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TargetPotassium voltage-gated channel subfamily H member 2(Human)
University of Washington

Curated by ChEMBL
LigandPNGBDBM50365230(CHEMBL1956285 | US9238653, Table 5, Compound 10 | ...)
Affinity DataEC50:  1.60E+3nMAssay Description:Inhibition of human ERG by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
University of Washington

Curated by ChEMBL
LigandPNGBDBM50365230(CHEMBL1956285 | US9238653, Table 5, Compound 10 | ...)
Affinity DataEC50:  7.00E+3nMAssay Description:Inhibition of human ERG by IonWorks patch clamp electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
University of Washington

Curated by ChEMBL
LigandPNGBDBM50538344(CHEMBL4633246)
Affinity DataEC50: >3.30E+4nMAssay Description:Inhibition of human ERG by IonWorks patch clamp electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
University of Washington

Curated by ChEMBL
LigandPNGBDBM50538344(CHEMBL4633246)
Affinity DataEC50: >3.30E+4nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks patch clamp electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Human)
University of Washington

Curated by ChEMBL
LigandPNGBDBM50538344(CHEMBL4633246)
Affinity DataEC50: >3.30E+4nMAssay Description:Inhibition of human Cav1.2 by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily A member 5(Human)
University of Washington

Curated by ChEMBL
LigandPNGBDBM50538344(CHEMBL4633246)
Affinity DataEC50: >1.10E+4nMAssay Description:Inhibition of human Kv1.5 by IonWorks patch clamp electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Rat)
University of Texas At Dallas

Curated by ChEMBL
LigandPNGBDBM50018008(CHEMBL3289671 | US9238653, Table 5, Compound 43)
Affinity DataKd:  48nMAssay Description:Binding affinity to rat DHODH by isothermal titration calorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50337733(N-((2S,4S)-1-(4-(2,4-dichlorobenzyloxy)piperidin-1...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of CYP3A4More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337721(N-((2S,4S)-1-(4-(4-fluoro-2-methylphenethyl)piperi...)
Affinity DataIC50: 0.180nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337722(N-((2S,4S)-1-(4-(2-(3,5-dimethylisothiazol-4-yl)et...)
Affinity DataIC50: 0.260nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337723(N-((2S,4S)-1-(4-(4-chloro-2-methylphenethyl)piperi...)
Affinity DataIC50: 0.360nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337724(N-((2S,4S)-1-(4-(2-(2,5-dimethylpyridin-4-yl)ethyl...)
Affinity DataIC50: 0.430nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337727(N-((2S,4S)-1-(4-(2,5-dimethylphenethyl)piperidin-1...)
Affinity DataIC50: 0.480nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337725(N-((2S,4S)-1-(4-(2-chloro-4-(trifluoromethyl)phene...)
Affinity DataIC50: 0.480nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337726(N-((2S,4S)-1-(4-(2-bromo-4-fluorophenethyl)piperid...)
Affinity DataIC50: 0.480nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337736(N-((2S,4S)-4-(5-fluoropyrimidin-2-yl)-2-methyl-1-(...)
Affinity DataIC50: 0.490nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337731(N-((2S,4S)-1-(4-(4-fluoro-2-(trifluoromethyl)phene...)
Affinity DataIC50: 0.520nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337734(N-((2S,4S)-1-(4-(2-chloro-4-(methylsulfonyl)phenet...)
Affinity DataIC50: 0.570nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337739(N-((2S,4S)-1-(4-(2-(4,6-dimethylpyridin-3-yl)ethyl...)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337735(N-[(2S,4S)-1-({4-[2-(3,5-dimethyl-1,2-oxazol-4-yl)...)
Affinity DataIC50: 0.690nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337743(N-((2S,4S)-1-(4-(2-cyclopropyl-4-(trifluoromethyl)...)
Affinity DataIC50: 0.940nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337733(N-((2S,4S)-1-(4-(2,4-dichlorobenzyloxy)piperidin-1...)
Affinity DataIC50: 1nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337744(N-((2S,4S)-1-(4-(2,4-dichlorophenethyl)piperidin-1...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetProteasome subunit beta type-8(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50550643(CHEMBL4749207)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human 20S immunoproteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of P...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetProteasome subunit beta type-5(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50550643(CHEMBL4749207)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of human 20S constitutive proteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
LigandPNGBDBM50337730(N-((2S,4S)-1-(4-(4-fluorophenyl)piperazin-1-ylsulf...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50337730(N-((2S,4S)-1-(4-(4-fluorophenyl)piperazin-1-ylsulf...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of CYP3A4More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337737(N-((2S,4S)-1-(4-(2-(2,5-dimethylpyridin-3-yl)ethyl...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetProteasome subunit beta type-8(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50069989(CHEMBL325041 | (R)-3-methyl-1-((S)-3-phenyl-2-(pyr...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human 20S immunoproteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of P...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
LigandPNGBDBM50337740(N-((2S,4S)-4-(5-fluoropyrimidin-2-yl)-2-methyl-1-(...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337732(N-((2S,4S)-1-(4-(2-chloro-5-fluorophenethyl)piperi...)
Affinity DataIC50: 2.80nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337729(N-((2S,4S)-1-(4-(2,4-dichlorobenzyloxy)piperidin-1...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337745(N-((2S,4S)-1-(4-(2,4-dichlorophenethyl)piperazin-1...)
Affinity DataIC50: 3.80nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandPNGBDBM50337741(N-((2S,4S)-1-(4-(2-(3-chloro-5-(trifluoromethyl)py...)
Affinity DataIC50: 4.20nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetProteasome subunit beta type-9(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50550643(CHEMBL4749207)
Affinity DataIC50: 5nMAssay Description:Inhibition of human 20S immunoproteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA2...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetProteasome subunit beta type-9(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50069989(CHEMBL325041 | (R)-3-methyl-1-((S)-3-phenyl-2-(pyr...)
Affinity DataIC50: 5nMAssay Description:Inhibition of human 20S immunoproteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA2...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetProteasome subunit beta type-8(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50550642(CHEMBL4787081)
Affinity DataIC50: 5nMAssay Description:Inhibition of human 20S immunoproteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of P...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
LigandPNGBDBM50337742(N-((2S,4S)-1-(4-(2-(1,3-dimethyl-1H-pyrazol-5-yl)e...)
Affinity DataIC50: 5.40nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetProteasome subunit beta type-5(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50069989(CHEMBL325041 | (R)-3-methyl-1-((S)-3-phenyl-2-(pyr...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human 20S constitutive proteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetPlasmepsin X(Plasmodium falciparum (isolate 3D7))
Ucb

