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TargetProprotein convertase subtilisin/kexin type 7(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  0.120nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC7 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProprotein convertase subtilisin/kexin type 5(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  0.120nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC6 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuroendocrine convertase 2(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  0.360nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC2 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetType-2 angiotensin II receptor(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50156173((1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to AT2 receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFurin(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  1nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC1 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuroendocrine convertase 1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  2nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC3 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProprotein convertase subtilisin/kexin type 6(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  3.60nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC4 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRho-associated protein kinase 1(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM322155(US10183931, SLx-2119 | US10696660, SLx-2119 | US11...)
Affinity DataKi:  40nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetType-1 angiotensin II receptor(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50156173((1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-...)
Affinity DataKi:  1.00E+4nMAssay Description:Binding affinity to AT1 receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50241259((2S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetam...)
Affinity DataIC50:  0.0800nMAssay Description:Inhibition of gamma secretase in HEK293 cells expressing APP 695 assessed as reduction in amyloid beta levels after 5 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533414(CHEMBL4436451)
Affinity DataIC50:  0.270nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch activationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50241259((2S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetam...)
Affinity DataIC50:  0.390nMAssay Description:Inhibition of gamma secretase mediated Notch signaling in HEK293 cells after 5 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533419(CHEMBL4476008)
Affinity DataIC50:  0.410nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch signalingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  1nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533416(CHEMBL4303400)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of gamma secretase in human SupT1 cells assessed as reduction in amyloid beta 40 after 16 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533416(CHEMBL4303400)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of gamma secretase mediated Notch signaling in human SupT1 cells after 16 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533417(RO 4929097 | RO-4929097 | Rg 4733 | Rg-4733 | Ro49...)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant human gamma secretase expressing APP751 by electrochemiluminescence assayMore data for this Ligand-Target Pair
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50458158(Mk-0752)
Affinity DataIC50:  5nMAssay Description:Inhibition of gamma secretase in human MCF7 cells assessed as reduction in amyloid beta 40 after 3 days by Western blot analysisMore data for this Ligand-Target Pair
TargetDisintegrin and metalloproteinase domain-containing protein 10(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533418(CHEMBL4435465)
Affinity DataIC50:  5.30nMAssay Description:Inhibition of ADAM10 (unknown origin) assessed as blockage of TNF-alpha sheddingMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50468574(CHEMBL4116008 | US11414410, Example 100)
Affinity DataIC50:  6nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50364378(CHEMBL1950289)
Affinity DataIC50:  6nMAssay Description:Inhibition of JNK3 (unknown origin)More data for this Ligand-Target Pair
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50458159(Nirogacestat | PF 03084014 | PF 3084014 | PF-03084...)
Affinity DataIC50:  6.20nMAssay Description:Inhibition of gamma secretase isolated from human HeLa cell derived P2 membrane assessed as reduction in amyloid beta (1 to 40 residues) using recomb...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 9(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50364378(CHEMBL1950289)
Affinity DataIC50:  7nMAssay Description:Inhibition of JNK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50468574(CHEMBL4116008 | US11414410, Example 100)
Affinity DataIC50:  8nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28944((2S)-2-hydroxy-3-methyl-N-[(1S)-1-{[(1S)-3-methyl-...)
Affinity DataIC50:  11nMAssay Description:Inhibition of gamma secretase (unknown origin)More data for this Ligand-Target Pair
TargetPoly [ADP-ribose] polymerase tankyrase-1/tankyrase-2(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50188594(CHEBI:62878 | CHEMBL1086580)
Affinity DataIC50:  11nMAssay Description:Inhibition of tankyrase1/2 (unknown origin)More data for this Ligand-Target Pair
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50477339(BMS-299897 | CHEMBL247471)
Affinity DataIC50:  12nMAssay Description:Inhibition of gamma secretase (unknown origin) assessed as reduction in amyloid beta levels by sandwich ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50468574(CHEMBL4116008 | US11414410, Example 100)
Affinity DataIC50:  12nMAssay Description:Inhibition of JAK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28944((2S)-2-hydroxy-3-methyl-N-[(1S)-1-{[(1S)-3-methyl-...)
