AURKAIP1
gene geneOn this page
Also known as Cox24AKIPAIPFLJ20608mS38
Summary
AURKAIP1 (aurora kinase A interacting protein 1, HGNC:24114) is a protein-coding gene on chromosome 1p36.33, encoding Small ribosomal subunit protein bS22, mitochondrial (Q9NWT8). May act as a negative regulator of Aurora-A kinase, by down-regulation through proteasome-dependent degradation. It is a selective cancer dependency (DepMap: 35.3% of cell lines).
Acts upstream of or within positive regulation of proteolysis. Located in mitochondrial matrix and nucleoplasm.
Source: NCBI Gene 54998 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 35 total — 1 pathogenic
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- Cancer dependency (DepMap): dependent in 35.3% of screened cell lines
- MANE Select transcript:
NM_017900
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:24114 |
| Approved symbol | AURKAIP1 |
| Name | aurora kinase A interacting protein 1 |
| Location | 1p36.33 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Cox24, AKIP, AIP, FLJ20608, mS38 |
| Ensembl gene | ENSG00000175756 |
| Ensembl biotype | protein_coding |
| OMIM | 609183 |
| Entrez | 54998 |
Gene structure
Transcript identifiers
Ensembl transcripts: 17 — 15 protein_coding, 2 protein_coding_CDS_not_defined
ENST00000321751, ENST00000338338, ENST00000338370, ENST00000378853, ENST00000489799, ENST00000496905, ENST00000883185, ENST00000883186, ENST00000883187, ENST00000883188, ENST00000883189, ENST00000883190, ENST00000883191, ENST00000883192, ENST00000929719, ENST00000929720, ENST00000929721
RefSeq mRNA: 3 — MANE Select: NM_017900
NM_001127229, NM_001127230, NM_017900
CCDS: CCDS25
Canonical transcript exons
ENST00000338338 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001629775 | 1374000 | 1374445 |
| ENSE00001697866 | 1375154 | 1375207 |
| ENSE00001789693 | 1374705 | 1374790 |
| ENSE00003926820 | 1373736 | 1373902 |
Expression profiles
Bgee: expression breadth ubiquitous, 288 present calls, max score 99.27.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 88.6017 / max 349.1398, expressed in 1821 samples.
FANTOM5 promoters (6 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 9772 | 84.3437 | 1821 |
| 9776 | 1.4668 | 541 |
| 9774 | 0.8802 | 606 |
| 9775 | 0.6736 | 429 |
| 9773 | 0.6557 | 406 |
| 201313 | 0.5817 | 301 |
Top tissues by expression
288 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right testis | UBERON:0004534 | 99.27 | gold quality |
| left testis | UBERON:0004533 | 99.25 | gold quality |
| apex of heart | UBERON:0002098 | 98.94 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 98.40 | gold quality |
| heart left ventricle | UBERON:0002084 | 98.32 | gold quality |
| cardiac ventricle | UBERON:0002082 | 98.30 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 98.27 | gold quality |
| testis | UBERON:0000473 | 98.25 | gold quality |
| gastrocnemius | UBERON:0001388 | 98.18 | gold quality |
| right atrium auricular region | UBERON:0006631 | 98.08 | gold quality |
| heart right ventricle | UBERON:0002080 | 97.87 | gold quality |
| cardiac atrium | UBERON:0002081 | 97.86 | gold quality |
| muscle of leg | UBERON:0001383 | 97.81 | gold quality |
| right lobe of liver | UBERON:0001114 | 97.74 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 97.69 | gold quality |
| cingulate cortex | UBERON:0003027 | 97.66 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 97.66 | gold quality |
| muscle organ | UBERON:0001630 | 97.65 | gold quality |
| right adrenal gland | UBERON:0001233 | 97.59 | gold quality |
| amygdala | UBERON:0001876 | 97.57 | gold quality |
| type B pancreatic cell | CL:0000169 | 97.55 | gold quality |
| prefrontal cortex | UBERON:0000451 | 97.51 | gold quality |
| vastus lateralis | UBERON:0001379 | 97.50 | gold quality |
| nucleus accumbens | UBERON:0001882 | 97.49 | gold quality |
| adult organism | UBERON:0007023 | 97.49 | gold quality |
| body of tongue | UBERON:0011876 | 97.47 | gold quality |
| putamen | UBERON:0001874 | 97.46 | gold quality |
| caudate nucleus | UBERON:0001873 | 97.45 | gold quality |
| body of stomach | UBERON:0001161 | 97.43 | gold quality |
| heart | UBERON:0000948 | 97.41 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 3.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-7037 | yes | 472.87 |
| E-ANND-3 | yes | 16.86 |
| E-CURD-88 | yes | 3.90 |
| E-MTAB-8060 | no | 587.08 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): EHMT2, GATA3, MTA3
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 35.3% of screened cell lines.
