BDBM50110183 Abemaciclib::LY-2835219::US10626107, Example LY2835219::US10662186, Compound LY2835219::US10696678, Example LY2835219::US10988476, Compound LY2835219::US11053238, LY2835219::US11091476, Example LY2835219::US11351170, Example Abemaciclib
SMILES CCN1CCN(Cc2ccc(Nc3ncc(F)c(n3)-c3cc(F)c4nc(C)n(C(C)C)c4c3)nc2)CC1
InChI Key InChIKey=UZWDCWONPYILKI-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 219 hits for monomerid = 50110183
Affinity DataIC50: 0.260nMAssay Description:Test compounds (compound of the present invention, reference compound Abemaciclib, and comparative example compounds) were dissolved in DMSO at 10 mM...More data for this Ligand-Target Pair
Affinity DataIC50: 0.260nMAssay Description:Test compounds (compound of the present invention, reference compound Abemaciclib, and comparative example compounds) were dissolved in DMSO at 10 mM...More data for this Ligand-Target Pair
Affinity DataIC50: 0.430nMAssay Description:Inhibition of human CDK6/cyclin D1 preincubated with compound for 20 mins followed by [33P]ATP addition and measured after 2 hrs by filter binding me...More data for this Ligand-Target Pair
Affinity DataIC50: 0.460nMAssay Description:Inhibition of human CDK4/cyclin D1 preincubated with compound for 20 mins followed by [33P]ATP addition and measured after 2 hrs by filter binding me...More data for this Ligand-Target Pair
Affinity DataKi: 0.600nMAssay Description:ATP competitive inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 expressed in Sf9 insect cells using C-termi...More data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of CDK4/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 0.851nMAssay Description:Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 1.02nMAssay Description:The standard Lance Ultra method was performed by a 10 μL enzyme reaction system containing 0.5 nM CDK2/cyclin A protein, 100 nM ULight-MBP polyp...More data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Inhibition of CDK4/Cyclin D1 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D1(Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 1.22nMAssay Description:The standard Lance Ultra method was performed by a 10 μL enzyme reaction system containing 0.3 nM CDK4/cyclin D1 protein, 50 nM ULight-4E-BP1 po...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of CDK6/Cyclin D1 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Human)
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibition of recombinant N-terminal GST/His6-fusion tagged human CDK4/Cyclin D3 expressed in Sf9 insect cells using 5-FAM-IPTSPITTTYFFFKKK as substr...More data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of CDK4 (unknown origin) after 90 mins by ADP-Glo assayMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Human)
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human full length N-terminal GST-tagged CDK4 (1 to 303 residues)/cyclin D3 (1 to 292 residues) expressed in baculovirus exp...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Human)
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human full-length N-terminal GST-fused CDK4 (1 to 303 residues)/GST-tagged CyclinD3 (1 to 292 residues) expressed in baculo...More data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Inhibition of CDK6 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kin...More data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Inhibition of CDK4 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kin...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 expressed in Sf9 insect cells using C-terminal Rb fragment ...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataKi: 2nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal ...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of Cdk4 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 2nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb prot...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Human)
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:To demonstrate that the compounds exhibit affinity for CDK kinases (CDK2/CycA2, CDK4/CycD3, CDK6/cycD3), CDK kinase assays were performed.Reaction bu...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of human CDK4 incubated for 18 hrs by microscopic analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of CDK4/CyclinD1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-E1(Human)
Shanghai Haihe Pharmaceutical
Curated by ChEMBL
Shanghai Haihe Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Inhibition of human CDK4/cyclin D1 using ULight-substrate after 1 hr by LANCE assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Human)
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:To demonstrate that the compounds exhibit affinity for CDK kinases (CDK2/CycA2, CDK4/CycD3, CDK6/cycD3), CDK kinase assays were performed.Reaction bu...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.40nMAssay Description:Inhibition of CDK6/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 2.40nMAssay Description:ATP competitive inhibition of recombinant human full-length N-terminal GST-fused CDK6 (M1 to A326 residues)/cyclin D1 (Q4 to I295 residues) expressed...More data for this Ligand-Target Pair
Affinity DataIC50: 2.51nMAssay Description:1. Take 10 mM stock solution of the test compound, in 96-well compound plate, DMSO was used to dilute the compound to an initial concentration of 100...More data for this Ligand-Target Pair
Affinity DataIC50: 2.51nMAssay Description:1. Take 10 mM stock solution of the test compound, in 96-well compound plate, DMSO was used to dilute the compound to an initial concentration of 100...More data for this Ligand-Target Pair
Affinity DataIC50: 2.60nMAssay Description:Inhibition of human CAMK2delta preincubated with compound for 20 mins followed by [33P]ATP addition and measured after 2 hrs by filter binding methodMore data for this Ligand-Target Pair
Affinity DataIC50: 3.20nMAssay Description:Inhibition of CDK4/Cyclin D1 in human MCF7 cellsMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals
Curated by ChEMBL
Perha Pharmaceuticals
Curated by ChEMBL
Affinity DataKd: 3.30nMAssay Description:Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.41nMAssay Description:Test compounds (compound of the present invention, reference compound Abemaciclib, and comparative example compounds) were respectively dissolved in ...More data for this Ligand-Target Pair
Affinity DataIC50: 3.41nMAssay Description:Test compounds (compound of the present invention, reference compound Abemaciclib, and comparative example compounds) were respectively dissolved in ...More data for this Ligand-Target Pair
Affinity DataIC50: 3.5nMAssay Description:Inhibition of human CAMK2beta preincubated with compound for 20 mins followed by [33P]ATP addition and measured after 2 hrs by filter binding methodMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Human)
Perha Pharmaceuticals
Curated by ChEMBL
Perha Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 3.5nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
Affinity DataIC50: 3.81nMAssay Description: 1.2.2 Preparation of kinase solution: Kinase solutions having the concentrations required for each reaction system were prepared from 100 ng/μl...More data for this Ligand-Target Pair
Affinity DataIC50: 3.81nMAssay Description: 1.2.2 Preparation of kinase solution: Kinase solutions having the concentrations required for each reaction system were prepared from 100 ng/μl...More data for this Ligand-Target Pair
Affinity DataIC50: 3.81nMAssay Description: 1.2.2 Preparation of kinase solution: Kinase solutions having the concentrations required for each reaction system were prepared from 100 ng/μl...More data for this Ligand-Target Pair
Affinity DataIC50: 3.81nMAssay Description: 1.2.2 Preparation of kinase solution: Kinase solutions having the concentrations required for each reaction system were prepared from 100 ng/μl...More data for this Ligand-Target Pair
Affinity DataIC50: 3.92nMAssay Description: 1.2.2 Preparation of kinase solution: Kinase solutions having the concentrations required for each reaction system were prepared from 100 ng/μl...More data for this Ligand-Target Pair
Affinity DataIC50: 3.92nMAssay Description: 1.2.2 Preparation of kinase solution: Kinase solutions having the concentrations required for each reaction system were prepared from 100 ng/μl...More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 5nMAssay Description:Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in pres...More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair