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Found 902 with Last Name = 'tonn' and Initial = 'g'
TargetProstaglandin D2 receptor 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50302828(2-(4-(4-(butylcarbamoyl)-2-(2,4-dichlorophenylsulf...)
Affinity DataKi:  1nMAssay Description:Inhibition of PGD2-induced CRTH2 receptor internalization of CD16 negative granulocytes in human whole blood by flow cytometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50229378((R)-N-(1-(3-(4-cyanophenyl)H-imidazo[1,2-a]pyridin...)
Affinity DataKi:  3nMAssay Description:Displacement of [125I]-IP-10 from CXCR3 receptor expressed in human PBMC in RPMI-1640 buffer supplemented with 0.5% BSAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProstaglandin D2 receptor(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50302828(2-(4-(4-(butylcarbamoyl)-2-(2,4-dichlorophenylsulf...)
Affinity DataKi:  148nMAssay Description:Antagonist activity at DP receptor in human platelets assessed as inhibition of PGD2-induced cAMP production by competitive ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  730nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as unbound inhibitor concentration required for half maximal enz...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  740nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate assessed as unbound inhibitor concentration required for half maximal ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  1.90E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate assessed as residual enzyme activity after 2 to 10 mins by LC-MS/MS an...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  1.90E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as residual enzyme activity after 2 to 10 mins by LC-MS/MS analy...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProstaglandin E2 receptor EP4 subtype(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50302828(2-(4-(4-(butylcarbamoyl)-2-(2,4-dichlorophenylsulf...)
Affinity DataKi:  4.40E+4nMAssay Description:Inhibition of EP4 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProstaglandin E2 receptor EP2 subtype(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50302828(2-(4-(4-(butylcarbamoyl)-2-(2,4-dichlorophenylsulf...)
Affinity DataKi:  4.40E+4nMAssay Description:Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50458169(Avagacestat | BMS 708163 | BMS-708163 | BMS-708163...)
Affinity DataIC50:  0.130nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492082(CHEMBL2396959)
Affinity DataIC50:  0.220nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492094(CHEMBL2396964)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492093(CHEMBL2396778)
Affinity DataIC50:  0.340nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310487((R)-N-(2-(ethylsulfonyl)ethyl)-2-(4-fluoro-3-(trif...)
Affinity DataIC50:  0.400nMAssay Description:Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to IP10 in bufferMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50371494(CHEMBL256589)
Affinity DataIC50:  0.400nMAssay Description:Displacement of [125I]IP10 from human recombinant CXCR3 receptor expressed in IL2-activated human PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492085(CHEMBL2396953)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492083(CHEMBL2396960)
Affinity DataIC50:  0.570nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310487((R)-N-(2-(ethylsulfonyl)ethyl)-2-(4-fluoro-3-(trif...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to MIG in bufferMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50229439((R)-N-(1-(1-(4-cyanophenyl)-4-phenyl-1H-imidazol-2...)
Affinity DataIC50:  0.700nMAssay Description:Displacement of [125I]IP10 from human recombinant CXCR3 receptor expressed in IL2-activated human PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50229439((R)-N-(1-(1-(4-cyanophenyl)-4-phenyl-1H-imidazol-2...)
Affinity DataIC50:  0.700nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50229381((R)-N-(1-(3-(4-cyanophenyl)quinolin-2-yl)ethyl)-N-...)
Affinity DataIC50:  0.800nMAssay Description:Displacement of [125I]-IP-10 from CXCR3 receptor expressed in human PBMC in RPMI-1640 buffer supplemented with 0.5% BSAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310487((R)-N-(2-(ethylsulfonyl)ethyl)-2-(4-fluoro-3-(trif...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in RPMI bufferMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300900((R)-N-(1-(3-(4-cyanophenyl)-8-methoxyimidazo[1,2-a...)
Affinity DataIC50:  0.900nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300899((R)-N-(1-(3-(4-cyanophenyl)-8-cyclopropylimidazo[1...)
Affinity DataIC50:  0.900nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300905(CHEMBL578192 | N-{(R)-1-[3-(4-Cyano-phenyl)-8-cycl...)
Affinity DataIC50:  0.900nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300907(CHEMBL576097 | N-{(R)-1-[3-(4-Cyano-phenyl)-8-cycl...)
Affinity DataIC50:  0.900nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50229462((R)-N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydroquin...)
Affinity DataIC50:  1nMAssay Description:Displacement of [125I]IP10 from human recombinant CXCR3 receptor expressed in IL2-activated human PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310487((R)-N-(2-(ethylsulfonyl)ethyl)-2-(4-fluoro-3-(trif...)
Affinity DataIC50:  1nMAssay Description:Displacement of [125I]-ITAC from human CXCR3 expressed in human PBMC after 2 hrs in RPMI buffer by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310487((R)-N-(2-(ethylsulfonyl)ethyl)-2-(4-fluoro-3-(trif...)
Affinity DataIC50:  1nMAssay Description:Displacement of [125I]-1P10 from human CXCR3 expressed in PBMC after 2 hrs in RPMI buffer by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352621(CHEMBL1822152)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310486((R)-N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyri...)
Affinity DataIC50:  1nMAssay Description:Displacement of [125I]-1P10 from human CXCR3 expressed in PBMC after 2 hrs in RPMI buffer by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352620(CHEMBL1822151)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492098(CHEMBL2396963)
Affinity DataIC50:  1nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50310483((R)-N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyri...)
Affinity DataIC50:  1nMAssay Description:Displacement of [125I]-1P10 from human CXCR3 expressed in PBMC after 2 hrs in RPMI buffer by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352624(CHEMBL1822305 | US9796706, Compound 139)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300909(CHEMBL576099 | N-{(R)-1-[3-(4-Cyano-phenyl)-8-cycl...)
Affinity DataIC50:  1.10nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300906(CHEMBL576096 | N-{(R)-1-[3-(4-Cyano-phenyl)-8-cycl...)
Affinity DataIC50:  1.10nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300902((R)-N-(1-(3-(4-cyanophenyl)-8-ethylimidazo[1,2-a]p...)
Affinity DataIC50:  1.10nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492097(CHEMBL2396965)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300898(CHEMBL570858 | N-{(R)-1-[3-(4-Cyano-phenyl)-8-cycl...)
Affinity DataIC50:  1.30nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300903(CHEMBL570857 | rac-N-(1-(3-(4-cyanophenyl)-8-(dime...)
Affinity DataIC50:  1.40nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50458169(Avagacestat | BMS 708163 | BMS-708163 | BMS-708163...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300901((R)-N-(1-(3-(4-cyanophenyl)-8-methylimidazo[1,2-a]...)
Affinity DataIC50:  1.60nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50300908(CHEMBL576098 | N-{(R)-1-[3-(4-Cyano-phenyl)-8-cycl...)
Affinity DataIC50:  1.70nMAssay Description:Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50371490(CHEMBL269932)
Affinity DataIC50:  1.80nMAssay Description:Displacement of [125I]IP10 from human recombinant CXCR3 receptor expressed in IL2-activated human PBMCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492092(CHEMBL2396961)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPresenilin-1(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50492084(CHEMBL2396958)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50229383((R)-N-(1-(3-(4-cyanophenyl)-1,8-naphthyridin-2-yl)...)
Affinity DataIC50:  2nMAssay Description:Displacement of [125I]-IP-10 from CXCR3 receptor expressed in human PBMC in RPMI-1640 buffer supplemented with 0.5% BSAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352620(CHEMBL1822151)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant JNK3 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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