AURKA

Summary

AURKA (aurora kinase A, HGNC:11393) is a protein-coding gene on chromosome 20q13.2, encoding Aurora kinase A (O14965). Mitotic serine/threonine kinase that contributes to the regulation of cell cycle progression. In precision oncology, AURKA EXPRESSION confers sensitivity to Radiation Therapy + Fluorouracil + Cisplatin in Esophagus Squamous Cell Carcinoma (CIViC Level B); 6 further curated variant–drug associations are listed below. It is a common-essential gene (DepMap: required in 99.4% of cancer cell lines).

The protein encoded by this gene is a cell cycle-regulated kinase that appears to be involved in microtubule formation and/or stabilization at the spindle pole during chromosome segregation. The encoded protein is found at the centrosome in interphase cells and at the spindle poles in mitosis. This gene may play a role in tumor development and progression. A processed pseudogene of this gene has been found on chromosome 1, and an unprocessed pseudogene has been found on chromosome 10. Multiple transcript variants encoding the same protein have been found for this gene.

Source: NCBI Gene 6790 — RefSeq curated summary.

At a glance

• Gene–disease (curated): intellectual disability (Limited, GenCC) — +1 more curated relationship
• GWAS associations: 4
• Clinical variants (ClinVar): 55 total — 1 pathogenic, 1 likely-pathogenic
• Phenotypes (HPO): 8
• Druggable target: yes — 65 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 7 curated variant–drug associations
• Cancer dependency (DepMap): dependent in 99.4% of screened cell lines (common-essential)
• MANE Select transcript: NM_198437

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11393
Approved symbol	AURKA
Name	aurora kinase A
Location	20q13.2
Locus type	gene with protein product
Status	Approved
Aliases	BTAK, AurA, STK7, ARK1, PPP1R47, AIK
Ensembl gene	ENSG00000087586
Ensembl biotype	protein_coding
OMIM	603072
Entrez	6790

Gene structure

Transcript identifiers

Ensembl transcripts: 51 — 51 protein_coding

ENST00000312783, ENST00000347343, ENST00000371356, ENST00000395907, ENST00000395911, ENST00000395913, ENST00000395914, ENST00000395915, ENST00000420474, ENST00000422322, ENST00000441357, ENST00000451915, ENST00000456249, ENST00000892432, ENST00000892433, ENST00000892434, ENST00000892435, ENST00000892436, ENST00000892437, ENST00000930726, ENST00000930727, ENST00000930728, ENST00000930729, ENST00000930730, ENST00000930731, ENST00000930732, ENST00000930733, ENST00000930734, ENST00000930735, ENST00000930736, ENST00000930737, ENST00000930738, ENST00000930739, ENST00000930740, ENST00000930741, ENST00000930742, ENST00000930743, ENST00000930744, ENST00000930745, ENST00000930746, ENST00000930747, ENST00000930748, ENST00000930749, ENST00000930750, ENST00000930751, ENST00000930752, ENST00000930753, ENST00000930754, ENST00000966821, ENST00000966822, ENST00000966823

RefSeq mRNA: 13 — MANE Select: NM_198437 NM_001323303, NM_001323304, NM_001323305, NM_001424417, NM_001424418, NM_001424419, NM_001424420, NM_003600, NM_198433, NM_198434, NM_198435, NM_198436, NM_198437

CCDS: CCDS13451

Canonical transcript exons

ENST00000395915 — 9 exons

Exon	Start	End
ENSE00000512389	56381433	56381571
ENSE00000512391	56370485	56370659
ENSE00000662874	56373408	56373556
ENSE00000845695	56388156	56388202
ENSE00000991660	56384270	56384324
ENSE00001257584	56369390	56370340
ENSE00001270104	56392168	56392215
ENSE00003789159	56386257	56386533
ENSE00003790958	56382985	56383176

Expression profiles

Bgee: expression breadth ubiquitous, 236 present calls, max score 99.96.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 25.5609 / max 443.1959, expressed in 1614 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
188084	25.3841	1608
188083	0.1767	61

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
oocyte	CL:0000023	99.96	gold quality
secondary oocyte	CL:0000655	99.94	gold quality
ventricular zone	UBERON:0003053	94.78	gold quality
endometrium epithelium	UBERON:0004811	94.39	gold quality
sperm	CL:0000019	93.44	gold quality
adrenal tissue	UBERON:0018303	92.29	gold quality
male germ cell	CL:0000015	91.84	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	90.07	gold quality
trabecular bone tissue	UBERON:0002483	90.02	gold quality
embryo	UBERON:0000922	89.68	gold quality
ganglionic eminence	UBERON:0004023	87.97	gold quality
amniotic fluid	UBERON:0000173	87.07	gold quality
esophagus squamous epithelium	UBERON:0006920	86.40	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	86.26	gold quality
testis	UBERON:0000473	85.66	gold quality
bone element	UBERON:0001474	85.24	gold quality
left testis	UBERON:0004533	85.23	gold quality
mucosa of transverse colon	UBERON:0004991	85.11	gold quality
bone marrow	UBERON:0002371	84.75	gold quality
right testis	UBERON:0004534	84.72	gold quality
squamous epithelium	UBERON:0006914	84.11	gold quality
epithelium of esophagus	UBERON:0001976	84.06	gold quality
rectum	UBERON:0001052	83.65	gold quality
cervix squamous epithelium	UBERON:0006922	82.32	silver quality
gingival epithelium	UBERON:0001949	82.28	gold quality
duodenum	UBERON:0002114	82.25	gold quality
endothelial cell	CL:0000115	81.45	gold quality
stromal cell of endometrium	CL:0002255	81.42	gold quality
vermiform appendix	UBERON:0001154	80.59	gold quality
thymus	UBERON:0002370	80.04	gold quality

Single-cell (SCXA)

Detected in 7 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-GEOD-99795	yes	472.37
E-MTAB-8559	yes	436.39
E-MTAB-7052	yes	306.43
E-ANND-3	yes	3.43
E-MTAB-6142	no	1150.58
E-MTAB-6911	no	453.43
E-MTAB-9689	no	240.08

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CDR2, E2F1, E2F3, ESR1, EWSR1, FLI1, GABPA, GATA3, HIF1A, ID1, MED1, MYC, NFYA, OLIG2, OTX2, SRSF1, SRSF2, STAT5A, STAT5B, TBP, TP53

miRNA regulators (miRDB)

50 targeting AURKA, 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-8485	100.00	77.57	4731
HSA-MIR-12118	100.00	65.88	1270
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4715-3P	99.98	66.03	670
HSA-MIR-6891-5P	99.98	66.53	1372
HSA-MIR-3173-3P	99.98	66.49	1217
HSA-MIR-32-5P	99.98	75.21	1964
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-367-3P	99.98	74.83	1819
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-329-3P	99.91	66.56	1234
HSA-MIR-362-3P	99.91	66.38	1267
HSA-MIR-506-3P	99.89	73.55	3057
HSA-MIR-3941	99.86	70.54	2735
HSA-MIR-1321	99.84	65.30	1811
HSA-MIR-4739	99.84	65.25	1832
HSA-MIR-4756-5P	99.84	64.98	1809
HSA-MIR-4307	99.82	70.45	3374
HSA-MIR-448	99.79	72.37	2103
HSA-MIR-3680-3P	99.75	72.51	3095
HSA-MIR-561-3P	99.64	70.90	3647
HSA-MIR-578	99.46	68.36	1787
HSA-MIR-140-5P	99.44	67.20	792
HSA-MIR-4777-5P	99.33	67.53	1148
HSA-MIR-8077	99.17	66.67	862
HSA-MIR-4326	98.97	67.63	962

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 99.4% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 40)

• Cell-cycle-dependent regulation of human aurora A transcription is mediated by periodic repression of E4TF1 (PMID:11790771)
• overexpression shows tetraploidization as a mjor route to centrosome amplification in p53-/- cells (PMID:11847097)
• Aurora-A binds to TPX2, a prominent component of the spindle apparatus (PMID:12177045)
• The suppression of STK15 oncogenic activity by p53 might be explained by the finding that p53 inhibited STK15 kinase activity via direct interaction with the latter’s Aurora box. This revealed a novel mechanism for the tumor suppressor function of p53. (PMID:12198151)
• crystal structure of Aurora-2 kinase in complex with adenosine (PMID:12237287)
• Results describe the identification of a novel negative regulator of Aurora-A, named AIP (Aurora-A kinase Interacting Protein). (PMID:12244051)
• role in phosphorylating and associating with MBD3 (PMID:12354758)
• elevated Aurora-A expression causes resistance to apoptosis in human cancer cell line (PMID:12559175)
• results show that STK15 is overexpressed in pancreatic tumors and carcinoma cell lines and suggest that overexpression of STK15 may play a role in pancreatic carcinogenesis (PMID:12631597)
• BTAK may play a critical role in development of ovarian cancer (PMID:12684414)
• Overexpression of STK15 gene in laryngeal carcinoma was discovered the first time, it may caused chromosomal instability through abnormal centrosome, therefore having some effect during the occurrence and development of laryngeal carcinoma. (PMID:12693093)
• likely prognostic indicator for patients with breast tumors (PMID:12833450)
• a candidate skin tumor susceptibility gene (PMID:12881723)
• amplification of the STK15 gene may be a non-random genetic alteration in human gliomas playing a role in the genetic pathways of tumorigenesis (PMID:12883693)
• Aurora A protein kinase has a role in G2/M progression [introduction] (PMID:13678575)
• phosphorylation of CENP-A on Ser-7 by Aurora-A in prophase is essential for kinetochore function. (PMID:14667408)
• STK15 expression associated with nuclear grade in breast carcinoma (PMID:14692019)
• induces telomerase activity and hTERT by up-regulation of c-Myc (PMID:14744757)
• overexpressed frequently in hepatocellular carcinoma and correlated with high grade and high stage (PMID:15041727)
• immunohistochemistry of tissues taken directly from patients demonstrated an overexpression of Aurora-2 in 26 of 28 pancreatic cancers compared with 18 normal pancreas samples (PMID:15078988)
• STK15 polymorphism is a genetic susceptibility factor for the occurrence and aggression of esophageal squamous cell carcinoma. (PMID:15087379)
• Phosphorylation of CDC25B by AURA at the centrosome contributes to the G2-M transition. (PMID:15128871)
• Aurora-A induces phosphorylation of Lats2 and this phosphorylation plays a role of the centrosomal localization of Lats2 (PMID:15147269)
• protein phosphatase inhibitor-2 is a bifunctional signaling protein with separate domains to inhibit PP1 and directly stimulate Aurora-A kinase (PMID:15173575)
• Taken together, our study suggests that Plk3 and Aurora A kinases may lie in the same regulatory pathway and that Plk3 and Aurora A as well as BubR1 may play an important role in polyploidization and megakaryocytic differentiation. (PMID:15190214)
• STK15 may represent a low penetrance type breast cancer susceptibility gene. (PMID:15271853)
• Aurora-A may have a role in differentiated type gastric carcinogenesis (PMID:15289843)
• phosphorylation of p53 at Ser-215 by Aurora-A is a major mechanism to inactivate p53 (PMID:15469940)
• Aurora A may have a role in ESCC occurrence and progression (PMID:15534106)
• analysis of sequences required for human Aurora-A kinase destruction (PMID:15536123)
• Aurora-A gene amplification and overexpression play a role in human carcinogenesis, largely due to the effect of Aurora-A on oncogenic cell growth, rather than a loss of maintenance of centrosomal or chromosomal integrity (PMID:15592510)
• Breast cancer development is driven by genomic instability associated with variant Aurora-A (PMID:15688402)
• PML3 has a direct role in the control of centrosome duplication through suppression of Aurora A activation to prevent centrosome reduplication (PMID:15749021)
• Over-expression of Aurora-A is present in some normal and the majority of high-grade prostatic intraepithelial neoplasia lesions indicating that this may be an early event that leads to the genetic instability seen in prostate carcinogenesis (PMID:15754349)
• STK15 T+91A variant is a low penetrance cancer susceptibility allele affecting multiple cancer types. (PMID:15802297)
• overexpression of STK15 significantly correlates with nude mice tumorigenicity and chromosomal aneuploidy in human ovarian cancer cells grown in vitro (PMID:15839305)
• AURKA amplification contributes to pancreatic carcinogenesis by increasing chromosome instability and centrosome abnormality. (PMID:15860351)
• Amplification and overexpression of AURKA is a common and significant event during immortalization of ovarian epithelial cells. (PMID:15880741)
• Data indicate that the highly increased level of STK15 protein in breast cancer cell line MCF7 cannot be explained by gene amplification alone. (PMID:15944763)
• Aurora-A phosphorylates HURP in vitro and in vivo. (PMID:15987997)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	aurka	ENSDARG00000012485
mus_musculus	Aurka	ENSMUSG00000027496
rattus_norvegicus	Aurka	ENSRNOG00000004479
drosophila_melanogaster	aurA	FBGN0000147

Paralogs (2): AURKC (ENSG00000105146), AURKB (ENSG00000178999)

Protein

Protein identifiers

Aurora kinase A — O14965 (reviewed: O14965)

Alternative names: Aurora 2, Aurora/IPL1-related kinase 1, Breast tumor-amplified kinase, Ipl1- and aurora-related kinase 1, Serine/threonine-protein kinase 15, Serine/threonine-protein kinase 6, Serine/threonine-protein kinase Ayk1, Serine/threonine-protein kinase aurora-A

All UniProt accessions (7): O14965, A3KFJ0, A3KFJ1, A3KFJ2, Q5QPD1, Q5QPD2, Q5QPD4

UniProt curated annotations — full annotation on UniProt →

Function. Mitotic serine/threonine kinase that contributes to the regulation of cell cycle progression. Associates with the centrosome and the spindle microtubules during mitosis and plays a critical role in various mitotic events including the establishment of mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. Required for normal spindle positioning during mitosis and for the localization of NUMA1 and DCTN1 to the cell cortex during metaphase. Required for initial activation of CDK1 at centrosomes. Phosphorylates numerous target proteins, including ARHGEF2, BORA, BRCA1, CDC25B, DLGP5, HDAC6, KIF2A, LATS2, NDEL1, PARD3, PPP1R2, PLK1, RASSF1, TACC3, p53/TP53 and TPX2. Phosphorylates MCRS1 which is required for MCRS1-mediated kinetochore fiber assembly and mitotic progression. Regulates KIF2A tubulin depolymerase activity. Important for microtubule formation and/or stabilization. Required for normal axon formation. Plays a role in microtubule remodeling during neurite extension. Also acts as a key regulatory component of the p53/TP53 pathway, and particularly the checkpoint-response pathways critical for oncogenic transformation of cells, by phosphorylating and destabilizing p53/TP53. Phosphorylates its own inhibitors, the protein phosphatase type 1 (PP1) isoforms, to inhibit their activity. Inhibits cilia outgrowth. Required for cilia disassembly via phosphorylation of HDAC6 and subsequent deacetylation of alpha-tubulin. Regulates protein levels of the anti-apoptosis protein BIRC5 by suppressing the expression of the SCF(FBXL7) E3 ubiquitin-protein ligase substrate adapter FBXL7 through the phosphorylation of the transcription factor FOXP1.

Subunit / interactions. Part of a complex composed of NEDD9, AURKA and CTTN; within the complex NEDD9 acts as a scaffold protein and is required for complex formation. Identified in a complex with AUNIP and NIN. Interacts with FBXL7. Interacts with CPEB1, JTB, TACC1, TPX2, PPP2CA, as well as with the protein phosphatase type 1 (PP1) isoforms PPP1CA, PPP1CB and PPP1CC. Also interacts with its substrates ARHGEF2, BORA, KIF2A, PARD3, and p53/TP53. Interaction with BORA promotes phosphorylation of PLK1. Interacts with CIMAP3. Interacts with GADD45A, competing with its oligomerization. Interacts (via C-terminus) with AUNIP (via C-terminus). Interacts with FRY; this interaction facilitates AURKA-mediated PLK1 phosphorylation. Interacts with SIRT2. Interacts with MYCN; interaction is phospho-independent and triggers AURKA activation; AURKA competes with FBXW7 for binding to unphosphorylated MYCN but not for binding to phosphorylated MYCN. Interacts with HNRNPU. Interacts with AAAS. Interacts with KLHL18 and CUL3. Interacts with FOXP1. Interacts with HDAC6; AURKA-mediated phosphorylation of HDAC6 promotes deacetylation of alpha-tubulin.

Subcellular location. Cytoplasm. Cytoskeleton. Microtubule organizing center. Centrosome. Spindle pole. Centriole. Cell projection. Neuron projection. Cilium. Cilium basal body. Basolateral cell membrane.

Tissue specificity. Highly expressed in testis and weakly in skeletal muscle, thymus and spleen. Also highly expressed in colon, ovarian, prostate, neuroblastoma, breast and cervical cancer cell lines.

Post-translational modifications. Activated by phosphorylation at Thr-288; this brings about a change in the conformation of the activation segment. Phosphorylation at Thr-288 varies during the cell cycle and is highest during M phase. Autophosphorylated at Thr-288 upon TPX2 binding. Thr-288 can be phosphorylated by several kinases, including PAK and PKA. Protein phosphatase type 1 (PP1) binds AURKA and inhibits its activity by dephosphorylating Thr-288 during mitosis. Phosphorylation at Ser-342 decreases the kinase activity. PPP2CA controls degradation by dephosphorylating Ser-51 at the end of mitosis. Ubiquitinated by the E3 ubiquitin-protein ligase complex SCF(FBXL7) during mitosis, leading to its degradation by the proteasome. Ubiquitinated by CHFR, leading to its degradation by the proteasome. Ubiquitinated by the anaphase-promoting complex (APC), leading to its degradation by the proteasome. Ubiquitinated by the CUL3-KLHL18 ligase leading to its activation at the centrosome which is required for initiating mitotic entry. Ubiquitination mediated by CUL3-KLHL18 ligase does not lead to its degradation by the proteasome.

