Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 50 hits for monomerid = 14712,85305,85306,85307,85308,50018011,14712,85305,85306,85307,85308,50018011   

LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 9nMAssay Description:Inhibitory activity against rat dihydroorotate dehydrogenaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 13nMAssay Description:Inhibitory concentration tested against enzyme dihydroorotate dehydrogenase in ratMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/2/2012
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 17nMAssay Description:Inhibition of C-terminal His6-tagged rat DHODH expressed in Escherichia coli BL21(DE3) cells using L-DHO as substrate by DCIP dye based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 18nMAssay Description:Inhibition of rat DHODH (amino acid residues 30 to 396) expressed in Escherichia coli BL21 cells assessed as orotic acid production using dihydroorot...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 20nMAssay Description:Inhibition of dihydroorotate dehydrogenase in Wistar rat liver mitochondrial/microsomal membranes measured for 5 mins by 2,6-dichlorophenolindophenol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 20nMAssay Description:Inhibition of DHODH in Wistar rat liver homogenates by DCIP reduction assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2011
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 26nMAssay Description:Inhibition of rat dihydroorotate dehydrogenaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataKi:  30nM IC50: 260nMAssay Description:The assays were carried out by using a colorimetric DCIP method, which uses the colorimetric reagent 2, 6-dichlorophenolindophenol as the final elect...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/2/2007
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataKi:  32nM IC50: 261nMAssay Description:The assays were carried out by using a colorimetric DCIP method, which uses the colorimetric reagent 2, 6-dichlorophenolindophenol as the final elect...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/25/2009
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 64nMpH: 8.0Assay Description:Recombinant human DHODH (final enzyme concentration between 20 and 60 nM in the assay well) were incubated at 37 °C in 50 mM Tris-HCl, 0.1% Triton X-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/16/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Mouse)
Hoechst Marion Roussel

Curated by ChEMBL
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 69nMAssay Description:Inhibitory concentration tested on enzyme dihydroorotate dehydrogenase in mouseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/2/2012
Entry Details Article
PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Mouse)
Hoechst Marion Roussel

Curated by ChEMBL
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 110nMAssay Description:Inhibition of C-terminal His6-tagged mouse DHODH expressed in Escherichia coli BL21(DE3) cells using L-DHO as substrate by DCIP dye based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 130nMAssay Description:Inhibition of human DHODH expressed in Escherichia coli BL21(DE3) using L-dihydroorotate as substrate after 10 mins by DCIP dye reduction assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 137nMAssay Description:Inhibition of N-terminal His10-tagged human DHODH (Met30 to Arg396) expressed in Escherichia coli BL21 (DE3) using dihydroorotate as substrate measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Mouse)
Hoechst Marion Roussel

Curated by ChEMBL
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 150nMAssay Description:Inhibition of mouse DHODH (amino acid residues 30 to 396) expressed in Escherichia coli BL21 cells assessed as orotic acid production using dihydroor...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Mouse)
Hoechst Marion Roussel

Curated by ChEMBL
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 156nMAssay Description:Inhibitory activity against mouse dihydroorotate dehydrogenaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 163nMAssay Description:Inhibition of human DHODH using dihydroorotate substrate by DCIP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 200nMAssay Description:Immunosuppressive activity expressed as ability to inhibit human recombinant dihydroorotate dehydrogenase (DHODH)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 210nMAssay Description:Inhibition of C-terminal His6-tagged human DHODH (amino acid residues 30 to 396) expressed in Escherichia coli BL21 cells assessed as orotic acid pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 227nMAssay Description:Inhibition of human recombinant DHODH expressed in Escherichia coli BL21 (DE3) using dihydroorotate as substrate and CoQ6 as co-substrate incubated f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 230nMAssay Description:Spectrophotometric assay using crude human, recombinant DHODHase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2012
Entry Details

LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 300nMAssay Description:Inhibition of C-terminal His6-tagged human DHODH expressed in Escherichia coli BL21(DE3) cells using L-DHO as substrate by DCIP dye based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 312nMAssay Description:Inhibition of human DHODH using DHO as substrate measured at 4 secs interval for 60 secs by DCIP reduction based indirect assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 320nMAssay Description:Inhibition of human DHODHMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 356nMAssay Description:Inhibition of human DHODH assessed as decrease in DCIP using dihydroorotate as substrate measured every 30 seconds for 6 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/14/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDihydrofolate reductase(Human)
University of Torino

