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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
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
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
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
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
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
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
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
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305056((R)-(5-chloro-6-(6-methylpyridin-3-ylamino)pyridin...)
Affinity DataKi:  30nMAssay Description:Displacement of [3H]ABP688 from mGluR5 in rat brain cortexMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305056((R)-(5-chloro-6-(6-methylpyridin-3-ylamino)pyridin...)
Affinity DataKi:  38nMAssay Description:Displacement of [3H]ABP688 from human recombinant mGluR5 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239101(US10195181, Example 2.2 | US9403810, 2.2)
Affinity DataIC50:  0.900nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239101(US10195181, Example 2.2 | US9403810, 2.2)
Affinity DataIC50:  0.900nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239117(US10195181, Example 22c | US9403810, 22)
Affinity DataIC50:  1.40nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239132(US9403810, 22c)
Affinity DataIC50:  1.40nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239094(US10195181, Example 1.3 | US9403810, 1.3)
Affinity DataIC50:  1.80nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239094(US10195181, Example 1.3 | US9403810, 1.3)
Affinity DataIC50:  1.80nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239092(US10195181, Example 1.1 | US9403810, 1.1)
Affinity DataIC50:  2.10nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239092(US10195181, Example 1.1 | US9403810, 1.1)
Affinity DataIC50:  2.10nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239099(US10195181, Example 2 | US9403810, 2)
Affinity DataIC50:  2.5nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239099(US10195181, Example 2 | US9403810, 2)
Affinity DataIC50:  2.5nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239091(US10195181, Example 1 | US9403810, 1)
Affinity DataIC50:  2.80nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239091(US10195181, Example 1 | US9403810, 1)
Affinity DataIC50:  2.80nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50437055(CHEMBL2403370)
Affinity DataIC50:  3nMAssay Description:Inhibition of human LRRK2 (1885 to 2132) using 5-Fluo-Ahx-RLGRDKYKTLRQIRQGNTK-OH as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239095(US10195181, Example 1.4 | US9403810, 1.4)
Affinity DataIC50:  3.20nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239095(US10195181, Example 1.4 | US9403810, 1.4)
Affinity DataIC50:  3.20nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50437061(CHEMBL2403377)
Affinity DataIC50:  4nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase 8(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50191770(CHEMBL3912476)
Affinity DataIC50:  4nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50437059(CHEMBL2403366)
Affinity DataIC50:  4nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50437051(CHEMBL2403375)
Affinity DataIC50:  4nMAssay Description:Inhibition of human LRRK2 (1885 to 2132) using 5-Fluo-Ahx-RLGRDKYKTLRQIRQGNTK-OH as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50437052(CHEMBL2403374)
Affinity DataIC50:  4nMAssay Description:Inhibition of human LRRK2 (1885 to 2132) using 5-Fluo-Ahx-RLGRDKYKTLRQIRQGNTK-OH as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305054(CHEMBL594767 | rac-(2-butylpiperidin-1-yl)(5-chlor...)
Affinity DataIC50:  5nMAssay Description:Antagonist activity at human mGluR5 assessed as inhibition of quisqualate-induced intracellular inositol phosphate accumulationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50437053(CHEMBL2403373)
Affinity DataIC50:  5nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239105(US10195181, Example 6 | US9403810, 6)
Affinity DataIC50:  5.70nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239105(US10195181, Example 6 | US9403810, 6)
Affinity DataIC50:  5.70nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 8(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50191681(CHEMBL3939592)
Affinity DataIC50:  6nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetE3 ubiquitin-protein ligase SMURF1 [420-757](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239096(US10195181, Example 1.5 | US9403810, 1.5)
Affinity DataIC50:  6nMT: 2°CAssay Description:For the biochemical assay panel, 50 nl of the test compounds, reference compounds and buffer/DMSO control are transferred to the respective wells of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239102(US10195181, Example 3 | US9403810, 3)
Affinity DataIC50:  6nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase SMURF1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM239096(US10195181, Example 1.5 | US9403810, 1.5)
Affinity DataIC50:  6nMAssay Description:To determine the HECT E3 ligase selectivity of the compounds, a panel of biochemical HECT E3 ligase autoubiquitinylation assays was employed (Smurf-1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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