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Found 749 with Last Name = 'thomas' and Initial = 'ag'
TargetGlutamate carboxypeptidase 2(Homo sapiens (Human))
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM17659((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)
Affinity DataKi:  0.200nMAssay Description:Concentration of the compound required for the neuroprotective effect determined by inhibition of GCP IIMore data for this Ligand-Target Pair
TargetBacterial leucyl aminopeptidase(Vibrio proteolyticus)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50129200((R)-2-Amino-4-methyl-pentanoic acid hydroxyamide |...)
Affinity DataKi:  2nMAssay Description:Inhibition of metalloprotease from family M28, Aeromonas proteolytica aminopeptidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD-amino-acid oxidase(Homo sapiens (Human))
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50117763(CHEMBL3613921 | US9505753, 5u)
Affinity DataKi:  60nMAssay Description:Competitive inhibition of recombinant human DAAO expressed in HEK cells by double reciprocal plot analysis in presence of D-serineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBacterial leucyl aminopeptidase(Vibrio proteolyticus)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50129202((S)-2-Amino-4-methyl-pentanoic acid hydroxyamide |...)
Affinity DataKi:  350nMAssay Description:Inhibition of metalloprotease from family M28, Aeromonas proteolytica aminopeptidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminase kidney isoform, mitochondrial(Homo sapiens (Human))
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM108460(CHEMBL2178393 | US11191732, Example 1 | US8604016,...)
Affinity DataKi:  2.00E+3nMAssay Description:Uncompetitive inhibition of human kidney glutaminase (124 to 669) assessed as reduction of glutamine hydrolysis by double-reciprocal plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAndrogen receptor(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50432188(CHEMBL2346976)
Affinity DataKi:  2.20E+3nMAssay Description:Displacement of [3H]R1881 from full length androgen receptor in human LNCAP cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAndrogen receptor(Rattus norvegicus (Rat))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50432188(CHEMBL2346976)
Affinity DataKi:  5.00E+3nMAssay Description:Binding affinity to rat androgen receptor ligand binding domain by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD-amino-acid oxidase(Sus scrofa (pig))
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50031467(5-HYDROXY-2-(HYDROXYMETHYL)-4H-PYRAN-4-ONE | 5-Hyd...)
Affinity DataKi:  2.10E+4nMAssay Description:Competitive inhibition of pig kidney DAAO using D-Alanine as substrate by Michaelis-Menten plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Eisai

Curated by ChEMBL
LigandPNGBDBM50509099(CHEMBL4565294)
Affinity DataKi:  7.27E+4nMAssay Description:Displacement of [3H]DAMGO from mu opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDelta-type opioid receptor(Rattus norvegicus (rat))
Eisai

Curated by ChEMBL
LigandPNGBDBM50509099(CHEMBL4565294)
Affinity DataKi:  2.20E+5nMAssay Description:Displacement of [3H]DADLE from delta opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Rattus norvegicus (rat))
Eisai

Curated by ChEMBL
LigandPNGBDBM50509099(CHEMBL4565294)
Affinity DataKi:  1.43E+6nMAssay Description:Displacement of [3H]U-69,593 from kappa opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDelta-type opioid receptor(Rattus norvegicus (rat))
Eisai

Curated by ChEMBL
LigandPNGBDBM50509101(CHEMBL4460098)
Affinity DataKi:  2.47E+6nMAssay Description:Displacement of [3H]DADLE from delta opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
Eisai

Curated by ChEMBL
LigandPNGBDBM50509101(CHEMBL4460098)
Affinity DataKi:  3.73E+6nMAssay Description:Displacement of [3H]DAMGO from mu opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Rattus norvegicus (rat))
Eisai

Curated by ChEMBL
LigandPNGBDBM50509101(CHEMBL4460098)
Affinity DataKi:  1.21E+7nMAssay Description:Displacement of [3H]U-69,593 from kappa opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate carboxypeptidase 2 [44-750](Homo sapiens (Human))
Guilford Pharmaceuticals

LigandPNGBDBM17759((2S)-2-(phosphonomethyl)pentanedioic acid | (S)-2-...)
Affinity DataIC50:  0.100nMpH: 7.4 T: 2°CAssay Description:GCPII activity in vitro is monitored through the hydrolysis [3H]NAAG to NAA and [3H]Glu. The radioactivity-based assay was miniaturized to a 96-well ...More data for this Ligand-Target Pair
TargetGlutamate carboxypeptidase 2 [44-750](Homo sapiens (Human))
Guilford Pharmaceuticals

LigandPNGBDBM17659((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)
Affinity DataIC50:  0.300nMpH: 7.4 T: 2°CAssay Description:GCPII activity in vitro is monitored through the hydrolysis [3H]NAAG to NAA and [3H]Glu. The radioactivity-based assay was miniaturized to a 96-well ...More data for this Ligand-Target Pair
TargetGlutamate carboxypeptidase 2(Homo sapiens (Human))
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM17659((R,S)-2-phosphonomethylpentanedioic acid | 2-(phos...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of Glutamate carboxypeptidase IIMore data for this Ligand-Target Pair
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50459018(CHEMBL4166405)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50535970(CHEMBL4569967)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50459007(CHEMBL4218734)
Affinity DataIC50: <1.20nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50535972(CHEMBL4565988)
Affinity DataIC50:  2nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50208517(2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one | C...)
Affinity DataIC50: <2nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
TargetCystine/glutamate transporter(Homo sapiens (Human))
Columbia University

Curated by ChEMBL
LigandPNGBDBM50126160(CHEMBL3629669)
Affinity DataIC50:  4nMAssay Description:Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDNA-dependent protein kinase catalytic subunit(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50535972(CHEMBL4565988)
Affinity DataIC50:  5nMAssay Description:Inhibition of DNAPK (unknown origin) using p53-based peptide substrate preincubated for 5 min prior to ATP additionMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50535972(CHEMBL4565988)
Affinity DataIC50:  8nMAssay Description:Inhibition of human recombinant PI3Kalpha using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent base...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50535971(CHEMBL4593348)
Affinity DataIC50:  8nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521402(CHEMBL4471834)
Affinity DataIC50:  10nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50459011(CHEMBL4215266)
Affinity DataIC50:  10nMAssay Description:Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCystine/glutamate transporter(Homo sapiens (Human))
Columbia University

Curated by ChEMBL
LigandPNGBDBM50126159(CHEMBL3629668)
Affinity DataIC50:  10nMAssay Description:Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCystine/glutamate transporter(Homo sapiens (Human))
Columbia University

Curated by ChEMBL
LigandPNGBDBM50126156(CHEMBL3629579)
Affinity DataIC50:  10nMAssay Description:Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50535995(CHEMBL4517663)
Affinity DataIC50:  19nMAssay Description:Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521405(CHEMBL4551018)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521425(CHEMBL4449305)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM67506(4-(4,5-diphenyl-1,3-dihydroimidazol-2-ylidene)-2,6...)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCystine/glutamate transporter(Homo sapiens (Human))
Columbia University

Curated by ChEMBL
LigandPNGBDBM50126155(CHEMBL3629578)
Affinity DataIC50:  20nMAssay Description:Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521404(CHEMBL4449307)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521420(CHEMBL4467223)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50145038(CHEMBL2143829)
Affinity DataIC50:  21nMAssay Description:Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50535972(CHEMBL4565988)
Affinity DataIC50:  21nMAssay Description:Inhibition of human recombinant PI3Kbeta using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate carboxypeptidase 2 [44-750](Homo sapiens (Human))
Guilford Pharmaceuticals

LigandPNGBDBM17758((2R)-2-(phosphonomethyl)pentanedioic acid | (R)-2-...)
Affinity DataIC50:  30nMpH: 7.4 T: 2°CAssay Description:GCPII activity in vitro is monitored through the hydrolysis [3H]NAAG to NAA and [3H]Glu. The radioactivity-based assay was miniaturized to a 96-well ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521419(CHEMBL1342201)
Affinity DataIC50:  30nMAssay Description:Inhibition of human recombinant nSMase expressed in HEK293 cells using sphingomyelin as substrate by alkaline phosphatase, choline oxidase and horser...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminase kidney isoform, mitochondrial(Homo sapiens (Human))
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50547684(CHEMBL4740067)
Affinity DataIC50:  30nMAssay Description:Allosteric inhibition of human kidney glutaminase using [3H]-Glutamine as substrate in presence of inhibitor incubated for 45 mins by Perkin Elmer ba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCystine/glutamate transporter(Homo sapiens (Human))
Columbia University

Curated by ChEMBL
LigandPNGBDBM50126162(CHEMBL3629671)
Affinity DataIC50:  30nMAssay Description:Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSphingomyelin phosphodiesterase 3(Homo sapiens)
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50521419(CHEMBL1342201)
Affinity DataIC50:  30nMAssay Description:Inhibition of human recombinant full-length nSMase expressed in HEK293 cells using sphingomyelin as substrate measured after 1 hr by alkaline phospha...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCystine/glutamate transporter(Homo sapiens (Human))
Columbia University

Curated by ChEMBL
LigandPNGBDBM50126153(CHEMBL3629576)
Affinity DataIC50:  30nMAssay Description:Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50459018(CHEMBL4166405)
Affinity DataIC50:  33nMAssay Description:Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate carboxypeptidase 2 [44-750](Homo sapiens (Human))
Guilford Pharmaceuticals

LigandPNGBDBM17754((2S)-2-({hydroxy[(2,3,4,5,6-pentafluorophenyl)meth...)
Affinity DataIC50:  34nMpH: 7.4 T: 2°CAssay Description:GCPII activity in vitro is monitored through the hydrolysis [3H]NAAG to NAA and [3H]Glu. The radioactivity-based assay was miniaturized to a 96-well ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD-amino-acid oxidase(Homo sapiens (Human))
Johns Hopkins University

Curated by ChEMBL
LigandPNGBDBM50467718(CHEMBL4287507)
Affinity DataIC50:  36nMAssay Description:Inhibition of human DAO using D-serine as substrate after 20 mins in presence of FADMore data for this Ligand-Target Pair
LigandPNGBDBM50535990(CHEMBL4527822)
Affinity DataIC50:  36nMAssay Description:Inhibition of human recombinant PI3Kalpha using PIP2/ATP as substrate incubated for 20 mins followed by substrate addition by Kinase Glo reagent base...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50536001(CHEMBL4576302)
Affinity DataIC50:  39nMAssay Description:Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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