Curated by ChEMBL
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 388nMAssay Description:Inhibition of recombinant human N-terminal truncated GST-tagged DHFR (31 to 395 residues) expressed in Escherichia coli BL21(DE3) pyrD using DHO as s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/5/2019
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 388nMAssay Description:Inhibition of recombinant N-terminal GST-tagged human DHODH (31 to 395 residues) expressed in Escherichia coli BL21(DE3) assessed as inhibition of DC...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 408nMAssay Description:Inhibition of human N-terminal SUMO-tagged DHODH expressed in Escherichia coli BL21(DE3) using dihydroorotate substrate by DCIP based microplate read...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 408nMAssay Description:Inhibition of human DHODH incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 420nMAssay Description:Inhibition of N-terminally truncated recombinant human dihydroorotate dehydrogenase using in vitro enzyme assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 435nMAssay Description:In vitro inhibitory activity against human dihydroorotate dehydrogenase (DHODH)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 440nMAssay Description:Inhibition of C-terminal His6-tagged human DHODH (amino acid residues 30 to 396) expressed in Escherichia coli BL21 cells assessed as orotic acid pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of human recombinant DHODHMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 1.08E+3nMAssay Description:Inhibition of human dihydroorotate dehydrogenaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of recombinant N-terminal His-tagged human DHODH (31 to 395 residues) expressed in Escherichia coli using DL-dihydroorotic acid as substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataKi:  2.70E+3nMAssay Description:Inhibition of dihydroorotate dehydrogenaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2012
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 4.30E+3nMAssay Description:Inhibition of STIM1/Orai1 (unknown origin) expressed in HEK293 cells assessed as reduction in tBHQ-induced calcium responseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 5.01E+3nMAssay Description:Inhibition of His-tagged human DHODH assessed as reduction of DCIP by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataEC50:  8.90E+3nMAssay Description:Inhibition of DHODH in human HEK-293 cells transfected with ISRE-luciferase reporter gene assessed as increase in IFN-alpha mediated cellular respons...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataEC50:  8.91E+3nMAssay Description:Inhibition of DHODH in human HEK-293 cells transfected with ISRE-luciferase reporter gene assessed as increase in IFN-alpha mediated cellular respons...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(malaria parasite P. falciparum)
State Key Laboratory of Bioreactor Engineering

Curated by ChEMBL
LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataIC50: 1.14E+4nMAssay Description:Inhibition of Plasmodium falciparum DHODH expressed in Escherichia coli BL21 (DE3) using L-dihydroorotate as substrate after 10 mins by DCIP dye redu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Plasmodium falciparum (isolate 3D7))
University of Leeds

LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataKi:  2.20E+4nM ΔG°:  -6.35kcal/mole IC50: 1.90E+5nMpH: 8.0 T: 2°CAssay Description:The assays were carried out by using a colorimetric DCIP method, which uses the colorimetric reagent 2, 6-dichlorophenolindophenol as the final elect...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/25/2009
Entry Details Article
PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Plasmodium falciparum (isolate 3D7))
University of Leeds

LigandPNGBDBM14712(A77 1726 | CHEMBL973 | (2Z)-2-cyano-3-hydroxy-N-[4...)
Affinity DataKi:  2.34E+4nM ΔG°:  -6.31kcal/mole IC50: 1.90E+5nMpH: 8.0 T: 2°CAssay Description:The assays were carried out by using a colorimetric DCIP method, which uses the colorimetric reagent 2, 6-dichlorophenolindophenol as the final elect...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/2/2007
Entry Details Article
PubMed
LigandPNGBDBM85308(Tetrahydropyranyl derivative, 8 (E))
Affinity DataIC50: 5.00E+4nMAssay Description:Spectrophotometric assay using crude human, recombinant DHODHase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2012
Entry Details

LigandPNGBDBM85306(Tetrahydropyranyl derivative, 8 (Z))
Affinity DataIC50: 5.00E+4nMAssay Description:Spectrophotometric assay using crude human, recombinant DHODHase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2012
Entry Details

LigandPNGBDBM85307(Tetrahydrofuranyl derivative, 7 (E))
Affinity DataIC50: 5.00E+4nMAssay Description:Spectrophotometric assay using crude human, recombinant DHODHase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2012
Entry Details

TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Blood fluke)
University of Turin (Unito)

Curated by ChEMBL
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Schistosoma mansoni DHODHMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
LigandPNGBDBM85305(Tetrahydrofuranyl derivative, 7 (Z))
Affinity DataIC50: 5.00E+4nMAssay Description:Spectrophotometric assay using crude human, recombinant DHODHase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2012
Entry Details

TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Blood fluke)
University of Turin (Unito)

Curated by ChEMBL
LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of Schistosoma mansoni DHODH using DHO as substrate measured at 4 secs interval for 60 secs by DCIP reduction based indirect assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Plasmodium falciparum (isolate 3D7))
University of Leeds

LigandPNGBDBM50018011(CHEBI:68540 | HMR-1726 | Aubagio | TERIFLUNOMIDE)
Affinity DataIC50: 1.91E+5nMAssay Description:Inhibition of Plasmodium falciparum HIs6-tagged DHODH expressed in Escherichia coli DH5alpha using L-dihydroorotate as substrate by DCIP-based spectr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2020
Entry Details Article
PDB3D3D Structure (crystal)