AURKB

Summary

AURKB (aurora kinase B, HGNC:11390) is a protein-coding gene on chromosome 17p13.1, encoding Aurora kinase B (Q96GD4). Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. It is a common-essential gene (DepMap: required in 99.7% of cancer cell lines).

This gene encodes a member of the aurora kinase subfamily of serine/threonine kinases. The genes encoding the other two members of this subfamily are located on chromosomes 19 and 20. These kinases participate in the regulation of alignment and segregation of chromosomes during mitosis and meiosis through association with microtubules. A pseudogene of this gene is located on chromosome 8. Alternatively spliced transcript variants have been found for this gene.

Source: NCBI Gene 9212 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 48 total — 1 likely-pathogenic
• Druggable target: yes — 82 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 99.7% of screened cell lines (common-essential)
• MANE Select transcript: NM_004217

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11390
Approved symbol	AURKB
Name	aurora kinase B
Location	17p13.1
Locus type	gene with protein product
Status	Approved
Aliases	Aik2, IPL1, AurB, AIM-1, ARK2, STK5, PPP1R48
Ensembl gene	ENSG00000178999
Ensembl biotype	protein_coding
OMIM	604970
Entrez	9212

Gene structure

Transcript identifiers

Ensembl transcripts: 33 — 28 protein_coding, 4 retained_intron, 1 nonsense_mediated_decay

ENST00000316199, ENST00000534871, ENST00000577833, ENST00000578549, ENST00000578753, ENST00000580390, ENST00000580998, ENST00000581511, ENST00000582368, ENST00000583124, ENST00000583915, ENST00000584561, ENST00000584972, ENST00000585124, ENST00000881953, ENST00000932557, ENST00000932558, ENST00000932559, ENST00000932560, ENST00000932561, ENST00000932562, ENST00000932563, ENST00000932564, ENST00000932565, ENST00000932566, ENST00000932567, ENST00000932568, ENST00000932569, ENST00000932570, ENST00000932571, ENST00000932572, ENST00000932573, ENST00000932574

RefSeq mRNA: 9 — MANE Select: NM_004217 NM_001256834, NM_001284526, NM_001313950, NM_001313951, NM_001313952, NM_001313953, NM_001313954, NM_001313955, NM_004217

CCDS: CCDS11134, CCDS58514, CCDS67162, CCDS82065

Canonical transcript exons

ENST00000585124 — 9 exons

Exon	Start	End
ENSE00001235883	8206750	8206888
ENSE00001235888	8207176	8207367
ENSE00002721099	8210530	8210575
ENSE00002733805	8204734	8205044
ENSE00003526889	8207571	8207625
ENSE00003617867	8210177	8210249
ENSE00003672784	8207738	8207840
ENSE00003682160	8205216	8205390
ENSE00003784670	8206491	8206639

Expression profiles

Bgee: expression breadth ubiquitous, 187 present calls, max score 96.81.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 25.3793 / max 295.0910, expressed in 1406 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
164421	24.4573	1370
164420	0.9220	572

Top tissues by expression

285 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
ventricular zone	UBERON:0003053	96.81	gold quality
ganglionic eminence	UBERON:0004023	93.38	gold quality
oocyte	CL:0000023	92.52	gold quality
endometrium epithelium	UBERON:0004811	92.27	gold quality
embryo	UBERON:0000922	91.37	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	90.97	gold quality
mucosa of transverse colon	UBERON:0004991	90.32	gold quality
tibial nerve	UBERON:0001323	88.75	gold quality
lower esophagus mucosa	UBERON:0035834	88.19	gold quality
stromal cell of endometrium	CL:0002255	87.14	gold quality
sural nerve	UBERON:0015488	85.25	gold quality
esophagus mucosa	UBERON:0002469	85.14	gold quality
rectum	UBERON:0001052	84.74	gold quality
bone marrow	UBERON:0002371	84.14	gold quality
vermiform appendix	UBERON:0001154	84.13	gold quality
bone marrow cell	CL:0002092	82.40	gold quality
lymph node	UBERON:0000029	80.97	gold quality
secondary oocyte	CL:0000655	79.72	gold quality
spleen	UBERON:0002106	79.57	gold quality
thymus	UBERON:0002370	79.14	gold quality
caecum	UBERON:0001153	79.07	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	78.48	gold quality
colonic epithelium	UBERON:0000397	77.22	gold quality
trabecular bone tissue	UBERON:0002483	77.22	gold quality
small intestine Peyer’s patch	UBERON:0003454	76.69	gold quality
transverse colon	UBERON:0001157	76.36	gold quality
small intestine	UBERON:0002108	75.46	gold quality
skin of abdomen	UBERON:0001416	75.27	gold quality
duodenum	UBERON:0002114	75.20	gold quality
skin of leg	UBERON:0001511	75.11	gold quality

Single-cell (SCXA)

Detected in 14 experiment(s), a significant marker in 11.

Experiment	Marker?	Max mean expression
E-MTAB-9067	yes	372.12
E-GEOD-93593	yes	357.12
E-GEOD-75688	yes	291.25
E-GEOD-84465	yes	152.82
E-MTAB-7052	yes	148.25
E-MTAB-7051	yes	91.08
E-HCAD-10	yes	41.53
E-CURD-112	yes	40.97
E-MTAB-6678	yes	8.60
E-CURD-88	yes	6.21
E-MTAB-6142	no	593.93
E-CURD-11	no	338.30
E-MTAB-8271	no	177.74
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): E2F1, E2F4, EWSR1, FLI1, FOXM1, MBD1, MBD2, NR1I2, SRSF1, SRSF2

miRNA regulators (miRDB)

22 targeting AURKB, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-12118	100.00	65.88	1270
HSA-MIR-4500	99.99	72.72	2367
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-3173-3P	99.98	66.49	1217
HSA-MIR-6891-5P	99.98	66.53	1372
HSA-LET-7D-5P	99.96	71.76	1632
HSA-MIR-4458	99.96	71.64	1650
HSA-MIR-765	99.84	68.24	2442
HSA-MIR-11181-3P	99.75	66.38	2205
HSA-MIR-4672	99.50	71.58	2893
HSA-MIR-4650-3P	99.01	68.39	1062
HSA-MIR-5088-3P	98.29	66.63	1310
HSA-MIR-6892-5P	97.27	68.60	847
HSA-MIR-6750-5P	93.94	66.68	797
HSA-MIR-6822-5P	93.94	66.34	812

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 99.7% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 40)

• Aurora B kinase. Human Aurora-B is activated by okadaic acid and forms complexes with the protein serine/threonine phosphatase type 1 (PP1) or PP2A, but not with PP5. Human Aurora-B is likely a mitotic histone H3 kinase. (PMID:12082625)
• These results indicate that survivin stimulates Aurora-B kinase activity and helps correctly target Aurora-B to its substrates during the cell cycle, thus providing a mechanism as to how survivin exerts its function in human cells. (PMID:12419797)
• topoisomerase II alpha is an Aurora B substrate on metaphase chromosomes (PMID:12466558)
• Aurora B kinase activity is stimulated by INCENP and C-terminal region of INCENP is sufficient for activation (PMID:12925766)
• aurora-B may regulate targeting of survivin by phosphorylating it at threonine 117 (PMID:14610074)
• Aurora-B might undergo degradation by binding to HC8 in a proteasome-dependent manner during mitosis (PMID:14674694)
• phosphorylation of Thr-232 is an essential regulatory mechanism for Aurora-B activation (PMID:14722118)
• aurora B mRNA level is regulated by its cell cycle-dependent element (CDE) and cell cycle-gene homology region and a subset of E2F/DP family proteins binds to the CDE (PMID:15033491)
• Aurora B knocked down prevents the formation of the midbody - and consequently affects TACC1 localization at this site - and leads to abnormal cell division and multinucleated cells (PMID:15064709)
• Aurora-B/AIM-1 was highly expressed in high-grade gliomas and its expression was well correlated with histological malignancy and clinical outcomes. (PMID:15072448)
• results suggest that endomitotic MKs appropriately express functional Aurora-B kinase and related proteins in early anaphase, making a simple deficiency of this protein an unlikely explanation for polyploidy in this cell type. (PMID:15130946)
• propose that MKlp2 is involved in the localization of Plk1, Aurora B, and Cdc14A to the central spindle during anaphase, and that the integration of signaling by these proteins is necessary for proper cytokinesis. (PMID:15263015)
• Changes in rates of survivin turnover at centromeres were regulated by stage of the cell cycle, microtubule attachment, and Aurora B kinase activity. (PMID:15280424)
• Aurora-B interacts with the inner centromere protein (INCENP) at the carboxyl terminal end spanning the conserved IN box domain. (PMID:15499654)
• a small C-terminal sequence of Aurora B is essential for the distinct localization and function of Aurora B (PMID:15509656)
• Block of Aurora B expression induced by RNA interference or by using an inhibitor of Aurora kinase activity significantly reduced the growth of thyroid anaplastic carcinoma cells. (PMID:15562011)
• multinucleated giant tumor cells remain in the early mitotic phase because of aurora-B dysfunction, effecting aberrations in cytoplasmic cleavage without affecting nuclear division. (PMID:15597762)
• An important protein in the progresesion of anaplastic carcinoma of the thyroid. (PMID:15699543)
• Aurora-C is a chromosomal passenger protein that disrupts the association of INCENP with Aurora-B and may serve as a key regulator in cell division (PMID:15917996)
• Aurora B is responsible for mitotic arrest in the absence of aurora A. (PMID:15922328)
• Results identify the degradation pathway for Aurora-B, and show that overexpression of a stable form of Aurora-B alone induces aneuploidy and anchorage-independent growth. (PMID:15923616)
• Rebamipide significantly downregulates in AGS cell survivin expression, its association with Aurora-B and cell proliferation. Rebamipide-induced downregulation of survivin is at the transcription level and does not involve ubiquitin-proteasome pathway. (PMID:15993841)
• The two spindle checkpoint arms respond to different spindle cues: whereas the Bub1 arm monitors kinetochore-microtubule attachment, the aurora B arm monitors biorientation. (PMID:16046481)
• Anti-proliferative effect of p53 tumor suppressor is activated by aurora B in normal and glioblastoma cells containing intact p53. (PMID:16171786)
• Aurora-B binds and phosphorylates Septin1. (PMID:16179162)
• The specific inhibition of Aurora-B kinase activity by PARP-1 contributes to the physiological response to DNA damage. (PMID:16179389)
• H3 phosphorylation by Aurora B is therefore part of a ‘methyl/phos switch’ mechanism that displaces HP1 and perhaps other proteins from mitotic heterochromatin (PMID:16222244)
• Overexpression of aurora B kinase leading to genetic instability is associated with primary non-small cell lung carcinoma (PMID:16222316)
• Overexpression of aurora kinase B is associated with Esophageal Neoplasms (PMID:16572587)
• the direct interaction of Survivin and Aurora B was critical for the correct location of Survivin and the function of the Survivin complex in cell division (PMID:16762323)
• Data show that small molecule-mediated inhibition of Aurora A and Aurora B yields distinct phenotypes, suggesting that the Auroras may present two avenues for anti-cancer drug discovery. (PMID:16912073)
• These results indicate that RKIP regulates Aurora B kinase and the spindle checkpoint via the Raf-1/MEK/ERK cascade and demonstrate that small changes in the MAP kinase (MAPK) pathway can profoundly impact the fidelity of the cell cycle. (PMID:16916643)
• Deacetylation of H3 in mitosis requires AKAP95/HA95 and HDAC3 and provides a hypoacetylated H3 tail that is the preferred substrate for Aurora B kinase. (PMID:16980585)
• chromosome passenger complex, consisting of multiple proteins including Aurora B kinase and INCENP is thought to be responsible for H3 phosphorylation, chromosome condensation and the subsequent segregation of chromosomes (PMID:17001311)
• Aurora B regulates cohesin removal through its effect on the localization of Shugoshin. (PMID:17084365)
• Aberrant alterative splicing of Aurora-B kinase is associated with hepatocarcinogenesis (PMID:17094487)
• role of DNA methylation in Aurora-B targeting to pericentromeres (PMID:17164288)
• These results indicate that Aurora-B participates to regulate the assembly of nucleolar RNA-processing machinery and the RNA methyltransferase activity of NSUN2 via phosphorylation at Ser139 during mitosis. (PMID:17215513)
• Aurora-B may be involved in tumor progression and can be a new diagnostic and therapeutic target for oral squamous cell carcinoma. (PMID:17235564)
• data indicate that Aurora B contributes to chromosome rigidity and segregation by promoting the binding of condensin I to chromatin (PMID:17356064)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	aurkb	ENSDARG00000037640
mus_musculus	Aurkb	ENSMUSG00000020897
rattus_norvegicus	Aurkb	ENSRNOG00000005659
caenorhabditis_elegans	air-2	WBGENE00000099

Paralogs (2): AURKA (ENSG00000087586), AURKC (ENSG00000105146)

Protein

Protein identifiers

Aurora kinase B — Q96GD4 (reviewed: Q96GD4)

Alternative names: Aurora 1, Aurora- and IPL1-like midbody-associated protein 1, Aurora/IPL1-related kinase 2, STK-1, Serine/threonine-protein kinase 12, Serine/threonine-protein kinase 5, Serine/threonine-protein kinase aurora-B

All UniProt accessions (7): Q96GD4, J3KRF8, J3KRJ2, J3KT86, J3KTD6, J3QLN8, J3QR41

UniProt curated annotations — full annotation on UniProt →

Function. Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis. Required for central/midzone spindle assembly and cleavage furrow formation. Key component of the cytokinesis checkpoint, a process required to delay abscission to prevent both premature resolution of intercellular chromosome bridges and accumulation of DNA damage: phosphorylates CHMP4C, leading to retain abscission-competent VPS4 (VPS4A and/or VPS4B) at the midbody ring until abscission checkpoint signaling is terminated at late cytokinesis. AURKB phosphorylates the CPC complex subunits BIRC5/survivin, CDCA8/borealin and INCENP. Phosphorylation of INCENP leads to increased AURKB activity. Other known AURKB substrates involved in centromeric functions and mitosis are CENPA, DES/desmin, GPAF, KIF2C, NSUN2, RACGAP1, SEPTIN1, VIM/vimentin, HASPIN, and histones H1.4 and H3. A positive feedback loop involving HASPIN and AURKB contributes to localization of CPC to centromeres. Phosphorylation of VIM controls vimentin filament segregation in cytokinetic process, whereas histone H3 is phosphorylated at ‘Ser-10’ and ‘Ser-28’ during mitosis (H3S10ph and H3S28ph, respectively). AURKB is also required for kinetochore localization of BUB1 and SGO1. Phosphorylation of p53/TP53 negatively regulates its transcriptional activity. Key regulator of active promoters in resting B- and T-lymphocytes: acts by mediating phosphorylation of H3S28ph at active promoters in resting B-cells, inhibiting RNF2/RING1B-mediated ubiquitination of histone H2A and enhancing binding and activity of the USP16 deubiquitinase at transcribed genes. Acts as an inhibitor of CGAS during mitosis: catalyzes phosphorylation of the N-terminus of CGAS during the G2-M transition, blocking CGAS liquid phase separation and activation, and thereby preventing CGAS-induced autoimmunity. Phosphorylates KRT5 during anaphase and telophase. Phosphorylates ATXN10 which promotes phosphorylation of ATXN10 by PLK1 and may play a role in the regulation of cytokinesis and stimulating the proteasomal degradation of ATXN10.

Subunit / interactions. Component of the chromosomal passenger complex (CPC) composed of at least BIRC5/survivin, CDCA8/borealin, INCENP, AURKB or AURKC; predominantly independent AURKB- and AURKC-containing complexes exist. Associates with RACGAP1 during M phase. Interacts with SPDYC; this interaction may be required for proper localization of active, Thr-232-phosphorylated AURKB form during prometaphase and metaphase. Interacts with p53/TP53. Interacts (via the middle kinase domain) with NOC2L (via the N- and C-terminus domains). Interacts with CDCA1. Interacts with EVI5. Interacts with JTB. Interacts with NDC80. Interacts with PSMA3. Interacts with RNF2/RING1B. Interacts with SEPTIN1. Interacts with SIRT2. Interacts with TACC1. Interacts with TTC28.

Subcellular location. Nucleus. Chromosome. Centromere. Kinetochore. Cytoplasm. Cytoskeleton. Spindle. Midbody.

Tissue specificity. High level expression seen in the thymus. It is also expressed in the spleen, lung, testis, colon, placenta and fetal liver. Expressed during S and G2/M phase and expression is up-regulated in cancer cells during M phase. Not expressed in normal liver, high expression in metastatic liver.

Post-translational modifications. The phosphorylation of Thr-232 requires the binding to INCENP and occurs by means of an autophosphorylation mechanism. Thr-232 phosphorylation is indispensable for the AURKB kinase activity. Acetylated at Lys-215 by KAT5 at kinetochores, increasing AURKB activity and promoting accurate chromosome segregation in mitosis. Ubiquitinated by different BCR (BTB-CUL3-RBX1) E3 ubiquitin ligase complexes. Ubiquitinated by the BCR(KLHL9-KLHL13) E3 ubiquitin ligase complex, ubiquitination leads to removal from mitotic chromosomes and is required for cytokinesis. During anaphase, the BCR(KLHL21) E3 ubiquitin ligase complex recruits the CPC complex from chromosomes to the spindle midzone and mediates the ubiquitination of AURKB. Ubiquitination of AURKB by BCR(KLHL21) E3 ubiquitin ligase complex may not lead to its degradation by the proteasome. Deubiquitinated by USP35; inhibiting CDH1-mediated degradation of AURKB.

Disease relevance. Disruptive regulation of expression is a possible mechanism of the perturbation of chromosomal integrity in cancer cells through its dominant-negative effect on cytokinesis.

Activity regulation. Activity is greatly increased when AURKB is within the CPC complex. In particular, AURKB-phosphorylated INCENP acts as an activator of AURKB. Positive feedback between HASPIN and AURKB contributes to CPC localization. Inhibited by ZM447439.

Induction. Expression is cell cycle-regulated, with a low in G1/S, an increase during G2 and M. Expression decreases again after M phase.

Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family. Aurora subfamily.

Isoforms (5)

UniProt ID	Names	Canonical?
Q96GD4-1	1	yes
Q96GD4-2	2, aurkb-sv1
Q96GD4-3	3, aurkb-sv2
Q96GD4-4	4
Q96GD4-5	5

RefSeq proteins (9): NP_001243763, NP_001271455, NP_001300879, NP_001300880, NP_001300881, NP_001300882, NP_001300883, NP_001300884, NP_004208* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR030616	Aur-like	Family

Pfam: PF00069

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (53 total): helix 13, sequence conflict 8, strand 7, modified residue 6, splice variant 5, sequence variant 4, mutagenesis site 3, binding site 2, chain 1, domain 1, region of interest 1, active site 1, turn 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
4AF3	X-RAY DIFFRACTION	2.75

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96GD4-F1	79.71	0.63

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 200 (proton acceptor)

Ligand- & substrate-binding residues (2): 83–91; 106

Post-translational modifications (6): 227, 232, 35, 62, 64, 215

Mutagenesis-validated functional residues (3):

Position	Phenotype
106	leads to loss of kinase activity and severely impairs mitotic progression.
215	mimics acetylation, promoting accurate chromosome segregation.
215	abolished acetylation by kat5, leading to impaired chromosome segregation.

Function

Pathways and Gene Ontology

Reactome pathways

34 pathways

ID	Pathway
R-HSA-141444	Amplification of signal from unattached kinetochores via a MAD2 inhibitory signal
R-HSA-174178	APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
R-HSA-2467813	Separation of Sister Chromatids
R-HSA-2500257	Resolution of Sister Chromatid Cohesion
R-HSA-4615885	SUMOylation of DNA replication proteins
R-HSA-5663220	RHO GTPases Activate Formins
R-HSA-6804756	Regulation of TP53 Activity through Phosphorylation
R-HSA-68877	Mitotic Prometaphase
R-HSA-9022692	Regulation of MECP2 expression and activity
R-HSA-9648025	EML4 and NUDC in mitotic spindle formation
R-HSA-141424	Amplification of signal from the kinetochores
R-HSA-162582	Signal Transduction
R-HSA-1640170	Cell Cycle
R-HSA-174143	APC/C-mediated degradation of cell cycle proteins
R-HSA-194315	Signaling by Rho GTPases
R-HSA-195258	RHO GTPase Effectors
R-HSA-212436	Generic Transcription Pathway
R-HSA-2555396	Mitotic Metaphase and Anaphase
R-HSA-2990846	SUMOylation
R-HSA-3108232	SUMO E3 ligases SUMOylate target proteins
R-HSA-3700989	Transcriptional Regulation by TP53
R-HSA-392499	Metabolism of proteins
R-HSA-453276	Regulation of mitotic cell cycle
R-HSA-5633007	Regulation of TP53 Activity
R-HSA-597592	Post-translational protein modification
R-HSA-68882	Mitotic Anaphase
R-HSA-68886	M Phase
R-HSA-69278	Cell Cycle, Mitotic
R-HSA-69618	Mitotic Spindle Checkpoint
R-HSA-69620	Cell Cycle Checkpoints

MSigDB gene sets: 569 (showing top): GNF2_CKS1B, GOBP_MITOTIC_CYTOKINESIS, GOBP_CHROMOSOME_ORGANIZATION, WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, GOBP_ATTACHMENT_OF_SPINDLE_MICROTUBULES_TO_KINETOCHORE, GOBP_REGULATION_OF_CELL_CYCLE_CHECKPOINT, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, HORIUCHI_WTAP_TARGETS_DN, REACTOME_APC_C_CDH1_MEDIATED_DEGRADATION_OF_CDC20_AND_OTHER_APC_C_CDH1_TARGETED_PROTEINS_IN_LATE_MITOSIS_EARLY_G1, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, MORF_ESPL1, GOBP_REGULATION_OF_MICROTUBULE_BASED_PROCESS, GOBP_NEGATIVE_REGULATION_OF_CELL_DIVISION, GOBP_CELLULAR_RESPONSE_TO_UV, GOBP_REGULATION_OF_NUCLEAR_DIVISION

GO Biological Process (39): negative regulation of transcription by RNA polymerase II (GO:0000122), mitotic cell cycle (GO:0000278), mitotic cytokinesis (GO:0000281), negative regulation of B cell apoptotic process (GO:0002903), spindle organization (GO:0007051), mitotic spindle organization (GO:0007052), positive regulation of microtubule depolymerization (GO:0031117), positive regulation of telomere maintenance (GO:0032206), regulation of cytokinesis (GO:0032465), negative regulation of cytokinesis (GO:0032466), positive regulation of cytokinesis (GO:0032467), protein localization to kinetochore (GO:0034501), cellular response to UV (GO:0034644), cleavage furrow formation (GO:0036089), post-translational protein modification (GO:0043687), cell cycle G2/M phase transition (GO:0044839), mitotic cytokinesis checkpoint signaling (GO:0044878), negative regulation of innate immune response (GO:0045824), mitotic spindle midzone assembly (GO:0051256), regulation of chromosome segregation (GO:0051983), midbody abscission (GO:0061952), positive regulation of mitotic sister chromatid segregation (GO:0062033), positive regulation of mitotic cell cycle spindle assembly checkpoint (GO:0090267), mitotic spindle assembly (GO:0090307), negative regulation of protein localization to chromatin (GO:0120186), repair of mitotic kinetochore microtubule attachment defect (GO:0140273), negative regulation of cGAS/STING signaling pathway (GO:0160049), regulation of signal transduction by p53 class mediator (GO:1901796), positive regulation of mitotic sister chromatid separation (GO:1901970), positive regulation of attachment of mitotic spindle microtubules to kinetochore (GO:1902425), positive regulation of mitotic cytokinesis (GO:1903490), positive regulation of lateral attachment of mitotic spindle microtubules to kinetochore (GO:1905116), mitotic sister chromatid biorientation (GO:1990758), protein phosphorylation (GO:0006468), regulation of microtubule-based process (GO:0032886), cell division (GO:0051301), attachment of mitotic spindle microtubules to kinetochore (GO:0051315), positive regulation of cell cycle process (GO:0090068), cGAS/STING signaling pathway (GO:0140896)

GO Molecular Function (11): protein serine/threonine kinase activity (GO:0004674), protein serine/threonine/tyrosine kinase activity (GO:0004712), ATP binding (GO:0005524), kinase binding (GO:0019900), protein serine kinase activity (GO:0106310), histone H1-4S27 kinase activity (GO:0140197), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (21): kinetochore (GO:0000776), condensed chromosome, centromeric region (GO:0000779), chromatin (GO:0000785), spindle pole (GO:0000922), nucleus (GO:0005634), nucleoplasm (GO:0005654), centrosome (GO:0005813), spindle (GO:0005819), cytosol (GO:0005829), spindle microtubule (GO:0005876), chromocenter (GO:0010369), microtubule cytoskeleton (GO:0015630), midbody (GO:0030496), chromosome passenger complex (GO:0032133), spindle midzone (GO:0051233), mitotic spindle pole (GO:0097431), mitotic spindle midzone (GO:1990023), chromosome, centromeric region (GO:0000775), chromosome (GO:0005694), cytoplasm (GO:0005737), cytoskeleton (GO:0005856)

Reactome top-level categories

Rollup of top-16 pathways:

Category	Pathways
Mitotic Prometaphase	2
M Phase	2
Amplification of signal from the kinetochores	1
APC/C-mediated degradation of cell cycle proteins	1
Mitotic Anaphase	1
SUMO E3 ligases SUMOylate target proteins	1
RHO GTPase Effectors	1
Regulation of TP53 Activity	1
Transcriptional Regulation by MECP2	1
Mitotic Spindle Checkpoint	1
Regulation of mitotic cell cycle	1
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1
Signaling by Rho GTPases	1
RNA Polymerase II Transcription	1
Post-translational protein modification	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	7
intracellular membraneless organelle	4
cytokinesis	3
protein kinase activity	3
spindle	3
mitotic nuclear division	2
mitotic cell cycle	2
cytoskeleton-dependent cytokinesis	2
mitotic cell cycle process	2
regulation of cell cycle process	2
regulation of cytokinesis	2
mitotic spindle	2
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
negative regulation of DNA-templated transcription	1
cell cycle	1
B cell apoptotic process	1
regulation of B cell apoptotic process	1
negative regulation of lymphocyte apoptotic process	1
microtubule cytoskeleton organization	1
cell cycle process	1
spindle organization	1
microtubule cytoskeleton organization involved in mitosis	1
microtubule depolymerization	1
positive regulation of microtubule polymerization or depolymerization	1
regulation of microtubule depolymerization	1
positive regulation of protein depolymerization	1
positive regulation of supramolecular fiber organization	1
telomere maintenance	1
regulation of telomere maintenance	1
positive regulation of DNA metabolic process	1
positive regulation of chromosome organization	1
regulation of cell division	1
negative regulation of cell cycle process	1
negative regulation of cell division	1
positive regulation of cell division	1
positive regulation of cell cycle process	1
protein localization to chromosome, centromeric region	1
protein localization to condensed chromosome	1
response to UV	1

Protein interactions and networks

STRING

4868 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
AURKB	INCENP	Q9NQS7	999
AURKB	CDCA8	Q53HL2	998
AURKB	BIRC5	O15392	997
AURKB	BUB1B	O60566	993
AURKB	BUB1	O43683	985
AURKB	KIF2C	Q99661	975
AURKB	CDC20	Q12834	966
AURKB	RCC2	Q9P258	959
AURKB	CENPE	Q02224	946
AURKB	ESPL1	Q14674	933
AURKB	OGA	O60502	927
AURKB	CENPA	P49450	917
AURKB	SGO1	Q5FBB7	912
AURKB	HASPIN	Q8TF76	908
AURKB	CDCA5	Q96FF9	907

IntAct

245 interactions, top by confidence:

A	B	Type	Score
AURKB	INCENP	psi-mi:“MI:0914”(association)	0.960
INCENP	AURKB	psi-mi:“MI:0915”(physical association)	0.960
CDCA8	BIRC5	psi-mi:“MI:0914”(association)	0.960
AURKB	INCENP	psi-mi:“MI:0915”(physical association)	0.960
AURKB	INCENP	psi-mi:“MI:0407”(direct interaction)	0.960
AURKB	BIRC5	psi-mi:“MI:0914”(association)	0.950
BIRC5	AURKB	psi-mi:“MI:0915”(physical association)	0.950
AURKB	BIRC5	psi-mi:“MI:0915”(physical association)	0.950
BIRC5	AURKB	psi-mi:“MI:0217”(phosphorylation reaction)	0.950
INCENP	BIRC5	psi-mi:“MI:0914”(association)	0.920
CDCA8	AURKB	psi-mi:“MI:0914”(association)	0.870
AURKB	CDCA8	psi-mi:“MI:0915”(physical association)	0.870
KLHL9	CUL3	psi-mi:“MI:0914”(association)	0.860
AURKB	CDC37	psi-mi:“MI:0914”(association)	0.830
KLHL13	CUL3	psi-mi:“MI:0914”(association)	0.810
INCENP	CBX5	psi-mi:“MI:0914”(association)	0.800
HSP90AB1	AURKB	psi-mi:“MI:0915”(physical association)	0.780
AURKC	BIRC5	psi-mi:“MI:0914”(association)	0.740
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
SEPTIN1	AURKB	psi-mi:“MI:0915”(physical association)	0.700

BioGRID (1018): AURKB (Affinity Capture-Western), AURKB (Reconstituted Complex), AURKB (Affinity Capture-MS), AURKB (Affinity Capture-MS), AURKB (Affinity Capture-Western), AURKB (Biochemical Activity), ENDOG (Affinity Capture-MS), HSP90AA1 (Affinity Capture-MS), HSP90AB1 (Affinity Capture-MS), HSP90AA5P (Affinity Capture-MS), HSP90AA4P (Affinity Capture-MS), CDC37 (Affinity Capture-MS), RBM12B (Affinity Capture-MS), TTK (Affinity Capture-MS), AURKB (Proximity Label-MS)

ESM2 similar proteins: A0A8I3S724, A4IGM9, A4IIW7, A5GFW1, B0VXL7, B6A7Q3, C0RW22, D7UQM5, F4I4F2, O08605, O14965, O35495, O55099, O59790, O70126, O80673, O94921, P18266, P27466, P49841, P59241, P97477, Q00771, Q0VD22, Q13555, Q16566, Q2TA06, Q501Q9, Q58D94, Q5XIT0, Q66JF3, Q6BVA0, Q6C3J2, Q6CWQ4, Q6DE08, Q6DGS3, Q6GPL3, Q6Z8C8, Q755C4, Q7YRC6

Diamond homologs: A0A8I3S724, A2VDZ4, A2XFF4, A4IGM9, A5GFW1, A7SNN5, B0WAU8, B2GUY1, B3DL84, B3M6I4, B3NE99, B4HBU3, B4IAQ8, B4J3F1, B4KYX8, B4LDJ6, B4MXR8, B4PDM5, B4QK53, B8BBT7, D7UQM5, E2RTQ7, O00444, O01427, O14965, O55099, O59790, O64629, O70126, O88445, O97143, P05986, P06244, P0C8M8, P38991, P59241, P92937, P97477, Q0JI49, Q10LQ2

SIGNOR signaling

135 interactions.

A	Effect	B	Mechanism
AURKB	“up-regulates activity”	RACGAP1	phosphorylation
AURKB	“down-regulates activity”	H3C1	phosphorylation
AURKB	up-regulates	INCENP	phosphorylation
AURKB	“up-regulates activity”	H3-3A	phosphorylation
AURKB	“up-regulates activity”	H3C1	phosphorylation
AURKB	up-regulates	AURKB	phosphorylation
AURKB	down-regulates	NSUN2	phosphorylation
CHEK1	up-regulates	AURKB	phosphorylation
AURKB	down-regulates	BIRC5	phosphorylation
AURKB	up-regulates	KIF2C	phosphorylation
AURKB	down-regulates	KIF2C	phosphorylation
ATM	down-regulates	AURKB
AURKB	unknown	MYBBP1A	phosphorylation
AURKB	up-regulates	CKAP2	phosphorylation
AURKB	down-regulates	KNL1	phosphorylation
AURKB	down-regulates	DSN1	phosphorylation
AURKB	down-regulates	NDC80	phosphorylation
AURKB	up-regulates	NINL	phosphorylation
AURKB	down-regulates	TP53	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 153 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Constitutive Signaling by EGFRvIII	5	33.4×	2e-05
Signaling by ERBB2 ECD mutants	5	31.4×	2e-05
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	5	26.7×	5e-05
Regulation of TP53 Expression and Degradation	5	24.3×	7e-05
Signaling by ERBB2 TMD/JMD mutants	5	22.2×	1e-04
Signaling by ERBB2 KD Mutants	5	19.8×	1e-04
HSF1 activation	5	17.8×	2e-04
Regulation of TP53 Degradation	6	16.4×	7e-05

GO biological processes:

GO term	Partners	Fold	FDR
regulation of cytokinesis	5	15.3×	2e-03
cellular response to estradiol stimulus	5	14.9×	3e-03
mitotic spindle organization	6	11.8×	2e-03
G2/M transition of mitotic cell cycle	5	11.3×	6e-03
positive regulation of miRNA transcription	5	10.5×	7e-03
positive regulation of neuron apoptotic process	5	9.8×	9e-03
positive regulation of protein ubiquitination	6	9.3×	4e-03
regulation of protein localization	6	8.9×	4e-03

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

48 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	29
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
638622	NM_004217.4(AURKB):c.847C>T (p.Arg283Cys)	Likely pathogenic

SpliceAI

1226 predictions. Top by Δscore:

Variant	Effect	Δscore
17:8205040:TCCAC:T	acceptor_gain	1.0000
17:8205041:CCAC:C	acceptor_gain	1.0000
17:8205041:CCACC:C	acceptor_gain	1.0000
17:8205042:CAC:C	acceptor_gain	1.0000
17:8205042:CACC:C	acceptor_gain	1.0000
17:8205043:AC:A	acceptor_gain	1.0000
17:8205044:CC:C	acceptor_gain	1.0000
17:8205044:CCTG:C	acceptor_loss	1.0000
17:8205045:C:CC	acceptor_gain	1.0000
17:8205048:CAGG:C	acceptor_gain	1.0000
17:8205049:A:T	acceptor_gain	1.0000
17:8205051:G:C	acceptor_gain	1.0000
17:8205051:G:GC	acceptor_gain	1.0000
17:8205053:G:C	acceptor_gain	1.0000
17:8205053:G:GC	acceptor_gain	1.0000
17:8205389:TCC:T	acceptor_loss	1.0000
17:8206488:TACC:T	donor_loss	1.0000
17:8206489:ACC:A	donor_loss	1.0000
17:8206490:CCTC:C	donor_loss	1.0000
17:8206636:TGAT:T	acceptor_gain	1.0000
17:8206638:ATCTG:A	acceptor_loss	1.0000
17:8206639:TCTGG:T	acceptor_loss	1.0000
17:8206640:C:CC	acceptor_gain	1.0000
17:8206640:CTGGG:C	acceptor_loss	1.0000
17:8206886:TGG:T	acceptor_gain	1.0000
17:8206889:C:CC	acceptor_gain	1.0000
17:8207174:A:AC	donor_gain	1.0000
17:8207175:C:CC	donor_gain	1.0000
17:8207175:CTG:C	donor_gain	1.0000
17:8207210:G:C	donor_gain	1.0000

AlphaMissense

2237 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:8205308:A:G	W257R	1.000
17:8205308:A:T	W257R	1.000
17:8206516:A:G	W221R	1.000
17:8206516:A:T	W221R	1.000
17:8206520:G:C	F219L	1.000
17:8206520:G:T	F219L	1.000
17:8206521:A:G	F219S	1.000
17:8206522:A:G	F219L	1.000
17:8206523:G:C	D218E	1.000
17:8206523:G:T	D218E	1.000
17:8206524:T:A	D218V	1.000
17:8206524:T:C	D218G	1.000
17:8206524:T:G	D218A	1.000
17:8206525:C:G	D218H	1.000
17:8206560:A:G	L206P	1.000
17:8206562:A:C	N205K	1.000
17:8206562:A:T	N205K	1.000
17:8206564:T:C	N205D	1.000
17:8206571:C:A	K202N	1.000
17:8206571:C:G	K202N	1.000
17:8206573:T:C	K202E	1.000
17:8206577:G:C	D200E	1.000
17:8206577:G:T	D200E	1.000
17:8206578:T:A	D200V	1.000
17:8206578:T:C	D200G	1.000
17:8206578:T:G	D200A	1.000
17:8206579:C:G	D200H	1.000
17:8206581:C:A	R199I	1.000
17:8206581:C:G	R199T	1.000
17:8206826:A:G	L154P	1.000

dbSNP variants (sampled 300 via entrez): RS1000064659 (17:8205159 C>T), RS1000237490 (17:8212291 T>G), RS1000422409 (17:8205643 T>C), RS1000574839 (17:8210696 G>A), RS1000627099 (17:8210437 C>A), RS1000698354 (17:8211968 C>T), RS1001170071 (17:8204364 C>G,T), RS1001206517 (17:8212297 G>C), RS1003037828 (17:8208819 A>G), RS1003734241 (17:8208058 G>A), RS1003765567 (17:8208296 G>A), RS1003974336 (17:8204564 G>A), RS1003987329 (17:8205294 C>A,G,T), RS1004072028 (17:8210568 A>C), RS1004400664 (17:8211184 C>T)

Disease associations

OMIM: gene MIM:604970 | disease phenotypes:

GenCC curated gene-disease

Mondo (2): breast ductal adenocarcinoma (MONDO:0005590), NK-cell enteropathy (MONDO:0016996)

