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Found 1823 with Last Name = 'lesburg' and Initial = 'ca'
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50604026(CHEMBL5192384)
Affinity DataKi:  0.110nMAssay Description:Displacement of [3H] labeled-N-(4-Fluorophenyl)-3-(4-(4-(2-hydroxypropan-2-yl)-6-(trifluoromethyl)pyridin-3-yl)phenyl)oxetane-3-carboxamide from huma...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50604023(CHEMBL5192977)
Affinity DataKi:  0.150nMAssay Description:Displacement of [3H] labeled-N-(4-Fluorophenyl)-3-(4-(4-(2-hydroxypropan-2-yl)-6-(trifluoromethyl)pyridin-3-yl)phenyl)oxetane-3-carboxamide from huma...More data for this Ligand-Target Pair
TargetCoagulation factor XI(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM330035(Methyl [(7S)-7-[6-(aminomethyl)-1-oxo-3,4-dihydroi...)
Affinity DataKi:  2.40nMAssay Description:Factor XIa determinations were made in 50 mM HEPES buffer at pH 7.4 containing 150 mM NaCl, 5 mM CaCl2, and 0.1% PEG 8000 (polyethylene glycol; JT Ba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCoagulation factor XI(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM330036(US9663527, Example 2)
Affinity DataKi:  3.90nMAssay Description:Factor XIa determinations were made in 50 mM HEPES buffer at pH 7.4 containing 150 mM NaCl, 5 mM CaCl2, and 0.1% PEG 8000 (polyethylene glycol; JT Ba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCoagulation factor XI(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM330037(US9663527, Example 3)
Affinity DataKi:  70nMAssay Description:Factor XIa determinations were made in 50 mM HEPES buffer at pH 7.4 containing 150 mM NaCl, 5 mM CaCl2, and 0.1% PEG 8000 (polyethylene glycol; JT Ba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCoagulation factor XI(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM330038(US9663527, Example 4)
Affinity DataKi:  170nMAssay Description:Factor XIa determinations were made in 50 mM HEPES buffer at pH 7.4 containing 150 mM NaCl, 5 mM CaCl2, and 0.1% PEG 8000 (polyethylene glycol; JT Ba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569664(CHEMBL4859451)
Affinity DataIC50:  0.00500nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250920(CHEMBL4078799)
Affinity DataIC50:  0.0200nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569663(CHEMBL4870155)
Affinity DataIC50:  0.0270nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569667(CHEMBL4848845)
Affinity DataIC50:  0.0370nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569665(CHEMBL4864568)
Affinity DataIC50:  0.0370nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250934(CHEMBL4066906)
Affinity DataIC50:  0.0400nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM237874(US9394282, 9-9)
Affinity DataIC50:  0.0500nMAssay Description:Displacement of [35S]-MK499 from human ERG expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569669(CHEMBL4866139)
Affinity DataIC50:  0.0520nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250922(CHEMBL4096821)
Affinity DataIC50:  0.0600nMAssay Description:Inhibition of GST-tagged recombinant human JAK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569672(CHEMBL4865305)
Affinity DataIC50:  0.0610nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569666(CHEMBL4855158)
Affinity DataIC50:  0.0670nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250923(CHEMBL4072848 | US10766883, Ex-3)
Affinity DataIC50:  0.0700nMAssay Description:Inhibition of JAK1 in IL6-stimulated human ME180 cells expressing stably integrated beta-lactamase reporter gene under control of sis-inducible eleme...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50584324(CHEMBL5088471)
Affinity DataIC50: <0.0800nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) preincubated with enzyme for 15 mins follo...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50604021(CHEMBL5207194)
Affinity DataIC50:  0.0800nMAssay Description:Inhibition of IDO1 in IFNgamma/LPS stimulated human whole blood assessed as unbound concentration using kynurenine/tryptophan as substrate preincubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50538503(CHEMBL4645108)
Affinity DataIC50:  0.0900nMAssay Description:Inhibition of IDO1 in IFNgamma/LPS stimulated human whole blood assessed as unbound concentration using kynurenine/tryptophan as substrate preincubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569657(CHEMBL4863492)
Affinity DataIC50:  0.0940nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250919(CHEMBL4102140)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50567132(CHEMBL4863767)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of IDO1 in human whole blood assessed as unbound concentrationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250927(CHEMBL4071005 | US10766883, Ex-1)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569661(CHEMBL4872743)
Affinity DataIC50:  0.110nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM237869(US10766883, Comp. Ex-1 9-4 | US9394282, 9-4)
Affinity DataIC50:  0.130nMAssay Description:Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elemen...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50567128(CHEMBL4855797)
Affinity DataIC50:  0.130nMAssay Description:Inhibition of IDO1 in human whole blood assessed as unbound concentrationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569659(CHEMBL4866616)
Affinity DataIC50:  0.130nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM237900(US10766883, Comp. Ex-4 9-35 | US9394282, 9-35)
Affinity DataIC50:  0.150nMAssay Description:Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elemen...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250931(CHEMBL4079092)
Affinity DataIC50:  0.160nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM552514(2-((2-Methoxy-4-(4-methylpiperazine-1-carbonyl)phe...)
Affinity DataIC50:  0.160nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569671(CHEMBL4860645)
Affinity DataIC50:  0.160nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250928(CHEMBL4092626)
Affinity DataIC50:  0.180nMAssay Description:Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elemen...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250938(CHEMBL4088262)
Affinity DataIC50:  0.190nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250920(CHEMBL4078799)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human TYK2 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50575884(CHEMBL4849371)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569660(CHEMBL4849567)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50604556(CHEMBL5175703)
Affinity DataIC50:  0.200nMAssay Description:Displacement of radiolabeled [3H]-2',3'-cGAMP from wild type human STING incubated for 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569668(CHEMBL4857184)
Affinity DataIC50:  0.220nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250930(CHEMBL4076473)
Affinity DataIC50:  0.240nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM237866(US9394282, 9-1)
Affinity DataIC50:  0.240nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM552521(WO2022098809, Example 4-8)
Affinity DataIC50:  0.25nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569662(CHEMBL4874375)
Affinity DataIC50:  0.260nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50604026(CHEMBL5192384)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of IDO1 in IFNgamma/LPS stimulated human whole blood assessed as unbound concentration using kynurenine/tryptophan as substrate preincubat...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetIndoleamine 2,3-dioxygenase 1(Homo sapiens (Human))
Pharmaron Beijing

Curated by ChEMBL
LigandPNGBDBM50567131(CHEMBL4848630)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of IDO1 in human whole blood assessed as unbound concentrationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50569656(CHEMBL4871382)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of HPK1 (unknown origin) using SLP76 as substrate incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50250918(CHEMBL4104623)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of JAK1 in human whole blood assessed as decrease in cytokine-stimulated STAT phosphorylation preincubated for 20 mins followed by cytokin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM147735(US8962608, 28-47)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of GST-tagged recombinant human JAK1 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50609728(CHEMBL5267350)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
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