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Found 189 with Last Name = 'karim' and Initial = 'a'
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027656(CHEBI:63616 | LY-2315 | LY-231514 | PEMETREXED | U...)
Affinity DataKi:  259nMAssay Description:Inhibition of [3H]MTX uptake at human PCFT expressed in Chinese hamster R2/PCFT4 cells at pH 5.5 measured after 2 mins by Dixon plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457435(CHEMBL4214638)
Affinity DataKi:  332nMAssay Description:Inhibition of [3H]MTX uptake at human PCFT expressed in Chinese hamster R2/PCFT4 cells at pH 5.5 measured after 2 mins by Dixon plot analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50171511((S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[...)
Affinity DataKi:  460nMAssay Description:Inhibition of [3H]MTX uptake at human PCFT expressed in Chinese hamster R2/PCFT4 cells at pH 5.5 measured after 2 mins by Dixon plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222139(Chymostatin | US11859014, Compound chymostatin)
Affinity DataKi:  2.60E+3nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM50289012(2-(2-Fluoro-phenyl)-benzo[d][1,3]oxazin-4-one | 2-...)
Affinity DataKi:  4.70E+3nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM50077011(2-Phenyl-4H-3,1-benzoxazin-4-one (3) | 2-Phenyl-be...)
Affinity DataKi:  8.70E+3nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222117(2-(2-Thienyl)-4H-3,1-benzoxazin-4-one (4) | US1158...)
Affinity DataKi:  9.10E+3nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM50289006(2-(2-Bromo-phenyl)-benzo[d][1,3]oxazin-4-one | 2-(...)
Affinity DataKi:  9.10E+3nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222124(2-(2-Methylphenyl)-4H-3,1-benzoxazin-4-one (13))
Affinity DataKi:  9.80E+3nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM50289000(2-(2-Methoxy-phenyl)-benzo[d][1,3]oxazin-4-one | 2...)
Affinity DataKi:  1.25E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222118(2-(4-Methoxyphenyl)-4H-3,1-benzoxazin-4-one (5))
Affinity DataKi:  1.26E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222121(2-(3-Methylphenyl)-4H-3,1-benzoxazin-4-one (10))
Affinity DataKi:  1.61E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222119(2-(4-Methylphenyl)-4H-3,1-benzoxazin-4-one (7))
Affinity DataKi:  1.64E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222123(2-(3-Fluorophenyl)-4H-3,1-benzoxazin-4-one (12))
Affinity DataKi:  1.78E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM33703(2-(2-Nitro-phenyl)-benzo[d][1,3]oxazin-4-one | 2-(...)
Affinity DataKi:  2.24E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222125(2-(3-Chlorophenyl)-4H-3,1-benzoxazin-4-one (14))
Affinity DataKi:  2.26E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222122(2-(2,6-Dimethoxyphenyl)-4H-3,1-benzoxazin-4-one (1...)
Affinity DataKi:  2.77E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222120(2-(2,6-Difluorophenyl)-4H-3,1-benzoxazin-4-one (8))
Affinity DataKi:  3.01E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222127(2-(4-Fluorophenyl)-4H-3,1-benzoxazin-4-one (16))
Affinity DataKi:  9.41E+4nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222126(2-(3-Methylphenyl)-7-nitro-4H-3,1-benzoxazin-4-one...)
Affinity DataKi:  1.62E+5nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM222128(7-Chloro-2-(2-fluorophenyl)-4H-3,1-benzoxazin-4-on...)
Affinity DataKi:  3.03E+5nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
University of Karachi

LigandPNGBDBM50449429(2-(3-Nitrophenyl)-4H-3,1-benzoxazin-4-one (18) | C...)
Affinity DataKi:  3.41E+5nMAssay Description:The change in optical density per minute (OD/min) was obtained by incorporating various concentrations of compounds over a range of substrate (SPpNA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor beta(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457435(CHEMBL4214638)
Affinity DataIC50:  0.580nMAssay Description:Binding affinity to human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReduced folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457437(CHEBI:71223 | Folotyn | PDX | Pralatrexate)
Affinity DataIC50:  0.690nMAssay Description:Binding affinity to human RFC expressed in Chinese hamster PC43-10 cells assessed as antiproliferative activity measured as reduction in cell viabili...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50: <1nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457435(CHEMBL4214638)
Affinity DataIC50:  1.30nMAssay Description:Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in c...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457435(CHEMBL4214638)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of GARFTase in human KB cells assessed as decrease in [14C]formyl GAR accumulation preincubated for 30 mins followed by [14C]glycine addit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Vanderbilt University

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  3.29nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457433(CHEMBL4213181)
Affinity DataIC50:  4.40nMAssay Description:Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in c...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457432(CHEMBL4205344)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of GARFTase in human KB cells assessed as decrease in [14C]formyl GAR accumulation preincubated for 30 mins followed by [14C]glycine addit...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTrifunctional purine biosynthetic protein adenosine-3(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50171511((S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[...)
Affinity DataIC50:  5.60nMAssay Description:Inhibition of GARFTase in human KB cells assessed as decrease in [14C]formyl GAR accumulation preincubated for 30 mins followed by [14C]glycine addit...More data for this Ligand-Target Pair
TargetFolate receptor beta(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50171511((S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[...)
Affinity DataIC50:  5.60nMAssay Description:Binding affinity to human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlatelet-derived growth factor receptor beta(Homo sapiens (Human))
Vanderbilt University

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  6.14nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReduced folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027655(CHEBI:5847 | Raltitrexed | Tomudex | US9422297, Ra...)
Affinity DataIC50:  6.30nMAssay Description:Binding affinity to human RFC expressed in Chinese hamster PC43-10 cells assessed as antiproliferative activity measured as reduction in cell viabili...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50171511((S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[...)
Affinity DataIC50:  6.30nMAssay Description:Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in c...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReduced folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM66082((2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methy...)
Affinity DataIC50:  12nMAssay Description:Binding affinity to human RFC expressed in Chinese hamster PC43-10 cells assessed as antiproliferative activity measured as reduction in cell viabili...More data for this Ligand-Target Pair
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027656(CHEBI:63616 | LY-2315 | LY-231514 | PEMETREXED | U...)
Affinity DataIC50:  13nMAssay Description:Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as antiproliferative activity measured as reduction in cell viabi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027655(CHEBI:5847 | Raltitrexed | Tomudex | US9422297, Ra...)
Affinity DataIC50:  15nMAssay Description:Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in c...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457432(CHEMBL4205344)
Affinity DataIC50:  15nMAssay Description:Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in c...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetFolate receptor beta(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457433(CHEMBL4213181)
Affinity DataIC50:  19nMAssay Description:Binding affinity to human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetFolate receptor beta(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027655(CHEBI:5847 | Raltitrexed | Tomudex | US9422297, Ra...)
Affinity DataIC50:  22nMAssay Description:Binding affinity to human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Vanderbilt University

LigandPNGBDBM50262685(6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-...)
Affinity DataIC50:  25.1nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetActivin receptor type-1(Homo sapiens (Human))
Vanderbilt University

LigandPNGBDBM36356(DMH3 | N,N-dimethyl-3-(4- (3-(quinolin-4-yl)pyrazo...)
Affinity DataIC50:  26.7nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFolate receptor beta(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457432(CHEMBL4205344)
Affinity DataIC50:  37nMAssay Description:Binding affinity to human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetActivin receptor type-1(Homo sapiens (Human))
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  40.7nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
TargetFolate receptor alpha(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027656(CHEBI:63616 | LY-2315 | LY-231514 | PEMETREXED | U...)
Affinity DataIC50:  42nMAssay Description:Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in c...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetActivin receptor type-1(Homo sapiens (Human))
Vanderbilt University

LigandPNGBDBM36355(4-(2-(4-(3-(quinolin-4-yl)pyrazolo[1,5-a]pyrimidin...)
Affinity DataIC50:  42.8nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457437(CHEBI:71223 | Folotyn | PDX | Pralatrexate)
Affinity DataIC50:  57nMAssay Description:Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as antiproliferative activity measured as reduction in cell viabi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProton-coupled folate transporter(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50457435(CHEMBL4214638)
Affinity DataIC50:  58nMAssay Description:Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as antiproliferative activity measured as reduction in cell viabi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetFolate receptor beta(Homo sapiens (Human))
Duquesne University

Curated by ChEMBL
LigandPNGBDBM50027656(CHEBI:63616 | LY-2315 | LY-231514 | PEMETREXED | U...)
Affinity DataIC50:  60nMAssay Description:Binding affinity to human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell...More data for this Ligand-Target Pair
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