UBA2
gene geneOn this page
Also known as FLJ13058HRIHFB2115
Summary
UBA2 (ubiquitin like modifier activating enzyme 2, HGNC:30661) is a protein-coding gene on chromosome 19q13.11, encoding SUMO-activating enzyme subunit 2 (Q9UBT2). The heterodimer acts as an E1 ligase for SUMO1, SUMO2, SUMO3, and probably SUMO4. It is a common-essential gene (DepMap: required in 99.1% of cancer cell lines).
Posttranslational modification of proteins by the addition of the small protein SUMO (see SUMO1; MIM 601912), or sumoylation, regulates protein structure and intracellular localization. SAE1 (MIM 613294) and UBA2 form a heterodimer that functions as a SUMO-activating enzyme for the sumoylation of proteins (Okuma et al., 1999 [PubMed 9920803]).
Source: NCBI Gene 10054 — RefSeq curated summary.
At a glance
- Gene–disease (curated): ACCES syndrome (Definitive, ClinGen) — +1 more curated relationship
- GWAS associations: 4
- Clinical variants (ClinVar): 124 total — 12 pathogenic, 10 likely-pathogenic
- Phenotypes (HPO): 38
- Druggable target: yes — 3 molecules with ChEMBL bioactivity
- Cancer dependency (DepMap): dependent in 99.1% of screened cell lines (common-essential)
- MANE Select transcript:
NM_005499
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:30661 |
| Approved symbol | UBA2 |
| Name | ubiquitin like modifier activating enzyme 2 |
| Location | 19q13.11 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | FLJ13058, HRIHFB2115 |
| Ensembl gene | ENSG00000126261 |
| Ensembl biotype | protein_coding |
| OMIM | 613295 |
| Entrez | 10054 |
Gene structure
Transcript identifiers
Ensembl transcripts: 10 — 5 protein_coding, 2 nonsense_mediated_decay, 2 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000246548, ENST00000439527, ENST00000586313, ENST00000588585, ENST00000590048, ENST00000591016, ENST00000592672, ENST00000592791, ENST00000592841, ENST00000607361
RefSeq mRNA: 2 — MANE Select: NM_005499
NM_001411139, NM_005499
CCDS: CCDS12439, CCDS92583
Canonical transcript exons
ENST00000246548 — 17 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000862687 | 34428381 | 34428570 |
| ENSE00000862690 | 34433348 | 34433412 |
| ENSE00002813476 | 34469040 | 34471251 |
| ENSE00003468579 | 34451981 | 34452147 |
| ENSE00003496317 | 34458769 | 34458924 |
| ENSE00003500032 | 34443844 | 34443911 |
| ENSE00003504279 | 34434868 | 34434968 |
| ENSE00003595902 | 34430576 | 34430659 |
| ENSE00003601380 | 34454444 | 34454556 |
| ENSE00003608749 | 34460470 | 34460566 |
| ENSE00003660760 | 34438645 | 34438766 |
| ENSE00003664506 | 34445000 | 34445121 |
| ENSE00003669057 | 34431861 | 34431931 |
| ENSE00003682170 | 34454260 | 34454353 |
| ENSE00003695083 | 34464026 | 34464131 |
| ENSE00003701944 | 34466878 | 34467014 |
| ENSE00003791247 | 34450265 | 34450364 |
Expression profiles
Bgee: expression breadth ubiquitous, 204 present calls, max score 98.58.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 114.8419 / max 802.2854, expressed in 1827 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 175144 | 114.8419 | 1827 |
Top tissues by expression
249 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| ventricular zone | UBERON:0003053 | 98.58 | gold quality |
| embryo | UBERON:0000922 | 98.46 | gold quality |
| ganglionic eminence | UBERON:0004023 | 98.46 | gold quality |
| calcaneal tendon | UBERON:0003701 | 98.43 | gold quality |
| popliteal artery | UBERON:0002250 | 98.37 | gold quality |
| tibial artery | UBERON:0007610 | 98.37 | gold quality |
| cortical plate | UBERON:0005343 | 98.00 | gold quality |
| right coronary artery | UBERON:0001625 | 97.82 | gold quality |
| artery | UBERON:0001637 | 97.78 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 97.66 | gold quality |
| aorta | UBERON:0000947 | 97.63 | gold quality |
| left coronary artery | UBERON:0001626 | 97.34 | gold quality |
| adrenal tissue | UBERON:0018303 | 97.10 | gold quality |
| thoracic aorta | UBERON:0001515 | 97.08 | gold quality |
| ascending aorta | UBERON:0001496 | 97.06 | gold quality |
| islet of Langerhans | UBERON:0000006 | 97.02 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 96.95 | gold quality |
| gastrocnemius | UBERON:0001388 | 96.89 | gold quality |
| colonic epithelium | UBERON:0000397 | 96.74 | gold quality |
| muscle of leg | UBERON:0001383 | 96.74 | gold quality |
| right testis | UBERON:0004534 | 96.63 | gold quality |
| stromal cell of endometrium | CL:0002255 | 96.56 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 96.54 | gold quality |
| omental fat pad | UBERON:0010414 | 96.54 | gold quality |
| peritoneum | UBERON:0002358 | 96.45 | gold quality |
| left testis | UBERON:0004533 | 96.43 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 96.23 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 96.19 | gold quality |
| ectocervix | UBERON:0012249 | 96.10 | gold quality |
| cerebellar cortex | UBERON:0002129 | 96.08 | gold quality |
Single-cell (SCXA)
Detected in 7 experiment(s), a significant marker in 6.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-10287 | yes | 46.47 |
| E-HCAD-10 | yes | 40.20 |
| E-MTAB-8142 | yes | 36.85 |
| E-GEOD-134144 | yes | 28.39 |
| E-HCAD-11 | yes | 23.11 |
| E-ANND-3 | yes | 11.25 |
| E-CURD-112 | no | 2.20 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
45 targeting UBA2, 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-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-548AN | 99.97 | 70.91 | 2817 |
| HSA-MIR-302C-5P | 99.97 | 72.56 | 3642 |
| HSA-MIR-3910 | 99.95 | 71.13 | 2227 |
| HSA-MIR-3143 | 99.93 | 71.96 | 3104 |
| HSA-MIR-323A-3P | 99.79 | 70.30 | 1739 |
| HSA-MIR-204-5P | 99.79 | 71.62 | 2439 |
| HSA-MIR-211-5P | 99.79 | 71.65 | 2440 |
| HSA-MIR-5002-5P | 99.76 | 70.84 | 1763 |
| HSA-MIR-4446-5P | 99.72 | 69.19 | 2544 |
| HSA-MIR-4699-3P | 99.71 | 70.15 | 3142 |
| HSA-MIR-4755-5P | 99.71 | 70.34 | 2716 |
| HSA-MIR-5006-3P | 99.71 | 70.26 | 2728 |
| HSA-MIR-4729 | 99.69 | 72.18 | 4233 |
| HSA-MIR-586 | 99.65 | 70.40 | 2051 |
| HSA-MIR-1287-3P | 99.63 | 66.93 | 492 |
| HSA-MIR-3685 | 99.62 | 68.83 | 1621 |
| HSA-MIR-497-3P | 99.61 | 69.71 | 1990 |
| HSA-MIR-7844-5P | 99.55 | 68.56 | 1428 |
| HSA-MIR-510-3P | 99.54 | 70.06 | 2965 |
| HSA-MIR-543 | 99.52 | 69.03 | 2595 |
| HSA-MIR-4672 | 99.50 | 71.58 | 2893 |
| HSA-MIR-889-3P | 99.40 | 69.76 | 2103 |
| HSA-MIR-3160-5P | 99.28 | 69.07 | 1938 |
| HSA-MIR-133A-3P | 99.27 | 71.53 | 1270 |
| HSA-MIR-133B | 99.27 | 71.53 | 1270 |
| HSA-MIR-196A-3P | 99.19 | 67.34 | 1204 |
| HSA-MIR-1911-3P | 99.15 | 66.17 | 528 |
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 99.1% of screened cell lines, common-essential.
Literature-anchored findings (GeneRIF, showing 24)
- structures of heterodimeric Sae1/Sae2-Mg.ATP and Sae1/Sae2-SUMO-1-Mg.ATP complexes (PMID:15660128)
- UBA2 stabilizes APOBEC3G by preventing ubiquitin chain elongation and proteasome-mediated proteolysis. (PMID:18680593)
- The mammalian E1 subunits can be imported separately, identify nuclear localization signals (NLSs) in Aos1 and in Uba2, and demonstrate that their import is mediated by importin alpha/beta in vitro and in intact cells. (PMID:21209321)
- loss of SAE1/2 activity drives synthetic lethality with Myc; inactivation of SAE2 leads to mitotic catastrophe and cell death upon Myc hyperactivation; findings in Myc-high breast cancers suggest low tumor SAE1 and SAE2 correlates metastasis-free survival (PMID:22157079)
- Data show that the SAE2 subunit of the small ubiquitin-like modifier (SUMO) E1 is autoSUMOylated at residue Lys-236, and SUMOylation was catalyzed by Ubc9 at several additional Lys residues surrounding the catalytic Cys-173 of SAE2. (PMID:22403398)
- Data indicate the role of anti-SUMO activating enzyme SAE1 and SAE2 antibody as marker of dermatomyositis. (PMID:22884621)
- This study has identified the mechanism used to localize SAE to the nucleus. (PMID:23095757)
- Here, we show that hHR23A utilizes both the UBA2 and XPCB domains to form a stable complex with Vpr, linking Vpr directly to cellular DNA repair pathways and their probable exploitation by the virus. (PMID:24318982)
- We propose that disturbance of the SUMOylation pathway, mediated by pathogenic variants in UBA2, is a novel mechanism for aplasia cutis congenita and other phenotypic abnormalities. (PMID:28110515)
- Calcium/calpain-induced cleavage of the SAE2 leads to sumoylation inhibition reslting in bacillary dysentery. (PMID:29231810)
- the results suggest that Uba2 participates in the progression, invasion, and metastasis of colorectal cancer, and the possible mechanism is via regulating the Wnt signaling pathway and enhancing epithelial-mesenchymal transition behaviors of colorectal cancer cells. (PMID:29744931)
- The findings suggest that the UBA2-WTIP fusion is an oncogenic fusion gene, as well as a promising therapeutic target for the treatment of acute myeloid leukemia. (PMID:30179602)
- results from the present study indicated that UBA2 expression may enhance colorectal cancer cell proliferation and inhibit apoptosis. (PMID:30387828)
- Uba2 plays a vital role in gastric cancer cell migration and invasion, possibly by regulating the Wnt/beta-catenin signaling pathway and epithelial-mesenchymal transition. (PMID:30479464)
- Identifying UBA2 as a proliferation and cell cycle regulator in lung cancer A549 cells. (PMID:30848500)
- the results together with previous data such as the development of Split-hand/foot malformation (SHFM) in Lrp6 knockout mice, the presence of SHFM in two subjects with 19q13 deletions involving UBA2, and strong mouse Uba2 expression in the developing limb buds, imply that LRP6 and UBA2 represent plausible candidate genes for SHFM. (PMID:31332306)
- Increased SUMO-activating enzyme SAE1/UBA2 promotes glycolysis and pathogenic behavior of rheumatoid fibroblast-like synoviocytes. (PMID:32938830)
- UBA2 activates Wnt/beta-catenin signaling pathway during protection of R28 retinal precursor cells from hypoxia by extracellular vesicles derived from placental mesenchymal stem cells. (PMID:33008487)
- Targeting SUMOylation dependency in human cancer stem cells through a unique SAE2 motif revealed by chemical genomics. (PMID:33979648)
- UBA2 variants underlie a recognizable syndrome with variable aplasia cutis congenita and ectrodactyly. (PMID:34040189)
- Genome sequencing in families with congenital limb malformations. (PMID:34159400)
- UBA2 promotes the progression of renal cell carcinoma by suppressing the p53 signaling. (PMID:34467471)
- UBA2 as a Prognostic Biomarker and Potential Therapeutic Target in Glioma. (PMID:38682183)
- UBA2 SUMOylates NQO1 and promotes the proliferation of hepatocellular carcinoma by modulating the MAPK pathway. (PMID:39013843)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | uba2 | ENSDARG00000101332 |
| mus_musculus | Uba2 | ENSMUSG00000052997 |
| rattus_norvegicus | Uba2 | ENSRNOG00000021113 |
| drosophila_melanogaster | Uba2 | FBGN0029113 |
| caenorhabditis_elegans | uba-2 | WBGENE00006700 |
Paralogs (9): UBA6 (ENSG00000033178), UBA5 (ENSG00000081307), MOCS3 (ENSG00000124217), UBA1 (ENSG00000130985), SAE1 (ENSG00000142230), UBA3 (ENSG00000144744), NAE1 (ENSG00000159593), UBA7 (ENSG00000182179), ATG7 (ENSG00000197548)
Protein
Protein identifiers
SUMO-activating enzyme subunit 2 — Q9UBT2 (reviewed: Q9UBT2)
Alternative names: Anthracycline-associated resistance ARX, Ubiquitin-like 1-activating enzyme E1B, Ubiquitin-like modifier-activating enzyme 2
All UniProt accessions (6): Q9UBT2, K7EPL2, K7ES38, K7ESK7, U3KQ55, U3KQ93
UniProt curated annotations — full annotation on UniProt →
Function. The heterodimer acts as an E1 ligase for SUMO1, SUMO2, SUMO3, and probably SUMO4. It mediates ATP-dependent activation of SUMO proteins followed by formation of a thioester bond between a SUMO protein and a conserved active site cysteine residue on UBA2/SAE2.
Subunit / interactions. Heterodimer of SAE1 and UBA2/SAE2. The heterodimer corresponds to the two domains that are encoded on a single polypeptide chain in ubiquitin-activating enzyme E1. Interacts with UBE2I.
Subcellular location. Cytoplasm. Nucleus.
Post-translational modifications. Sumoylated with SUMO1 and SUMO2/3 and by UBC9. Sumoylation at Lys-236 inhibits enzymatic activity. Sumoylation at the C-terminal lysine cluster plays an essential role in nuclear trafficking.
Disease relevance. ACCES syndrome (ACCES) [MIM:619959] An autosomal dominant syndrome characterized by a highly variable phenotypic spectrum. Clinical features include aplasia cutis congenita, thin scalp hair, dry skin, dental anomalies, ectrodactyly, and skeletal and neurodevelopmental abnormalities. Craniofacial, cardiac, renal and genital anomalies have also been reported. Affected individuals have early growth deficiencies that improve with age. The disease is caused by variants affecting the gene represented in this entry.
Pathway. Protein modification; protein sumoylation.
Similarity. Belongs to the ubiquitin-activating E1 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9UBT2-1 | 1 | yes |
| Q9UBT2-2 | 2 |
RefSeq proteins (2): NP_001398068, NP_005490* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000594 | ThiF_NAD_FAD-bd | Domain |
| IPR018074 | UBQ-activ_enz_E1_CS | Conserved_site |
| IPR023318 | Ub_act_enz_dom_a_sf | Homologous_superfamily |
| IPR028077 | UAE_UbL_dom | Domain |
| IPR030661 | Uba2 | Family |
| IPR032426 | UBA2_C | Domain |
| IPR033127 | UBQ-activ_enz_E1_Cys_AS | Active_site |
| IPR035985 | Ubiquitin-activating_enz | Homologous_superfamily |
| IPR042449 | Ub-E1_IAD_1 | Homologous_superfamily |
| IPR045886 | ThiF/MoeB/HesA | Family |
Pfam: PF00899, PF14732, PF16195
UniProt features (126 total): helix 28, strand 24, cross-link 16, mutagenesis site 12, binding site 10, turn 10, sequence variant 7, compositionally biased region 6, modified residue 5, sequence conflict 3, region of interest 2, chain 1, splice variant 1, active site 1
Structure
Experimental structures (PDB)
16 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9QN5 | X-RAY DIFFRACTION | 1.97 |
| 6XOG | X-RAY DIFFRACTION | 1.98 |
| 6XOI | X-RAY DIFFRACTION | 2 |
| 5FQ2 | X-RAY DIFFRACTION | 2.2 |
| 6XOH | X-RAY DIFFRACTION | 2.23 |
| 1Y8Q | X-RAY DIFFRACTION | 2.25 |
| 3KYC | X-RAY DIFFRACTION | 2.45 |
| 6CWY | X-RAY DIFFRACTION | 2.46 |
| 4W5V | X-RAY DIFFRACTION | 2.5 |
| 9IF6 | X-RAY DIFFRACTION | 2.51 |
| 3KYD | X-RAY DIFFRACTION | 2.61 |
| 9DRJ | ELECTRON MICROSCOPY | 2.7 |
| 1Y8R | X-RAY DIFFRACTION | 2.75 |
| 6CWZ | X-RAY DIFFRACTION | 3.1 |
| 9DQB | ELECTRON MICROSCOPY | 3.6 |
| 2PX9 | SOLUTION NMR |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UBT2-F1 | 85.72 | 0.67 |
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): 173 (glycyl thioester intermediate)
Ligand- & substrate-binding residues (10): 24–29; 48; 56–59; 72; 95–96; 117–122; 158; 161; 441; 444
Post-translational modifications (21): 207, 271, 507, 592, 613, 164, 190, 236, 236, 257, 257, 271, 275, 371, 420, 420, 540, 611, 613, 617 …
Mutagenesis-validated functional residues (12):
| Position | Phenotype |
|---|---|
| 56 | abolishes atp-dependent activation of sumo proteins. |
| 57 | strongly reduces atp-dependent activation of sumo proteins. |
| 59 | strongly reduces atp-dependent activation of sumo proteins. |
| 72 | abolishes atp-dependent activation of sumo proteins. |
| 117 | abolishes atp-dependent activation of sumo proteins. |
| 173 | loss of enzyme activity. |
| 174 | slightly reduced enzyme activity. |
| 184 | no effect on enzyme activity. |
| 235 | strongly reduced interaction with ube2i; when associated with a-238. |
| 238 | strongly reduced interaction with ube2i; when associated with a-235. |
| 484 | strongly reduced interaction with ube2i. |
| 485 | strongly reduced interaction with ube2i. |
Function
Pathways and Gene Ontology
Reactome pathways
6 pathways
| ID | Pathway |
|---|---|
| R-HSA-3065676 | SUMO is conjugated to E1 (UBA2:SAE1) |
| R-HSA-3065678 | SUMO is transferred from E1 to E2 (UBE2I, UBC9) |
| R-HSA-2990846 | SUMOylation |
| R-HSA-3215018 | Processing and activation of SUMO |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-597592 | Post-translational protein modification |
MSigDB gene sets: 307 (showing top):
BORCZUK_MALIGNANT_MESOTHELIOMA_UP, MORF_SMC1L1, GOBP_REGULATION_OF_PROTEIN_SUMOYLATION, MORF_UBE2I, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, MORF_HDAC1, MORF_UBE2N, MORF_RAD21, MORF_HDAC2, CTATGCA_MIR153, ATGTTAA_MIR302C, PATIL_LIVER_CANCER, PUJANA_CHEK2_PCC_NETWORK, GOBP_PEPTIDYL_LYSINE_MODIFICATION, MORF_SKP1A
GO Biological Process (2): protein sumoylation (GO:0016925), positive regulation of protein sumoylation (GO:0033235)
GO Molecular Function (12): magnesium ion binding (GO:0000287), ATP binding (GO:0005524), transferase activity (GO:0016740), SUMO activating enzyme activity (GO:0019948), SUMO binding (GO:0032183), small protein activating enzyme binding (GO:0044388), ubiquitin-like protein conjugating enzyme binding (GO:0044390), protein heterodimerization activity (GO:0046982), nucleotide binding (GO:0000166), protein binding (GO:0005515), ubiquitin-like modifier activating enzyme activity (GO:0008641), metal ion binding (GO:0046872)
GO Cellular Component (5): nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytoplasm (GO:0005737), SUMO activating enzyme complex (GO:0031510), nucleus (GO:0005634)
Reactome top-level categories
Rollup of top-4 pathways:
| Category | Pathways |
|---|---|
| Processing and activation of SUMO | 2 |
| Post-translational protein modification | 1 |
| SUMOylation | 1 |
