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Found 306 with Last Name = 'czerwinski' and Initial = 'rm'
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  27nMAssay Description:Inhibition of full length recombinant human GST-tagged cytoplasmic ITK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase TXK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  131nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged TXK using GEPLYWSFPAKKK as substrate measured every 60 secs for 1 hr by PK/LDH coupled spectrop...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  545nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BMX expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Tec(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  679nMAssay Description:Inhibition of full length human His-tagged TEC by KT178 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  6.31E+3nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system by KT2...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  3.24E+4nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BLK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  6.23E+4nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BTK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50501537(CHEMBL4085582)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50501536(CHEMBL4064018)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM316524(US11111242, Example 12 | US9617258, Example 12)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399459(CHEMBL2179805)
Affinity DataIC50:  2nMAssay Description:Covalent inhibition of ITK in presence of 5 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399459(CHEMBL2179805)
Affinity DataIC50:  2nMAssay Description:Covalent inhibition of ITK in presence of 1 mM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399459(CHEMBL2179805)
Affinity DataIC50:  2nMAssay Description:Inhibition of BTK in presence of 50 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399460(CHEMBL2179804)
Affinity DataIC50:  5nMAssay Description:Inhibition of BTK in presence of 50 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM372964(US10597366, Compound 8 | US9896418, Compound 8)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM373015(US10597366, Compound 185 | US9896418, Compound 185)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM372991(US10597366, Compound 63 | US9896418, Compound 63)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM50450475(CHEMBL4168682)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM372976(US10597366, Compound 15 | US9896418, Compound 15)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM372960(US10597366, Compound 1 | US9896418, Compound 1)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM372979(US10597366, Compound 17 | US9896418, Compound 17)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282572((R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy-...)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282598(5-(3-Chloro-5-fluorophenoxy)-2,2-difluoro-3- hydro...)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282581(4-Bromo-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro-...)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282632(5-(3-Chloro-5-fluorophenoxy)-4-(difluoromethyl)- 2...)
Affinity DataIC50: <5nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM373040(US10597366, Compound 289 | US9896418, Compound 289)
Affinity DataIC50:  9nMAssay Description:Inhibition of N-(3-Chlorophenyl-4,6-t2)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine binding to his-tagged HIF-2alpha PAS-B domain (unknown origin) measur...More data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM373041(US10597366, Compound 292 | US9896418, Compound 292)
Affinity DataIC50:  9nMAssay Description:Inhibition of N-(3-Chlorophenyl-4,6-t2)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine binding to his-tagged HIF-2alpha PAS-B domain (unknown origin) measur...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399461(CHEMBL2179790)
Affinity DataIC50:  10nMAssay Description:Covalent inhibition of ITK in presence of 5 uM ATPMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399471(CHEMBL2179781)
Affinity DataIC50:  10nMAssay Description:Covalent inhibition of ITK in presence of 1 mM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399458(CHEMBL2179806)
Affinity DataIC50:  10nMAssay Description:Covalent inhibition of ITK in presence of 1 mM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399460(CHEMBL2179804)
Affinity DataIC50:  10nMAssay Description:Covalent inhibition of ITK in presence of 1 mM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399458(CHEMBL2179806)
Affinity DataIC50:  10nMAssay Description:Covalent inhibition of ITK in presence of 5 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM372972(US10597366, Compound 11 | US9896418, Compound 11)
Affinity DataIC50:  10nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282656(4-(Difluoromethyl)-5-(3,5-difluorophenoxy)-2,2- di...)
Affinity DataIC50:  11nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399458(CHEMBL2179806)
Affinity DataIC50:  12nMAssay Description:Inhibition of BTK in presence of 50 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM373008(US10597366, Compound 163 | US9896418, Compound 163)
Affinity DataIC50:  12nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM373008(US10597366, Compound 163 | US9896418, Compound 163)
Affinity DataIC50:  12nMAssay Description:Inhibition of N-(3-Chlorophenyl-4,6-t2)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine binding to his-tagged HIF-2alpha PAS-B domain (unknown origin) measur...More data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282685(3-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-...)
Affinity DataIC50:  14nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399461(CHEMBL2179790)
Affinity DataIC50:  15nMAssay Description:Inhibition of BTK in presence of 50 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM50450483(CHEMBL4176537)
Affinity DataIC50:  16nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM316642(US11111242, Example 133 | US9617258, Example 133)
Affinity DataIC50:  18nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282597(US9884843, Compound 13)
Affinity DataIC50:  20nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM282584(4-Chloro-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro...)
Affinity DataIC50:  20nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399460(CHEMBL2179804)
Affinity DataIC50:  20nMAssay Description:Covalent inhibition of ITK in presence of 5 uM ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50501537(CHEMBL4085582)
Affinity DataIC50:  29nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50399459(CHEMBL2179805)
Affinity DataIC50:  31nMAssay Description:Covalent inhibition of ITK in human Jurkat cells assessed as inhibition of anti-CD3 antibody-stimulated PLCgamma phosphorylation pre-incubated before...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM50450495(CHEMBL4159016 | US10597366, Compound 206)
Affinity DataIC50:  31nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50501537(CHEMBL4085582)
Affinity DataIC50:  32nMAssay Description:Inhibition of JAK3 in human PBMC assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 75 mins followed by IL-15 addition an...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics

Curated by ChEMBL
LigandPNGBDBM50450486(CHEMBL4168279)
Affinity DataIC50:  32nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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