartate glutamate receptor by using [3H]-MDL-105,519 bin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtaxin-1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM418919(US10450298, Compound CHEM-US-00037 | US10865195, C...)
Affinity DataIC50:  6nMAssay Description:ATX activity was determined by measurement of released choline in reactions containing ATX (10 nM), choline oxidase (0.1 U/ml), HRP (100 U/ml), ample...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 1(RAT)
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50069471(CHEMBL357190 | N-(7-Bromo-2,3-dioxo-1,2,3,4-tetrah...)
Affinity DataIC50:  7nMAssay Description:In vitro binding assay for the displacement of [3H]MDL-105519 from the glycine-site of NMDA receptorsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50198702((E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-en...)
Affinity DataIC50:  7nMAssay Description:Displacement of [3H]M-MPEP from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
University Hospital Zurich

Curated by ChEMBL
LigandPNGBDBM50073930(CHEMBL82963 | {(S)-1-[(2,3-Dioxo-7-trifluoromethyl...)
Affinity DataIC50:  8nMAssay Description:Compound was evaluated for its binding affinity for the glycine binding site on N-methyl-D-aspartate glutamate receptor by using [3H]-MDL-105,519 bin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
University Hospital Zurich

Curated by ChEMBL
LigandPNGBDBM50084062(CHEMBL354295 | {(S)-1-[(7-Iodo-2,3-dioxo-1,2,3,4-t...)
Affinity DataIC50:  8nMAssay Description:Compound was evaluated for its binding affinity for the glycine binding site on N-methyl-D-aspartate glutamate receptor by using [3H]-MDL-105,519 bin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
University Hospital Zurich

Curated by ChEMBL
LigandPNGBDBM50084063(CHEMBL162675 | {(S)-1-[(7-Fluoro-2,3-dioxo-1,2,3,4...)
Affinity DataIC50:  9nMAssay Description:Compound was evaluated for its binding affinity for the glycine binding site on N-methyl-D-aspartate glutamate receptor by using [3H]-MDL-105,519 bin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1(RAT)
Novartis Pharma

Curated by ChEMBL
LigandPNGBDBM50069458(CHEMBL147895 | N-(7-Bromo-2,3-dioxo-1,2,3,4-tetrah...)
Affinity DataIC50:  10nMAssay Description:In vitro binding assay for the displacement of [3H]MDL-105519 from the glycine-site of NMDA receptorsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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