Activity regulation. Activation of CDK1, appears to be an upstream event of AURKA activation. Phosphatase inhibitor-2 (PPP1R2) and TPX2 act also as activators. Inactivated by the G2 checkpoint. Inhibited by GADD45A and p53/TP53, and through dephosphorylation by protein phosphatase type 1 (PP1). MLN8054 is also a potent and selective inhibitor. Activated during the early phase of cilia disassembly in the presence of CIMAP3. Inhibited by the small molecule inhibitor VX-680.

Induction. Expression is cell-cycle regulated, low in G1/S, accumulates during G2/M, and decreases rapidly after.

Miscellaneous. Centrosome amplification can occur when the cycles are uncoupled, and this amplification is associated with cancer and with an increase in the levels of chromosomal instability.

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

RefSeq proteins (13): NP_001310232, NP_001310233, NP_001310234, NP_001411346, NP_001411347, NP_001411348, NP_001411349, NP_003591, NP_940835, NP_940836, NP_940837, NP_940838, NP_940839* (*=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
IPR030611	AURKA	Domain
IPR030616	Aur-like	Family

Pfam: PF00069

Enzyme classification (BRENDA):

• EC 2.7.11.1 — non-specific serine/threonine protein kinase (BRENDA: 71 organisms, 682 substrates, 228 inhibitors, 23 Km, 6 kcat entries)

Substrate kinetics (BRENDA)

8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0007–0.64	11
KKRAARATSNVFA	0.013–0.045	3
PAH1 PHOSPHATIDATE PHOSPHATASE	0.0002	2
RRRLSSLRA	0.0036–0.0037	2
GTP	0.46	1
KKRAARASSNVFA	0.02	1
LYS-LYS-PHE-ASN-ARG-THR-LEU-SER-VAL-ALA	0.0093	1
MYELIN BASIC PROTEIN	0.145	1

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 (73 total): helix 18, mutagenesis site 14, strand 13, sequence variant 8, binding site 5, modified residue 5, compositionally biased region 3, region of interest 2, chain 1, domain 1, cross-link 1, turn 1, active site 1

Structure

Experimental structures (PDB)

193 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
6VPM	X-RAY DIFFRACTION	1.58
5L8L	X-RAY DIFFRACTION	1.67
5L8J	X-RAY DIFFRACTION	1.68
5ORL	X-RAY DIFFRACTION	1.69
5G1X	X-RAY DIFFRACTION	1.72
6C2T	X-RAY DIFFRACTION	1.73
5OS0	X-RAY DIFFRACTION	1.74
5OS5	X-RAY DIFFRACTION	1.74
5L8K	X-RAY DIFFRACTION	1.79
9BZG	X-RAY DIFFRACTION	1.8
5OS3	X-RAY DIFFRACTION	1.81
9BZL	X-RAY DIFFRACTION	1.81
4J8M	X-RAY DIFFRACTION	1.85
6VPL	X-RAY DIFFRACTION	1.86
5ORV	X-RAY DIFFRACTION	1.88
5ORX	X-RAY DIFFRACTION	1.88
5OS4	X-RAY DIFFRACTION	1.88
5OSF	X-RAY DIFFRACTION	1.89
1MQ4	X-RAY DIFFRACTION	1.9
3FDN	X-RAY DIFFRACTION	1.9
4UYN	X-RAY DIFFRACTION	1.9
5OS1	X-RAY DIFFRACTION	1.9
5OSE	X-RAY DIFFRACTION	1.9
7ZTL	X-RAY DIFFRACTION	1.9
5ORZ	X-RAY DIFFRACTION	1.92
5OS2	X-RAY DIFFRACTION	1.92
8C1F	X-RAY DIFFRACTION	1.92
8C14	X-RAY DIFFRACTION	1.93
6R4A	X-RAY DIFFRACTION	1.94
5DNR	X-RAY DIFFRACTION	1.95

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O14965-F1	76.07	0.57

Antibody-complex structures (SAbDab): 3 — 5L8J, 5L8K, 5L8L

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): 256 (proton acceptor)

Ligand- & substrate-binding residues (5): 211–213; 260–261; 274; 143; 162

Post-translational modifications (6): 41, 51, 287, 288, 342, 258

Mutagenesis-validated functional residues (14):

Position	Phenotype
162	loss of kinase activity.
165	decreases the interaction with phosphatase type 1 isoforms.
198	reduces interaction with tpx2. reduces kinase activity tenfold. promotes interaction with the aurkb binding partners inc
205	reduces ubiquitination and proteasomal degradation.
274	abolishes cilia disassembly and kinase activity.
287	no direct effect on catalytic activity.
287	enhances interaction with tpx2.
288	reduces cilia disassembly and kinase activity.
288	mimics phosphorylation state and increases kinase activity.
290	enhances stability; when associated with a-393.
334	reduces binding to mycn.
335	reduces binding to mycn.
346	decreases the interaction with phosphatase type 1 isoforms.
393	enhances stability; when associated with a-290.

Function

Pathways and Gene Ontology

Reactome pathways

24 pathways

ID	Pathway
R-HSA-174178	APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1
R-HSA-2565942	Regulation of PLK1 Activity at G2/M Transition
R-HSA-4615885	SUMOylation of DNA replication proteins
R-HSA-6804114	TP53 Regulates Transcription of Genes Involved in G2 Cell Cycle Arrest
R-HSA-6804756	Regulation of TP53 Activity through Phosphorylation
R-HSA-8854050	FBXL7 down-regulates AURKA during mitotic entry and in early mitosis
R-HSA-8854518	AURKA Activation by TPX2
R-HSA-8854521	Interaction between PHLDA1 and AURKA
R-HSA-1640170	Cell Cycle
R-HSA-174143	APC/C-mediated degradation of cell cycle proteins
R-HSA-212436	Generic Transcription Pathway
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-453274	Mitotic G2-G2/M phases
R-HSA-453276	Regulation of mitotic cell cycle
R-HSA-5633007	Regulation of TP53 Activity
R-HSA-597592	Post-translational protein modification
R-HSA-6791312	TP53 Regulates Transcription of Cell Cycle Genes
R-HSA-69275	G2/M Transition
R-HSA-69278	Cell Cycle, Mitotic
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)

MSigDB gene sets: 701 (showing top): BROWNE_HCMV_INFECTION_30MIN_DN, GOBP_MEIOTIC_CHROMOSOME_SEGREGATION, GOBP_POSITIVE_REGULATION_OF_MITOTIC_NUCLEAR_DIVISION, WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, GOBP_POSITIVE_REGULATION_OF_REPRODUCTIVE_PROCESS, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GOBP_HEPATICOBILIARY_SYSTEM_DEVELOPMENT, GOBP_PROTEIN_LOCALIZATION_TO_CYTOSKELETON, HORIUCHI_WTAP_TARGETS_DN, REACTOME_APC_C_CDH1_MEDIATED_DEGRADATION_OF_CDC20_AND_OTHER_APC_C_CDH1_TARGETED_PROTEINS_IN_LATE_MITOSIS_EARLY_G1, GOBP_REGULATION_OF_CELL_MATURATION, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, GOBP_REGULATION_OF_PROTEASOMAL_UBIQUITIN_DEPENDENT_PROTEIN_CATABOLIC_PROCESS, KANG_DOXORUBICIN_RESISTANCE_UP, GOBP_REGULATION_OF_PROTEIN_BINDING