| Metabolism of proteins | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| enzyme binding | 2 |
| nuclear lumen | 2 |
| cellular anatomical structure | 2 |
| peptidyl-lysine modification | 1 |
| protein modification by small protein conjugation | 1 |
| protein sumoylation | 1 |
| regulation of protein sumoylation | 1 |
| positive regulation of protein modification by small protein conjugation or removal | 1 |
| metal ion binding | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| catalytic activity | 1 |
| ubiquitin-like modifier activating enzyme activity | 1 |
| ubiquitin-like protein binding | 1 |
| protein dimerization activity | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| ligase activity, forming carbon-sulfur bonds | 1 |
| catalytic activity, acting on a protein | 1 |
| ATP-dependent activity | 1 |
| cation binding | 1 |
| intracellular membraneless organelle | 1 |
| intracellular anatomical structure | 1 |
| nuclear protein-containing complex | 1 |
| catalytic complex | 1 |
| intracellular membrane-bounded organelle | 1 |
Protein interactions and networks
STRING
3476 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| UBA2 | UBE2I | P50550 | 993 |
| UBA2 | SAE1 | Q9UBE0 | 993 |
| UBA2 | SUMO1 | P55856 | 971 |
| UBA2 | SUMO2 | P55855 | 945 |
| UBA2 | RANGAP1 | P46060 | 908 |
| UBA2 | RAD23A | P54725 | 855 |
| UBA2 | SENP1 | Q9P0U3 | 851 |
| UBA2 | NEDD8 | Q15843 | 810 |
| UBA2 | PIAS3 | Q9Y6X2 | 776 |
| UBA2 | PIAS2 | O75928 | 772 |
| UBA2 | LSM14A | Q8ND56 | 771 |
| UBA2 | SENP3 | Q9H4L4 | 744 |
| UBA2 | NSMCE2 | Q96MF7 | 737 |
| UBA2 | RANBP2 | P49792 | 720 |
| UBA2 | USP5 | P45974 | 718 |
IntAct
83 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| UBA2 | SAE1 | psi-mi:“MI:0407”(direct interaction) | 0.950 |
| SAE1 | UBA2 | psi-mi:“MI:0407”(direct interaction) | 0.950 |
| UBA2 | SAE1 | psi-mi:“MI:0915”(physical association) | 0.950 |
| SAE1 | UBA2 | psi-mi:“MI:0915”(physical association) | 0.950 |
| SUMO1 | UBA2 | psi-mi:“MI:0915”(physical association) | 0.850 |
| UBA2 | SUMO1 | psi-mi:“MI:0915”(physical association) | 0.850 |
| UBA2 | SUMO1 | psi-mi:“MI:0407”(direct interaction) | 0.850 |
| UBE2I | UBA2 | psi-mi:“MI:0407”(direct interaction) | 0.850 |
| UBA2 | UBE2I | psi-mi:“MI:0566”(sumoylation reaction) | 0.850 |
| UBE2I | UBA2 | psi-mi:“MI:0566”(sumoylation reaction) | 0.850 |
| SAE1 | SUMO1 | psi-mi:“MI:0915”(physical association) | 0.730 |
| CFTR | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.710 |
| CFTR | ESYT2 | psi-mi:“MI:0914”(association) | 0.710 |
| SUMO1P1 | UBA2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| UBA2 | SUMO1P1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MEOX2 | UBA2 | psi-mi:“MI:0915”(physical association) | 0.560 |
BioGRID (327): UBA2 (Two-hybrid), SUMO1P1 (Two-hybrid), UBE2I (Biochemical Activity), SUMO1 (Reconstituted Complex), UBE2I (Biochemical Activity), SAE1 (Two-hybrid), FOXK1 (Co-fractionation), PSMA3 (Co-fractionation), PSMA4 (Co-fractionation), PSMB3 (Co-fractionation), SAE1 (Co-fractionation), UBA2 (Co-fractionation), UBA2 (Co-fractionation), UBA2 (Co-fractionation), UBA2 (Co-fractionation)
ESM2 similar proteins: A0A0G2KTI4, A0A7U2QYM2, O00763, O55236, O60942, P10687, P10894, P29074, P48722, P55014, P55015, P91926, P97789, Q03330, Q07722, Q13621, Q15147, Q28BT8, Q28EX9, Q28GH3, Q29N38, Q338B9, Q4V7N2, Q59WH0, Q641F1, Q642Q1, Q66HV4, Q6DI37, Q6H8D6, Q6NY98, Q6YXZ7, Q756G9, Q7QG73, Q7SXG4, Q7ZVX6, Q7ZY60, Q8BPM2, Q8C878, Q8WZM0, Q924I2
Diamond homologs: A1A4L8, A1CAZ7, A1DED8, A2BDX3, A2R3H4, A3ACF3, A3LQF9, A4RPM5, A5DMB6, A5DSR2, A5GFZ6, A6ZT19, A7F582, A7THV5, A8WRE3, B0W377, B0WQV1, B0Y0P7, B3LSM6, B3MLX7, B3NUC9, B4FAT0, B4GKQ3, B4HYP0, B4IK21, B4JBC4, B4JIY0, B4KI53, B4L1K2, B4LRB9, B4M357, B4N7R4, B4NXF7, B4PYA4, B4R345, B5DS72, B5VK45, B6TNK6, D1GY43, D4GSF3
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| UBA2 | “form complex” | “SAE1/SAE2 complex” | binding |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 64 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 |
|---|---|---|---|
| SUMOylation of SUMOylation proteins | 5 | 37.1× | 2e-05 |
| SUMOylation of RNA binding proteins | 6 | 32.4× | 3e-06 |
| SUMOylation of DNA replication proteins | 5 | 28.2× | 4e-05 |
| SUMOylation of transcription cofactors | 5 | 27.6× | 4e-05 |
| SUMOylation of DNA damage response and repair proteins | 7 | 23.3× | 3e-06 |
| SUMOylation of chromatin organization proteins | 6 | 21.6× | 2e-05 |
| SARS-CoV-2 activates/modulates innate and adaptive immune responses | 6 | 12.2× | 2e-04 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
124 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 12 |
| Likely pathogenic | 10 |
| Uncertain significance | 68 |
| Likely benign | 5 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (22)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1696427 | NM_005499.3(UBA2):c.1324dup (p.Tyr442fs) | Pathogenic |
| 1696428 | NM_005499.3(UBA2):c.327del (p.Phe109fs) | Pathogenic |
| 1696429 | NM_005499.3(UBA2):c.612del (p.Glu205fs) | Pathogenic |
| 1801368 | NM_005499.3(UBA2):c.1118del (p.Arg373fs) | Pathogenic |
| 3024531 | NM_005499.3(UBA2):c.649+1G>A | Pathogenic |
| 3064270 | NM_005499.3(UBA2):c.460-2A>G | Pathogenic |
| 3375345 | NM_005499.3(UBA2):c.336dup (p.Met113fs) | Pathogenic |
| 3767658 | NM_005499.3(UBA2):c.650-1G>C | Pathogenic |
| 521193 | NM_005499.3(UBA2):c.816_817del (p.Trp273fs) | Pathogenic |
| 523936 | NM_005499.3(UBA2):c.1376dup (p.Thr460fs) | Pathogenic |
| 654989 | NM_005499.3(UBA2):c.364C>T (p.Arg122Ter) | Pathogenic |
| 977797 | NM_005499.3(UBA2):c.800T>A (p.Leu267Ter) | Pathogenic |
| 2584538 | NM_005499.3(UBA2):c.1173_1174dup (p.Ala392fs) | Likely pathogenic |
