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TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50196926(Rocaglamide | CHEMBL438139 | US10085988, Compound ...)
Affinity DataKd:  156nMAssay Description:Binding affinity to full length recombinant eIF4A1 (unknown origin) assessed as induction ternary complex formation in presence of AGAGAG by measurin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataKd:  21nMAssay Description:Binding affinity to full length recombinant eIF4A1 (unknown origin) assessed as induction ternary complex formation in presence of AGAGAG by measurin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataKd:  3.19E+3nMAssay Description:Binding affinity to full length recombinant eIF4A1 (unknown origin) assessed as induction ternary complex formation in presence of AGAGAG by measurin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataKd:  9.60E+3nMAssay Description:Binding affinity to full length recombinant eIF4A1 (unknown origin) assessed as induction ternary complex formation in presence of AGAGAG by measurin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataKd:  2.43E+3nMAssay Description:Binding affinity to full length recombinant eIF4A1 (unknown origin) assessed as induction ternary complex formation in presence of AGAGAG by measurin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetGlutamate racemase(Helicobacter pylori (strain ATCC 700392 / 26695) (...)
Astrazeneca Global Structural Chemistry

Curated by ChEMBL
LigandPNGBDBM50215444(7-isobutyl-5-methyl-2-(naphthalen-1-ylmethyl)-3-(p...)
Affinity DataKd:  3.90E+3nMAssay Description:Binding affinity to Helicobacter pylori MurI by protein fluorescence binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGlutamate racemase(Helicobacter pylori (strain ATCC 700392 / 26695) (...)
Astrazeneca Global Structural Chemistry

Curated by ChEMBL
LigandPNGBDBM50215445(5-(2-((6-chloroquinolin-4-yl)methyl)-7-(cyclopropy...)
Affinity DataKd:  25nMAssay Description:Binding affinity to Helicobacter pylori MurI by protein fluorescence binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
TargetGlutamate racemase(Helicobacter pylori (strain ATCC 700392 / 26695) (...)
Astrazeneca Global Structural Chemistry

Curated by ChEMBL
LigandPNGBDBM50215444(7-isobutyl-5-methyl-2-(naphthalen-1-ylmethyl)-3-(p...)
Affinity DataKd:  2.90E+3nMAssay Description:Binding affinity to Helicobacter pylori MurI by isothermal titration calorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM50213021(CHEBI:63621 | Fortovase | Invirase | Ro-31-8959 | ...)
Affinity DataIC50: 0.0500nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468573(US10806794, Compound mPEG5-NHCO-Saquinavir)
Affinity DataIC50: 0.0500nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468574(US10806794, Compound mPEG7-NHCO-Saquinavir)
Affinity DataIC50: 0.0500nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468572(US10806794, Compound mPEG3-NHCO-Saquinavir)
Affinity DataIC50: 0.0700nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360964(CHEMBL1935285)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360965(CHEMBL1935286)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468568(US10806794, Compound mPEG1-OCONH-Tipranavir)
Affinity DataIC50: 0.188nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360966(CHEMBL1935287)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360967(CHEMBL1935288)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468563(US10806794, Compound mPEG5-O-Darunavir)
Affinity DataIC50: 0.210nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468567(US10806794, Compound mPEG0-OCONH-Tipranavir)
Affinity DataIC50: 0.292nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360956(CHEMBL1935304)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468564(US10806794, Compound mPEG7-O-Darunavir)
Affinity DataIC50: 0.358nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468366(US10806794, Compound mono-mPEG3-Atazanavir)
Affinity DataIC50: 0.366nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50295489((S)-2-(8-(Methoxycarbonylamino)dibenzo[b,d]thiophe...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human recombinant MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360963(CHEMBL1935284)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360968(CHEMBL1935290)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468570(US10806794, Compound mPEG5-OCONH-Tipranavir)
Affinity DataIC50: 0.462nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468562(US10806794, Compound mPEG3-O-Darunavir)
Affinity DataIC50: 0.475nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468569(US10806794, Compound mPEG3-OCONH-Tipranavir)
Affinity DataIC50: 0.617nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360959(CHEMBL1935280)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50401097(CHEMBL2204469)
Affinity DataIC50: 0.800nMAssay Description:Binding affinity to human CRTH2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50401116(CHEMBL2204474)
Affinity DataIC50: 0.800nMAssay Description:Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in CHO-K1 cells after 30 min by FRET methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50006915(CHEMBL3236929)
Affinity DataIC50: 0.800nMAssay Description:Antagonist activity at human recombinant CRTh2 expressed in CHO-K1 cells by cAMP TR FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2015
Entry Details Article
PubMed
TargetHistone deacetylase 1(Human)
Broad Institute of Harvard and Mit

LigandPNGBDBM29589(Panobinostat | Faridak | LBH-589B | LBH-589 | US10...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Purified HDAC1-9 (0.5~5 nM) were incubated with 2 μM carboxyfluorescein (FAM)-labeled acetylated peptide substrate A or B and test compound for ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/2/2016
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50026624(CHEMBL1935289)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360969(CHEMBL1935291)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50006823(CHEMBL3236950)
Affinity DataIC50: 1nMAssay Description:Antagonist activity at human recombinant CRTh2 expressed in CHO-K1 cells by cAMP TR FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2015
Entry Details Article
PubMed
TargetHistone deacetylase 1(Human)
Broad Institute of Harvard and Mit

LigandPNGBDBM19423(N-[2-amino-5-(thiophen-2-yl)phenyl]-4-acetamidoben...)
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyw...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/14/2017
Entry Details Article
PubMed
TargetHistone deacetylase 1(Human)
Broad Institute of Harvard and Mit

LigandPNGBDBM29589(Panobinostat | Faridak | LBH-589B | LBH-589 | US10...)
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyw...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/14/2017
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468560(US10806794, Compound mPEG5-N-Darunavir)
Affinity DataIC50: 1.10nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetCollagenase 3(Human)
Wyeth Research

Curated by ChEMBL
LigandPNGBDBM50295488((R)-2-(8-(Methoxycarbonylamino)dibenzo[b,d]thiophe...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of human recombinant MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50360970(CHEMBL1935292)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of human MMP-12More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50401097(CHEMBL2204469)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of CRTH2 receptor-mediated chemotaxis in human basophilsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50006830(CHEMBL3236948)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of CRTH2 receptor-mediated chemotaxis in human basophilsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2015
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468557(US10806794, Compound mono-mPEG7-Atazanavir)
Affinity DataIC50: 1.29nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetCollagenase 3(Human)
Wyeth Research

Curated by ChEMBL
LigandPNGBDBM28485((2S)-2-({4-[4-(1-benzofuran-2-amido)phenyl]benzene...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human recombinant MMP13More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM468372(US10806794, Compound mono-mPEG6-Atazanavir)
Affinity DataIC50: 1.31nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetMacrophage metalloelastase(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50295479((S)-3-Methyl-2-(8-(2-oxooxazolidin-3-yl)dibenzo[b,...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of human recombinant MMP12More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetProstaglandin D2 receptor 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50006830(CHEMBL3236948)
Affinity DataIC50: 1.40nMAssay Description:Binding affinity to human CRTH2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2015
Entry Details Article
PubMed
TargetHIV-1 protease(Human immunodeficiency virus)
Nektar Therapeutics

US Patent
LigandPNGBDBM8125(Darunavir (DRV) | CHEMBL1323 | (3R,3aS,6aR)-hexahy...)
Affinity DataIC50: 1.5nMAssay Description:Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2021
Entry Details
Go to US Patent

TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
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