BDBM50306576 (S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)-butyl]-thiophene-2-carbonyl}-amino)-pentanedioicAcid::AGF71::CHEMBL590740

SMILES Nc1nc2[nH]c(CCCCc3ccc(s3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)cc2c(=O)[nH]1

InChI Key InChIKey=ADFLVKAWSSGDBU-ZDUSSCGKSA-N

Data  4 KI  8 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 12 hits for monomerid = 50306576   

TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataKi:  130nMpH: 5.5Assay Description:Displacement of [3H]MTX from human PCFT expressed in Chinese hamster R2 cells at pH 5.5 by Dixon plotMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataKi:  230nMpH: 5.5Assay Description:Inhibition of [3H]MTX transport at human PCFT expressed in Chinese hamster R2 cells at pH 5.5 by Dixon plotMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataKi:  1.95E+3nMpH: 6.8Assay Description:Displacement of [3H]MTX from human PCFT expressed in Chinese hamster R2 cells at pH 6.8 by Dixon plotMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataKi:  7.23E+3nMpH: 6.8Assay Description:Inhibition of [3H]MTX transport at human PCFT expressed in Chinese hamster R2 cells at pH 6.8 by Dixon plotMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  3.10nMAssay Description:Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as incorporation of [U-14C]-glycine into [14C]-formyl glycinamide ribon...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Mus musculus)
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  60nMAssay Description:Inhibition of mouse recombinant GARFtase assessed as FGAR formation by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  630nMAssay Description:Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  43nMAssay Description:Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReduced folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50: >1.00E+3nMAssay Description:Binding affinity to human RFC expressed in Chinese hamster PC43-10 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  22nMpH: 7.5Assay Description:GARFTase activity was determined by measuring the rate of 5,8-dideazatetrahydrofolate production in the presence of varying concentrations of antifol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  3.46nMAssay Description:Inhibition of GARFTase in human IGROV1 cells assessed as reduction in [14C]glycine incorporation into [14C]formyl GAR incubated for 15 hrs in complet...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50306576((S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo...)
Affinity DataIC50:  1.80nMAssay Description:Binding affinity to human FRalpha expressed in Chinese hamster RT16 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed