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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
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263270(CHEMBL4086747)
Affinity DataIC50: 0.0840nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263254(CHEMBL4094975)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263253(CHEMBL4067557)
Affinity DataIC50: 0.140nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168214(US9669031, 207 6′-((6-aminopyrimidin-4-yl)am...)
Affinity DataIC50: 0.310nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263270(CHEMBL4086747)
Affinity DataIC50: 0.360nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168214(US9669031, 207 6′-((6-aminopyrimidin-4-yl)am...)
Affinity DataIC50: 0.510nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263254(CHEMBL4094975)
Affinity DataIC50: 0.620nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263269(CHEMBL4076439)
Affinity DataIC50: 0.650nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263269(CHEMBL4076439)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263269(CHEMBL4076439)
Affinity DataIC50: 0.790nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263254(CHEMBL4094975)
Affinity DataIC50: 0.880nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263263(CHEMBL4073443)
Affinity DataIC50: 1nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263255(CHEMBL4065802)
Affinity DataIC50: 1nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168216(US9669031, 79 3,3-dimethyl-6-(pyrimidin-4-ylamino)...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168222(US9669031, 93 6-[(6-aminopyrimidin-4-yl)amino]-8-c...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263255(CHEMBL4065802)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263264(CHEMBL4094080)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
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
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168222(US9669031, 93 6-[(6-aminopyrimidin-4-yl)amino]-8-c...)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168214(US9669031, 207 6′-((6-aminopyrimidin-4-yl)am...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168222(US9669031, 93 6-[(6-aminopyrimidin-4-yl)amino]-8-c...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297345(US10112955, Example 12 | N-(6-((1-oxoisoindolin-5-...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263253(CHEMBL4067557)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM164271(US9669031, 10 N-(6-((3,3-dimethyl-1,5-dioxo-1,2,3,...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263263(CHEMBL4073443)
Affinity DataIC50: 2.40nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168241(US9669031, 69 8-fluoro-3,3-dimethyl-6-(pyrimidin-4...)
Affinity DataIC50: 2.60nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM164271(US9669031, 10 N-(6-((3,3-dimethyl-1,5-dioxo-1,2,3,...)
Affinity DataIC50: 2.70nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168216(US9669031, 79 3,3-dimethyl-6-(pyrimidin-4-ylamino)...)
Affinity DataIC50: 3.30nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50196926(Rocaglamide | CHEMBL438139 | US10085988, Compound ...)
Affinity DataIC50: 4.70nMAssay 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
PubMedPDB3D3D Structure (crystal)
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297345(US10112955, Example 12 | N-(6-((1-oxoisoindolin-5-...)
Affinity DataIC50: 5.70nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263263(CHEMBL4073443)
Affinity DataIC50: 6nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataIC50: 6.30nMAssay Description:Inhibition of eIF4A1 in human HAP1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168241(US9669031, 69 8-fluoro-3,3-dimethyl-6-(pyrimidin-4...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263264(CHEMBL4094080)
Affinity DataIC50: 7.80nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168239(US9669031, 67 3,3,8-trimethyl-6-(pyrimidin-4-ylami...)
Affinity DataIC50: 10nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM164271(US9669031, 10 N-(6-((3,3-dimethyl-1,5-dioxo-1,2,3,...)
Affinity DataIC50: 12nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263253(CHEMBL4067557)
Affinity DataIC50: 12nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(Zotatifin | Eft226 | EFT-226)
Affinity DataIC50: 14nMAssay 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
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168239(US9669031, 67 3,3,8-trimethyl-6-(pyrimidin-4-ylami...)
Affinity DataIC50: 19nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297336(US10112955, Example 1 | 5-((9H-purin-6-yl)amino)is...)
Affinity DataIC50: 23nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM50263255(CHEMBL4065802)
Affinity DataIC50: 24nMAssay Description:Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297342(US10112955, Example 8 | 3-methyl-5-(pyrimidin-4-yl...)
Affinity DataIC50: 28nMAssay Description:Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297342(US10112955, Example 8 | 3-methyl-5-(pyrimidin-4-yl...)
Affinity DataIC50: 45nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMed
TargetEukaryotic initiation factor 4A-I(Human)
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50196926(Rocaglamide | CHEMBL438139 | US10085988, Compound ...)
Affinity DataIC50: 47nMAssay 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
PubMedPDB3D3D Structure (crystal)
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM164243(US9669031, 2 3,3-dimethyl-6-(pyrimidin-4-ylamino)-...)
Affinity DataIC50: 57nMAssay Description:Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/29/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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