| 3349701 | NM_005499.3(UBA2):c.806del (p.Met269fs) | Likely pathogenic |
| 3370512 | NM_005499.3(UBA2):c.319C>T (p.Arg107Ter) | Likely pathogenic |
| 4086135 | NM_005499.3(UBA2):c.582-1G>C | Likely pathogenic |
| 4280641 | NM_005499.3(UBA2):c.1038+1G>A | Likely pathogenic |
| 4527602 | NM_005499.3(UBA2):c.357_358del (p.Arg119fs) | Likely pathogenic |
| 4796799 | NM_005499.3(UBA2):c.439C>T (p.Gln147Ter) | Likely pathogenic |
| 4819087 | NM_005499.3(UBA2):c.149A>G (p.Asp50Gly) | Likely pathogenic |
| 979177 | NM_005499.3(UBA2):c.167A>C (p.Asn56Thr) | Likely pathogenic |
| 979178 | NM_005499.3(UBA2):c.1447G>A (p.Glu483Lys) | Likely pathogenic |
SpliceAI
2531 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 19:34428568:CTGGT:C | donor_loss | 1.0000 |
| 19:34428571:GTGA:G | donor_loss | 1.0000 |
| 19:34428572:T:G | donor_loss | 1.0000 |
| 19:34431929:G:GT | donor_gain | 1.0000 |
| 19:34431929:GAA:G | donor_gain | 1.0000 |
| 19:34431932:G:GG | donor_gain | 1.0000 |
| 19:34431942:G:GG | donor_gain | 1.0000 |
| 19:34433346:A:AG | acceptor_gain | 1.0000 |
| 19:34433347:G:GG | acceptor_gain | 1.0000 |
| 19:34433347:GCCCT:G | acceptor_gain | 1.0000 |
| 19:34434860:A:AG | acceptor_gain | 1.0000 |
| 19:34434863:TCCA:T | acceptor_loss | 1.0000 |
| 19:34434866:A:AG | acceptor_gain | 1.0000 |
| 19:34434866:AGCT:A | acceptor_gain | 1.0000 |
| 19:34434867:G:GT | acceptor_gain | 1.0000 |
| 19:34434867:GC:G | acceptor_gain | 1.0000 |
| 19:34434867:GCT:G | acceptor_gain | 1.0000 |
| 19:34434867:GCTG:G | acceptor_gain | 1.0000 |
| 19:34434867:GCTGC:G | acceptor_gain | 1.0000 |
| 19:34434955:C:G | donor_gain | 1.0000 |
| 19:34434966:AAGGT:A | donor_loss | 1.0000 |
| 19:34434967:AGGTA:A | donor_loss | 1.0000 |
| 19:34434968:GGTAA:G | donor_loss | 1.0000 |
| 19:34434969:G:GA | donor_loss | 1.0000 |
| 19:34434969:G:GG | donor_gain | 1.0000 |
| 19:34434970:T:A | donor_loss | 1.0000 |
| 19:34438767:G:GG | donor_gain | 1.0000 |
| 19:34443843:GCCA:G | acceptor_gain | 1.0000 |
| 19:34443907:TGCCT:T | donor_gain | 1.0000 |
| 19:34443908:GCCT:G | donor_gain | 1.0000 |
AlphaMissense
4243 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 19:34428502:G:A | G24R | 1.000 |
| 19:34428502:G:C | G24R | 1.000 |
| 19:34428502:G:T | G24W | 1.000 |
| 19:34430585:G:C | D50H | 1.000 |
| 19:34430586:A:C | D50A | 1.000 |
| 19:34430586:A:T | D50V | 1.000 |
| 19:34430587:T:A | D50E | 1.000 |
| 19:34430587:T:G | D50E | 1.000 |
| 19:34430591:A:T | I52F | 1.000 |
| 19:34430592:T:A | I52N | 1.000 |
| 19:34430600:A:C | S55R | 1.000 |
| 19:34430602:C:A | S55R | 1.000 |
| 19:34430602:C:G | S55R | 1.000 |
| 19:34430603:A:G | N56D | 1.000 |
| 19:34430605:C:A | N56K | 1.000 |
| 19:34430605:C:G | N56K | 1.000 |
| 19:34430607:T:A | L57H | 1.000 |
| 19:34430607:T:C | L57P | 1.000 |
| 19:34430611:C:A | N58K | 1.000 |
| 19:34430611:C:G | N58K | 1.000 |
| 19:34430612:A:G | R59G | 1.000 |
| 19:34430613:G:C | R59T | 1.000 |
| 19:34430613:G:T | R59I | 1.000 |
| 19:34430614:A:C | R59S | 1.000 |
| 19:34430614:A:T | R59S | 1.000 |
| 19:34430617:G:C | Q60H | 1.000 |
| 19:34430617:G:T | Q60H | 1.000 |
| 19:34430618:T:C | F61L | 1.000 |
| 19:34430619:T:C | F61S | 1.000 |
| 19:34430620:T:A | F61L | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000087071 (19:34467663 C>G), RS1000090604 (19:34463058 C>G,T), RS1000094275 (19:34428683 G>T), RS1000145096 (19:34456344 C>T), RS1000164033 (19:34444732 A>G), RS1000234210 (19:34440140 A>C,G), RS1000341773 (19:34468511 T>C,G), RS1000352764 (19:34439488 C>G), RS1000433483 (19:34428665 C>T), RS1000487870 (19:34427478 T>C), RS1000531677 (19:34457794 G>T), RS1000579087 (19:34449380 C>T), RS1000585031 (19:34451715 T>A), RS1000702554 (19:34464884 T>C,G), RS1000818715 (19:34458700 A>G)
Disease associations
OMIM: gene MIM:613295 | disease phenotypes: MIM:619959, MIM:613026, MIM:183600
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| ACCES syndrome | Definitive | Autosomal dominant |
| multiple congenital anomalies/dysmorphic syndrome | Strong | Autosomal dominant |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| ACCES syndrome | Definitive | AD |
Mondo (4): ACCES syndrome (MONDO:0859262), chromosome 19q13.11 deletion syndrome, distal (MONDO:0700107), split hand-foot malformation (MONDO:0016576), multiple congenital anomalies/dysmorphic syndrome (MONDO:0019042)
Orphanet (1): Isolated split hand-split foot malformation (Orphanet:2440)
HPO phenotypes
38 total (30 of 38 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0000085 | Horseshoe kidney |
| HP:0000278 | Retrognathia |
| HP:0000348 | High forehead |
| HP:0000369 | Low-set ears |
| HP:0000411 | Protruding ear |
| HP:0000486 | Strabismus |
| HP:0000729 | Autistic behavior |
| HP:0000750 | Delayed speech and language development |
| HP:0001057 | Aplasia cutis congenita |
| HP:0001263 | Global developmental delay |
| HP:0001270 | Motor delay |
| HP:0001362 | Calvarial skull defect |
| HP:0001385 | Hip dysplasia |
| HP:0001508 | Failure to thrive |
| HP:0001770 | Toe syndactyly |
| HP:0001839 | Split foot |
| HP:0002205 | Recurrent respiratory infections |
| HP:0002209 | Sparse scalp hair |
| HP:0002558 | Supernumerary nipple |
| HP:0002575 | Tracheoesophageal fistula |
| HP:0002827 | Hip dislocation |
| HP:0003010 | Prolonged bleeding time |
| HP:0003577 | Congenital onset |
| HP:0004209 | Clinodactyly of the 5th finger |
| HP:0004348 | Abnormality of bone mineral density |
| HP:0004471 | Aplasia cutis congenita over the scalp vertex |
| HP:0006101 | Finger syndactyly |
| HP:0007383 | Congenital localized absence of skin |
| HP:0007385 | Aplasia cutis congenita of scalp |
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST009391_387 | Metabolite levels | 5.000000e-06 |
| GCST009391_543 | Metabolite levels | 3.000000e-06 |