Literature-anchored findings (GeneRIF, showing 10)
- Results describe the identification of a novel negative regulator of Aurora-A, named AIP (Aurora-A kinase Interacting Protein). (PMID:12244051)
- Phe31Ile polymorphism in Aurora A may be a genetic modifier for developing breast carcinoma. (PMID:15271856)
- We propose that AURKAIP1 might function upstream of the Az1 by enhancing the binding affinity of Az1 to Aurora-A to promote recognition, targeting to proteasome and subsequent degradation. (PMID:17452972)
- AKURA phosphorylation of AIP and stabilization of the enzyme-substrate complex are reported. (PMID:17957726)
- GSK-3beta modulates the early mitotic Aurora-A level through binding and phosphorylating AIP. (PMID:18391981)
- Plk1 controls Aurora A localization and function by regulating cellular levels of hBora. (PMID:18521620)
- Aurora A is necessary for the maintenance of the mitotic delay induced in response to microtubule-perturbing agents. (PMID:19221504)
- Aurora-A protein increased in stomach cancer cells in response to cisplatin and was degraded upon combined treatment with capsaicin with cisplatin. (PMID:21932983)
- Encodes a mitochondrial protein (PMID:22356826)
- AURKAIP1 actuates tumor progression through stabilizing DDX5 in triple negative breast cancer. (PMID:38040691)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | aurkaip1 | ENSDARG00000074985 |
| mus_musculus | Aurkaip1 | ENSMUSG00000065990 |
Protein
Protein identifiers
Small ribosomal subunit protein bS22, mitochondrial — Q9NWT8 (reviewed: Q9NWT8)
Alternative names: 28S ribosomal protein S38, mitochondrial, Aurora kinase A-interacting protein, Small ribosomal subunit protein mS38
All UniProt accessions (1): Q9NWT8
UniProt curated annotations — full annotation on UniProt →
Function. May act as a negative regulator of Aurora-A kinase, by down-regulation through proteasome-dependent degradation.
Subunit / interactions. Component of the mitochondrial small ribosomal subunit (mt-SSU). Mature mammalian 55S mitochondrial ribosomes consist of a small (28S) and a large (39S) subunit. The 28S small subunit contains a 12S ribosomal RNA (12S mt-rRNA) and 30 different proteins. The 39S large subunit contains a 16S rRNA (16S mt-rRNA), a copy of mitochondrial valine transfer RNA (mt-tRNA(Val)), which plays an integral structural role, and 52 different proteins. Interacts with Aurora-A.
Subcellular location. Mitochondrion matrix. Nucleus.
Tissue specificity. Ubiquitously expressed and especially highly expressed in heart, skeletal muscle and testis.
Miscellaneous. Initially thought to be mitochondrial specific, comparison with ribosomes from Actinomycetota shows this protein is also found in some bacteria. Thus it has been renamed.
Similarity. Belongs to the bacterial ribosomal protein bS22 family.
RefSeq proteins (3): NP_001120701, NP_001120702, NP_060370* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR013177 | Ribosomal_bS22_C | Domain |
Pfam: PF08213
UniProt features (6 total): helix 2, transit peptide 1, chain 1, sequence variant 1, strand 1
Structure
Experimental structures (PDB)
73 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7QI4 | ELECTRON MICROSCOPY | 2.21 |
| 8CSS | ELECTRON MICROSCOPY | 2.36 |
| 7P2E | ELECTRON MICROSCOPY | 2.4 |
| 8RRI | ELECTRON MICROSCOPY | 2.4 |
| 9OLF | ELECTRON MICROSCOPY | 2.46 |
| 9OJM | ELECTRON MICROSCOPY | 2.5 |
| 8CSQ | ELECTRON MICROSCOPY | 2.54 |
| 8CSR | ELECTRON MICROSCOPY | 2.54 |
| 6ZM6 | ELECTRON MICROSCOPY | 2.59 |
| 7QI5 | ELECTRON MICROSCOPY | 2.63 |
| 7PNX | ELECTRON MICROSCOPY | 2.76 |
| 8ANY | ELECTRON MICROSCOPY | 2.85 |
| 8CST | ELECTRON MICROSCOPY | 2.85 |
| 6ZM5 | ELECTRON MICROSCOPY | 2.89 |
| 7PO0 | ELECTRON MICROSCOPY | 2.9 |
| 8K2A | ELECTRON MICROSCOPY | 2.9 |
| 9PGL | ELECTRON MICROSCOPY | 2.9 |
| 7PO1 | ELECTRON MICROSCOPY | 2.92 |
| 7PO3 | ELECTRON MICROSCOPY | 2.92 |
| 9PGF | ELECTRON MICROSCOPY | 2.93 |
| 6VMI | ELECTRON MICROSCOPY | 2.96 |
| 6RW4 | ELECTRON MICROSCOPY | 2.97 |
| 6VLZ | ELECTRON MICROSCOPY | 2.97 |
| 7QI6 | ELECTRON MICROSCOPY | 2.98 |
| 8QRN | ELECTRON MICROSCOPY | 2.98 |
| 9PSM | ELECTRON MICROSCOPY | 2.98 |
| 8OIS | ELECTRON MICROSCOPY | 3 |
| 9G5C | ELECTRON MICROSCOPY | 3 |
| 9G5D | ELECTRON MICROSCOPY | 3 |
| 9HFM | ELECTRON MICROSCOPY | 3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9NWT8-F1 | 70.14 | 0.38 |
Function
Pathways and Gene Ontology
Reactome pathways
7 pathways
| ID | Pathway |
|---|---|
| R-HSA-5368286 | Mitochondrial translation initiation |
| R-HSA-5389840 | Mitochondrial translation elongation |
| R-HSA-5419276 | Mitochondrial translation termination |
| R-HSA-9937383 | Mitochondrial ribosome-associated quality control |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-5368287 | Mitochondrial translation |
| R-HSA-72766 | Translation |
MSigDB gene sets: 650 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_DN, REACTOME_BIOLOGICAL_OXIDATIONS, MODY_HIPPOCAMPUS_POSTNATAL, TGCGCANK_UNKNOWN, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, MODULE_255, PAL_PRMT5_TARGETS_UP, GOBP_PROTEIN_TARGETING, GOBP_MITOCHONDRIAL_TRANSLATION, MODULE_317, GOBP_ESTABLISHMENT_OF_PROTEIN_LOCALIZATION_TO_ORGANELLE, chr11q13, GOBP_TRANSLATION, GOBP_PROTEIN_MATURATION, YY1_02
GO Biological Process (2): mitochondrial translation (GO:0032543), positive regulation of proteolysis (GO:0045862)
GO Molecular Function (1): protein binding (GO:0005515)
GO Cellular Component (8): nucleus (GO:0005634), nucleoplasm (GO:0005654), mitochondrion (GO:0005739), mitochondrial inner membrane (GO:0005743), mitochondrial matrix (GO:0005759), mitochondrial small ribosomal subunit (GO:0005763), ribosome (GO:0005840), ribonucleoprotein complex (GO:1990904)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| Mitochondrial translation | 4 |
| Translation | 1 |
| Metabolism of proteins | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| mitochondrion | 2 |
| intracellular membrane-bounded organelle | 2 |
