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TargetTryptase beta-2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50156461(3-[4-(5-Aminomethyl-2-fluoro-phenyl)-piperidine-1-...)
Affinity DataKi:  1.30nMAssay Description:Inhibitory activity against human mast cell tryptase betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTryptase beta-2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50156460(3-[4-(3-Aminomethyl-phenyl)-piperidine-1-carbonyl]...)
Affinity DataKi:  1.5nMAssay Description:Inhibitory activity against human mast cell tryptase betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTryptase beta-2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50156457(CHEMBL186730 | [4-(5-Aminomethyl-2-fluoro-phenyl)-...)
Affinity DataKi:  4.30nMAssay Description:Inhibitory activity against human mast cell tryptase betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTryptase beta-2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50156459(3-[4-(5-Aminomethyl-2-fluoro-phenyl)-piperidine-1-...)
Affinity DataKi:  59nMAssay Description:Inhibitory activity against human mast cell tryptase betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTryptase beta-2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50156458(3-[4-(5-Aminomethyl-2-fluoro-phenyl)-piperidine-1-...)
Affinity DataKi:  88nMAssay Description:Inhibitory activity against human mast cell tryptase betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521421(6-(2,4- dichlorophenyl)- 1-fluoro-5-[6- [(3S)-1-(3...)
Affinity DataIC50:  0.400nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521262(6-(6-ethoxy-2- fluoro-3- pyridyl)-5-[4- [[(3S)-1-(...)
Affinity DataIC50:  0.5nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521255(3-(6-ethoxy-2- fluoro-3- pyridyl)-4-[6- [(3S)-1-(3...)
Affinity DataIC50:  0.5nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521384(4-(6-ethoxy-2- fluoro-3- pyridyl)-5-[6- [(3S)-1-(3...)
Affinity DataIC50:  0.600nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521413(6-(2-fluoro-4- methyl-phenyl)- 5-[6-[(3S)-1-(3- fl...)
Affinity DataIC50:  0.600nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521428(6-(6-ethoxy-2- fluoro-3- pyridyl)-1- fluoro-5-[6- ...)
Affinity DataIC50:  0.700nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521382(4-(2-chloro-4- methyl-phenyl)- 5-[6-[(3S)-1-(3- fl...)
Affinity DataIC50:  0.700nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263706(6-(2- chloro-4- ethoxy- phenyl)-5- [4-[(3S)-1- (3-...)
Affinity DataIC50:  0.800nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetRAC-alpha serine/threonine-protein kinase(Human)
Sanofi

US Patent
LigandPNGBDBM180347(US9133168, Example 1c | US9133168, Example 2c | US...)
Affinity DataIC50:  1nMAssay Description:This test is based on measurement of the expression of AKT protein phosphorylated on serine 473 (P-AKT-S473) in the PC3 human prostate carcinoma line...More data for this Ligand-Target Pair
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521394(4-[4- (fluoromethoxy) phenyl]-5-[4- [(3S)-1-(3- fl...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetRAC-alpha serine/threonine-protein kinase(Human)
Sanofi

US Patent
LigandPNGBDBM180433(US9133168, Example 9e)
Affinity DataIC50:  1nMAssay Description:This test is based on measurement of the expression of AKT protein phosphorylated on serine 473 (P-AKT-S473) in the PC3 human prostate carcinoma line...More data for this Ligand-Target Pair
In DepthDetails US Patent


