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TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 0.910nMAssay Description:Inhibition of MB-COMT in Wistar rat brain assessed as metanephrine formation preincubated for 20 mins followed by addition of adrenaline as substrate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 0.912nMAssay Description:Inhibition of MB-COMT in Wistar rat brain assessed as metanephrine formation preincubated for 20 mins followed by addition of adrenaline as substrate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetLanosterol synthase(Rat)
Lieber Institute For Brain Development

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 1nMAssay Description:Inhibition of c-terminal hexa-His tagged human MB-COMT (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetLanosterol synthase(Rat)
Lieber Institute For Brain Development

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MB-COMT expressed in HEK293 cells using dopamine as substrate and SAM as cofactor preincubated for 30 mins followed by substrate ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of Catechol O-methyltransferase activity in rat brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of rat COMTMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of MB-COMT in rat brain homogenates using adrenaline as substrate and SAM as cofactor preincubated for 20 mins followed by substrate addit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 17nMAssay Description:Inhibition of MB-COMT in rat liver homogenates using adrenaline as substrate and SAM as cofactor preincubated for 20 mins followed by substrate addit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 31nMAssay Description:Inhibition of S-COMT in Wistar rat liver assessed as metanephrine formation preincubated for 20 mins followed by addition of adrenaline as substrate ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 53nMAssay Description:Inhibition of S-COMT in rat liver homogenates using adrenaline as substrate and SAM as cofactor preincubated for 20 mins followed by substrate additi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetLanosterol synthase(Rat)
Lieber Institute For Brain Development

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 127nMAssay Description:Inhibition of human recombinant His-tagged soluble COMT expressed in Escherichia coli BL21 using aesculetin as substrate after 60 mins by microplate ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/23/2017
Entry Details Article
PubMed
TargetGenome polyprotein(DENV-2)
Queensland University of Technology

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 640nMAssay Description:Inhibition of DENV2 NS2B-NS3 serine protease expressed using Benzoyl-Nle-Lys-Arg-Arg-AMC as substrate measured preincubated for 3 mins followed by su...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
TargetGenome polyprotein(DENV-2)
Queensland University of Technology

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 640nMAssay Description:Inhibition of Dengue Virus 4 recombinant NS2B-NS3 protease expressed in Escherichia coli using Bz-Nle-Arg-Arg-AMC as substrate incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
TargetGenome polyprotein(DENV-2)
Queensland University of Technology

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 640nMAssay Description:Inhibition of Dengue Virus 3 recombinant NS2B-NS3 protease expressed in Escherichia coli using Bz-Nle-Arg-Arg-AMC as substrate incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
TargetGenome polyprotein(DENV-2)
Queensland University of Technology

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 640nMAssay Description:Inhibition of Dengue Virus 1 recombinant NS2B-NS3 protease expressed in Escherichia coli using Bz-Nle-Arg-Arg-AMC as substrate incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
TargetGenome polyprotein(DENV-2)
Queensland University of Technology

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 640nMAssay Description:Inhibition of Dengue Virus 2 recombinant NS2B-NS3 protease expressed in Escherichia coli using Bz-Nle-Arg-Arg-AMC as substrate incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
TargetGenome polyprotein(WNV)
Australian National University Canberra

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 700nMAssay Description:Inhibition of West Nile virus NS2B-NS3 protease expressed in Escherichia coli using Bz-Nle-Lys-Arg-Arg-AMC as substrate assessed as proteolytic activ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details Article
PubMed
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 930nMAssay Description:Inhibitory activity against COMT in rat liverMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibitory activity against COMT in rat brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransthyretin(Human)
University of Toyama

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 3.20E+3nMAssay Description:Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 1.67E+4nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetTransthyretin(Human)
University of Toyama

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 3.00E+4nMAssay Description:Stabilization of wild type TTR (unknown origin) expressed in Escherichia coli assessed as reduction in methanol-induced aggregation incubated for 60 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 3.39E+4nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 3.45E+4nMAssay Description:Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 3.66E+4nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetBile salt export pump(Rat)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 4.72E+4nMAssay Description:Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate up...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetKrueppel-like factor 10(Human)
Beth Israel Deaconess Medical Center

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter d...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2016
Entry Details Article
PubMed
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 8.50E+4nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 1.20E+5nMAssay Description:Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptakeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetCatechol O-methyltransferase(Rat)
University of Porto

Curated by ChEMBL
LigandPNGBDBM50108877(CHEMBL1324 | Tasmar | Ro-40-7592 | (3,4-dihydroxy-...)
Affinity DataIC50: 9.27E+5nMAssay Description:Inhibition of Catechol O-methyltransferase activity in rat liverMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)