| translation | 1 |
| mitochondrial gene expression | 1 |
| proteolysis | 1 |
| regulation of proteolysis | 1 |
| positive regulation of protein metabolic process | 1 |
| binding | 1 |
| nuclear lumen | 1 |
| cellular anatomical structure | 1 |
| cytoplasm | 1 |
| organelle inner membrane | 1 |
| mitochondrial membrane | 1 |
| intracellular organelle lumen | 1 |
| organellar small ribosomal subunit | 1 |
| mitochondrial ribosome | 1 |
| mitochondrial protein-containing complex | 1 |
| intracellular membraneless organelle | 1 |
| protein-containing complex | 1 |
Protein interactions and networks
STRING
1636 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| AURKAIP1 | AURKA | O14965 | 731 |
| AURKAIP1 | AKIP1 | Q9NQ31 | 642 |
| AURKAIP1 | MRM1 | Q6IN84 | 554 |
| AURKAIP1 | MRPS31 | Q92665 | 524 |
| AURKAIP1 | CHCHD1 | Q96BP2 | 489 |
| AURKAIP1 | PET117 | Q6UWS5 | 483 |
| AURKAIP1 | RALGPS2 | Q86X27 | 467 |
| AURKAIP1 | NBEA | Q8NFP9 | 463 |
| AURKAIP1 | CCDC77 | Q9BR77 | 448 |
| AURKAIP1 | MRPS28 | Q9Y2Q9 | 446 |
| AURKAIP1 | HYAL2 | Q12891 | 437 |
| AURKAIP1 | PRKACA | P17612 | 434 |
| AURKAIP1 | CCDC124 | Q96CT7 | 432 |
| AURKAIP1 | NFKB1 | P19838 | 427 |
| AURKAIP1 | NBR1 | Q14596 | 418 |
IntAct
51 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| AURKAIP1 | FAM9B | psi-mi:“MI:0915”(physical association) | 0.560 |
| FAM9B | AURKAIP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| DEFB127 | AURKAIP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| ABHD4 | AURKAIP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MRPS34 | MRPS12 | psi-mi:“MI:0914”(association) | 0.530 |
| AURKAIP1 | AURKA | psi-mi:“MI:0915”(physical association) | 0.520 |
| COQ4 | COQ9 | psi-mi:“MI:0914”(association) | 0.500 |
| AURKAIP1 | NRDC | psi-mi:“MI:0914”(association) | 0.480 |
| DDX21 | MED19 | psi-mi:“MI:2364”(proximity) | 0.480 |
| AURKAIP1 | SEPTIN7 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GSK3A | AURKAIP1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| CNOT1 | IBTK | psi-mi:“MI:0914”(association) | 0.350 |
| Rad21 | ZNF768 | psi-mi:“MI:0914”(association) | 0.350 |
| Cxxc1 | HCFC1 | psi-mi:“MI:0914”(association) | 0.350 |
| GEMIN7 | CSNK1D | psi-mi:“MI:0914”(association) | 0.350 |
| Cul3 | psi-mi:“MI:0914”(association) | 0.350 | |
| CUL3 | PXDNL | psi-mi:“MI:0914”(association) | 0.350 |
| AURKAIP1 | HNRNPR | psi-mi:“MI:0914”(association) | 0.350 |
| CHCHD2 | POLRMT | psi-mi:“MI:0914”(association) | 0.350 |
| CHCHD1 | ALDH1L1 | psi-mi:“MI:0914”(association) | 0.350 |
| PRSS35 | NDUFAB1 | psi-mi:“MI:0914”(association) | 0.350 |
| COQ2 | NME6 | psi-mi:“MI:0914”(association) | 0.350 |
| PRKRA | GTPBP10 | psi-mi:“MI:0914”(association) | 0.350 |
| MRPS25 | POLRMT | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (352): FAM9B (Two-hybrid), AURKAIP1 (Proximity Label-MS), AURKAIP1 (Affinity Capture-MS), AURKAIP1 (Affinity Capture-MS), AURKAIP1 (Affinity Capture-MS), AURKAIP1 (Affinity Capture-MS), AURKAIP1 (Affinity Capture-MS), AURKAIP1 (Affinity Capture-MS), MMADHC (Affinity Capture-MS), NRD1 (Affinity Capture-MS), NOA1 (Affinity Capture-MS), WDR83 (Affinity Capture-MS), STRBP (Affinity Capture-MS), NSUN4 (Affinity Capture-MS), MRPS18C (Affinity Capture-MS)
