Compile Data Set for Download or QSAR
Report error Found 97 Enz. Inhib. hit(s) with all data for entry = 50018524
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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetCyclin-dependent kinase 2(Human)
Pfizer

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
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetCyclin-dependent kinase 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM370258(US10233188, Example 145 | BDBM467153)
Affinity DataEC50:  200nMAssay Description:Inhibition of XO44 binding to CDK2 in human KURAMOCHI cells preincubated with compound by Western blot analysisMore data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetCyclin-dependent kinase 1(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM370258(US10233188, Example 145 | BDBM467153)
Affinity DataEC50:  4.00E+3nMAssay Description:Inhibition of XO44 binding to CDK1 in human KURAMOCHI cells preincubated with compound by Western blot analysisMore data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetRetinoblastoma-associated protein(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM370258(US10233188, Example 145 | BDBM467153)
Affinity DataIC50: 270nMAssay 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
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetRetinoblastoma-associated protein(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM6309(8-cyclopentyl-6-acetyl-5-methyl-2-{[5-(piperazin-1...)
Affinity DataIC50: 1.00E+4nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370133(US10233188, Example 22 | US10800783, Example 22 | ...)
Affinity DataKi:  0.0470nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM467013((-)-6-(2,2-difluoroethyl)-8-[(1R*,2R*)-2-hydroxy-2...)
Affinity DataKi:  0.0640nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370147(US10233188, Example 36 | US10800783, Example 36 | ...)
Affinity DataKi:  0.0900nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609170(CHEMBL5266837)
Affinity DataKi:  0.100nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM467013((-)-6-(2,2-difluoroethyl)-8-[(1R*,2R*)-2-hydroxy-2...)
Affinity DataKi:  0.110nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370205(US10233188, Example 92 | US10800783, Example 92 | ...)
Affinity DataKi:  0.120nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370256(US10233188, Example 143 | BDBM467151)
Affinity DataKi:  0.190nMAssay 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
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM467013((-)-6-(2,2-difluoroethyl)-8-[(1R*,2R*)-2-hydroxy-2...)
Affinity DataKi:  0.190nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370257(US10233188, Example 144 | BDBM467152)
Affinity DataKi:  0.196nMAssay 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
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370120(6-chloro-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]...)
Affinity DataKi:  0.200nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609166(CHEMBL5280928)
Affinity DataKi:  0.200nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM6309(8-cyclopentyl-6-acetyl-5-methyl-2-{[5-(piperazin-1...)
Affinity DataKi:  0.200nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609166(CHEMBL5280928)
Affinity DataKi:  0.200nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370113(8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-{[1-(m...)
Affinity DataKi:  0.200nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609171(CHEMBL5288078)
Affinity DataKi:  0.210nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370205(US10233188, Example 92 | US10800783, Example 92 | ...)
Affinity DataKi:  0.240nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370248((8-cyclopentyl-2-{[1-(methylsulfonyl)piperidin-4-y...)
Affinity DataKi:  0.300nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370140(US10233188, Example 29 | US10800783, Example 29 | ...)
Affinity DataKi:  0.300nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370133(US10233188, Example 22 | US10800783, Example 22 | ...)
Affinity DataKi:  0.330nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370140(US10233188, Example 29 | US10800783, Example 29 | ...)
Affinity DataKi:  0.360nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370130(US10233188, Example 19 | US10800783, Example 19 | ...)
Affinity DataKi:  0.360nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370120(6-chloro-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]...)
Affinity DataKi:  0.370nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370120(6-chloro-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]...)
Affinity DataKi:  0.450nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370248((8-cyclopentyl-2-{[1-(methylsulfonyl)piperidin-4-y...)
Affinity DataKi:  0.480nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370258(US10233188, Example 145 | BDBM467153)
Affinity DataKi:  0.480nMAssay 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
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370277(US10233188, Example 164 | BDBM467172)
Affinity DataKi:  0.520nMAssay 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
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370130(US10233188, Example 19 | US10800783, Example 19 | ...)
Affinity DataKi:  0.560nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370133(US10233188, Example 22 | US10800783, Example 22 | ...)
Affinity DataKi:  0.610nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370112(8-cyclopentyl-2-{[1-(methylsulfonyl)piperidin-4-yl...)
Affinity DataKi:  0.670nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370112(8-cyclopentyl-2-{[1-(methylsulfonyl)piperidin-4-yl...)
Affinity DataKi:  0.710nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370147(US10233188, Example 36 | US10800783, Example 36 | ...)
Affinity DataKi:  0.800nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM6309(8-cyclopentyl-6-acetyl-5-methyl-2-{[5-(piperazin-1...)
Affinity DataKi:  0.800nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609169(CHEMBL5275378)
Affinity DataKi:  0.860nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609168(CHEMBL5277190)
Affinity DataKi:  0.880nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370112(8-cyclopentyl-2-{[1-(methylsulfonyl)piperidin-4-yl...)
Affinity DataKi:  0.880nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370248((8-cyclopentyl-2-{[1-(methylsulfonyl)piperidin-4-y...)
Affinity DataKi:  0.900nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370258(US10233188, Example 145 | BDBM467153)
Affinity DataKi:  0.920nMAssay 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
Ligand InfoSimilars
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370205(US10233188, Example 92 | US10800783, Example 92 | ...)
Affinity DataKi:  1.10nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370113(8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-{[1-(m...)
Affinity DataKi:  1.10nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM370130(US10233188, Example 19 | US10800783, Example 19 | ...)
Affinity DataKi:  1.20nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609168(CHEMBL5277190)
Affinity DataKi:  1.20nMAssay 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 Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
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