GO Biological Process (41): G2/M transition of mitotic cell cycle (GO:0000086), mitotic cell cycle (GO:0000278), protein phosphorylation (GO:0006468), apoptotic process (GO:0006915), spindle organization (GO:0007051), mitotic spindle organization (GO:0007052), spindle assembly involved in female meiosis I (GO:0007057), mitotic centrosome separation (GO:0007100), response to wounding (GO:0009611), anterior/posterior axis specification (GO:0009948), regulation of G2/M transition of mitotic cell cycle (GO:0010389), negative regulation of gene expression (GO:0010629), peptidyl-serine phosphorylation (GO:0018105), regulation of protein stability (GO:0031647), negative regulation of protein binding (GO:0032091), positive regulation of proteasomal ubiquitin-dependent protein catabolic process (GO:0032436), regulation of cytokinesis (GO:0032465), negative regulation of apoptotic process (GO:0043066), proteasome-mediated ubiquitin-dependent protein catabolic process (GO:0043161), positive regulation of mitotic nuclear division (GO:0045840), positive regulation of mitotic cell cycle (GO:0045931), regulation of centrosome cycle (GO:0046605), protein autophosphorylation (GO:0046777), cell division (GO:0051301), centrosome localization (GO:0051642), cilium disassembly (GO:0061523), protein localization to centrosome (GO:0071539), positive regulation of mitochondrial fission (GO:0090141), liver regeneration (GO:0097421), positive regulation of oocyte maturation (GO:1900195), regulation of signal transduction by p53 class mediator (GO:1901796), neuron projection extension (GO:1990138), meiotic spindle organization (GO:0000212), microtubule cytoskeleton organization (GO:0000226), chromatin remodeling (GO:0006338), centrosome cycle (GO:0007098), cell projection organization (GO:0030030), regulation of microtubule-based process (GO:0032886), cell cycle G2/M phase transition (GO:0044839), meiotic cell cycle (GO:0051321)

GO Molecular Function (14): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), protein serine/threonine/tyrosine kinase activity (GO:0004712), ATP binding (GO:0005524), protein kinase binding (GO:0019901), ubiquitin protein ligase binding (GO:0031625), histone H3S10 kinase activity (GO:0035175), protein heterodimerization activity (GO:0046982), protein serine kinase activity (GO:0106310), molecular function activator activity (GO:0140677), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (34): kinetochore (GO:0000776), spindle pole (GO:0000922), nucleus (GO:0005634), nucleoplasm (GO:0005654), centrosome (GO:0005813), centriole (GO:0005814), spindle (GO:0005819), cytosol (GO:0005829), microtubule (GO:0005874), postsynaptic density (GO:0014069), microtubule cytoskeleton (GO:0015630), basolateral plasma membrane (GO:0016323), midbody (GO:0030496), spindle pole centrosome (GO:0031616), chromosome passenger complex (GO:0032133), ciliary basal body (GO:0036064), germinal vesicle (GO:0042585), axon hillock (GO:0043203), pronucleus (GO:0045120), perinuclear region of cytoplasm (GO:0048471), spindle midzone (GO:0051233), mitotic spindle (GO:0072686), meiotic spindle (GO:0072687), mitotic spindle pole (GO:0097431), glutamatergic synapse (GO:0098978), cytoplasm (GO:0005737), microtubule organizing center (GO:0005815), cytoskeleton (GO:0005856), spindle microtubule (GO:0005876), plasma membrane (GO:0005886), cilium (GO:0005929), membrane (GO:0016020), cell projection (GO:0042995), neuron projection (GO:0043005)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
G2/M Transition	4
Cell Cycle, Mitotic	2
Transcriptional Regulation by TP53	2
APC/C-mediated degradation of cell cycle proteins	1
SUMO E3 ligases SUMOylate target proteins	1
TP53 Regulates Transcription of Cell Cycle Genes	1
Regulation of TP53 Activity	1
Regulation of mitotic cell cycle	1
RNA Polymerase II Transcription	1
Post-translational protein modification	1
SUMOylation	1
Generic Transcription Pathway	1
Metabolism of proteins	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	6
mitotic nuclear division	3
protein kinase activity	3
intracellular membraneless organelle	3
microtubule organizing center	3
mitotic cell cycle	2
microtubule cytoskeleton	2
cytoplasm	2
mitotic cell cycle phase transition	1
cell cycle G2/M phase transition	1
cell cycle	1
phosphorylation	1
protein modification process	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	1
microtubule cytoskeleton organization	1
cell cycle process	1
spindle organization	1
microtubule cytoskeleton organization involved in mitosis	1
spindle assembly involved in female meiosis	1
female meiosis I	1
centrosome separation	1
mitotic cell cycle process	1
response to stress	1
axis specification	1
anterior/posterior pattern specification	1
G2/M transition of mitotic cell cycle	1
regulation of mitotic cell cycle phase transition	1
regulation of cell cycle G2/M phase transition	1
gene expression	1
regulation of gene expression	1
negative regulation of macromolecule biosynthetic process	1
protein phosphorylation	1
peptidyl-serine modification	1
regulation of biological quality	1
protein binding	1
regulation of protein binding	1
negative regulation of binding	1
regulation of proteasomal ubiquitin-dependent protein catabolic process	1

Protein interactions and networks

STRING

4938 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
AURKA	TPX2	Q9ULW0	995
AURKA	NEDD9	Q14511	987
AURKA	TP53	P04637	978
AURKA	CKAP5	Q14008	959
AURKA	TACC3	Q9Y6A5	939
AURKA	MYCN	P04198	919
AURKA	MYC	P01106	894
AURKA	BRCA1	P38398	893
AURKA	HDAC6	Q9UBN7	892
AURKA	BORA	Q6PGQ7	890
AURKA	BIRC5	O15392	866
AURKA	INCENP	Q9NQS7	856
AURKA	CCNB1	P14635	846
AURKA	PLK1	P53350	841
AURKA	KIF2C	Q99661	834

IntAct

260 interactions, top by confidence:

A	B	Type	Score
TPX2	AURKA	psi-mi:“MI:0407”(direct interaction)	0.890
AURKA	TPX2	psi-mi:“MI:0915”(physical association)	0.890
TPX2	AURKA	psi-mi:“MI:0914”(association)	0.890
MYCN	AURKA	psi-mi:“MI:0914”(association)	0.830
MYCN	AURKA	psi-mi:“MI:2364”(proximity)	0.830
AURKA	MYCN	psi-mi:“MI:0915”(physical association)	0.830
MYCN	AURKA	psi-mi:“MI:0915”(physical association)	0.830
AURKA	EGFR	psi-mi:“MI:2364”(proximity)	0.670
AURKA	BORA	psi-mi:“MI:0915”(physical association)	0.660
BORA	AURKA	psi-mi:“MI:0217”(phosphorylation reaction)	0.660
PAK5	AURKA	psi-mi:“MI:0914”(association)	0.640
TP73	AURKA	psi-mi:“MI:0217”(phosphorylation reaction)	0.630
TP73	AURKA	psi-mi:“MI:0915”(physical association)	0.630
TP73	AURKA	psi-mi:“MI:0914”(association)	0.630
AURKA	TP73	psi-mi:“MI:0915”(physical association)	0.630

BioGRID (1178): AURKA (Reconstituted Complex), AURKA (Affinity Capture-MS), AURKA (Affinity Capture-Western), AURKA (Biochemical Activity), AURKA (Reconstituted Complex), DHX9 (Affinity Capture-MS), AURKA (Affinity Capture-MS), AURKA (Affinity Capture-MS), AURKA (Affinity Capture-MS), AURKA (Affinity Capture-MS), CEP192 (Affinity Capture-MS), PPP6R2 (Affinity Capture-MS), AMER1 (Affinity Capture-MS), REL (Affinity Capture-MS), DICER1 (Affinity Capture-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

138 interactions.

A	Effect	B	Mechanism
PPP1CA	down-regulates	AURKA	dephosphorylation
AURKA	“up-regulates activity”	TP53	phosphorylation
AURKA	up-regulates	BRCA1	phosphorylation
AURKA	up-regulates	LATS2	phosphorylation
AURKA	down-regulates	TP53	phosphorylation
AURKA	up-regulates	CDC25B	phosphorylation
BORA	up-regulates	AURKA	binding
AURKA	down-regulates	RASSF1	phosphorylation
AURKA	up-regulates	MAP9	phosphorylation
anthra[1,9-cd]pyrazol-6(2H)-one	down-regulates	AURKA	“chemical inhibition”
AURKA	up-regulates	CETN2	phosphorylation
AURKA	unknown	WWC1	phosphorylation
AURKA	up-regulates	FADD	phosphorylation
AURKA	up-regulates	PLK1	phosphorylation
AURKA	“down-regulates activity”	FAF1	phosphorylation
AURKA	up-regulates	MAPRE3	phosphorylation
AURKA	up-regulates	PARD3	phosphorylation
“AMG 900”	down-regulates	AURKA	“chemical inhibition”
AT9283	down-regulates	AURKA	“chemical inhibition”
N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide	down-regulates	AURKA	“chemical inhibition”
CCT129202	down-regulates	AURKA	“chemical inhibition”
CCT137690	down-regulates	AURKA	“chemical inhibition”
CYC-116	down-regulates	AURKA	“chemical inhibition”
N-[5-[(2R)-2-methoxy-1-oxo-2-phenylethyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methyl-1-piperazinyl)benzamide	down-regulates	AURKA	“chemical inhibition”
ENMD-2076	down-regulates	AURKA	“chemical inhibition”
4-[[5-amino-1-[(2,6-difluorophenyl)-oxomethyl]-1,2,4-triazol-3-yl]amino]benzenesulfonamide	down-regulates	AURKA	“chemical inhibition”
“4-(3-chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-1-cyclohexanecarboxylic acid”	down-regulates	AURKA	“chemical inhibition”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 140 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
MAP3K8 (TPL2)-dependent MAPK1/3 activation	5	39.6×	3e-05
RIP-mediated NFkB activation via ZBP1	5	37.3×	3e-05
Activation of NF-kappaB in B cells	6	13.1×	4e-04
TP53 Regulates Transcription of DNA Repair Genes	6	12.1×	4e-04
SUMO E3 ligases SUMOylate target proteins	6	11.9×	4e-04
PKR-mediated signaling	7	11.0×	3e-04
Amplification of signal from the kinetochores	5	10.9×	2e-03
SUMOylation	6	10.9×	6e-04