| GCST009391_885 | Metabolite levels | 7.000000e-06 |
| GCST009391_958 | Metabolite levels | 3.000000e-06 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0010437 | triacylglycerol 58:10 measurement |
| EFO:0010439 | triacylglycerol 58:12 measurement |
| EFO:0010444 | triacylglycerol 60:12 measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (3): CHEMBL1615389 (SINGLE PROTEIN), CHEMBL2095174 (PROTEIN COMPLEX), CHEMBL3137290 (PROTEIN COMPLEX)
Molecules with ChEMBL bioactivity
3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 41,249 (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 |
|---|---|---|---|
| CHEMBL1231160 | PEVONEDISTAT | 3 | 1,480 |
| CHEMBL33864 | LIPOIC ACID, ALPHA | 3 | 19,339 |
| CHEMBL269277 | BETULINIC ACID | 1 | 20,430 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
36 measured of 134 human assays (135 total across all organisms); most potent 36 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| MLS000079917 | EC50 | 0.0133 nM | |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-phenylpyrazolo[1,5-a]pyrimidin-7- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-[(1R,2R,3S,4R)-2,3-dihydroxy-4-{[2-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-[(1R,2R,3S,4R)-4-{[2-(2,4-dichlorophenyl)pyrazolo[1,5-a]pyrimidin-7-yl]amino}- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(2-(3,3-dimethyl-2,3-dihydrobenzofuran-7-yl)pyrazolo[1,5- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(quinolin-3-yl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-Dihydroxy-4-((2-(3-phenoxyphenyl)pyrazolo[1,5- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(2-(trifluoromethyl)pyridin-4- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-Dihydroxy-4-((2-(5-(trifluoromethyl)thiophen-2- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(6-(trifluoromethyl)pyridin-2- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(2-phenoxyphenyl)pyrazolo[1,5- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(2-(3-benzylpenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)-2,3- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(2-(3-benzoylphenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-[(1R,2R,3S,4R)-2,3-dihydroxy-4-{[2-(1H-indol-5-yl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(2-(trifluoromethylthio)phenyl)pyrazolo[1,5- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(4-(trifluoromethylthio)phenyl)pyrazolo[1,5- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(2-(6-chlorobenzo[b]thiophen-2-yl)pyrazolo[1,5-a]pyrimidin- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(2-(5-ethylbenzo[b]thiophen-2-yl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (s.e.)-((1R,2R,3S,4R)-4-(2-(2,4-dichloronaphthalen-1-yl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 55 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-{(1R,2R,3S,4R)-2,3-dihydroxy-4-[(5-methyl-2-phenylpyrazolo[1,5-a]pyrimidin- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-{(1R,2R,3S,4R)-4-[(5-chloro-2-phenylpyrazolo[1,5-a]pyrimidin-7-yl)amino]-2,3- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(2-(4-bromophenyl)-5-chloropyrazolo[1,5-a]pyrimidin-7- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-{[5-chloro-2-(1-naphthyl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-((1R,2R,3S,4R)-4-(5-chloro-2-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidin-7- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-[(1R,2R,3S,4R)-4-{[5-chloro-2-(4-methoxyphenyl)pyrazolo[1,5-a]-pyrimidin-7- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (rac)-{(1R,2R,3S,4R)-2,3-dihydroxy-4-[(6-methyl-2-phenylpyrazolo[1,5-a]pyrimidin- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (s.e.)-{(1R,2R,3S,4R)-4-[(3,6-dichloro-2-{3- | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| (s.e.)-{(1R,2R,3S,4R)-4-[(6-chloro-2-{3-[(trifluoromethyl)sulfanyl]phenyl}pyrazolo[1, | IC50 | 550 nM | US-9796725: Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| 1-benzyl-N-butyl-2-[(2-chlorobenzoyl)amino]pyrrolo[3,2-b]quinoxaline-3-carboxamide | IC50 | 1100 nM | US-9045483: Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines |
| MLS000588669 | IC50 | 1610 nM | |
| N-(1-butyl-3-cyano-6,7-dimethylpyrrolo[3,2-b]quinoxalin-2-yl)-4-chlorobenzamide | IC50 | 4500 nM | US-9045483: Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines |
| N-(1-butyl-3-cyanopyrrolo[3,2-b]quinoxalin-2-yl)furan-2-carboxamide | IC50 | 5700 nM | US-9045483: Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines |
| MLS000068755 | IC50 | 6150 nM | |
| MLS000054842 | IC50 | 23500 nM | |
| 3-(benzenesulfonyl)-1-butylpyrrolo[3,2-b]quinoxalin-2-amine | IC50 | 64000 nM | US-9045483: Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines |
| N-[3-(benzenesulfonyl)-1-butylpyrrolo[3,2-b]quinoxalin-2-yl]benzamide | IC50 | 98000 nM | US-9045483: Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines |
ChEMBL bioactivities
490 potent at pChembl≥5 of 853 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.00 | IC50 | 0.1 | nM | CHEMBL4878832 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL4858933 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4860263 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4854038 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4864361 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4850183 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4873487 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL4848442 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL4852516 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL4860917 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL4848140 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL4870385 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL4877684 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL4856793 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL4848114 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL4873956 |
