BDBM370121 6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one::US10233188, Example 10::US10800783, Example 10::US11396512, Example 10

SMILES C[C@@]1(O)CCC[C@H]1n1c2nc(NC3CCN(CC3)S(C)(=O)=O)ncc2cc(C(F)F)c1=O

InChI Key InChIKey=QIEKHLDZKRQLLN-FOIQADDNSA-N

Data  20 KI  3 IC50  3 EC50

PDB links: 1 PDB ID matches this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 26 hits for monomerid = 370121   

LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.0800nMAssay Description:The purpose of the CDK6/Cyclin D1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitor...More data for this Ligand-Target Pair
In DepthDetails US Patent

TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D1(Human)
Therachem Research Medilab

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.0800nMAssay Description:Inhibition of non-phosphorylated CDK6/Cyclin D1 (unknown origin) assessed as reduction in production of ADP using 5-FAM-RRRFRPASPLRGPPK peptide as su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.0800nMAssay Description:The purpose of the CDK6/Cyclin D1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitor...More data for this Ligand-Target Pair
In DepthDetails US Patent

LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.0800nMAssay Description:The purpose of the CDK6/Cyclin D1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitor...More data for this Ligand-Target Pair
In DepthDetails US Patent

TargetCyclin-dependent kinase 2(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.0900nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.110nMAssay Description:Inhibition of CDK6/cyclin D1 (unknown origin) assessed as reduction in substrate peptide phosphorylation using DYRKtide peptide as substrate preincub...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.120nMAssay Description:The mobility shift assay electrophoretically separates the fluorescently labeled peptides (substrate and phosphorylated product) following the kinase...More data for this Ligand-Target Pair
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.120nMAssay Description:The purpose of the CDK2/Cyclin E1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) of small molecule inhibitors by using a flu...More data for this Ligand-Target Pair
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.120nMAssay Description:Inhibition of recombinant full length wild-type phosphorylated CDK2/Cyclin E1 (unknown origin) expressed in baculovirus expression system assessed as...More data for this Ligand-Target Pair
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.120nMAssay Description:The purpose of the CDK2/Cyclin E1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) of small molecule inhibitors by using a flu...More data for this Ligand-Target Pair
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.130nMAssay Description:Inhibition of CDK2/cyclin E1 (unknown origin) assessed as reduction in substrate peptide phosphorylation using DYRKtide peptide as substrate preincub...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 4(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.130nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 6(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  0.160nMAssay Description:Antagonist activity against CCK2 receptor estimated from single shifts of pentagastrin concentration-effect curves in the isolated rat stomachMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  1nMAssay Description:Inhibition of CDK2/cyclin E (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  1.30nMAssay Description:Inhibition of CDK4/cyclin D1 (unknown origin) assessed as reduction in substrate peptide phosphorylation using DYRKtide peptide as substrate preincub...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  1.37nMAssay Description:The purpose CDK4/Cyclin D3 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitors by us...More data for this Ligand-Target Pair
In DepthDetails US Patent

LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  1.37nMAssay Description:The purpose CDK4/Cyclin D3 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitors by us...More data for this Ligand-Target Pair
In DepthDetails US Patent

LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  1.37nMAssay Description:The purpose CDK4/Cyclin D3 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitors by us...More data for this Ligand-Target Pair
In DepthDetails US Patent

LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  1.40nMAssay Description:Inhibition of non-phosphorylated CDK4/Cyclin D3 (unknown origin) assessed as reduction in production of ADP using 5-FAM-RRRFRPASPLRGPPK peptide as su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataKi:  20nMAssay Description:Inhibition of CDK9/Cyclin-T1 (unknown origin) assessed as reduction in substrate peptide phosphorylation using DYRKtide peptide as substrate preincub...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataIC50:  30nMAssay Description:Inhibition of CDK6/Cyclin D3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataIC50:  40nMAssay Description:Inhibition of CDK4/Cyclin D1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataIC50:  20nMAssay Description:Inhibition of CDK2/Cyclin E (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 2(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataEC50:  9nMAssay Description:Inhibition of XO44 binding to CDK2 in human HCC1806 cells preincubated with compound by Western blot analysisMore data for this Ligand-Target Pair
TargetRetinoblastoma-associated protein(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataEC50:  19nMAssay Description:Inhibition of RB1 phosphorylation in human OVCAR-3 cells assessed as reduction in phosphorylation at Serine 807/811 residue incubated for 1 hr by ELI...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-dependent kinase 1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM370121(6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcy...)
Affinity DataEC50:  597nMAssay Description:Inhibition of XO44 binding to CDK1 in human HCC1806 cells preincubated with compound by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed