Target family: CDK4 subfamily (type: enzyme)
Target: cyclin dependent kinase 6

Ligand: abemaciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine.
Published in: Invest New Drugs

Ligand: AT-7519 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pIC50
Reference (Journal): Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.
Published in: Mol Cancer Ther

Ligand: BSJ-03-123 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.420000076293945 pIC50
Reference (Journal): Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.
Published in: Angew Chem Int Ed Engl

Ligand: BSJ-03-204 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.980000019073486 pIC50
Reference (Journal): Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.
Published in: Angew Chem Int Ed Engl

Ligand: BSJ-04-132 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.
Published in: Angew Chem Int Ed Engl

Ligand: Cdk/Crk inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: cimpuciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.020000457763672 pIC50
Reference (Patent): Benzimidazole compound kinase inhibitor, preparation method therefor and application thereof

Ligand: CP-10 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.579999923706055 pIC50
Reference (Journal): Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders.
Published in: J Med Chem

Ligand: crozbaciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Published in: Eur J Med Chem

Ligand: dalpiciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2021)
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Patent): Thiophene miazines derivate, preparation method therefor, and medical application thereof

Ligand: inixaciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Heterocyclic compounds as kinase inhibitors

Ligand: lerociclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.329999923706055 pIC50
Reference (Patent): Transient protection of normal cells during chemotherapy

Ligand: narazaciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.010000228881836 pIC50
Reference (Journal): Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).
Published in: J Med Chem

Ligand: palbociclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 7.440000057220459 pIC50
Reference (Patent): Thiophene miazines derivate, preparation method therefor, and medical application thereof

Ligand: palbociclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders.
Published in: J Med Chem

Ligand: palbociclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: yes
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts.
Published in: Mol Cancer Ther

Ligand: PF-06873600 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKi
Reference (Patent): Pyridopyrimdinone cdk2/4/6 inhibitors.

Ligand: RGB-286638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.260000228881836 pIC50
Reference (Journal): Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs.
Published in: Leukemia

Ligand: tanuxiciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.46999979019165 pIC50
Reference (Patent): Heterocyclic compound and pharmaceutical composition comprising same

Ligand: tibremciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Patent): Crystal form of compound for inhibiting the activity of cdk4/6 and use thereof

Ligand: trilaciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2021)
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression.
Published in: Mol Cancer Ther

Ligand: ulecaciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pKi
Reference (Journal): Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.
Published in: J Med Chem

Ligand: voruciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.679999828338623 pIC50
Reference (Journal): Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells.
Published in: PLoS ONE