ESM2 similar proteins: A2A8U2, A6H773, A6QPI4, D4A6L0, E1BBQ2, O60232, P54098, Q05B67, Q08BI9, Q148E1, Q2KI76, Q2KJ58, Q2NL34, Q32Q90, Q4R4I0, Q5C9Z4, Q5RE99, Q5SNT2, Q5T6X4, Q5T848, Q5VUE5, Q5XIJ4, Q5ZLJ4, Q6DVA0, Q6P3B9, Q7T076, Q80YR4, Q86UK7, Q8C419, Q8CEG5, Q8IYL2, Q8N0V3, Q8NC56, Q8TBN0, Q8VDV3, Q8VE22, Q8VHV8, Q921N7, Q96IL0, Q96ND0
Diamond homologs: Q9DCJ7, Q9NWT8
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| AURKAIP1 | “form complex” | “28S mitochondrial small ribosomal subunit” | binding |
| AURKA | “up-regulates quantity by stabilization” | AURKAIP1 | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 56 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 |
|---|---|---|---|
| Mitochondrial ribosome-associated quality control | 6 | 19.4× | 9e-05 |
| Mitochondrial translation initiation | 5 | 16.7× | 4e-04 |
| Mitochondrial translation elongation | 5 | 16.7× | 4e-04 |
| Mitochondrial translation termination | 5 | 14.4× | 7e-04 |
| mRNA Splicing - Major Pathway | 6 | 8.6× | 2e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| mitochondrial translation | 5 | 18.5× | 2e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
35 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 0 |
| Uncertain significance | 29 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 393899 | GRCh37/hg19 1p36.33-36.32(chr1:19225-4401691)x3 | Pathogenic |
SpliceAI
1552 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 11:67483216:G:GT | donor_gain | 1.0000 |
| 11:67487001:CACA:C | acceptor_loss | 1.0000 |
| 11:67487003:CA:C | acceptor_loss | 1.0000 |
| 11:67487004:A:AG | acceptor_gain | 1.0000 |
| 11:67487004:AG:A | acceptor_gain | 1.0000 |
| 11:67487004:AGG:A | acceptor_loss | 1.0000 |
| 11:67487005:G:GG | acceptor_gain | 1.0000 |
| 11:67487005:GG:G | acceptor_gain | 1.0000 |
| 11:67487005:GGC:G | acceptor_gain | 1.0000 |
| 11:67487005:GGCC:G | acceptor_gain | 1.0000 |
| 11:67487005:GGCCA:G | acceptor_gain | 1.0000 |
| 11:67487104:G:GT | donor_gain | 1.0000 |
| 11:67487108:TTC:T | donor_gain | 1.0000 |
| 11:67487155:G:T | donor_gain | 1.0000 |
| 11:67487182:CAAG:C | donor_loss | 1.0000 |
| 11:67487183:AAG:A | donor_loss | 1.0000 |
| 11:67487184:AGG:A | donor_loss | 1.0000 |
| 11:67487186:G:GG | donor_loss | 1.0000 |
| 11:67489261:CCGCA:C | acceptor_loss | 1.0000 |
| 11:67489263:GCAG:G | acceptor_loss | 1.0000 |
| 11:67489264:CA:C | acceptor_loss | 1.0000 |
| 11:67489265:A:AC | acceptor_loss | 1.0000 |
| 11:67489265:A:AG | acceptor_gain | 1.0000 |
| 11:67489265:AGCAT:A | acceptor_gain | 1.0000 |
| 11:67489266:G:GG | acceptor_gain | 1.0000 |
| 11:67489266:GC:G | acceptor_gain | 1.0000 |
| 11:67489266:GCAT:G | acceptor_gain | 1.0000 |
| 11:67489266:GCATG:G | acceptor_gain | 1.0000 |
| 11:67489454:AGGT:A | donor_loss | 1.0000 |
| 11:67489455:GGTGA:G | donor_loss | 1.0000 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000297776 (1:1376957 G>A), RS1000639625 (1:1375720 G>C), RS1001558956 (1:1375854 G>A,C), RS1001885257 (1:1376068 C>T), RS1002260828 (1:1375124 G>A,C), RS1002291060 (1:1374851 G>A,C), RS1002719732 (1:1374956 TCCCAAG>T), RS1003151813 (1:1375057 G>C), RS1003793207 (1:1375082 G>A,C), RS1003845351 (1:1375300 C>T), RS1004203967 (1:1375163 G>A), RS1005849645 (1:1373298 T>C,G), RS1006150260 (1:1373346 C>T), RS1007108912 (1:1376905 G>A), RS1007372368 (1:1375517 G>A)
