DCUN1D4
gene geneOn this page
Also known as KIAA0276
Summary
DCUN1D4 (defective in cullin neddylation 1 domain containing 4, HGNC:28998) is a protein-coding gene on chromosome 4q12, encoding DCN1-like protein 4 (Q92564). Contributes to the neddylation of all cullins by transferring NEDD8 from N-terminally acetylated NEDD8-conjugating E2s enzyme to different cullin C-terminal domain-RBX complexes which are necessary for the activation of cullin-RING E3 ubiquitin ligases (CRLs).
Enables cullin family protein binding activity. Involved in positive regulation of protein neddylation. Located in nucleus.
Source: NCBI Gene 23142 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 38 total
- Druggable target: yes
- MANE Select transcript:
NM_001040402
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:28998 |
| Approved symbol | DCUN1D4 |
| Name | defective in cullin neddylation 1 domain containing 4 |
| Location | 4q12 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | KIAA0276 |
| Ensembl gene | ENSG00000109184 |
| Ensembl biotype | protein_coding |
| OMIM | 612977 |
| Entrez | 23142 |
Gene structure
Transcript identifiers
Ensembl transcripts: 28 — 11 protein_coding, 7 nonsense_mediated_decay, 7 protein_coding_CDS_not_defined, 3 retained_intron
ENST00000334635, ENST00000381441, ENST00000451288, ENST00000477560, ENST00000502930, ENST00000504113, ENST00000504661, ENST00000504923, ENST00000505403, ENST00000505634, ENST00000506673, ENST00000507659, ENST00000507741, ENST00000508257, ENST00000509068, ENST00000509376, ENST00000510518, ENST00000510587, ENST00000510808, ENST00000511675, ENST00000512199, ENST00000513800, ENST00000893398, ENST00000893399, ENST00000927742, ENST00000927743, ENST00000960096, ENST00000960097
RefSeq mRNA: 4 — MANE Select: NM_001040402
NM_001040402, NM_001287755, NM_001287757, NM_015115
CCDS: CCDS33982, CCDS3487, CCDS75123
Canonical transcript exons
ENST00000334635 — 11 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003503148 | 51863670 | 51863709 |
| ENSE00003508164 | 51874271 | 51874385 |
| ENSE00003522712 | 51913529 | 51916837 |
| ENSE00003523283 | 51886568 | 51886638 |
| ENSE00003577884 | 51913290 | 51913392 |
| ENSE00003587175 | 51843153 | 51843267 |
| ENSE00003611116 | 51899270 | 51899378 |
| ENSE00003648100 | 51877763 | 51877854 |
| ENSE00003651554 | 51863437 | 51863507 |
| ENSE00003681637 | 51911070 | 51911174 |
| ENSE00003789645 | 51891760 | 51891851 |
Expression profiles
Bgee: expression breadth ubiquitous, 290 present calls, max score 98.11.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 25.7649 / max 169.1686, expressed in 1807 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 47604 | 25.7649 | 1807 |
Top tissues by expression
295 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| calcaneal tendon | UBERON:0003701 | 98.11 | gold quality |
| colonic epithelium | UBERON:0000397 | 95.44 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 94.62 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 93.64 | gold quality |
| left ovary | UBERON:0002119 | 93.35 | gold quality |
| right ovary | UBERON:0002118 | 93.12 | gold quality |
| cauda epididymis | UBERON:0004360 | 93.05 | gold quality |
| mucosa of stomach | UBERON:0001199 | 92.88 | gold quality |
| popliteal artery | UBERON:0002250 | 92.88 | gold quality |
| tibial artery | UBERON:0007610 | 92.87 | gold quality |
| stromal cell of endometrium | CL:0002255 | 92.68 | gold quality |
| blood vessel layer | UBERON:0004797 | 92.55 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 92.55 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 92.53 | gold quality |
| lower esophagus | UBERON:0013473 | 92.53 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 92.43 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 92.41 | gold quality |
| tendon | UBERON:0000043 | 92.40 | gold quality |
| ovary | UBERON:0000992 | 92.40 | gold quality |
| aorta | UBERON:0000947 | 92.39 | gold quality |
| left testis | UBERON:0004533 | 92.29 | gold quality |
| right adrenal gland | UBERON:0001233 | 92.05 | gold quality |
| right testis | UBERON:0004534 | 92.05 | gold quality |
| urinary bladder | UBERON:0001255 | 92.01 | gold quality |
| testis | UBERON:0000473 | 91.95 | gold quality |
| right coronary artery | UBERON:0001625 | 91.95 | gold quality |
| adenohypophysis | UBERON:0002196 | 91.94 | gold quality |
| tibial nerve | UBERON:0001323 | 91.91 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 91.89 | gold quality |
