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Found 998 with Last Name = 'goldstein' and Initial = 'dm'
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  1.30nMAssay Description:Irreversible inhibition of human FGFR2 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  1.60nMAssay Description:Irreversible inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated with enzyme followed by peptide substrate addition by ca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  2.20nMAssay Description:Irreversible inhibition of human FGFR3 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50314073(3-(3-bromo-4-(2,4-difluorobenzyloxy)-6-methyl-2-ox...)
Affinity DataKi:  5.80nMAssay Description:Binding affinity to p38alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50418610(GW-856553 | GW856553X | LOSMAPIMOD | US10550073, C...)
Affinity DataKi:  7.90nMAssay Description:Binding affinity to p38alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 11(Homo sapiens (Human))
Roche Palo Alto

Curated by ChEMBL
LigandPNGBDBM50418610(GW-856553 | GW856553X | LOSMAPIMOD | US10550073, C...)
Affinity DataKi:  25nMAssay Description:Binding affinity to p38betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  73nMAssay Description:Irreversible inhibition of human FGFR4 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis methodMore data for this Ligand-Target Pair
TargetCytochrome P450 3A4(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50394918(CHEMBL2165504)
Affinity DataKi:  6.60E+3nMAssay Description:Time dependent inhibition of CYP3A4 in human liver microsomes preincubated for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50394917(CHEMBL2165505)
Affinity DataKi:  7.80E+4nMAssay Description:Time dependent inhibition of CYP3A4 in human liver microsomes preincubated for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589205(CHEMBL5174021)
Affinity DataIC50:  0nMAssay Description:Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192799(US9187487, 50)
Affinity DataIC50:  0.200nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192809(US9187487, 71)
Affinity DataIC50:  0.200nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM521835(US11155544, Compound 67)
Affinity DataIC50:  0.200nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of BTK kinase activity of a compound of the pre...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192818(US9187487, 83)
Affinity DataIC50:  0.200nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192804(US9187487, 64)
Affinity DataIC50:  0.200nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM521834(US11155544, Compound 66)
Affinity DataIC50:  0.300nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of BTK kinase activity of a compound of the pre...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50388189(CHEMBL2057918)
Affinity DataIC50:  0.300nMAssay Description:Competitive inhibition of BTK by TR-FRET based competitive assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589186(CHEMBL5189379)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM521782(US11155544, Compound 8)
Affinity DataIC50:  0.300nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of BTK kinase activity of a compound of the pre...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589207(CHEMBL5169419)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192802(US9187487, 60)
Affinity DataIC50:  0.400nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM287008(8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-d...)
Affinity DataIC50:  0.400nMAssay Description:In vitro antagonist activity against rat prostatic androgen receptor (AR)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192803(US9187487, 62)
Affinity DataIC50:  0.400nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM197250(US9090621, 85A | US9572811, Example 41A)
Affinity DataIC50:  0.400nMT: 2°CAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM197248(US9090621, 84B)
Affinity DataIC50:  0.400nMT: 2°CAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50394916(CHEMBL2165506)
Affinity DataIC50:  0.480nMAssay Description:Binding affinity to PI3Kdelta after 30 mins by competitive fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589186(CHEMBL5189379)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of BLK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | PCI-32765 | US10124003, Ref. Ex. Compo...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of BLKMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Tec(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589186(CHEMBL5189379)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of TEC (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192807(US9187487, 69)
Affinity DataIC50:  0.5nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM521833(US11155544, Compound 65)
Affinity DataIC50:  0.600nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of BTK kinase activity of a compound of the pre...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589186(CHEMBL5189379)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of BMX (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589202(CHEMBL5191633)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of biotinylated-labeled BTK-selective probe binding to BTK in human Ramos assessed as target occupancy pretreated for 1 hr followed by pro...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192816(US9187487, 81)
Affinity DataIC50:  0.600nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM197275(US9090621, 27B | US9572811, Example 34)
Affinity DataIC50:  0.600nMT: 2°CAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50392144(CHEMBL2152774)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of PI3K p110delta using PIP2 as substrate assessed as PIP3 formation by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50394910(CHEMBL2165512)
Affinity DataIC50:  0.670nMAssay Description:Binding affinity to PI3Kdelta after 30 mins by competitive fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192805(US9187487, 66)
Affinity DataIC50:  0.700nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3 [781-1124](Homo sapiens (Human))
Principia Biopharma

US Patent
LigandPNGBDBM192815(US9187487, 80)
Affinity DataIC50:  0.700nMpH: 7.5 T: 2°CAssay Description:Phosphorylation of the appropriate peptide substrate (fluorescently labeled Srctide) by recombinant JAK3 (catalytic domain, aa 781-1124) was measured...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM197225(US9090621, 188 | US9572811, Example 188)
Affinity DataIC50:  0.700nMT: 2°CAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286381(8-(2-((1-acryloylpiperidin-3-yl)oxy)ethyl)-6-(2,6-...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM197220(BDBM197237 | US9090621, 95B | US9572811, Example 9...)
Affinity DataIC50:  0.700nMT: 2°CAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50388185(CHEMBL2057919)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of human BTK by enzymatic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM50238813(CHEMBL4083740)
Affinity DataIC50:  0.700nMAssay Description:In vitro antagonist activity against rat prostatic androgen receptor (AR)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM521832(US11155544, Compound 64)
Affinity DataIC50:  0.800nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of BTK kinase activity of a compound of the pre...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50589212(CHEMBL5195816)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM50238811(CHEMBL4073347)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Principia Biopharma, A Sanofi

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | PCI-32765 | US10124003, Ref. Ex. Compo...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of BMXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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