GO biological processes:

GO term	Partners	Fold	FDR
mitotic spindle assembly	8	22.7×	3e-06
mitotic spindle organization	8	18.0×	9e-06
positive regulation of miRNA transcription	7	16.8×	6e-05
canonical NF-kappaB signal transduction	5	15.1×	2e-03
mitotic cytokinesis	5	10.7×	7e-03
mitotic cell cycle	7	7.7×	3e-03
protein phosphorylation	11	6.2×	3e-04
cell division	11	4.2×	5e-03

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	1
Uncertain significance	29
Likely benign	5
Benign	4

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
152492	GRCh38/hg38 20q13.2-13.32(chr20:54594888-58190583)x1	Pathogenic
800338	NM_198437.3(AURKA):c.1038C>A (p.Phe346Leu)	Likely pathogenic

SpliceAI

1826 predictions. Top by Δscore:

Variant	Effect	Δscore
20:56381426:CACTT:C	donor_loss	1.0000
20:56381427:ACTT:A	donor_loss	1.0000
20:56381428:CT:C	donor_loss	1.0000
20:56381429:T:TA	donor_loss	1.0000
20:56381430:TACAG:T	donor_loss	1.0000
20:56381431:A:AC	donor_gain	1.0000
20:56381431:A:T	donor_loss	1.0000
20:56381432:C:CT	donor_gain	1.0000
20:56381432:CA:C	donor_gain	1.0000
20:56384268:A:AC	donor_gain	1.0000
20:56384269:C:CC	donor_gain	1.0000
20:56388151:TTTAC:T	donor_loss	1.0000
20:56388152:TTA:T	donor_loss	1.0000
20:56388154:ACCTT:A	donor_loss	1.0000
20:56388198:GATGC:G	acceptor_gain	1.0000
20:56388199:ATGC:A	acceptor_gain	1.0000
20:56388199:ATGCC:A	acceptor_loss	1.0000
20:56388200:TGC:T	acceptor_gain	1.0000
20:56388201:GC:G	acceptor_gain	1.0000
20:56388201:GCC:G	acceptor_loss	1.0000
20:56388202:CC:C	acceptor_gain	1.0000
20:56388202:CCT:C	acceptor_loss	1.0000
20:56388203:C:CC	acceptor_gain	1.0000
20:56388203:CTG:C	acceptor_loss	1.0000
20:56392512:G:GT	donor_gain	1.0000
20:56392535:GCCA:G	donor_gain	1.0000
20:56392539:G:GG	donor_gain	1.0000
20:56370659:CCT:C	acceptor_loss	0.9900
20:56370660:C:A	acceptor_loss	0.9900
20:56370660:C:CC	acceptor_gain	0.9900

AlphaMissense

2609 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
20:56370577:A:G	W313R	1.000
20:56370577:A:T	W313R	1.000
20:56373441:T:A	D274V	1.000
20:56373495:T:A	D256V	1.000
20:56373495:T:G	D256A	1.000
20:56373498:C:A	R255I	1.000
20:56381515:A:G	L208P	1.000
20:56383065:T:A	K162N	1.000
20:56383065:T:G	K162N	1.000
20:56383119:A:C	F144L	1.000
20:56383119:A:T	F144L	1.000
20:56383121:A:G	F144L	1.000
20:56370527:A:C	F329L	0.999
20:56370527:A:T	F329L	0.999
20:56370529:A:G	F329L	0.999
20:56370567:C:T	G316E	0.999
20:56370568:C:G	G316R	0.999
20:56370568:C:T	G316R	0.999
20:56370575:C:A	W313C	0.999
20:56370575:C:G	W313C	0.999
20:56370627:A:G	L296P	0.999
20:56370642:C:T	G291D	0.999
20:56373433:A:G	W277R	0.999
20:56373433:A:T	W277R	0.999
20:56373435:C:T	G276E	0.999
20:56373437:A:C	F275L	0.999
20:56373437:A:T	F275L	0.999
20:56373439:A:G	F275L	0.999
20:56373440:A:C	D274E	0.999
20:56373440:A:T	D274E	0.999

dbSNP variants (sampled 300 via entrez): RS1000100584 (20:56377189 A>C), RS1000209810 (20:56393513 A>G), RS1000638371 (20:56391902 C>T), RS1000862064 (20:56389860 C>A,T), RS1000875903 (20:56372554 A>G), RS1000908473 (20:56383701 G>A,C), RS1000918515 (20:56383930 T>A), RS1001036935 (20:56379197 A>G), RS1001210435 (20:56374244 G>A), RS1001238124 (20:56385196 T>C), RS1001384737 (20:56379637 G>A,T), RS1001424129 (20:56380411 T>C,G), RS1001452897 (20:56371605 G>C), RS1001503876 (20:56389715 C>A), RS1001569143 (20:56371820 G>A,C)

Disease associations

OMIM: gene MIM:603072 | disease phenotypes: MIM:114500, MIM:254500

GenCC curated gene-disease

Disease	Classification	Inheritance
intellectual disability	Limited	Autosomal dominant
breast cancer	Limited	Autosomal dominant

Mondo (4): colorectal cancer (MONDO:0005575), plasma cell myeloma (MONDO:0009693), intellectual disability (MONDO:0001071), breast cancer (MONDO:0007254)

Orphanet (3): Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443), NON RARE IN EUROPE: Colorectal cancer (Orphanet:466667)

HPO phenotypes

8 total (8 of 8 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0001442	Typified by somatic mosaicism
HP:0002891	Uterine leiomyosarcoma
HP:0003003	Colon cancer
HP:0005584	Renal cell carcinoma
HP:0006716	Hereditary nonpolyposis colorectal carcinoma
HP:0006740	Transitional cell carcinoma of the bladder
HP:0006753	Neoplasm of the stomach

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST009391_1927	Metabolite levels	3.000000e-06
GCST90002390_676	Mean corpuscular hemoglobin	2.000000e-11
GCST90002392_115	Mean corpuscular volume	9.000000e-13
GCST90002397_288	Mean spheric corpuscular volume	5.000000e-10

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0010461	argininosuccinate measurement
EFO:0004527	mean corpuscular hemoglobin

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D009101	Multiple Myeloma	C04.557.595.500; C14.907.454.460; C15.378.147.780.650; C15.378.463.515.460; C20.683.515.845; C20.683.780.650

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (6): CHEMBL3430911 (PROTEIN FAMILY), CHEMBL3883303 (PROTEIN FAMILY), CHEMBL3883304 (PROTEIN COMPLEX), CHEMBL4722 (SINGLE PROTEIN), CHEMBL4748216 (PROTEIN-PROTEIN INTERACTION), CHEMBL5465201 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

65 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 733,570 (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
CHEMBL12856	INAMRINONE	4	9,690
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL1448	NICLOSAMIDE	4	14,322
CHEMBL1983268	ENTRECTINIB	4	3,510
CHEMBL2103830	FOSTAMATINIB	4	3,841
CHEMBL2105717	CABOZANTINIB	4	11,177
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL3545311	BRIGATINIB	4	5,634
CHEMBL3622821	UPADACITINIB	4	2,726
CHEMBL439	SULFADIAZINE	4	31,545
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL53463	DOXORUBICIN	4	314,282
CHEMBL535	SUNITINIB	4	79,020
CHEMBL5416410	DASATINIB	4	655
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL601719	CRIZOTINIB	4	14,403
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL223360	LINIFANIB	3	3,925
CHEMBL274654	ORANTINIB	3
CHEMBL3137331	DEFACTINIB	3
CHEMBL415049	BARASERTIB	3
CHEMBL483158	ALISERTIB	3
CHEMBL603469	LESTAURTINIB	3
CHEMBL1230609	FORETINIB	2
CHEMBL1231124	AZD-1480	2
CHEMBL1822792	MK-2461	2
CHEMBL1967878	CENISERTIB	2
CHEMBL1980297	ILORASERTIB	2

Clinical evidence (CIViC)

Drug × variant × indication: 7 predictive associations from 7 curated evidence items; also 1 prognostic.

