Compile Data Set for Download or QSAR
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Report error Found 35 Enz. Inhib. hit(s) with all data for entry = 50000118
TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataKi:  2.20nMAssay Description:Inhibition of human recombinant His6-tagged PLK1 (1 to 603 residues) using casein as substrate preincubated for 60 mins followed by polo box peptide ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM3096(2-aminopyrido[2,3-d]pyrimidin-7(8H)-one deriv. | 6...)
Affinity DataKd:  5nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  27nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240828(CHEMBL4067978)
Affinity DataKd:  4.70nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM4552(4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-...)
Affinity DataKd:  106nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM31090((E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-eth...)
Affinity DataKd:  498nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  481nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM3096(2-aminopyrido[2,3-d]pyrimidin-7(8H)-one deriv. | 6...)
Affinity DataKd:  247nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM31090((E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-eth...)
Affinity DataKd:  172nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50240828(CHEMBL4067978)
Affinity DataKd:  444nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

LigandPNGBDBM31090((E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-eth...)
Affinity DataKd:  1.11E+3nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  150nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

LigandPNGBDBM12255(AZD0530 | CHEMBL217092 | Compound 33 | N-(5-chloro...)
Affinity DataKd:  2.82E+3nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTyrosine-protein kinase JAK2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  110nMAssay Description:Binding affinity to human JAK2 JH1 domain assessed as dissociation constant by quantitative real-time PCR methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase PLK1(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  3nMAssay Description:Binding affinity to human PLK1 assessed as dissociation constant by quantitative real-time PCR methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  3.90nMAssay Description:Binding affinity to recombinant human full-length N-terminal His8-tagged Wee2 (1 to 567 residues) expressed in human Expi293F cells assessed as desso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTyrosine-protein kinase JAK3(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  26nMAssay Description:Binding affinity to human JAK3 JH1 domain assessed as dissociation constant by quantitative real-time PCR methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  3.20nMAssay Description:Binding affinity to recombinant human full-length N-terminal His8-tagged Wee1 (1 to 646 residues) expressed in human Expi293F cells assessed as desso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
Affinity DataKd:  27nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase 2(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240827(CHEMBL4075828)
Affinity DataKd:  128nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  324nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

LigandPNGBDBM4552(4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-...)
Affinity DataKd:  270nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240828(CHEMBL4067978)
Affinity DataKd:  44nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  5.70E+3nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240827(CHEMBL4075828)
Affinity DataKd:  79nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM4552(4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-...)
Affinity DataKd:  78nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
Affinity DataKd:  14nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM50240826(AZD-1775 | MK-1775 | US11124518, Example AZD1775 |...)
Affinity DataKd:  13nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetWee1-like protein kinase(Human)
Moffitt Cancer Center

Curated by ChEMBL
LigandPNGBDBM3096(2-aminopyrido[2,3-d]pyrimidin-7(8H)-one deriv. | 6...)
Affinity DataKd:  11nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by iso...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

LigandPNGBDBM31545(Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxami...)
Affinity DataKd:  990nMAssay Description:Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)