Target family: Aurora kinase (Aur) family (type: enzyme)
Target: aurora kinase B

Ligand: AMG-900 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
Published in: Cancer Res

Ligand: AT-9283 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Published in: J Med Chem

Ligand: aurora kinase inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: barasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.430000305175781 pIC50
Reference (Journal): AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo.
Published in: Blood

Ligand: barasertib-hQPA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.34000015258789 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: barasertib-hQPA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Discovery and development of aurora kinase inhibitors as anticancer agents.
Published in: J Med Chem

Ligand: BX-795 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation.
Published in: J Biol Chem

Ligand: Cdk2 inhibitor IV (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pIC50
Reference (Journal): How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?
Published in: J Med Chem

Ligand: cenisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.269999980926514 pIC50
Reference (Journal): Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Published in: Bioorg Med Chem Lett

Ligand: cenisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Patent): Cycloalkyl substituted pyrimidinediamine compounds and their uses.

Ligand: compound 10 [PMID: 19402633] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.46999979019165 pIC50
Reference (Journal): A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Published in: J Med Chem

Ligand: compound 1 [PMID: 21742770] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.550000190734863 pIC50
Reference (Journal): A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.
Published in: ACS Med Chem Lett

Ligand: compound 25 [PMID: 20855207] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 38 [PMID: 20817473] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.349999904632568 pIC50
Reference (Journal): Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Published in: Bioorg Med Chem

Ligand: compound 46 [PMID: 16451062] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Published in: J Med Chem

Ligand: danusertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.
Published in: J Med Chem

Ligand: dubermatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.909999847412109 pIC50
Reference (Journal): Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
Published in: ACS Med Chem Lett

Ligand: GSK1070916 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.420000076293945 pKi
Reference (Journal): Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
Published in: J Med Chem

Ligand: GSK2646264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.599999904632568 pIC50
Reference (Journal): Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.
Published in: Bioorg Med Chem Lett

Ligand: hesperadin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint.
Published in: J Cell Biol

Ligand: ibcasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency.
Published in: Cancer Sci

Ligand: ilorasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-7706621 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?
Published in: J Med Chem

Ligand: KW-2449 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation.
Published in: Blood

Ligand: MK-5108 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel.
Published in: Mol Cancer Ther

Ligand: MLN-8054 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.029999732971191 pIC50
Reference (Journal): A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Published in: J Med Chem

Ligand: NIK inhibitor 12f (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.360000133514404 pIC50
Reference (Journal): Identification of <i>N</i>-Phenyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-amine Derivatives as Novel, Potent, and Selective NF-κB Inducing Kinase (NIK) Inhibitors for the Treatment of Psoriasis.
Published in: J Med Chem

Ligand: SNS-314 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.510000228881836 pIC50
Reference (Journal): Discovery of a potent and selective aurora kinase inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: SU6656 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 pIC50
Reference (Journal): The selectivity of protein kinase inhibitors: a further update.
Published in: Biochem J

Ligand: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.179999828338623 pIC50
Reference (Journal): Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Published in: J Med Chem

Ligand: tinengotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 pIC50
Reference (Patent): Multi-kinase inhibitor compound, and crystal form and use thereof

Ligand: tozasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.739999771118164 pKi
Reference (Journal): VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.
Published in: Nat Med

Ligand: VIC 1911 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Patent): Piperidine compound or salt thereof

Ligand: XMD-12 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.
Published in: ACS Chem Biol

Ligand: ZM447439 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7 pIC50
Reference (Journal): Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores.
Published in: J Cell Biol