Variant	Therapy	Indication	Effect	Level	CIViC
AURKA EXPRESSION	Radiation Therapy + Fluorouracil + Cisplatin	Esophagus Squamous Cell Carcinoma	Sensitivity/Response	CIViC B	EID1653
AURKA Overexpression	Platinum Compound	Ovarian Serous Carcinoma	Resistance	CIViC B	EID1650
AURKA Overexpression	Cisplatin	Lung Non-small Cell Carcinoma	Resistance	CIViC B	EID871
AURKA Overexpression	Alisertib + Cisplatin	Esophagus Adenocarcinoma	Sensitivity/Response	CIViC D	EID9627
AURKA EXPRESSION	Tamoxifen	Estrogen-receptor Positive Breast Cancer	Resistance	CIViC D	EID1959
AURKA Overexpression	Paclitaxel	Cervical Adenocarcinoma	Resistance	CIViC D	EID457
AURKA Amplification	Alisertib + Cisplatin	Esophagus Adenocarcinoma	Sensitivity/Response	CIViC E	EID456

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 (39 total), top 25:

Ligand	Action	Affinity	Parameter
MK-5108	Inhibition	10.19	pIC50
VIC 1911	Inhibition	9.4	pIC50
tozasertib	Inhibition	9.22	pKi
alisertib	Inhibition	9.0	pIC50
compound 46 [PMID: 16451062]	Inhibition	9.0	pIC50
tinengotinib	Inhibition	8.92	pIC50
AT-9283	Inhibition	8.52	pIC50
dubermatinib	Inhibition	8.52	pIC50
compound 10 [PMID: 19402633]	Inhibition	8.47	pIC50
compound 25 [PMID: 20855207]	Inhibition	8.4	pIC50
GSK143	Inhibition	8.32	pIC50
AMG-900	Inhibition	8.3	pIC50
XMD-12	Inhibition	8.25	pIC50
MLN-8054	Inhibition	8.19	pKd
SNS-314	Inhibition	8.05	pIC50
mobinitinib	Inhibition	8.01	pKd
danusertib	Inhibition	7.89	pIC50
ENMD-2076	Inhibition	7.85	pIC50
JNJ-7706621	Inhibition	7.74	pIC50
compound 38 [PMID: 20817473]	Inhibition	7.74	pIC50
SK5527	Binding	7.7	pIC50
BI-847325	Inhibition	7.6	pIC50
aurora kinase inhibitor III	Inhibition	7.38	pIC50
KW-2449	Inhibition	7.32	pIC50
juglone	Inhibition	7.3	pIC50

Binding affinities (BindingDB)

1133 measured of 1387 human assays (1387 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[[(1R)-1-[3-[(4-fluoro-3-hydroxybenzoyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.01 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-1-[3-[(5-propan-2-yl-1H-pyrazole-3-carbonyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.03 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-1-[3-[(5-tert-butyl-1H-pyrazole-3-carbonyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.03 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-1-[3-[(2,2-difluorocyclopropanecarbonyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.04 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[1-[3-[(4-bromobenzoyl)amino]phenyl]-3-methoxypropyl]amino]quinazoline-8-carboxamide	IC50	0.05 nM	US-8637532: Amino azaheterocyclic carboxamides
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-[[(1R)-1-[3-[(6-methoxypyridine-3-carbonyl)amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.07 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-1-[3-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl]ethyl]amino]quinazoline-8-carboxamide	IC50	0.07 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-[[(1R)-1-[3-[(4-cyano-2-pyridinyl)amino]phenyl]ethyl]amino]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-[(4-chloro-2,6-difluorobenzoyl)amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.08 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(5-fluoro-4-methylcyclohexa-1,5-diene-1-carbonyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.09 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-hydroxy-1-[3-[(4-methoxybenzoyl)amino]phenyl]propyl]amino]quinazoline-8-carboxamide	IC50	0.09 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[3-[[6-[2-methoxyethyl(methyl)amino]pyridine-3-carbonyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.09 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[1-[3-[(6-methoxypyridine-3-carbonyl)amino]phenyl]ethylamino]quinazoline-8-carboxamide	IC50	0.1 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[1-[3-[[(5-cyclopropyl-1H-pyrazol-3-yl)-hydroxymethyl]amino]phenyl]-3-hydroxypropyl]amino]quinazoline-8-carboxamide	IC50	0.1 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-[[(1R)-1-[3-[[2-fluoro-5-(trifluoromethyl)benzoyl]amino]phenyl]ethyl]amino]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
1-[[(1R)-1-[4-fluoro-3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl]ethyl]amino]isoquinoline-5-carboxamide	IC50	0.12 nM	US-8637532: Amino azaheterocyclic carboxamides
4-[[(1R)-1-[3-(cyclopentanecarbonylamino)phenyl]ethyl]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-[[2-(methylamino)pyridine-4-carbonyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.15 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-[[4-(trifluoromethyl)-2-pyridinyl]amino]phenyl]methylamino]quinazoline-8-carboxamide	IC50	0.15 nM	US-8637532: Amino azaheterocyclic carboxamides
3-chloro-4-fluoro-N-[5-({6-methoxy-7-[3-(morpholin-4-yl)propoxy]quinazolin-4-yl}amino)pyrimidin-2-yl]benzamide	IC50	0.15 nM
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-[[4-hydroxy-1-[3-[(4-methoxybenzoyl)amino]phenyl]butyl]amino]quinazoline-8-carboxamide	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-[[1-[3-[(4-bromobenzoyl)amino]phenyl]-2-(methylamino)ethyl]amino]quinazoline-8-carboxamide	IC50	0.17 nM	US-8637532: Amino azaheterocyclic carboxamides
10-[[2-(methylamino)-1-[3-[[4-(trifluoromethoxy)benzoyl]amino]phenyl]ethyl]amino]-1,3-diazecine-5-carboxamide	IC50	0.17 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-(1H-indole-6-carbonylamino)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

ChEMBL bioactivities

4079 potent at pChembl≥5 of 4257 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	IC50	0.01	nM	CHEMBL3685304
11.00	Kd	0.01	nM	CHEMBL4227082
11.00	Kd	0.01	nM	CHEMBL4225923
10.92	IC50	0.012	nM	CHEMBL4462759
10.92	IC50	0.012	nM	CHEMBL4476212
10.92	IC50	0.012	nM	CHEMBL4443279
10.52	IC50	0.03	nM	CHEMBL3675439
10.52	IC50	0.03	nM	CHEMBL3675462
10.40	IC50	0.04	nM	CHEMBL3680540
10.40	IC50	0.04	nM	ALISERTIB
10.34	IC50	0.046	nM	MK-5108
10.30	IC50	0.05	nM	CHEMBL3680479
10.30	IC50	0.05	nM	CHEMBL3675508
10.22	IC50	0.06	nM	CHEMBL3685244
10.22	IC50	0.06	nM	CHEMBL3639841
10.22	IC50	0.06	nM	CHEMBL3680420
10.22	IC50	0.06	nM	CHEMBL4563026
10.19	IC50	0.064	nM	MK-5108
10.15	IC50	0.07	nM	CHEMBL3675437
10.15	IC50	0.07	nM	CHEMBL3675509
10.15	IC50	0.07	nM	CHEMBL3915221
10.15	IC50	0.07	nM	CHEMBL3951333
10.10	IC50	0.08	nM	CHEMBL3675537
10.10	IC50	0.08	nM	CHEMBL3685272
10.10	IC50	0.08	nM	CHEMBL3685256
10.10	IC50	0.08	nM	CHEMBL3685305
10.10	IC50	0.08	nM	CHEMBL3685262
10.10	IC50	0.08	nM	CHEMBL3675465
10.10	IC50	0.08	nM	CHEMBL3904174
10.05	IC50	0.09	nM	CHEMBL3680477
10.05	IC50	0.09	nM	CHEMBL3675524
10.05	IC50	0.09	nM	CHEMBL3675443
10.05	IC50	0.09	nM	CHEMBL3892660
10.00	IC50	0.1	nM	CHEMBL3680541
10.00	IC50	0.1	nM	CHEMBL3675484
10.00	IC50	0.1	nM	CHEMBL3685241
10.00	Kd	0.1	nM	MK-5108
9.96	IC50	0.11	nM	CHEMBL3670470
9.96	IC50	0.11	nM	CHEMBL3675457
9.96	IC50	0.11	nM	CHEMBL3685306
9.96	IC50	0.11	nM	CHEMBL3685250
9.96	IC50	0.11	nM	CHEMBL3923139
9.96	IC50	0.11	nM	CHEMBL4460717
9.92	IC50	0.12	nM	CHEMBL3685307
9.92	IC50	0.12	nM	CHEMBL3685245
9.92	IC50	0.12	nM	CHEMBL3675459
9.92	IC50	0.12	nM	CHEMBL3680402
9.92	IC50	0.12	nM	CHEMBL3675446
9.92	IC50	0.12	nM	CHEMBL3685237
9.92	IC50	0.12	nM	CHEMBL3680488

