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

Data  43 IC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 43 hits for monomerid = 148264   

TargetCyclin-dependent kinase 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails US Patent
TargetCyclin-dependent kinase 6(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  39nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails US Patent
TargetCyclin-dependent kinase 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails US Patent
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails US Patent
TargetCyclin-dependent kinase 6(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  39nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  10nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  13nMAssay Description:Inhibition of human CDK4/CyclinD3 by enzymatic radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  197nMAssay Description:Inhibition of human CDK9/CyclinT1 by enzymatic radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  197nMAssay Description:Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  13nMAssay Description:Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Beijing Normal University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  2nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 6(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  6nMAssay Description:Inhibition of CDK6 (unknown origin)More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails US Patent
TargetCyclin-dependent kinase 6(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5 activator 1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Beijing Normal University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D3(Homo sapiens (Human))
Nankai University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  10nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 6(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CDK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CDK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CDK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Beijing Normal University

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  29nMAssay Description:Inhibition of CDK4/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of CDK2/Cyclin E (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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£

Curated by ChEMBL
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  23nMAssay Description:Inhibition of CDK4/cyclin D1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
Affinity DataIC50:  10nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM148264(7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)p...)
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
In DepthDetails US Patent