Orphanet (1): NK-cell enteropathy (Orphanet:263665)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST009838_1	Anxiety disorders	2.000000e-08
GCST010241_434	Apolipoprotein A1 levels	8.000000e-12

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004614	apolipoprotein A 1 measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D018270	Carcinoma, Ductal, Breast	C04.557.470.200.025.232.500; C04.557.470.615.132.500; C04.588.180.390; C17.800.090.500.390

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL2185 (SINGLE PROTEIN), CHEMBL3430907 (PROTEIN COMPLEX), CHEMBL3430908 (SELECTIVITY GROUP), CHEMBL3430911 (PROTEIN FAMILY), CHEMBL3883303 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

82 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 501,837 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1200485	SORAFENIB TOSYLATE	4	30,403
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289494	TIVOZANIB	4	4,455
CHEMBL1289601	LENVATINIB	4	8,784
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL1983268	ENTRECTINIB	4	3,510
CHEMBL2005186	BELUMOSUDIL	4	1,817
CHEMBL2035187	PACRITINIB	4	3,345
CHEMBL2103830	FOSTAMATINIB	4	3,841
CHEMBL221959	TOFACITINIB	4	10,408
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL3622821	UPADACITINIB	4	2,726
CHEMBL3813873	PEXIDARTINIB	4	3,586
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL5416410	DASATINIB	4	655
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL554	LAPATINIB	4	69,326
CHEMBL576982	QUIZARTINIB	4
CHEMBL601719	CRIZOTINIB	4
CHEMBL608533	MIDOSTAURIN	4
CHEMBL12856	INAMRINONE	4
CHEMBL2105717	CABOZANTINIB	4
CHEMBL1091644	LINSITINIB	3
CHEMBL1879463	DACTOLISIB	3
CHEMBL223360	LINIFANIB	3
CHEMBL274654	ORANTINIB	3
CHEMBL3137331	DEFACTINIB	3

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Aurora kinase (Aur) family

Most potent curated ligand interactions (35 total), top 25:

Ligand	Action	Affinity	Parameter
barasertib	Inhibition	9.43	pIC50
GSK1070916	Inhibition	9.42	pKi
compound 1 [PMID: 21742770]	Inhibition	8.55	pIC50
AT-9283	Inhibition	8.52	pIC50
tinengotinib	Inhibition	8.48	pIC50
AMG-900	Inhibition	8.4	pIC50
barasertib-hQPA	Inhibition	8.34	pKd
compound 46 [PMID: 16451062]	Inhibition	8.15	pIC50
ilorasertib	Inhibition	8.15	pIC50
ibcasertib	Inhibition	8.05	pIC50
MLN-8054	Inhibition	8.03	pIC50
dubermatinib	Inhibition	7.91	pIC50
JNJ-7706621	Inhibition	7.89	pIC50
compound 25 [PMID: 20855207]	Inhibition	7.89	pIC50
MK-5108	Inhibition	7.85	pIC50
XMD-12	Inhibition	7.74	pIC50
tozasertib	Inhibition	7.74	pKi
SU6656	Inhibition	7.72	pIC50
BX-795	Inhibition	7.51	pIC50
SNS-314	Inhibition	7.51	pIC50
Cdk2 inhibitor IV	Inhibition	7.46	pIC50
NIK inhibitor 12f	Inhibition	7.36	pIC50
compound 38 [PMID: 20817473]	Inhibition	7.35	pIC50
KW-2449	Inhibition	7.32	pIC50
cenisertib	Inhibition	7.27	pIC50

Binding affinities (BindingDB)

546 measured of 842 human assays (857 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[[3-methoxy-1-[3-[[4-(trifluoromethoxy)benzoyl]amino]phenyl]propyl]amino]quinazoline-8-carboxamide	IC50	0.05 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(5-propan-2-yl-1H-pyrazole-3-carbonyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.06 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(4-methoxybenzoyl)amino]phenyl]methylamino]-6-(2-methoxyethoxy)quinazoline-8-carboxamide	IC50	0.06 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(2,2-difluoro-1,3-benzodioxole-5-carbonyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.06 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(5-tert-butyl-1H-pyrazole-3-carbonyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.08 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(4-morpholin-4-ylcyclohexa-1,5-diene-1-carbonyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.08 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(4-chlorobenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.08 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[4-chloro-3-(trifluoromethyl)benzoyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.08 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(2-methylbenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.1 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[4-(dimethylamino)benzoyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.11 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.11 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(2,6-difluoro-4-methoxybenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.11 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(2,4-dichlorobenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.12 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[1-[3-[(4-bromobenzoyl)amino]phenyl]-3-(dimethylamino)propyl]amino]quinazoline-8-carboxamide	IC50	0.12 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(5-propan-2-yl-1H-pyrazole-3-carbonyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.12 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[2-fluoro-4-(trifluoromethyl)benzoyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.12 nM	US-8637532: Amino azaheterocyclic carboxamides
6-hydroxy-4-[[3-[(4-methoxybenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.12 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-1-[3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.13 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(4-ethoxybenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.13 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-(pyridin-2-ylamino)phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.15 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(2,4-difluorobenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.16 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[1-[3-[(4-methoxybenzoyl)amino]phenyl]-3-[methyl(prop-2-enyl)amino]propyl]amino]quinazoline-8-carboxamide	IC50	0.16 nM	US-8637532: Amino azaheterocyclic carboxamides
ethyl 2-[3-[[(8-carbamoylquinazolin-4-yl)amino]methyl]anilino]-1,3-thiazole-5-carboxylate	IC50	0.16 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-(cyclohexanecarbonylamino)phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.16 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[[2-fluoro-5-(trifluoromethyl)phenyl]-hydroxymethyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.17 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(3-methylbenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.17 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(3-chlorobenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.17 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-methoxy-1-[3-[[4-(trifluoromethyl)benzoyl]amino]phenyl]propyl]amino]quinazoline-8-carboxamide	IC50	0.18 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[1-(3-benzamidophenyl)-3-(dimethylamino)propyl]amino]quinazoline-8-carboxamide	IC50	0.18 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methylamino]-6,7-dihydroquinazoline-8-carboxamide	IC50	0.18 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-(1,3-thiazol-2-ylamino)phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.19 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(5-amino-1H-pyrazole-4-carbonyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.19 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(4-chloro-3-fluorobenzoyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.2 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[1-[3-[(3,4-difluorobenzoyl)amino]phenyl]-3-methoxypropyl]amino]quinazoline-8-carboxamide	IC50	0.2 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(5Z)-5-[hydroxy-(4-methoxy-3-methylphenyl)methyl]iminocyclohex-3-en-1-yl]methylamino]quinazoline-8-carboxamide	IC50	0.2 nM	US-8637532: Amino azaheterocyclic carboxamides
6-(4-hydroxybutyl)-4-[[3-[(4-methoxybenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.2 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-3-methoxy-1-[3-[(4-methoxybenzoyl)amino]phenyl]propyl]amino]quinazoline-8-carboxamide	IC50	0.21 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[5-(trifluoromethyl)-1H-pyrazole-3-carbonyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.22 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[5-(aminomethyl)-1,3-thiazol-2-yl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.22 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(4-cyano-2-pyridinyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.22 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[3-(dimethylamino)benzoyl]amino]phenyl]methylamino]-6,7-dihydroquinazoline-8-carboxamide	IC50	0.22 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[4-fluoro-3-[[4-(trifluoromethoxy)benzoyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.22 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[2-(trifluoromethyl)benzoyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.22 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-(2,3-dihydro-1-benzofuran-5-carbonylamino)phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.23 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(5-cyclopropyl-1H-pyrazole-3-carbonyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.23 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-(4,5,6,7-tetrahydro-1H-indazole-3-carbonylamino)phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.24 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.25 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(4-bromocyclohexa-1,5-diene-1-carbonyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.26 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[2-(dimethylamino)-1-[3-[(2-pyrrolidin-1-ylpyridine-4-carbonyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.27 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[(4-methoxybenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.29 nM	US-8637532: Amino azaheterocyclic carboxamides