PubChem BioAssay actives

2316 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-chloro-4-(2-fluorophenoxy)-N-[4-(2H-tetrazol-5-yl)phenyl]pyrimidin-2-amine	1567369: Inhibition of Aurora A (unknown origin)	ic50	<0.0001	uM
5-chloro-4-(4-methoxyphenoxy)-N-[4-(2H-tetrazol-5-yl)phenyl]pyrimidin-2-amine	1567369: Inhibition of Aurora A (unknown origin)	ic50	<0.0001	uM
5-chloro-4-(4-fluorophenoxy)-N-[4-(2H-tetrazol-5-yl)phenyl]pyrimidin-2-amine	1567369: Inhibition of Aurora A (unknown origin)	ic50	<0.0001	uM
4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)-2-pyridinyl]methyl]cyclohexane-1-carboxylic acid	1331759: Inhibition of human recombinant His-tagged Aurora A expressed in Escherichia coli using RRR(GLRRASLG)4R-NH2 as substrate after 40 mins in presence of [gamma-33P]-ATP by liquid scintillation counting	ic50	<0.0001	uM
4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid	1323327: Inhibition of His-tagged human Aurora A kinase (122 to 40 residues) expressed in Escherichia coli BL21 (DE3) Rosetta cells using biotinylated STK2 substrate incubated for 30 mins by HTRF assay	ic50	<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	1390881: Binding affinity to Aurora A (unknown origin) after 45 mins by fluorescence-based thermal stability shift assay	kd	<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	1390881: Binding affinity to Aurora A (unknown origin) after 45 mins by fluorescence-based thermal stability shift assay	kd	<0.0001	uM
3-chloro-N-[5-[[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinazolin-4-yl]amino]pyrimidin-2-yl]benzamide	1796896: Recombinant Aurora A Enzyme Assay from Article 10.1016/j.bmcl.2005.11.053: “SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.”	ic50	0.0001	uM
155514901	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0001	uM
155527907	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0001	uM
155559311	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0001	uM
3-chloro-4-fluoro-N-[5-[[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinazolin-4-yl]amino]pyrimidin-2-yl]benzamide	1796896: Recombinant Aurora A Enzyme Assay from Article 10.1016/j.bmcl.2005.11.053: “SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.”	ic50	0.0001	uM
155521505	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0002	uM
155525257	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0002	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	701395: Inhibition of Aurora A by 33P minase hotspot assay	ic50	0.0002	uM
4-[[4-(2-chloroanilino)-5-fluoropyrimidin-2-yl]amino]benzoic acid	701395: Inhibition of Aurora A by 33P minase hotspot assay	ic50	0.0002	uM
2-[[4-(3,4-dimethoxyanilino)-6-(quinolin-6-ylamino)-1,3,5-triazin-2-yl]amino]-3-(1H-pyrrolo[2,3-b]pyridin-3-yl)propanamide	495138: Inhibition of Aurora A ATP-binding site assessed as inhibition of [gamma-33P]ATP incorporation into substrate by scintillation counting	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	1811679: Inhibition of recombinant GST-tagged N-terminal truncated human Aurora A (123 to 401 residues) expressed in Sf9 insect cell using tetra-LRRASLG peptide as substrate incubated for 20 mins by Kinase-Glo plus luminescent kinase assay	ic50	0.0004	uM
4-(2,4-dimethyl-1,3-thiazol-5-yl)-N-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine	483576: Inhibition of human recombinant Aurora A after 30 mins	ki	0.0004	uM
[9-[4-[[(5S)-6-amino-5-[[(2S)-2-[[(2S)-2-[4-[[4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)-2-pyridinyl]methyl]cyclohexanecarbonyl]amino]butanoylamino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-6-oxohexyl]carbamoyl]-2-carboxyphenyl]-6-(dimethylamino)xanthen-3-ylidene]-dimethylazanium	1238154: Binding affinity to purified recombinant full-length Aurora A (unknown origin) by fluorescence polarisation/anisotropy based equilibrium binding assay	kd	0.0004	uM
5-methyl-4-propan-2-yloxy-N-[4-(2H-tetrazol-5-yl)phenyl]pyrimidin-2-amine	1567369: Inhibition of Aurora A (unknown origin)	ic50	0.0004	uM
155535101	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0005	uM
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	1846788: Inhibition of Aurora A (unknown origin) using kemptide as substrate incubated for 50 mins in the presence of ATP by ADP-Glo reagent based luminescence assay	ic50	0.0005	uM
(2,3-dichlorophenyl)-[4-[[3-(1,3-thiazol-2-ylamino)phenyl]methyl]piperazin-1-yl]methanone	551679: Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells	ic50	0.0005	uM
155519065	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0006	uM
155525581	1515217: Inhibition of Aurora A (unknown origin) using kemptide acetate salt as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0006	uM
N-[4-[4-(4-aminopiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	1977329: Inhibition of human N-terminal His-tagged aurora A assessed as inhibition constant incubated for 15 mins using Histone H3 as substrate in presence [gamma32P]-ATP by scintillation counter method	ki	0.0006	uM
3-[(7-cyclohexylpyrrolo[2,3-d]pyrimidin-2-yl)amino]benzoic acid	551679: Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells	ic50	0.0006	uM
2-[[(2S)-6-hydroxy-6-methylheptan-2-yl]amino]-4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile	598117: Inhibition of phosphotransferase activity of recombinant aurora A expressed in HeLa cells	ki	0.0006	uM
2-[3-[(7-cyclohexylpyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]acetic acid	273737: Inhibition of histone H3 phosphorylation by murine Aurora A kinase	ic50	0.0006	uM
ethyl (9S)-9-[3-(1H-benzimidazol-2-yloxy)phenyl]-8-oxo-2,4,5,6,7,9-hexahydropyrrolo[3,4-b]quinoline-3-carboxylate	1189500: Inhibition of poly-histidine tagged full length recombinant aurora A (unknown origin) assessed as phosphorylation of NuMA-histidine substrate by scintillation counting analysis	ic50	0.0006	uM
[9-[4-[[(5R)-6-amino-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(4-azidophenyl)-2-[6-[[4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)-2-pyridinyl]methyl]cyclohexanecarbonyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-oxohexyl]carbamoyl]-2-carboxyphenyl]-6-(dimethylamino)-9,9a-dihydroxanthen-3-ylidene]-dimethylazanium	1238154: Binding affinity to purified recombinant full-length Aurora A (unknown origin) by fluorescence polarisation/anisotropy based equilibrium binding assay	kd	0.0007	uM
4-[[4-(2-chloroanilino)pyrimidin-2-yl]amino]benzoic acid	701395: Inhibition of Aurora A by 33P minase hotspot assay	ic50	0.0007	uM
4-[[5-fluoro-4-(2-fluoroanilino)pyrimidin-2-yl]amino]benzoic acid	1572981: Inhibition of His6 tagged MBP fused human aurora A (123 to 390 residues) expressed in Escherichia coli Tuner (DE3) cells	ic50	0.0008	uM
3-chloro-N-[5-[[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]amino]pyrimidin-2-yl]benzamide	261774: Inhibitory activity against Aurora A	ic50	0.0008	uM
N-[2-[(1R,8S)-4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide	1419705: Inhibition of full-length His-tagged recombinant aurora A (unknown origin) expressed in insect cells using biotinylated LRRWSLG substrate by Z’-LYTE assay	ic50	0.0008	uM
N-[5-[[7-[(2S)-2-hydroxy-3-piperidin-1-ylpropoxy]-6-methoxyquinazolin-4-yl]amino]pyrimidin-2-yl]benzamide	273725: Inhibition of Aurora A	ic50	0.0008	uM
[2-fluoro-3-(trifluoromethyl)phenyl]-[4-[[6-(1H-pyrazol-5-ylamino)-2-pyridinyl]methyl]piperazin-1-yl]methanone	551679: Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells	ic50	0.0009	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]acetamide	1392522: Inhibition of Aurora A (unknown origin) using kemptide as substrate after 30 mins by kinase-Glo luminescence method	ic50	0.0010	uM
N-[4-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]quinazolin-2-yl]sulfanylphenyl]acetamide	420295: Inhibition of Aurora-A by coupled assay	ki	0.0010	uM
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]-6-phenylpyrimidin-2-yl]sulfanylphenyl]propanamide	420295: Inhibition of Aurora-A by coupled assay	ki	0.0010	uM
N-(5-methyl-1H-pyrazol-3-yl)-2-naphthalen-2-ylsulfanylquinazolin-4-amine	420295: Inhibition of Aurora-A by coupled assay	ki	0.0010	uM
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]quinazolin-2-yl]sulfanylphenyl]propanamide	420295: Inhibition of Aurora-A by coupled assay	ki	0.0010	uM
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]quinazolin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	420295: Inhibition of Aurora-A by coupled assay	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	273823: Inhibition of human recombinant Aurora A	ki	0.0010	uM
N-[4-[4-(4-ethylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]propanamide	353619: Inhibition of aurora A kinase	ic50	0.0010	uM
N-[4-[4-(4-cyclopropylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]propanamide	353619: Inhibition of aurora A kinase	ic50	0.0010	uM
2-[2-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1,3-thiazol-5-yl]-N-(3-fluorophenyl)acetamide	259729: Inhibition of Aurora A kinase activity	ic50	0.0010	uM
N-(3-fluorophenyl)-2-[2-[[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]amino]-1,3-thiazol-5-yl]acetamide	259729: Inhibition of Aurora A kinase activity	ic50	0.0010	uM
N-(3-fluorophenyl)-2-[2-[[7-[3-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1,3-thiazol-5-yl]acetamide	259729: Inhibition of Aurora A kinase activity	ic50	0.0010	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, affects cotreatment, decreases expression, increases expression, decreases reaction (+1 more)	8
Estradiol	affects cotreatment, increases expression	6
sodium arsenite	decreases reaction, increases phosphorylation, decreases expression, increases abundance, increases expression	5
Benzo(a)pyrene	decreases expression	5
Cyclosporine	decreases expression, increases methylation	5
Fluorouracil	decreases expression	4
Air Pollutants	affects cotreatment, increases abundance, increases expression, decreases expression	3
Arsenic	affects cotreatment, increases expression, increases activity, increases phosphorylation, affects reaction (+1 more)	3
Doxorubicin	increases expression, decreases expression, decreases reaction	3
Valproic Acid	decreases expression	3
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression	3
Aflatoxin B1	affects expression, decreases expression, increases expression	3
methylselenic acid	affects expression, decreases expression	2
trichostatin A	affects expression, decreases expression	2
afimoxifene	decreases expression, decreases response to substance	2
cobaltous chloride	decreases expression	2
MLN 8237	decreases activity, decreases phosphorylation	2
(+)-JQ1 compound	decreases expression	2
Acetaminophen	decreases expression	2
Cadmium	affects expression, increases abundance, decreases expression	2
Coumestrol	increases expression, affects reaction, affects cotreatment	2
Lipopolysaccharides	decreases expression, affects expression, affects response to substance, increases expression	2
Phenylmercuric Acetate	decreases expression, affects cotreatment	2
Progesterone	decreases expression, increases expression	2
Tobacco Smoke Pollution	decreases expression	2
Tunicamycin	decreases expression	2
Vincristine	increases response to substance, increases expression	2
Nocodazole	affects cotreatment, increases expression, increases phosphorylation, decreases expression, decreases reaction	2
Paclitaxel	decreases response to substance, increases expression	2
Cadmium Chloride	decreases expression, affects expression, increases abundance	2

