BDBM25121 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide::BI 2536::CHEMBL513909::US10450297, Example 300::US8598172, 5
SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NC3CCN(C)CC3)ncc2N(C)C1=O
InChI Key InChIKey=XQVVPGYIWAGRNI-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 602 hits for monomerid = 25121
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.0830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataKd: 0.190nMAssay Description:Binding constant for PLK1 kinase domainMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataKd: 0.190nMAssay Description:Binding affinity to PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataKi: 0.220nMAssay Description:Binding affinity to PLK1 (unknown origin) expressed in HEK293 cells after 1 hr by proprietary competition assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.510nMAssay Description:Inhibition of PLK1 (unknown origin) preincubated for 10 mins followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo assa...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataKd: 0.810nMAssay Description:Binding constant for PLK2 kinase domainMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
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
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged Plk1 (residues 1-603) expressed in baculovirus expression using casein as substrate in presence...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of recombinant N-terminal GST-tagged human PLK1 (1 to 603 residues) expressed in baculovirus expression system incubated for 45 mins using...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of Plk1 in human A549 cells incubated for 2 hrs by microplate reader methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Competitive inhibition of PLK1 (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of human recombinant GST-tagged PLK1 (1 to 603 residues) using casein as substrate incubated for 45 minsMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human PLK1 (1 to 603 residues) expressed in baculovirus expression system using bovine milk casein as...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of recombinant human 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
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate i...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of PLK1 (unknown origin) in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Competitive inhibition of human PLK1 in presence of ATPMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of PLK1 (unknown origin) preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assa...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataKi: <1nM ΔG°: <-12.1kcal/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataKi: <1nMAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataKi: <1nMAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of BRD4 (unknown origin) by alpha-screen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Inhibition of PLK3 (unknown origin) preincubated for 10 mins followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo assa...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 2.60nMAssay Description:Inhibition of PLK1 (unknown origin) using Ser/Thr 16 as substrate after 60 mins by Z-LYTE activity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.90nMAssay Description:Inhibition of PLK2 (unknown origin) preincubated for 10 mins followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo assa...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataKi: 3nMAssay Description:Inhibition of recombinant GST-tagged PLK1 using biotin-ahx-AKMETTFYDDALNASFLPSEKKK-amide as substrate after 30 mins by scintillation counting analysi...More data for this Ligand-Target Pair
Affinity DataIC50: 3.5nMAssay Description:Inhibition of PLK2 (unknown origin) in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 3.5nMAssay Description:Inhibition of PLK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3.5nMAssay Description:Inhibition of recombinant human plk2 using casein as substrate in presence of gamma-[33P]-ATP by invitro kinase assayMore data for this Ligand-Target Pair
Affinity DataKd: 4nMAssay Description:Binding constant for PLK3 kinase domainMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of human recombinant PLK1 by Z-Lyte assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 4.60nMAssay Description:Inhibition of PLK1 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one so...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 4.80nMAssay Description:Inhibition of PLK1 in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 5.30nMAssay Description:Inhibition human recombinant full length His-tagged Plk1 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 6.10nMAssay Description:Inhibition of PLK1 in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell prolifera...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 7.10nMAssay Description:Inhibition of recombinant full length human His-tagged PLK1 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 8nMpH: 7.5 T: 2°CAssay Description:Percent inhibition and IC50 values were determined with ATP concentrations at apparent Km using the Invitrogen SelectScreen Kinase Profiling Service ...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 8nMpH: 7.9Assay Description:The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 8nMAssay Description:Inhibition of recombinant full length human PLK1 using casein as substrate incubated for 40 mins in the presence of [gamma33P]ATP at Km concentration...More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of PLK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of PLK3 (unknown origin) in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged Plk3 (residues 19-301) using casein as substrate in presence of gamma-[33P]-ATP by invitro kin...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 9.30nMAssay Description:Inhibition of PLK1 in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proli...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 9.70nMAssay Description:Inhibition of PLK1 in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell prolifer...More data for this Ligand-Target Pair
Affinity DataKd: 12nMAssay Description:Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domainMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Human)
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Csir-Indian Institute of Integrative Medicine
Curated by ChEMBL
Affinity DataIC50: 12nMAssay Description:Inhibition of PLK1 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous on...More data for this Ligand-Target Pair