ChEMBL bioactivities

3167 potent at pChembl≥5 of 3401 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Kd	0.01	nM	CHEMBL4225923
10.92	Kd	0.012	nM	CHEMBL5176837
10.70	Ki	0.02	nM	TAK-901
10.38	IC50	0.042	nM	CHEMBL3680444
10.35	IC50	0.045	nM	CHEMBL3680508
10.34	IC50	0.046	nM	CHEMBL3680447
10.22	IC50	0.06	nM	CHEMBL3680552
10.21	IC50	0.061	nM	CHEMBL3685243
10.05	IC50	0.089	nM	CHEMBL3685277
10.00	Kd	0.1	nM	CHEMBL4227082
9.77	IC50	0.17	nM	CHEMBL3675525
9.74	IC50	0.18	nM	CHEMBL3685262
9.74	IC50	0.18	nM	CHEMBL3680596
9.70	IC50	0.2	nM	CHEMBL3639841
9.68	IC50	0.21	nM	CHEMBL3685245
9.66	IC50	0.22	nM	CHEMBL3685306
9.62	IC50	0.24	nM	CHEMBL3670499
9.60	IC50	0.25	nM	CHEMBL3675441
9.59	IC50	0.26	nM	CHEMBL3680500
9.57	IC50	0.27	nM	CHEMBL3680420
9.54	IC50	0.29	nM	CHEMBL4455202
9.52	IC50	0.3	nM	DEFOSBARASERTIB
9.52	IC50	0.3	nM	CHEMBL3680554
9.52	IC50	0.3	nM	CHEMBL3680403
9.51	IC50	0.31	nM	CHEMBL3685257
9.50	IC50	0.316	nM	CHEMBL4799738
9.49	IC50	0.32	nM	CHEMBL3675501
9.49	IC50	0.326	nM	DEFOSBARASERTIB
9.48	IC50	0.33	nM	CHEMBL3685237
9.47	IC50	0.34	nM	CHEMBL4443125
9.47	IC50	0.336	nM	CHEMBL4784002
9.46	IC50	0.35	nM	CHEMBL3675459
9.46	IC50	0.35	nM	CHEMBL3675446
9.46	IC50	0.35	nM	CHEMBL3670467
9.45	Ki	0.359	nM	DEFOSBARASERTIB
9.45	Ki	0.359	nM	BARASERTIB
9.44	Ki	0.36	nM	BARASERTIB
9.43	Ki	0.37	nM	BARASERTIB
9.43	IC50	0.37	nM	BARASERTIB
9.43	IC50	0.37	nM	DEFOSBARASERTIB
9.43	IC50	0.37	nM	CHEMBL4633715
9.43	Ki	0.37	nM	DEFOSBARASERTIB
9.42	IC50	0.38	nM	CHEMBL3685250
9.42	IC50	0.38	nM	CHEMBL3685252
9.42	IC50	0.38	nM	CHEMBL3680550
9.42	Ki	0.38	nM	GSK-1070916
9.41	IC50	0.39	nM	CHEMBL3680572
9.41	Ki	0.39	nM	GSK-1070916
9.40	IC50	0.4	nM	CHEMBL2380834
9.40	IC50	0.4	nM	CHEMBL3329684

PubChem BioAssay actives

2140 with measured affinity, of 6100 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide	1419647: Inhibition of Aurora B/INCENP (unknown origin) assessed as affinity constant pre-incubated for 1 hr followed by FL-PKAtide substrate and ATP addition	ki	<0.0001	uM
3-[(tert-butylamino)-pyridin-2-ylmethyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine	1390882: Binding affinity to Aurora B (unknown origin) after 45 mins by fluorescence-based thermal stability shift assay	kd	<0.0001	uM
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyridin-2-ylmethyl)-1,2-thiazol-5-amine	1390882: Binding affinity to Aurora B (unknown origin) after 45 mins by fluorescence-based thermal stability shift assay	kd	0.0001	uM
2-[4-[(6,7-dimethoxyquinazolin-4-yl)amino]pyrazol-1-yl]-N-(3-fluorophenyl)acetamide	639899: Inhibition of aurora-B	ic50	0.0002	uM
1-(3-fluorophenyl)-3-[3-[[7-(1-methylpyrazol-4-yl)quinazolin-4-yl]amino]phenyl]urea	1741600: Inhibition of recombinant human full-length His-tagged Aurora B expressed in baculovirus expression system using 5-FAM-LRRASLG-CONH2 as substrate preincubated for 60 mins followed by substrate addition by microfluidic assay	ic50	0.0003	uM
155516420	1515218: Inhibition of Aurora B (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0003	uM
155525257	1515218: Inhibition of Aurora B (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0003	uM
2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide	1186610: Inhibition of Aurora B (unknown origin) using HLRRASLG substrate	ic50	0.0003	uM
1-(3-fluorophenyl)-3-[4-[[7-(1-methylpyrazol-4-yl)quinazolin-4-yl]amino]phenyl]urea	1741600: Inhibition of recombinant human full-length His-tagged Aurora B expressed in baculovirus expression system using 5-FAM-LRRASLG-CONH2 as substrate preincubated for 60 mins followed by substrate addition by microfluidic assay	ic50	0.0003	uM
2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate	1304186: Inhibition of Aurora B (unknown origin)	ic50	0.0004	uM
2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethylphosphonic acid	1662195: Inhibition of Aurora B in human SW620 cells assessed as reduction in histone H3 phosphorylation on Ser10 by Alexafluor-488 goat anti-rabbit antibody/Hoechst staining based array scan method	ic50	0.0004	uM
3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea	1419701: Inhibition of human Aurora B/INCENP pre-incubated for 30 mins before 5-FAM-PKAtide substrate addition and measured after 120 mins	ki	0.0004	uM
4-fluoro-N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]-2-(trifluoromethyl)benzamide	746820: Inhibition of aurora-B (unknown origin)	ic50	0.0004	uM
5-[(Z)-[6-[(2-fluoro-4-methoxybenzoyl)carbamoylamino]-2-oxo-1H-indol-3-ylidene]methyl]-2,4-dimethyl-N-(2-pyrrolidin-1-ylethyl)-1H-pyrrole-3-carboxamide	1186610: Inhibition of Aurora B (unknown origin) using HLRRASLG substrate	ic50	0.0004	uM
2,3-difluoro-N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]benzamide	746820: Inhibition of aurora-B (unknown origin)	ic50	0.0005	uM
1-[3-[5-chloro-4-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]phenyl]-N,N-dimethylmethanamine	473665: Inhibition of human recombinant aurora B/INCENP complex after 120 mins by IMAP fluorescence polarization assay	ic50	0.0005	uM
4-[[4-benzyl-6-[(5-methyl-1,3-thiazol-2-yl)amino]pyrimidin-2-yl]amino]cyclohexan-1-ol	777299: Inhibition of Aurora-B (unknown origin) using 5FAM-PKAtide as substrate after 120 mins	ki	0.0005	uM
2,6-difluoro-N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]benzamide	746820: Inhibition of aurora-B (unknown origin)	ic50	0.0006	uM
1-[4-[5-chloro-4-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]phenyl]-N,N-dimethylmethanamine	473665: Inhibition of human recombinant aurora B/INCENP complex after 120 mins by IMAP fluorescence polarization assay	ic50	0.0006	uM
155540641	1515218: Inhibition of Aurora B (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0007	uM
3,5-difluoro-N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]benzamide	746820: Inhibition of aurora-B (unknown origin)	ic50	0.0007	uM
N-[4-[4-(4-tert-butylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]propanamide	420311: Inhibition of Aurora-B by time dependent kinetic study	ki	0.0008	uM
3,4-difluoro-N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]benzamide	746820: Inhibition of aurora-B (unknown origin)	ic50	0.0008	uM
4-amino-N-[3-[[(4-chlorophenyl)carbamoylamino]methyl]phenyl]pyrrolo[2,1-f][1,2,4]triazine-5-carboxamide	674421: Inhibition of Aurora B kinase by HTRF analysis in presence of 1 mM ATP	ic50	0.0009	uM
N-(3-fluorophenyl)-2-[3-[[7-[3-(2-hydroxyethylamino)propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(3,5-difluorophenyl)-2-[3-[[7-[3-[4-(hydroxymethyl)piperidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(2-methylpropyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(propyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-(4-hydroxypiperidin-1-yl)propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(3-fluorophenyl)-2-[3-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[4-(2-hydroxyethyl)piperidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
2-[4-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]pyrazol-1-yl]-N-(3-fluorophenyl)acetamide	1798666: Aurora B Kinase Inhibition Assay from Article 10.1016/j.bmcl.2008.02.002: “Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.”	ki	0.0010	uM
N-(3-fluorophenyl)-2-[4-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]pyrazol-1-yl]acetamide	1798666: Aurora B Kinase Inhibition Assay from Article 10.1016/j.bmcl.2008.02.002: “Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(propyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(3-fluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(propyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
N-(3-fluorophenyl)-2-[3-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide	1798662: Aurora B Kinase Inhibition Assay from Article 10.1021/jm061335f: “Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.”	ki	0.0010	uM
3-cyclopropyl-1-[5-methyl-2-[(3-methyl-1,2-thiazol-5-yl)amino]pyrimidin-4-yl]azetidin-3-ol	1981409: Inhibition of AURKB (unknown origin) incubated for 45 to 120 mins in presence of ATP by Kinase-Glo luminescent assay	ic50	0.0010	uM
N-[5-[[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinazolin-4-yl]amino]pyrimidin-2-yl]benzamide	353620: Inhibition of aurora B kinase	ic50	0.0010	uM
N-(2,3-difluorophenyl)-2-[4-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]pyrazol-1-yl]acetamide	1798666: Aurora B Kinase Inhibition Assay from Article 10.1016/j.bmcl.2008.02.002: “Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[4-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]pyrazol-1-yl]acetamide	1798666: Aurora B Kinase Inhibition Assay from Article 10.1016/j.bmcl.2008.02.002: “Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.”	ki	0.0010	uM
N-(3-fluorophenyl)-2-[4-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]quinazolin-4-yl]amino]pyrazol-1-yl]acetamide	1798666: Aurora B Kinase Inhibition Assay from Article 10.1016/j.bmcl.2008.02.002: “Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.”	ki	0.0010	uM
N-(2,3-difluorophenyl)-2-[4-[[7-[3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]quinazolin-4-yl]amino]pyrazol-1-yl]acetamide	1798666: Aurora B Kinase Inhibition Assay from Article 10.1016/j.bmcl.2008.02.002: “Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.”	ki	0.0010	uM
N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]benzamide	746820: Inhibition of aurora-B (unknown origin)	ic50	0.0010	uM