LigandPNGBDBM50447089(CHEMBL3112849)
Affinity DataIC50:  1nMAssay Description:Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50447088(CHEMBL3112850)
Affinity DataIC50:  1nMAssay Description:Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263764(6-(2,2- dimethyl- 3H- benzo- furan-5-yl)-5- [4-[(3...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263707(5-[4-[(3S)- 1-(3- fluoropropyl)- pyrrolidin-3- yl]...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263709(6-(4- ethoxy-2- methyl- phenyl)-1- fluoro-5-[4- [(...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263712(6-(2,3- dihydro- 1,4- benzodioxin-6-yl)-5- [4-[(3S...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263860(5-[4-[(3S)- 1-(3- fluoropropyl)- pyrrolidin-3- yl]...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263892(5-[4-[(3S)- 1-(3- fluoropropyl)- pyrrolidin-3- yl]...)
Affinity DataIC50: <1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263893(5-[4-[(3S)- 1-(3- fluoropropyl)- pyrrolidin-3- yl]...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263900(6-[2,3- difluoro-4- (1-piperidyl)- phenyl]-5- [4-[...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263911(US9714221, Example 207)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263847(6-(2,2-dimethylindolin-5-yl)-5-[4-[(3S)-1-(3-fluor...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521334(5-[4-[(3S)-1-(3- fluoropropyl)pyr- rolidin-3- yl]o...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263719(6-(1,3- benzoxazol- 5-yl)-5-[4- [(3S)-1-(3- fluoro...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263737(6-(6- ethoxy-2- fluoro-3- pyridyl)-5- [4-[(3S)- 1-...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263743(5-[4-[(3S)- 1-(3- fluoropropyl)- pyrrolidin-3- yl]...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetRAC-alpha serine/threonine-protein kinase(Human)
Sanofi

US Patent
LigandPNGBDBM180381(US9133168, Example 37c | US9133168, Example 38c)
Affinity DataIC50:  1nMAssay Description:This test is based on measurement of the expression of AKT protein phosphorylated on serine 473 (P-AKT-S473) in the PC3 human prostate carcinoma line...More data for this Ligand-Target Pair
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263748(US9714221, Example 82)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263755(6-(2- chloro-4- methoxy- phenyl)-5- [4-[(3S)-1- (3...)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521417(6-[4- (difluoromethoxy)- 3-fluoro- phenyl]-5-[6- [...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521418(6-(2,2- dimethylindolin- 5-yl)-5-[6-[(3S)- 1-(3- f...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521425(6-[4- (difluoromethoxy)- 3-fluoro- phenyl]-1- fluo...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521360(4-(benzofuran- 5-yl)-5-[4-[(3S)- 1-(3- fluoropropy...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521362(4-(4-ethoxy-2- methyl-phenyl)- 5-[4-[(3S)-1-(3- fl...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetRAC-alpha serine/threonine-protein kinase(Human)
Sanofi

US Patent
LigandPNGBDBM180362(US9133168, Example 17c | US9133168, Example 18c)
Affinity DataIC50:  1nMAssay Description:This test is based on measurement of the expression of AKT protein phosphorylated on serine 473 (P-AKT-S473) in the PC3 human prostate carcinoma line...More data for this Ligand-Target Pair
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521369(4-(2,2-difluoro- 1,3- benzodioxol-5- yl)-5-[4-[(3S...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521373(5-[4-[(3S)-1-(3- fluoropropyl)pyr- rolidin-3- yl]o...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521374(4-(2,2- dimethylindolin- 5-yl)-5-[4-[(3S)- 1-(3- f...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521377(4-(2,2-dimethyl- 3H-benzofuran- 5-yl)-5-[4-[(3S)- ...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521378(5-[4-[(3S)-1-(3- fluoropropyl)pyr- rolidin-3- yl]o...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521381(4-(2,4- dichlorophenyl)- 5-[(6-[(3S)-1-(3- fluorop...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263774(US9714221, Example 108)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor(Human)
Sanofi

US Patent
LigandPNGBDBM263775(US9714221, Example 109)
Affinity DataIC50:  1nMpH: 7.4 T: 25°CAssay Description:It is a competition assay, where binding of a test compound to a complex comprised of (i) His6-ERα298-554 protein representing ERα ligand-b...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


TargetEstrogen receptor [298-554](Human)
Sanofi

US Patent
LigandPNGBDBM521221(3-(2-fluoro-6- methoxy-3- pyridyl)-4-[4- [(3S)-1-(...)
Affinity DataIC50:  1nMAssay Description:Antagonistic potency of compounds was evaluated using LanthaScreenŽ TR-FRET ERα Coactivator Assay (ThermoFisher) with modifications. It is a com...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent


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