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Found 469 with Last Name = 'clarine' and Initial = 'j'
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168222(US9669031, 51 N-[6-[[8-chloro-3-(3-chlorophenyl)-3...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168216(US9669031, 181 3,3-dimethyl-1,5-dioxo-6-(pyrimidin...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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 DepthDetails ArticlePubMed
TargetEukaryotic initiation factor 4A-I(Homo sapiens (Human))
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(EFT-226 | Eft226 | Zotatifin)
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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168222(US9669031, 51 N-[6-[[8-chloro-3-(3-chlorophenyl)-3...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168222(US9669031, 51 N-[6-[[8-chloro-3-(3-chlorophenyl)-3...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297345(N-(6-((1-oxoisoindolin-5-yl)amino)pyrimidin-4-yl)c...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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 DepthDetails ArticlePubMed
TargetEukaryotic initiation factor 4A-I(Homo sapiens (Human))
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50576672(CHEMBL4857096)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of eIF4A (unknown origin) assessed as inhibition of translation of RNA featuring highly structured 5'-UTR of c-MycMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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 DepthDetails ArticlePubMed
LigandPNGBDBM98891(US8497265, 217 | US8497265, 239)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of human PDE10A2 using FAM-cAMP substrate by TR-FRET progressive binding assayMore data for this Ligand-Target Pair
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM99037(US8497265, 677)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of human PDE10A2 using FAM-cAMP substrate by TR-FRET progressive binding assayMore data for this Ligand-Target Pair
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579099(& 16-2 | US11479551, Example 16-1)
Affinity DataIC50:  3nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579099(& 16-2 | US11479551, Example 16-1)
Affinity DataIC50:  3nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM168216(US9669031, 181 3,3-dimethyl-1,5-dioxo-6-(pyrimidin...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM50585596(CHEMBL5076766)
Affinity DataIC50:  4nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM98933(US8497265, 345)
Affinity DataIC50:  4.70nMAssay Description:Inhibition of human PDE10A2 using FAM-cAMP substrate by TR-FRET progressive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEukaryotic initiation factor 4A-I(Homo sapiens (Human))
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50196926(CHEMBL438139 | Rocaglamide | 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
TargetEukaryotic initiation factor 4A-I(Homo sapiens (Human))
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50576670(CHEMBL4864162)
Affinity DataIC50:  5nMAssay Description:Inhibition of eIF4A (unknown origin) assessed as inhibition of translation of RNA featuring highly structured 5'-UTR of c-MycMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50463853(CHEMBL4237618)
Affinity DataIC50:  5nMAssay Description:Antagonist activity at human TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced intracellular calcium levels preincubated for 2.5 ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  5nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetEukaryotic initiation factor 4A-I(Homo sapiens (Human))
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50576669(CHEMBL4855528)
Affinity DataIC50:  5.60nMAssay Description:Inhibition of eIF4A (unknown origin) assessed as inhibition of translation of RNA featuring highly structured 5'-UTR of c-MycMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Homo sapiens (Human))
Effector Therapeutics

Curated by ChEMBL
LigandPNGBDBM297345(N-(6-((1-oxoisoindolin-5-yl)amino)pyrimidin-4-yl)c...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  6nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  6nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50463854(CHEMBL4251427)
Affinity DataIC50:  6nMAssay Description:Antagonist activity at human TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced intracellular calcium levels preincubated for 2.5 ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50463844(CHEMBL4247840)
Affinity DataIC50:  6nMAssay Description:Antagonist activity at mouse TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced intracellular calcium levels preincubated for 2.5 ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1/2(Homo sapiens (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
TargetEukaryotic initiation factor 4A-I(Homo sapiens (Human))
Inception Therapeutics

Curated by ChEMBL
LigandPNGBDBM50540861(EFT-226 | Eft226 | Zotatifin)
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 DepthDetails ArticlePubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 1(Homo sapiens (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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM98872(US8497265, 198)
Affinity DataIC50:  6.5nMAssay Description:Inhibition of human PDE10A2 using FAM-cAMP substrate by TR-FRET progressive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM98898(US8497265, 224)
Affinity DataIC50:  6.80nMAssay Description:Inhibition of human PDE10A2 using FAM-cAMP substrate by TR-FRET progressive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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