CTD chemical–gene interactions

137 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	increases phosphorylation, decreases expression, affects cotreatment, increases abundance, increases expression (+1 more)	10
bisphenol A	affects expression, decreases expression, increases expression	5
Estradiol	increases expression, decreases reaction	5
Cyclosporine	decreases expression	4
(+)-JQ1 compound	decreases expression	3
Benzo(a)pyrene	decreases expression, affects methylation	3
Cisplatin	increases expression, decreases response to substance	3
Doxorubicin	affects response to substance, decreases expression	3
Hydrogen Peroxide	affects localization, decreases reaction, affects cotreatment, decreases expression	3
arsenite	increases expression, decreases reaction, affects binding, increases reaction	2
cobaltous chloride	decreases expression	2
4-(4-(N-benzoylamino)anilino)-6-methoxy-7-(3-(1-morpholino)propoxy)quinazoline	affects localization, affects cotreatment, decreases reaction, increases phosphorylation	2
Fulvestrant	increases expression, affects cotreatment, decreases expression, decreases reaction	2
Arsenic	increases abundance, increases expression, affects cotreatment, decreases expression	2
Cadmium	decreases reaction, increases abundance, increases phosphorylation, increases expression	2
Tobacco Smoke Pollution	decreases expression, increases expression	2
Tretinoin	decreases expression	2
Valproic Acid	decreases expression	2
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression	2
Aflatoxin B1	affects expression, increases expression	2
Cadmium Chloride	decreases reaction, increases abundance, increases phosphorylation, affects expression	2
tert-Butylhydroperoxide	increases expression, decreases expression	2
Particulate Matter	decreases activity, decreases phosphorylation, decreases expression, decreases reaction	2
gamabufotalin	decreases expression	1
mivebresib	decreases expression	1
TAK-243	increases sumoylation	1
chloroacetaldehyde	affects expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	decreases expression	1

ChEMBL screening assays

1227 unique, capped per target: 1199 binding, 22 admet, 6 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1004137	Binding	Inhibition of Aurora B at 1 uM relative to control	Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. — J Med Chem
CHEMBL1963807	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: STK12	PubChem BioAssay data set
CHEMBL3998582	ADMET	Inhibition of N-terminal-GST-tagged recombinant full length human Aurora B expressed in baculovirus infected Sf9 cells at 10 uM using native Swine Myelin Basic Protein as substrate measured after 60 mins by ADP-Glo assay relative to control	Methoxylated 2’-hydroxychalcones as antiparasitic hit compounds. — Eur J Med Chem

Clinical trials (associated diseases)

11 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT03414970	PHASE3	ACTIVE_NOT_RECRUITING	Hypofractionated Radiation Therapy After Mastectomy in Preventing Recurrence in Patients With Stage IIa-IIIa Breast Cancer
NCT00461344	PHASE2	TERMINATED	Docetaxel + Doxorubicin as Neoadjuvant Chemotherapy in Patients With Breast Cancer
NCT07499999	PHASE2	NOT_YET_RECRUITING	Randomized Double-Blind Phase II Trial of Baby Exemestane Versus Baby Tamoxifen in Post-Menopausal Women at High Risk for Breast Cancer
NCT00637364	PHASE1/PHASE2	SUSPENDED	High Intensity Focused Ultrasound Tumor Treatment for Pancreatic Cancer Pain
NCT02779855	PHASE1/PHASE2	COMPLETED	Talimogene Laherparepvec in Combination With Neoadjuvant Chemotherapy in Triple Negative Breast Cancer
NCT01753908	EARLY_PHASE1	COMPLETED	Broccoli Sprout Extract in Treating Patients With Breast Cancer
NCT01796041	EARLY_PHASE1	COMPLETED	Intraoperative Imaging of Breast Cancer With Indocyanine Green
NCT01208974	Not specified	ACTIVE_NOT_RECRUITING	Nipple-Areola Complex (NAC) Irradiation After Nipple-Sparing Mastectomy and Reconstruction
NCT01875198	Not specified	TERMINATED	Oncologic Impact of Splenectomy-omitting Radical Pancreatectomy in Well-selected Left-sided Pancreatic Cancer
NCT03543397	Not specified	UNKNOWN	MRI in Ductal Carcinoma in Situ (DCIS)
NCT03834532	Not specified	COMPLETED	Living Well After Breast Surgery