| 9.30 | IC50 | 0.5 | nM | CHEMBL4861509 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL4847817 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL4864280 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL4874906 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL4862248 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL4856040 |
| 9.00 | IC50 | 1 | nM | CHEMBL4878088 |
| 9.00 | IC50 | 1 | nM | CHEMBL4870143 |
| 9.00 | IC50 | 1 | nM | CHEMBL4853360 |
| 9.00 | IC50 | 1 | nM | CHEMBL4860263 |
| 9.00 | IC50 | 1 | nM | CHEMBL4849766 |
| 9.00 | IC50 | 1 | nM | CHEMBL4862901 |
| 9.00 | IC50 | 1 | nM | CHEMBL4865157 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL4865787 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL4861240 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL4862322 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL4860960 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL4855964 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL4862248 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL4851718 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL4866755 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL4860740 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL4862587 |
| 8.70 | IC50 | 2 | nM | CHEMBL4865086 |
| 8.70 | IC50 | 2 | nM | CHEMBL4852740 |
| 8.70 | IC50 | 2 | nM | CHEMBL4866614 |
| 8.68 | IC50 | 2.1 | nM | CHEMBL4869144 |
| 8.64 | IC50 | 2.3 | nM | CHEMBL4860471 |
| 8.60 | IC50 | 2.5 | nM | CHEMBL4861656 |
| 8.54 | IC50 | 2.9 | nM | CHEMBL4859486 |
| 8.52 | IC50 | 3 | nM | CHEMBL4867650 |
| 8.52 | IC50 | 3 | nM | CHEMBL4856793 |
| 8.49 | IC50 | 3.2 | nM | CHEMBL4866833 |
| 8.44 | IC50 | 3.6 | nM | CHEMBL4872222 |
PubChem BioAssay actives
182 with measured affinity, of 258 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 |
|---|---|---|---|---|
| [(1R,2R,3S,4R)-4-[[5-[4-[1-(6-bromo-2-pyridinyl)-1-hydroxyethyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2,3-dihydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0001 | uM |
| [(1R,2S,4R)-4-[[5-[4-(2-chloro-6,8-dihydro-5H-pyrano[3,4-b]pyridin-8-yl)-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0001 | uM |
| [(1R,2S,4R)-4-[[5-[5-chloro-4-[(6-chloro-2-pyridinyl)-hydroxymethyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0002 | uM |
| [(1R,2S,4R)-4-[[5-[4-[1-(3-chlorophenyl)-1-hydroxyethyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0002 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(3-chlorophenyl)-hydroxymethyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0002 | uM |
| [(1R,2S,4R)-4-[[5-[4-[amino-(3-chlorophenyl)methyl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0002 | uM |
| [(1R,2S,4R)-4-[[5-[4-(6,8-dihydro-5H-pyrano[3,4-b]pyridin-8-yl)-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0002 | uM |
| [(1R,2S,4R)-4-[[5-[4-(3,4-dihydro-1H-isochromen-1-yl)-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0003 | uM |
| [(1R,2S,4R)-4-[[5-[5-chloro-4-[(3-chlorophenyl)-hydroxymethyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0003 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(3-chlorophenyl)-hydroxymethyl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0003 | uM |
| [(1R,2S,4R)-4-[[5-[4-[1-amino-1-(3-chlorophenyl)ethyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0003 | uM |
| [(1R,2S,4R)-4-[[5-[5-chloro-4-(7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0004 | uM |
| [(1R,2S,4R)-4-[[5-[4-(7-chloro-3,4-dihydro-1H-isochromen-1-yl)-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0004 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(1R)-3,4-dihydro-1H-isochromen-1-yl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0004 | uM |
| [(1R,2S,4R)-4-[[5-[4-[amino-(3-chlorophenyl)methyl]-5-chlorothiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0004 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(3-bromophenyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0004 | uM |
| [(1R,2S,4R)-4-[[5-[4-(7-chloro-3,4-dihydro-1H-isochromen-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0005 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(3-bromophenyl)methyl]pyrrole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0006 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(6-bromo-2-pyridinyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0007 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(3-chlorophenyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0007 | uM |
| [(1R,2S,4R)-4-[[5-[4-[amino-(3-chlorophenyl)methyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0007 | uM |
| [(1R,2S,4R)-4-[[5-[4-(7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0008 | uM |
| [(1R,2R,3S,4R)-4-[[5-(1-benzylpyrazole-3-carbonyl)pyrimidin-4-yl]amino]-2,3-dihydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0010 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(1R)-7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0010 | uM |
| [(1R,2S,4R)-4-[[5-[5-chloro-4-(7-chloro-3,4-dihydro-1H-isochromen-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0010 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(3-chlorophenyl)methyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0010 | uM |
| [(1R,2S,4R)-2-hydroxy-4-[[5-[4-(1,2,3,4-tetrahydroisoquinolin-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]cyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0010 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(6-chloro-2-pyridinyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0010 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(5-chlorofuran-2-yl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0011 | uM |