Curated by ChEMBL
LigandPNGBDBM50591317(CHEMBL5191783)
Affinity DataIC50: 7nMAssay Description:Inhibition of Plasmodium falciparum recombinant C-terminal TEV cleavable 8his-tagged PMX by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
TargetPlasmepsin X(Plasmodium falciparum (isolate 3D7))
Ucb

Curated by ChEMBL
LigandPNGBDBM50591320(CHEMBL5190700)
Affinity DataIC50: 7nMAssay Description:Inhibition of Plasmodium falciparum recombinant C-terminal TEV cleavable 8his-tagged PMX by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
TargetPlasmepsin X(Plasmodium falciparum (isolate 3D7))
Ucb

Curated by ChEMBL
LigandPNGBDBM50591320(CHEMBL5190700)
Affinity DataIC50: 7nMAssay Description:Inhibition of PMX in Plasmodium falciparum 3D7 HA epitopeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
LigandPNGBDBM50337728(N-((2S,4S)-1-(4-(4-fluorophenyl)piperazin-1-ylsulf...)
Affinity DataIC50: 7.30nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetMatrix metalloproteinase-14(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50337728(N-((2S,4S)-1-(4-(4-fluorophenyl)piperazin-1-ylsulf...)
Affinity DataIC50: 7.60nMAssay Description:Inhibition of recombinant human MMP14 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetCollagenase 3(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50337728(N-((2S,4S)-1-(4-(4-fluorophenyl)piperazin-1-ylsulf...)
Affinity DataIC50: 7.60nMAssay Description:Inhibition of recombinant human MMP13 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
TargetProteasome subunit beta type-9(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50550640(CHEMBL4749043)
Affinity DataIC50: 8nMAssay Description:Inhibition of human 20S immunoproteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA2...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetProteasome subunit beta type-5(Human)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50550642(CHEMBL4787081)
Affinity DataIC50: 9nMAssay Description:Inhibition of human 20S constitutive proteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetPlasmepsin X(Plasmodium falciparum (isolate 3D7))
Ucb

Curated by ChEMBL
LigandPNGBDBM50591318(CHEMBL5204196)
Affinity DataIC50: 9nMAssay Description:Inhibition of Plasmodium falciparum recombinant C-terminal TEV cleavable 8his-tagged PMX by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Plasmodium falciparum (isolate 3D7))
The Walter and Eliza Hall Institute of Medical Research

Curated by ChEMBL
LigandPNGBDBM50365230(CHEMBL1956285 | US9238653, Table 5, Compound 10 | ...)
Affinity DataIC50: 10nMAssay Description:Inhibition of Plasmodium falciparum DHODH expressed in Escherichia coli using L-dihydroorotate as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Plasmodium falciparum (isolate 3D7))
The Walter and Eliza Hall Institute of Medical Research

Curated by ChEMBL
LigandPNGBDBM50519564(CHEMBL4545127)
Affinity DataIC50: 10nMAssay Description:Inhibition of Plasmodium falciparum DHODH expressed in Escherichia coli using L-dihydroorotate as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
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