Disease associations
OMIM: gene MIM:609183 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004131_103 | Inflammatory bowel disease | 2.000000e-07 |
| GCST004133_40 | Ulcerative colitis | 3.000000e-06 |
| GCST005580_249 | Intraocular pressure | 1.000000e-10 |
| GCST005580_72 | Intraocular pressure | 1.000000e-11 |
| GCST006979_847 | Heel bone mineral density | 1.000000e-09 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004695 | intraocular pressure measurement |
| EFO:0009270 | heel bone mineral density |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5910 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 2,998 (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 |
|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | 2 | 2,998 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.22 | Ki | 0.6 | nM | TOZASERTIB |
| 5.10 | IC50 | 7943 | nM | CHEMBL520308 |
PubChem BioAssay actives
2 with measured affinity, of 3 total; 2 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 |
|---|---|---|---|---|
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 383102: Inhibition of Aurora A | ki | 0.0006 | uM |
| N-(2-hydroxyethyl)-N-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)benzenesulfonamide | 354259: Inhibition of Aurora A kinase | ic50 | 7.9433 | uM |
CTD chemical–gene interactions
21 total (human), top 21 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | affects cotreatment, increases abundance, increases expression | 3 |
| Valproic Acid | affects cotreatment, increases expression, increases methylation | 3 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | affects cotreatment, decreases methylation | 1 |
| arsenite | increases reaction, affects binding | 1 |
| manganese chloride | increases abundance, increases expression, affects cotreatment | 1 |
| chloropicrin | increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| Fulvestrant | affects cotreatment, decreases methylation | 1 |
| Air Pollutants | affects expression, increases abundance | 1 |
| Arsenic | increases expression, affects cotreatment, increases abundance | 1 |
| Atrazine | decreases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Dimethyl Sulfoxide | affects expression | 1 |
| Doxorubicin | increases expression | 1 |
| Hydralazine | affects cotreatment, increases expression | 1 |
| Manganese | increases abundance, increases expression, affects cotreatment | 1 |
| Ozone | affects expression, increases abundance | 1 |
| Smoke | decreases expression | 1 |
| Tretinoin | decreases expression | 1 |
| Cadmium Chloride | increases expression | 1 |
ChEMBL screening assays
2 unique, capped per target: 2 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL974017 | Binding | Inhibition of Aurora A | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. — Proc Natl Acad Sci U S A |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.