Affinity DataIC50:  14nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch signalingMore data for this Ligand-Target Pair
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50:  15nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50100434(CHEMBL302004 | L-68458 | L-685458 | tert-butyl (2S...)
Affinity DataIC50:  17nMAssay Description:Inhibition of gamma secretase (unknown origin) assessed as reduction in amyloid beta levels by HTRF assayMore data for this Ligand-Target Pair
TargetSphingosine 1-phosphate receptor 2(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50065628(CHEMBL1368758 | US9663511, Compound JTE013)
Affinity DataIC50:  20nMAssay Description:Antagonist activity at human S1P2 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSphingosine 1-phosphate receptor 2(Rat)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50065628(CHEMBL1368758 | US9663511, Compound JTE013)
Affinity DataIC50:  20nMAssay Description:Antagonist activity at rat S1P2 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50364378(CHEMBL1950289)
Affinity DataIC50:  61nMAssay Description:Inhibition of JNK1 (unknown origin)More data for this Ligand-Target Pair
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28986(N-{4-[(4-chlorobenzene)sulfonyl]-4-(2,5-difluoroph...)
Affinity DataIC50:  65nMAssay Description:Inhibition of gamma secretase in HEK293 cells expressing APP assessed as reduction in amyloid beta levelsMore data for this Ligand-Target Pair
TargetRho-associated protein kinase 2(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM322155(US10183931, SLx-2119 | US10696660, SLx-2119 | US11...)
Affinity DataIC50:  100nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50100434(CHEMBL302004 | L-68458 | L-685458 | tert-butyl (2S...)
Affinity DataIC50:  115nMAssay Description:Inhibition of full-length human gamma secretase expressed in SH-SY5Y spbetaA4CTF cells assessed as reduction in amyloid beta levels after 90 mins by ...More data for this Ligand-Target Pair
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50478375(CHEBI:86193 | CHEMBL255682)
Affinity DataIC50:  115nMAssay Description:Inhibition of gamma secretase in human primary neuronal cells assessed as reduction in amyloid beta 40More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533420(CHEMBL4560794)
Affinity DataIC50:  150nMAssay Description:Modulation of gamma secretase in HEK cells expressing APP Swedish mutant assessed as reduction in amyloid beta levels after 5 hrsMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50:  209nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch M1726V mutant activation in CHO K1 cells after 48 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 3(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50364378(CHEMBL1950289)
Affinity DataIC50:  480nMAssay Description:Inhibition of ERK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50478375(CHEBI:86193 | CHEMBL255682)
Affinity DataIC50:  500nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch signaling by cell based luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDisintegrin and metalloproteinase domain-containing protein 17(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533418(CHEMBL4435465)
Affinity DataIC50:  541nMAssay Description:Inhibition of ADAM17 (unknown origin) assessed as blockage of TNF-alpha sheddingMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50248764(2-bromo-4-(6,7-dimethoxyquinazolin-4-ylamino)pheno...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50110176(CHEMBL3604460)
Affinity DataIC50:  2.30E+3nMAssay Description:Inhibition of gamma secretase mediated Notch delta E activation in human HeLa cells expressing EGFP after 16 hrs by immunofluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCREB-binding protein(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50468575(CHEMBL2312139)
Affinity DataIC50:  3.00E+3nMAssay Description:Inhibition of CBP (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50364378(CHEMBL1950289)
Affinity DataIC50:  3.40E+3nMAssay Description:Inhibition of p38alpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDisintegrin and metalloproteinase domain-containing protein 17(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533421(CHEMBL4544135)
Affinity DataIC50:  8.10E+3nMAssay Description:Inhibition of ADAM17 (unknown origin) assessed as blockage of TNF-alpha sheddingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSphingosine kinase 2(Human)
Universitaire Vaudois

Curated by ChEMBL
LigandPNGBDBM50312869(4-(4-(4-chlorophenyl)thiazol-2-ylamino)phenol | CH...)
Affinity DataIC50:  2.00E+4nMAssay Description:Inhibition of SK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533415(CHEMBL149518)
Affinity DataIC50:  3.00E+4nMAssay Description:Inhibition of gamma secretase mediated amyloid beta level reduction in HEK293 cells expressing APP after 72 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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