| [(1R,2S,4R)-2-hydroxy-4-[[5-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]cyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0011 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(3-ethynylphenyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0011 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(3-chlorophenyl)methyl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0012 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(3-bromophenyl)methyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0013 | uM |
| [(1R,2S,4R)-4-[[5-[4-(6-chloro-2,3-dihydro-1H-isoindol-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0016 | uM |
| [(1R,2S,4R)-4-[[5-(1-benzylpyrrole-3-carbonyl)pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0017 | uM |
| [(1R,2S,4R)-2-hydroxy-4-[[5-[1-[(3-methylphenyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]cyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0017 | uM |
| [(1R,2S,4R)-4-[[5-[4-(5-chloro-3,4-dihydro-1H-isochromen-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0017 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(5-chlorothiophen-2-yl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0020 | uM |
| [(1R,2S,4R)-4-[[5-(1-benzylpyrazole-3-carbonyl)pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0020 | uM |
| [(1R,2S,4R)-4-[[5-[5-[(3-bromophenyl)methyl]furan-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0020 | uM |
| [(1R,2S,4R)-2-hydroxy-4-[[5-[1-[[3-(trifluoromethoxy)phenyl]methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]cyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0021 | uM |
| [(1R,2R,3R,4R)-4-[[5-(1-benzylpyrazole-3-carbonyl)pyrimidin-4-yl]amino]-3-fluoro-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0023 | uM |
| [(1R,2S,4R)-4-[[5-[4-(7-chloro-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0025 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(3-fluorophenyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0029 | uM |
| [(1R,2S,4R)-4-[[5-[5-chloro-4-(6-chloro-1,3-dihydro-2-benzofuran-1-yl)thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0030 | uM |
| [(1R,2S,4R)-4-[[5-[1-[(2-chlorophenyl)methyl]pyrazole-3-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0032 | uM |
| [(1R,2S,4R)-4-[[5-[5-chloro-4-[(3-chlorophenyl)methyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0036 | uM |
| [(1R,2S,4R)-4-[[5-[4-[(3-chlorophenyl)-(methylamino)methyl]thiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0037 | uM |
| [(1R,2R,3S,4R)-4-[[5-(1-benzylpyrazole-3-carbonyl)pyrimidin-4-yl]amino]-3-fluoro-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0038 | uM |
| [(1R,2R,4R)-4-[[5-(1-benzylpyrazole-3-carbonyl)pyrimidin-4-yl]amino]-3,3-difluoro-2-hydroxycyclopentyl]methyl sulfamate | 1775495: Inhibition of recombinant SAE (unknown origin) assessed as reduction in transfer of SUMO1 to UBC9 using SUMO1 as a substrate in presence of ATP at Km concentration by HTRF assay | ic50 | 0.0039 | uM |
CTD chemical–gene interactions
34 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Air Pollutants | affects expression, increases abundance, decreases expression | 2 |
| Benzo(a)pyrene | increases expression, affects methylation | 2 |
| aristolochic acid I | decreases expression, increases expression | 1 |
| FR900359 | increases phosphorylation | 1 |
| bisphenol F | increases expression | 1 |
| dicrotophos | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| arsenite | affects binding, decreases reaction | 1 |
| 1,6-hexamethylene diisocyanate | affects expression | 1 |
| trimellitic anhydride | affects expression | 1 |
| ammonium hexachloroplatinate | affects expression | 1 |
| aflatoxin B2 | decreases methylation | 1 |
| 1-UFT protocol | decreases response to substance | 1 |
| K 7174 | increases expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | increases expression, affects cotreatment | 1 |
| LDN 193189 | affects cotreatment, increases expression | 1 |
| Sunitinib | increases expression | 1 |
| Aspirin | increases expression | 1 |
| Benztropine | affects cotreatment, decreases expression | 1 |
| Clozapine | affects cotreatment, increases expression | 1 |
| Cuprizone | affects cotreatment, decreases expression, increases expression | 1 |
| Dietary Carbohydrates | decreases expression | 1 |
| Gold | decreases expression | 1 |
| Ivermectin | decreases expression | 1 |
| Nicotine | increases expression, increases sumoylation | 1 |
| Ozone | affects expression, increases abundance | 1 |
| Rotenone | decreases expression | 1 |
| Tetrachlorodibenzodioxin | affects expression | 1 |
| Thiram | decreases expression | 1 |
| Tobacco Smoke Pollution | increases expression | 1 |
ChEMBL screening assays
32 unique, capped per target: 30 binding, 2 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL5652744 | Binding | Binding affinity to human UBA2 incubated for 45 mins by Kinobead based pull down assay | NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem |
| CHEMBL1614105 | Functional | PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of SUMOylation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2006, AID2011, AID2069, AID2614, AID2658] | PubChem BioAssay data set |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Associated diseases: multiple congenital anomalies/dysmorphic syndrome, ACCES syndrome
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): ACCES syndrome, chromosome 19q13.11 deletion syndrome, distal, multiple congenital anomalies/dysmorphic syndrome, split hand-foot malformation