ChEMBL screening assays

1500 unique, capped per target: 1483 binding, 10 functional, 7 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3887043	Binding	HTRF Assay: The effect of the compounds of the invention on the activity of the enzyme PDE3 was evaluated by the company CEREP (Le bois I’Evêque, 86600 Celle I’Evescault, France; http://www.cerep.fr) in accordance with its standard protocol	Anti-cancer compound and pharmaceutical composition containing the same
CHEMBL1963727	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: STK6	PubChem BioAssay data set
CHEMBL4048563	ADMET	Inhibition of human recombinant AurKA after 4 hrs by ADP-Glo assay	Tozasertib Analogues as Inhibitors of Necroptotic Cell Death. — J Med Chem

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT05657860	PHASE4	COMPLETED	Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479	PHASE4	RECRUITING	Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829	PHASE4	WITHDRAWN	Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198	PHASE4	NOT_YET_RECRUITING	Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT00014638	PHASE4	COMPLETED	Letrozole in Treating Postmenopausal Women With Metastatic Breast Cancer
NCT00022386	PHASE4	COMPLETED	Epoetin Alfa in Treating Chemotherapy-Related Anemia in Women With Stage I, Stage II, or Stage III Breast Cancer
NCT00029224	PHASE4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00030758	PHASE4	UNKNOWN	Filgrastim or Pegfilgrastim in Preventing Neutropenia in Women Receiving Chemotherapy Following Surgery for Breast Cancer
NCT00082277	PHASE4	COMPLETED	Anastrozole Biphosphonate Study in Postmenopausal Women With Hormone-Receptor-Positive Early Breast Cancer
NCT00087620	PHASE4	TERMINATED	A Study of Capecitabine In Combination With Docetaxel vs Capecitabine Followed by Docetaxel As First-Line Treatment For Metastatic Breast Cancer
NCT00121836	PHASE4	COMPLETED	A Study of Xeloda (Capecitabine) in Women With HER2-Negative Metastatic Breast Cancer
NCT00126360	PHASE4	UNKNOWN	STARS Breast Trial (Study of Anastrozole and Radiotherapy Sequencing Pilot)
NCT00127933	PHASE4	COMPLETED	XeNA Study - A Study of Xeloda (Capecitabine) in Patients With Invasive Breast Cancer
NCT00128297	PHASE4	COMPLETED	Pamidronate Administration in Breast Cancer Patients With Bone Metastases
NCT00129597	PHASE4	UNKNOWN	Effect of Ketalar to Prevent Postoperative Chronic Pain After Mastectomy
NCT00131170	PHASE4	COMPLETED	Paravertebral Block for Breast Surgery
NCT00156039	PHASE4	COMPLETED	Randomized Trial of Follow-up Strategies in Breast Cancer
NCT00160901	PHASE4	COMPLETED	Complementary Therapies for the Reduction of Side Effects During Chemotherapy for Breast Cancer
NCT00171847	PHASE4	TERMINATED	Study of the Efficacy and Safety of Letrozole Combined With Trastuzumab in Patients With Metastatic Breast Cancer
NCT00176046	PHASE4	COMPLETED	Mistletoe Extract in Early or Advanced Breast Cancer, A Feasibility Study
NCT00190697	PHASE4	COMPLETED	A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment
NCT00234195	PHASE4	COMPLETED	Wellbutrin XL, Major Depressive Disorder and Breast Cancer
NCT00237133	PHASE4	COMPLETED	Treatment of Locally Advanced Breast Cancer With Letrozole in Postmenopausal Women
NCT00237224	PHASE4	COMPLETED	Open Label Study of Postmenopausal Women With ER and /or PgR Positive Breast Cancer Treated With Letrozole
NCT00241046	PHASE4	TERMINATED	Letrozole in the Treatment of 1st and 2nd Line Hormone Receptor Positive Breast Cancer: Pre-therapeutic Risk Assessment
NCT00277160	PHASE4	COMPLETED	A Study of Primary Prophylaxis With Neulasta (Pegfilgrastim) Versus Secondary Prophylaxis After Chemotherapy in Elderly Subjects (>/= 65 Years Old) With Cancer
NCT00323479	PHASE4	COMPLETED	Arthralgia During Anastrozole Therapy for Breast Cancer
NCT00334139	PHASE4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00356148	PHASE4	COMPLETED	The Efficacy of Prophylactic Antibiotic Administration During Breast Cancer Surgery in Overweight Patients.
NCT00372476	PHASE4	COMPLETED	Efficacy and Safety of Imatinib and Vinorelbine in Patients With Advanced Breast Cancer
NCT00413491	PHASE4	UNKNOWN	National Screening in Denmark With MR Versus Mammography and Ultrasound of Women With BRCA1 or BRCA2 Mutations
NCT00484614	PHASE4	UNKNOWN	Study the Role of Positron Emission Mammography in Pre-surgical Planning for Breast Cancer
NCT00485953	PHASE4	COMPLETED	Effect of Bisphosphonate on Bone Loss in Postmenopausal Women With Breast Cancer Initiating Aromatase Inhibitor Therapy
NCT00496678	PHASE4	COMPLETED	Trial of Patient Navigation-Activation
NCT00531973	PHASE4	UNKNOWN	A Study of Liposomal Doxorubicin in Women With Breast Cancer Exploiting Tissue Doppler Imaging
NCT00537771	PHASE4	COMPLETED	Liver Safety Under Upfront Arimidex vs Tamoxifen
NCT00544986	PHASE4	COMPLETED	A Prospective,Open-label Study of Anastrozole in Post-menopausal Women With Hormone Sensitive Advanced Breast Cancer
NCT00613275	PHASE4	COMPLETED	Patient Navigation in the Safety Net:CONNECTeDD
NCT00638599	PHASE4	COMPLETED	Comparison of Laryngeal Mask Airway (LMA®) and Tracheal Tube in Modified Radical Mastectomy on Breast Cancer
NCT00647075	PHASE4	UNKNOWN	Yunzhi as Dietary Supplement in Breast Cancer