Target family: CDK8 subfamily (type: enzyme)
Target: cyclin dependent kinase 8

Ligand: CCT251545 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.420000076293945 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: CDK12 inhibitor 2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.
Published in: J Med Chem

Ligand: compound 1 [PMID: 24793884] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.
Published in: Eur J Med Chem

Ligand: compound 20 [Bergeron et al., 2016] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.760000228881836 pIC50
Reference (Journal): Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.
Published in: ACS Med Chem Lett

Ligand: compound 51 [Mallinger et al., 2016] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.289999961853027 pIC50
Reference (Journal): 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
Published in: ACS Med Chem Lett

Ligand: cortistatin A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pKd
Reference (Journal): Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
Published in: Angew Chem Int Ed Engl

Ligand: DS96432529 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Discovery of 3-amino-4-{(3S)-3-[(2-ethoxyethoxy)methyl]piperidin-1-yl}thieno[2,3-b]pyridine-2-carboxamide (DS96432529): A potent and orally active bone anabolic agent.
Published in: Bioorg Med Chem Lett

Ligand: JH-VIII-49 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.
Published in: ACS Med Chem Lett

Ligand: JH-XI-10-02 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.
Published in: ACS Med Chem Lett

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.15999984741211 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: ponatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 8.170000076293945 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 7 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: voruciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 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