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Found 683 with Last Name = 'desrayaud' and Initial = 's'
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50336921(3-chloro-5-(7-chloro-1-propyl-1H-benzo[d]imidazol-...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [3H]ABP688 from human recombinant mGlu5 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50336921(3-chloro-5-(7-chloro-1-propyl-1H-benzo[d]imidazol-...)
Affinity DataKi:  30nMAssay Description:Displacement of [3H]ABP688 from mGlu5 receptor in rat brain tissueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
TBA

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
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50392323(CHEMBL2153782)
Affinity DataKi:  43nMAssay Description:Displacement of [3H]ABP688 from human mGluR5a transmembrane region expressed in mouse L(tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin E(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305527((4S)-4-[(1R)-1-hydroxy-2-({1-[3-(1-methylethyl)phe...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of cathepsin EMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305542(CHEMBL595016 | Propane-1-sulfonic acid{(S)-4-[(R)-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant BACE1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305544((S)-4-{(R)-1-Hydroxy-2-[1-(3-isopropyl-phenyl)-cyc...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant BACE1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin D(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305527((4S)-4-[(1R)-1-hydroxy-2-({1-[3-(1-methylethyl)phe...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cathepsin DMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin D(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50294218((3S,14R,16S)-16-((R)-1-hydroxy-2-((S)-6-isopropyl-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human cathepsin DMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  1.90nMAssay Description:Displacement of Alexa Fluor labelled Tracer-314 from human N-terminal GST-tagged mTOR incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386487(CHEMBL2048047)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386513(CHEMBL2048051)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386515(CHEMBL2048053)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305531(CHEMBL595136 | Propane-1-sulfonic acid((S)-4-{(R)-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386481(CHEMBL2048058)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM16047((4S)-4-[(2S)-2-[(2R,4S,5S)-5-[(2S)-2-[(2S)-2-[(4S)...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50294218((3S,14R,16S)-16-((R)-1-hydroxy-2-((S)-6-isopropyl-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of BACE1More data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386482(CHEMBL2048059)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386512(CHEMBL2048050)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore 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
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
TargetCathepsin D(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305536((S)-4-{(R)-1-Hydroxy-2-[1-(3-isopropyl-phenyl)-cyc...)
Affinity DataIC50:  3nMAssay Description:Inhibition of cathepsin DMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386516(CHEMBL2048054)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112822(CHEMBL3609525)
Affinity DataIC50:  4nMAssay Description:Inhibition of N-terminal myristoylated human PI3Kalpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylatuion at Ser473 by ELISAMore data for this Ligand-Target Pair
TargetCathepsin E(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305537((S)-4-{(R)-1-Hydroxy-2-[1-(3-isopropyl-phenyl)-cyc...)
Affinity DataIC50:  4nMAssay Description:Inhibition of cathepsin EMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50392324(CHEMBL2153783)
Affinity DataIC50:  4nMAssay Description:Antagonist activity at human mGluR5a expressed in mouse L(tk-) cells assessed as inhibition of glutamate-induced Ca2+ influx by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112823(CHEMBL3609526)
Affinity DataIC50:  4nMAssay Description:Inhibition of N-terminal myristoylated human PI3Kalpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylatuion at Ser473 by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112820(CHEMBL3609523)
Affinity DataIC50:  4nMAssay Description:Inhibition of N-terminal myristoylated human PI3Kalpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylatuion at Ser473 by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112826(CHEMBL3609529)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...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
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
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112819(CHEMBL3609522)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin E(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305536((S)-4-{(R)-1-Hydroxy-2-[1-(3-isopropyl-phenyl)-cyc...)
Affinity DataIC50:  5nMAssay Description:Inhibition of cathepsin EMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112817(CHEMBL3609520)
Affinity DataIC50:  5nMAssay Description:Inhibition of N-terminal myristoylated human PI3Kalpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylatuion at Ser473 by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
TBA

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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112820(CHEMBL3609523)
Affinity DataIC50:  5nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112824(CHEMBL3609527)
Affinity DataIC50:  5nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112822(CHEMBL3609525)
Affinity DataIC50:  5nMAssay Description:Inhibition of PI3Kgamma (unknown origin) using PI or PIP2:PS as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112823(CHEMBL3609526)
Affinity DataIC50:  5nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...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
LigandPNGBDBM50437053(CHEMBL2403373)
Affinity DataIC50:  5nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  5.30nMAssay Description:Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386483(CHEMBL2048060)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112819(CHEMBL3609522)
Affinity DataIC50:  6nMAssay Description:Inhibition of N-terminal myristoylated human PI3Kalpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylatuion at Ser473 by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112821(CHEMBL3609524)
Affinity DataIC50:  6nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...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
LigandPNGBDBM50437056(CHEMBL2403369)
Affinity DataIC50:  6nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386508(CHEMBL2048045)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386507(CHEMBL2048044)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112822(CHEMBL3609525)
Affinity DataIC50:  6nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 h...More data for this Ligand-Target Pair
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