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Found 520 with Last Name = 'aertgeerts' and Initial = 'k'
LigandPNGBDBM50150119(CHEMBL3769414)
Affinity DataIC50:  0.0580nMAssay Description:Inhibition of PDE1B (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Takeda Pharmaceutical

LigandPNGBDBM5446(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Affinity DataIC50:  0.700nMpH: 7.5Assay Description:The EGFR, HER2 and HER4 kinase assay were performed using radiolabeled [gamma-32P] ATP from GE Healthcare. More data for this Ligand-Target Pair
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236228(CHEMBL4076035 | US11186582, Example 6)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339608(3-(1-Amino-1-methylethyl)-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of RETMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236235(CHEMBL4066029 | US11186582, Example 4)
Affinity DataIC50:  1nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236271(CHEMBL4103411 | US11186582, Example 225)
Affinity DataIC50:  1nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM107767(US11419874, PF-05180999 | US8598155, 2)
Affinity DataIC50:  1nMAssay Description:Inhibition of human full length PDE2a using cGMP as substrate by Scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50333177(1-{[5-(Aminomethyl)-2-methyl-4-(4-methylphenyl)-6-...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of DDP4 in human Caco2 cells after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50333175(CHEMBL1644848 | Methyl 1-{[5-(aminomethyl)-2-methy...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of DDP4 in human Caco2 cells after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50336806(1-(3-(aminomethyl)-2-isobutyl-4-p-tolylquinolin-6-...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of DPP4 in human Caco2 cells after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339609(3-[(Dimethylamino)methyl]-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of Abl1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50401285(CHEMBL2204532)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of VEGFR2 in HUVEC assessed as reduction of VGF-stimulated cell proliferation after 5 daysMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50336806(1-(3-(aminomethyl)-2-isobutyl-4-p-tolylquinolin-6-...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of human Dipeptidyl peptidase-4 expressed in Caco-2 cells using Gly-Pro-pNA.Tos as substrate after 60 mins by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339609(3-[(Dimethylamino)methyl]-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of RETMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50317108(2-(1-{(2S)-3-[(6-Chloronaphthalen-2-yl)sulfonyl]-2...)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of human factor 10a assessed as p-nitroanilide release using S2765 as substrate by chromogenic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50333167(3-({[5-(Aminomethyl)-2-methyl-4-(4-methylphenyl)-6...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of DDP4 in human Caco2 cells after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50349380(CHEMBL1808468)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of human Dipeptidyl peptidase-4 expressed in Caco-2 cells using Gly-Pro-pNA.Tos as substrate after 60 mins by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50166893(2-(3,4-Dimethoxy-benzyl)-7-[(R)-1-((R)-1-hydroxy-e...)
Affinity DataIC50:  2nMAssay Description:Inhibition of PDE2a (unknown origin) using cAMP as substrate after 30 mins by Scintillation proximity assayMore data for this Ligand-Target Pair
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236231(CHEMBL4087945 | US11186582, Example 349 | US114198...)
Affinity DataIC50:  2nMAssay Description:Tested for the inhibitory activity against pepsin (Second pure eluting diastereomer )More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236243(CHEMBL4059930 | US11186582, Example 340)
Affinity DataIC50:  2nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
TargetCoagulation factor X(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50304619((S)-2-(1-(3-(6-chloronaphthalen-2-ylsulfonyl)-2-hy...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of human factor 10a assessed as p-nitroanilide release using S2765 as substrate by chromogenic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50358454(CHEMBL1923009)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of human N-terminus peptide (DYKDDDD)-tagged HER2 expressed in baculovirus infected insect cells using [gamma-32P]ATP as substrate after 6...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50317098(1-(1-{(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2...)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of human factor 10a using S2222 as substrate after 10 mins by chromogenic assayMore data for this Ligand-Target Pair
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50349384(CHEMBL1808473)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of human Dipeptidyl peptidase-4 expressed in Caco-2 cells using Gly-Pro-pNA.Tos as substrate after 60 mins by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339609(3-[(Dimethylamino)methyl]-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of C-RafMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50317107(2-(1-{(2S)-3-[(6-Chloronaphthalen-2-yl)sulfonyl]-2...)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of human factor 10a assessed as p-nitroanilide release using S2765 as substrate by chromogenic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50336818(5-(Aminomethyl)-2-benzyl-6-(2,2-dimethylpropyl)-4-...)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of DPP4 in human Caco2 cells after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339608(3-(1-Amino-1-methylethyl)-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of C-RafMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339609(3-[(Dimethylamino)methyl]-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of DDR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50349385(CHEMBL1808474)
Affinity DataIC50:  2.70nMAssay Description:Inhibition of human Dipeptidyl peptidase-4 expressed in Caco-2 cells using Gly-Pro-pNA.Tos as substrate after 60 mins by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50358467(CHEMBL1923022)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of human N-terminus peptide (DYKDDDD)-tagged HER2 expressed in baculovirus infected insect cells using [gamma-32P]ATP as substrate after 6...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50333171(2-[5-(Aminomethyl)-2-methyl-4-(4-methylphenyl)-6-(...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of DDP4 in human Caco2 cells after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50333176(1-{[5-(Aminomethyl)-2-methyl-4-(4-methylphenyl)-6-...)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of DDP4 in human Caco2 cells after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50335797(2-[2-(3-(R)-Aminopyrimidin-1-yl)-5-bromo-6-oxo-6H-...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human DPP4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM289647(11,11-Difluoro-6-(4-methoxybenzyl)-9-((tetrahydro-...)
Affinity DataIC50:  3nMAssay Description:Inhibitory activity against chymotrypsinogen; Range 1-10 uMMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236242(CHEMBL4093237 | US11186582, Example 516)
Affinity DataIC50:  3nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Takeda Pharmaceutical

LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  3nMpH: 7.5Assay Description:The EGFR, HER2 and HER4 kinase assay were performed using radiolabeled [gamma-32P] ATP from GE Healthcare. More data for this Ligand-Target Pair
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Dart Neuroscience

Curated by ChEMBL
LigandPNGBDBM50236226(CHEMBL4087412 | US11186582, Example 378 | US114198...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human full length GST-tagged PDE2a using FAM-labeled cAMP as substrate preincubated for 5 mins followed by substrate addition measured ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAF proto-oncogene serine/threonine-protein kinase(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339615((2S)-7-({2-[(Cyclopropylcarbonyl)amino]pyridin-4-y...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of C-Raf assessed as reduction in [33P]ATP incorporation into biotinylated substrate peptide after 3 hrs by flash plate assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50358448(CHEMBL1923003)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of human N-terminus peptide (DYKDDDD)-tagged HER2 expressed in baculovirus infected insect cells using [gamma-32P]ATP as substrate after 6...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50317098(1-(1-{(2S)-3-[(6-chloronaphthalen-2-yl)sulfonyl]-2...)
Affinity DataIC50:  3.5nMAssay Description:Inhibition of human factor 10a assessed as p-nitroanilide release using S2765 as substrate by chromogenic assayMore data for this Ligand-Target Pair
TargetCoagulation factor X(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50317096(4-(1-{(2S)-3-[(6-Chloronaphthalen-2-yl)sulfonyl]-2...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of human factor 10a assessed as p-nitroanilide release using S2765 as substrate by chromogenic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50333164(CHEMBL1644837 | Methyl3-({[5-(aminomethyl)-2-methy...)
Affinity DataIC50:  3.70nMAssay Description:Inhibition of DDP4 in human Caco2 cells after 60 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50335792(2-{6-[3(R)-Aminopiperidin-1-yl]-2,4-dioxo-3,4-dihy...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human DPP4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50335784(2-[6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human DPP4More data for this Ligand-Target Pair
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50335768(2-[2-(3-(R)-Aminopiperidin-1-yl)-5-methoxy-6-oxo-6...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human DPP4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50358451(CHEMBL1923006)
Affinity DataIC50:  4.10nMAssay Description:Inhibition of human N-terminus peptide (DYKDDDD)-tagged HER2 expressed in baculovirus infected insect cells using [gamma-32P]ATP as substrate after 6...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50349376(CHEMBL1808464)
Affinity DataIC50:  4.20nMAssay Description:Inhibition of human Dipeptidyl peptidase-4 expressed in Caco-2 cells using Gly-Pro-pNA.Tos as substrate after 60 mins by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Millennium Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50339608(3-(1-Amino-1-methylethyl)-N-{(2R)-7-[(7-oxo-5,6,7,...)
Affinity DataIC50:  4.20nMAssay Description:Inhibition of wild-type B-RafMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50358464(CHEMBL1923019)
Affinity DataIC50:  4.30nMAssay Description:Inhibition of human N-terminus peptide (DYKDDDD)-tagged HER2 expressed in baculovirus infected insect cells using [gamma-32P]ATP as substrate after 6...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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