General Information of the Protein
Protein ID
PT01671
Protein Name
Cyclin-dependent kinase 6
Secondarily
Protein Name
Cell division protein kinase 6
Serine/threonine-protein kinase PLSTIRE
Gene Name
CDK6
Secondarily
Gene Name
CDKN6
Sequence
MEKDGLCRADQQYECVAEIGEGAYGKVFKARDLKNGGRFVALKRVRVQTGEEGMPLSTIREVAVLRHLETFEHPNVVRLFDVCTVSRTDRETKLTLVFEHVDQDLTTYLDKVPEPGVPTETIKDMMFQLLRGLDFLHSHRVVHRDLKPQNILVTSSGQIKLADFGLARIYSFQMALTSVVVTLWYRAPEVLLQSSYATPVDLWSVGCIFAEMFRRKPLFRGSSDVDQLGKILDVIGLPGEEDWPRDVALPRQAFHSKSAQPIEKFVTDIDELGKDLLLKCLTFNPAKRISAYSALSHPYFQDLERCKENLDSHLPPSQNTSELNTA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
Function
Serine/threonine-protein kinase involved in the control of the cell cycle and differentiation; promotes G1/S transition. Phosphorylates pRB/RB1 and NPM1. Interacts with D-type G1 cyclins during interphase at G1 to form a pRB/RB1 kinase and controls the entrance into the cell cycle. Involved in initiation and maintenance of cell cycle exit during cell differentiation; prevents cell proliferation and negatively regulates cell differentiation, but is required for the proliferation of specific cell types (e.g. erythroid and hematopoietic cells). Essential for cell proliferation within the dentate gyrus of the hippocampus and the subventricular zone of the lateral ventricles. Required during thymocyte development. Promotes the production of newborn neurons, probably by modulating G1 length. Promotes, at least in astrocytes, changes in patterns of gene expression, changes in the actin cytoskeleton including loss of stress fibers, and enhanced motility during cell differentiation. Prevents myeloid differentiation by interfering with RUNX1 and reducing its transcription transactivation activity, but promotes proliferation of normal myeloid progenitors. Delays senescence. Promotes the proliferation of beta-cells in pancreatic islets of Langerhans. May play a role in the centrosome organization during the cell cycle phases (PubMed:23918663).
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Uniprot ID
Primary ID:
Q00534

Secondarily ID:
A4D1G0
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Ensembl ID
ENSG00000105810
HGNC ID
HGNC:1777
Subcellular Location
Cytoplasm
Nucleus
Cell projection
Ruffle
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0011047
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 0.9 nM
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CP0014062
4-(1-ethyl-5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-5-fluoro-N-[5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine
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C27H30F2N8
 1
1
IC50 = 2.4 nM
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CP0013121
5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridin-2-yl)pyrimidin-2-amine
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C26H28F2N8
 1
1
IC50 = 3.7 nM
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CP0005813
5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine
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C27H30F2N8
 1
1
IC50 = 4 nM
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CP0001256
Abemaciclib
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C27H32F2N8
 1
1
IC50 = 7.8 nM
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CP0013850
5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[[4-(2-fluoroethyl)piperazin-1-yl]methyl]pyridin-2-yl]pyrimidin-2-amine
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C28H31F3N8
 1
1
IC50 = 11.2 nM
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CP0014063
5-fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-propan-2-ylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 12.7 nM
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CP0005460
4-(1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoropyrimidin-2-amine
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C28H33FN8
 1
1
IC50 = 15.8 nM
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CP0011046
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C28H33FN8
 1
1
IC50 = 17.4 nM
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CP0012486
5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(6-m ethyl-5-(piperazin-1-ylmethyl)pyridin-2-yl)pyrimidin-2-amine
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C27H30F2N8
 1
1
IC50 = 18.7 nM
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CP0013120
N-[5-[(4-cyclopropylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C29H32F2N8
 1
1
IC50 = 19 nM
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CP0006215
4-(1-ethyl-5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoropyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 22 nM
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CP0006216
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C27H30F2N8
 1
1
IC50 = 28 nM
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CP0005812
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-2,2-dimethyl-1,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 36 nM
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CP0006218
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(6-fluoro-1,2,3,4-tetrahydropyrido[1,2-a]benzimidazol-8-yl)pyrimidin-2-amine
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C27H30F2N8
 1
1
IC50 = 45.6 nM
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CP0013849
N-[5-[(4-ethylpiperazin-1-yl)methyl]-6-methylpyridin-2-yl]-5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C29H34F2N8
 1
1
IC50 = 46 nM
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CP0012485
N-[5-[(4-ethylpiperazin-1-yl)methyl]-6-methylpyridin-2-yl]-5-fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 178 nM
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CP0013122
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C26H28F2N8
 1
1
IC50 = 244.1 nM
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CP0014064
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(4-fluoro-7,8,9,10-tetrahydro-6H-azepino[1,2-a]benzimidazol-2-yl)pyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 247.8 nM
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CP0011045
5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[6-methyl-5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 271 nM
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CP0014354
5-fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine
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C26H28F2N8
 1
1
IC50 = 275 nM
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CP0006217
4-(2-ethyl-5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoropyrimidin-2-amine
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C28H32F2N8
 1
1
IC50 = 339 nM
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CP0013119
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-2-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C27H30F2N8
 1
1
IC50 = 392 nM
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CP0003415
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine
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C27H31FN8
 1
1
IC50 = 752 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0001256
Abemaciclib
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C27H32F2N8
 3
1 IC50 = 1.9 nM
2 IC50 = 5 nM
3 IC50 = 10 nM
Clinical Information about the Protein
Target 1 ( Cyclin-dependent kinase 6 (CDK6) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Psoriasis vulgaris [ICD-11: EA90]
2 Breast cancer [ICD-11: 2C60-2C65]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Small-cell lung cancer [ICD-11: 2C25.Y]
5 Retinoblastoma [ICD-11: 2D02.2]
Approved Drug(s) 4 Approved Drugs  4
1 Apremilast Approved
Psoriasis vulgaris
2 LY2835219 Approved
Breast cancer
3 Palbociclib Approved
Breast cancer
4 Trilaciclib Approved
Small-cell lung cancer
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 LEE011 Phase 3
Solid tumour/cancer
2 G1T38 Phase 2
Breast cancer
3 FN-1501 Phase 1
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 PD-0183812 Terminated
Retinoblastoma