BDBM148264 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide::Kisqali::LEE011::Ribociclib::US10570141, Comparative Example 1::US8962630, 74
SMILES CN(C)C(=O)c1cc2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n1C1CCCC1
InChI Key InChIKey=RHXHGRAEPCAFML-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 43 hits for monomerid = 148264
Affinity DataIC50: >1.50E+4nMT: 2°CAssay Description:A 384-well microtiter IMAP-FPT (Molecular Devices Trade Mark Technology) endpoint assay was used for CDK1/cyclin B kinase activity measurements. The ...More data for this Ligand-Target Pair
Affinity DataIC50: 39nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: 10nMpH: 7.5 T: 2°CAssay Description:A 384-well microtiter Lance TR-FRET (time-resolved-fluorescence energy transfer) endpoint assay was used for CDK4/cyclin D1 kinase activity measureme...More data for this Ligand-Target Pair
Affinity DataIC50: 1.13E+5nMT: 2°CAssay Description:A 384-well microtiter IMAP-FPT (Molecular Devices Trade Mark Technology) endpoint assay was used for CDK1/cyclin B kinase activity measurements. The ...More data for this Ligand-Target Pair
Affinity DataIC50: 7.60E+4nMAssay Description:The assay was run under the conditions identical to that for CDK1/cyclin B except 0.25 nM CDK1/cyclin B was replaced with 0.3 nM CDK2/cyclin A. A 384...More data for this Ligand-Target Pair
Affinity DataIC50: 39nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Homo sapiens (Human))
Nankai University
Curated by ChEMBL
Nankai University
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Inhibition of human CDK4/CyclinD3 by enzymatic radiometric assayMore data for this Ligand-Target Pair
Affinity DataIC50: 197nMAssay Description:Inhibition of human CDK9/CyclinT1 by enzymatic radiometric assayMore data for this Ligand-Target Pair
Affinity DataIC50: 197nMAssay Description:Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Homo sapiens (Human))
Nankai University
Curated by ChEMBL
Nankai University
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Beijing Normal University
Curated by ChEMBL
Beijing Normal University
Curated by ChEMBL
Affinity DataIC50: 28nMAssay 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: 2nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.14nMAssay Description:LANCE method of PerkinElmer Inc. was used in the assay, and recombinant CDK4/CyclinD3 (Item No.: 04-105) and CDK6/CyclinD3 (Item No.: 04-107) kinases...More data for this Ligand-Target Pair
Affinity DataIC50: 26.9nMAssay Description:LANCE method of PerkinElmer Inc. was used in the assay, and recombinant CDK4/CyclinD3 (Item No.: 04-105) and CDK6/CyclinD3 (Item No.: 04-107) kinases...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [ga...More data for this Ligand-Target Pair
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP b...More data for this Ligand-Target Pair
TargetCDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as su...More data for this Ligand-Target Pair
Affinity DataIC50: 3.90E+3nMAssay Description:Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substr...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 5 activator 1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gam...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: 30nMAssay 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
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Beijing Normal University
Curated by ChEMBL
Beijing Normal University
Curated by ChEMBL
Affinity DataIC50: 71nMAssay Description:Inhibition of recombinant full-length human CDK6/cyclinD3 using histone H1 as substrate measured after 40 mins in presence of [gamma33P]ATP by scinti...More data for this Ligand-Target Pair
Affinity DataIC50: 197nMAssay Description:Inhibition of recombinant full-length human CDK9/cyclinT1 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC peptide as substrate measured after 40 mins i...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Homo sapiens (Human))
Nankai University
Curated by ChEMBL
Nankai University
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Inhibition of recombinant full-length human CDK4/cyclinD3 using Rb fragment as substrate measured after 40 mins in presence of [gamma33P]ATP by scint...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 39nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: 7.60E+4nMAssay Description:Inhibition of CDK2/CyclinA (unknown origin) assessed as reduction in TAMRA tagged peptide substrate phosphorylation by fluorescence polarization assa...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibition of CDK4/CyclinD1 (unknown origin) assessed as reduction in retinoblastoma phosphorylation at S473 residue by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CDK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CDK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CDK1 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of CDK1/cyclin B1 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition ...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: 30nMAssay Description:Inhibition of human CDK4/cyclin D (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addi...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of human CDK2/cyclin E (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addi...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Beijing Normal University
Curated by ChEMBL
Beijing Normal University
Curated by ChEMBL
Affinity DataIC50: 73nMAssay Description:Inhibition of CDK6/Cyclin D (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: 29nMAssay Description:Inhibition of CDK4/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of CDK2/Cyclin E (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D1(Homo sapiens (Human))
Chinese Academy of Medical Sciences and Peking Union Medical College
Curated by ChEMBL
Chinese Academy of Medical Sciences and Peking Union Medical College
Curated by ChEMBL
Affinity DataIC50: 20nMAssay Description:Inhibition of CDK6/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Palack£ University and Institute of Experimental Botany ASCR
Curated by ChEMBL
Affinity DataIC50: 23nMAssay Description:Inhibition of CDK4/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >1.50E+4nMAssay Description:The assay was run under the conditions identical to that for CDK1/cyclin B except 0.25 nM CDK1/cyclin B was replaced with 0.3 nM CDK2/cyclin A. A 384...More data for this Ligand-Target Pair