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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
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578782(US11492351, Example 1-7 | 4-(aminomethyl)-6-(1-met...)
Affinity DataKd:  1.10E+5nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM50585592(CHEMBL5082733)
Affinity DataKd:  1.00E+4nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of MTA by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578782(US11492351, Example 1-7 | 4-(aminomethyl)-6-(1-met...)
Affinity DataKd:  5nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of MTA by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11492351, Example 16-8 | US11479551, Example 16-...)
Affinity DataKd:  0nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of MTA by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM50585592(CHEMBL5082733)
Affinity DataKd:  5.10E+4nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of SAM by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578782(US11492351, Example 1-7 | 4-(aminomethyl)-6-(1-met...)
Affinity DataKd:  83nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of SAM by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11492351, Example 16-8 | US11479551, Example 16-...)
Affinity DataKd:  0.00900nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of SAM by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM50585593(CHEMBL5076988)
Affinity DataKd:  1.62E+3nMAssay Description:Binding affinity to MTA-bound human PRMT5 assessed as dissociation constant by SPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataKd:  1.10E+4nMAssay Description:Binding affinity to MTA-bound human PRMT5 assessed as dissociation constant by SPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM22111((2R,3R,4S,5S)-2-(6-aminopurin-9-yl)-5-(methylsulfa...)
Affinity DataKd:  661nMAssay Description:Inhibition of streptavidin sensor chip immobilized biotinylated human PRMT5/MEP50 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
LigandPNGBDBM50585598(CHEMBL1235831)
Affinity DataKd:  550nMAssay Description:Inhibition of streptavidin sensor chip immobilized biotinylated human PRMT5/MEP50 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
LigandPNGBDBM50325724((R)-1-phenyl-N-((6-(trifluoromethoxy)-4'-(trifluor...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325725((R)-N-benzyl-1-(3-methoxyphenyl)ethanamine | CHEMB...)
Affinity DataEC50:  1.20E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325726((R)-N-(2-chlorobenzyl)-1-(3-methoxyphenyl)ethanami...)
Affinity DataEC50:  3.70E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325727((R)-N-((2'-chlorobiphenyl-3-yl)methyl)-1-(3-methox...)
Affinity DataEC50:  350nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325728((R)-N-(4-methoxybenzyl)-1-(3-methoxyphenyl)ethanam...)
Affinity DataEC50:  370nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325729((R)-N-((2'-fluorobiphenyl-3-yl)methyl)-1-(3-methox...)
Affinity DataEC50:  2.70E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325730((R)-1-(3-methoxyphenyl)-N-((2'-methylbiphenyl-3-yl...)
Affinity DataEC50:  2.20E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325731((R)-N-((2'-methoxybiphenyl-3-yl)methyl)-1-(3-metho...)
Affinity DataEC50:  1.40E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325732((R)-N-((4'-methoxybiphenyl-3-yl)methyl)-1-(3-metho...)
Affinity DataEC50:  870nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325733((R)-1-(3-methoxyphenyl)-N-((4'-(trifluoromethyl)bi...)
Affinity DataEC50:  620nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325734((R)-N-((6-methoxy-4'-(trifluoromethyl)biphenyl-3-y...)
Affinity DataEC50:  23nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325735((R)-N-((6-methoxy-4'-(trifluoromethyl)biphenyl-3-y...)
Affinity DataEC50:  27nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325736((R)-1-(3-fluorophenyl)-N-((6-methoxy-4'-(trifluoro...)
Affinity DataEC50:  37nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325737(N-((6-methoxy-4'-(trifluoromethyl)biphenyl-3-yl)me...)
Affinity DataEC50:  160nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325738((R)-N-((6-chloro-4'-(trifluoromethyl)biphenyl-3-yl...)
Affinity DataEC50:  280nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325739((R)-1-(4-fluorophenyl)-N-((6-methoxy-4'-(trifluoro...)
Affinity DataEC50:  58nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325740((R)-1-(6-methoxy-4'-(trifluoromethyl)biphenyl-3-yl...)
Affinity DataEC50:  17nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325741((S)-1-(6-methoxy-4'-(trifluoromethyl)biphenyl-3-yl...)
Affinity DataEC50:  3.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325724((R)-1-phenyl-N-((6-(trifluoromethoxy)-4'-(trifluor...)
Affinity DataEC50:  110nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325727((R)-N-((2'-chlorobiphenyl-3-yl)methyl)-1-(3-methox...)
Affinity DataEC50:  1.70E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325740((R)-1-(6-methoxy-4'-(trifluoromethyl)biphenyl-3-yl...)
Affinity DataEC50:  2.10E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325739((R)-1-(4-fluorophenyl)-N-((6-methoxy-4'-(trifluoro...)
Affinity DataEC50:  1.70E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325737(N-((6-methoxy-4'-(trifluoromethyl)biphenyl-3-yl)me...)
Affinity DataEC50:  430nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325736((R)-1-(3-fluorophenyl)-N-((6-methoxy-4'-(trifluoro...)
Affinity DataEC50:  1.30E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325734((R)-N-((6-methoxy-4'-(trifluoromethyl)biphenyl-3-y...)
Affinity DataEC50:  720nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325725((R)-N-benzyl-1-(3-methoxyphenyl)ethanamine | CHEMB...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325726((R)-N-(2-chlorobenzyl)-1-(3-methoxyphenyl)ethanami...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325728((R)-N-(4-methoxybenzyl)-1-(3-methoxyphenyl)ethanam...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325729((R)-N-((2'-fluorobiphenyl-3-yl)methyl)-1-(3-methox...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325730((R)-1-(3-methoxyphenyl)-N-((2'-methylbiphenyl-3-yl...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325731((R)-N-((2'-methoxybiphenyl-3-yl)methyl)-1-(3-metho...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325732((R)-N-((4'-methoxybiphenyl-3-yl)methyl)-1-(3-metho...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325733((R)-1-(3-methoxyphenyl)-N-((4'-(trifluoromethyl)bi...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50325735((R)-N-((6-methoxy-4'-(trifluoromethyl)biphenyl-3-y...)
Affinity DataEC50: >5.00E+3nMAssay Description:Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
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