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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 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550562(8′-Methyl-6′-(thieno[2,3-d]pyrimidin-4...)
Affinity DataIC50: 0.100nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM50573219(CHEMBL4879010)
Affinity DataIC50: 0.150nMAssay Description:Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550512(US11311520, Example 6 | US11311520, Example 32 | 8...)
Affinity DataIC50: 0.300nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550561(8′-Methyl-6′-(7H-pyrrolo[2,3-d]pyrimid...)
Affinity DataIC50: 0.300nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550512(US11311520, Example 6 | US11311520, Example 32 | 8...)
Affinity DataIC50: 0.300nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

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 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550654(8′-Methyl-6′-(7H-pyrrolo[2,3-d]pyrimid...)
Affinity DataIC50: 0.400nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550702(8-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-...)
Affinity DataIC50: 0.5nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
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
LigandPNGBDBM218770(US9296757, 92)
Affinity DataIC50: 0.600nMpH: 7.5 T: 2°CAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2017
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550534(6′-({6-[(3-Aminoazetidin-1-yl)carbonyl]thien...)
Affinity DataIC50: 0.600nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

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

Curated by ChEMBL
LigandPNGBDBM50500934(CHEMBL3800585)
Affinity DataEC50:  0.600nMAssay Description:Inhibition of MNK1/2 in human KMS11-luc cells assessed as inhibition of EIF4E phosphorylation at S209 after 3 hrs by quantitative electrochemilumines...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
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)
Bayer Pharma Aktiengesellschaft

US Patent
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 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550573(8′-methyl-6′-(9H-purin-6-ylamino)-2...)
Affinity DataIC50: 0.700nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550638(3,3,8-Trimethyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl...)
Affinity DataIC50: 0.700nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550596(US11311520, Example 90 | 4,4-Difluoro-8′-met...)
Affinity DataIC50: 0.700nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

LigandPNGBDBM218771(US9296757, 93)
Affinity DataIC50: 0.700nMpH: 7.5 T: 2°CAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2017
Entry Details
US Patent

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)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM50635319(CHEMBL5558538)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/substrateby HTRF assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
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 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM50587869(CHEMBL5174006)
Affinity DataIC50: 1nMAssay Description:Inhibition of MNK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
LigandPNGBDBM420256((7S) N-(2-Methoxyethyl)-4-[(6-methoxypyrazolo[1,5-...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM50587868(CHEMBL5201681)
Affinity DataIC50: 1nMAssay Description:Inhibition of MNK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
LigandPNGBDBM420249((7S) N-Butyl-4-[(6-methoxypyrazolo[1,5-a]pyridin-5...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420250(1-((7S)-4-[(6-Methoxypyrazolo[1,5-a]pyridin-5-yl)a...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420251((7S) N-[3-(Dimethylamino)propyl]-4-[(6-methoxypyra...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420252((3-Hydroxy-3-methylazetidin-1-yl)(7S)-4-[(6-methox...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420246((7S) N-Ethyl-4-[(6-methoxypyrazolo[1,5-a]pyridin-5...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM50573221(CHEMBL4859971)
Affinity DataIC50: 1nMAssay Description:Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM50573222(CHEMBL4869634)
Affinity DataIC50: 1nMAssay Description:Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMed
LigandPNGBDBM420269((7S) N-Ethyl-N-(2-hydroxyethyl)-4-[(6-methoxypyraz...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420270((7S) N-Ethyl-N-(2-methoxyethyl)-4-[(6-methoxypyraz...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM259295(US9499547, 36)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2017
Entry Details
US Patent

LigandPNGBDBM218766(US9296757, 88)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2017
Entry Details
US Patent

LigandPNGBDBM420271((7S) N,N-Bis(2-methoxyethyl)-4-[(6-methoxypyrazolo...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM218768(US9296757, 90)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:For the assay 50 nL of a 100 fold concentrated solution of the test compound in DMSO was pipetted into a black low volume 384 well microtiter plate (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2017
Entry Details
US Patent

LigandPNGBDBM420265((7S)-4-[(6-Methoxypyrazolo[1,5-a]pyridin-5-yl)amin...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420266(4-[2-(Dimethylamino)ethyl]piperazin-1-yl(7S)-4-[(6...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420267((7S) N-[2-(Dimethylamino)ethyl]-N-ethyl-4-[(6-meth...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420268((7S)-4-[(6-Methoxypyrazolo[1,5-a]pyridin-5-yl)amin...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420261([4-(Dimethylamino)piperidin-1-yl](7S)-4-[(6-methox...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420262((4-[2-Dimethylamino)ethyl]methyl)aminopiperidin-1-...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420258([(3R)-3-(Dimethylamino)pyrrolidin-1-yl](7S)-4-[(6-...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420259([(3S)-3-(Dimethylamino)pyrrolidin-1-yl](7S)-4-[(6-...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

LigandPNGBDBM420260([(3S,4S)-3,4-Dihydroxypyrrolidin-1-yl](7S)-4-[(6-m...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1(Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM550634(4-Hydroxy-8′-methyl-6′-(7H-pyrrolo[2,3...)
Affinity DataIC50: 1nMAssay Description:MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
US Patent

TargetMAP kinase-interacting serine/threonine-protein kinase 1 [1-424](Human)
Bayer Pharma Aktiengesellschaft

US Patent
LigandPNGBDBM227719(US9556181, 4 | US9556181, 16 | US9556181, 7 | 3-br...)
Affinity DataIC50: 1nMpH: 7.5Assay Description:TBDA recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accessio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/30/2018
Entry Details
US Patent

LigandPNGBDBM420277((7S)-4-[(6-Methoxypyrazolo[1,5-a]pyridin-5-yl)amin...)
Affinity DataIC50: 1nMAssay Description:A recombinant fusion protein of Glutathione-S-Transferase (GST, N-terminally) and human full-length MKNK1 (amino acids 1-424 and T344D of accession n...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
9/20/2020
Entry Details
US Patent

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