| sperm | CL:0000019 | 91.88 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-6379 | no | 1316.61 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
289 targeting DCUN1D4, 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-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-513A-5P | 100.00 | 69.77 | 2465 |
| HSA-MIR-3064-3P | 100.00 | 70.09 | 1254 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-29A-3P | 100.00 | 73.11 | 1835 |
| HSA-MIR-29B-3P | 100.00 | 73.18 | 1833 |
| HSA-MIR-29C-3P | 100.00 | 73.15 | 1833 |
| HSA-MIR-9-5P | 100.00 | 72.28 | 2361 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-3689D | 100.00 | 66.14 | 1181 |
| HSA-MIR-6851-5P | 100.00 | 65.63 | 1294 |
| HSA-MIR-3162-3P | 100.00 | 65.37 | 363 |
| HSA-MIR-4789-3P | 99.99 | 70.75 | 2484 |
| HSA-MIR-186-5P | 99.99 | 70.83 | 3707 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-4789-5P | 99.98 | 70.76 | 2721 |
| HSA-MIR-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-9985 | 99.98 | 72.11 | 2939 |
| HSA-LET-7F-2-3P | 99.98 | 70.98 | 2588 |
| HSA-MIR-1185-1-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-1185-2-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-548P | 99.98 | 72.25 | 3784 |
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | dcun1d4 | ENSDARG00000092394 |
| mus_musculus | Dcun1d4 | ENSMUSG00000051674 |
| rattus_norvegicus | Dcun1d4 | ENSRNOG00000002152 |
| drosophila_melanogaster | SCCRO | FBGN0036510 |
| drosophila_melanogaster | SCCRO4 | FBGN0036967 |
| caenorhabditis_elegans | WBGENE00010428 |
Paralogs (4): DCUN1D1 (ENSG00000043093), DCUN1D5 (ENSG00000137692), DCUN1D2 (ENSG00000150401), DCUN1D3 (ENSG00000188215)
Protein
Protein identifiers
DCN1-like protein 4 — Q92564 (reviewed: Q92564)
Alternative names: DCUN1 domain-containing protein 4, Defective in cullin neddylation protein 1-like protein 4
All UniProt accessions (9): Q92564, D6RB33, D6RCB7, D6RDV8, D6RGX7, D6RIY3, H0Y907, H0Y9C5, H0YA35
UniProt curated annotations — full annotation on UniProt →
Function. Contributes to the neddylation of all cullins by transferring NEDD8 from N-terminally acetylated NEDD8-conjugating E2s enzyme to different cullin C-terminal domain-RBX complexes which are necessary for the activation of cullin-RING E3 ubiquitin ligases (CRLs).
Subunit / interactions. Interacts (via the DCUN1 domain) with the unneddylated cullins: interacts with CUL1, CUL2, CUL3, CUL4A, CUL4B and CUL5; these interactions promote the cullin neddylation and the identity of the cullin dictates the affinity of the interaction. Interacts with RBX1 and RNF7. Interacts with CAND1; this interaction is bridged by cullins such as CUL3 and strongly inhibits the neddylation of CUL3. These CAND-cullin-DCNL complexes can only be neddylated in the presence of a substrate adapter. Interacts (via DCUN1 domain) with UBE2M (N-terminally acetylated form) and probably with UBE2F (N-terminally acetylated form).
Subcellular location. Nucleus.
Domain organisation. The DCUN1 domain, also known as PONY domain, mediates the interaction with different cullins. The DCUN1 domain mediates the interaction with the N-terminally acetylated NEDD8-conjugating E2s enzyme leading to the NEDD8 transfer from N-terminally acetylated NEDD8-conjugating E2s enzyme to different cullin C-terminal domain-RBX complexes; the neddylation efficiency correlates with the DCUN1D5-cullin and DCUN1D5-E2 interaction affinities.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q92564-1 | 1 | yes |
| Q92564-2 | 2 | |
| Q92564-3 | 3 |
RefSeq proteins (4): NP_001035492, NP_001274684, NP_001274686, NP_055930 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR005176 | PONY_dom | Domain |
| IPR014764 | DCN-prot | Family |
| IPR042460 | DCN1-like_PONY | Homologous_superfamily |
Pfam: PF03556
UniProt features (27 total): helix 12, strand 3, mutagenesis site 3, turn 2, splice variant 2, chain 1, domain 1, region of interest 1, compositionally biased region 1, cross-link 1
Structure
Experimental structures (PDB)
1 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 5V89 | X-RAY DIFFRACTION | 1.55 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q92564-F1 | 81.39 | 0.65 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (1): 95
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 250 | does not affect localization at nucleus; when associated with r-274 and a-280. |
| 274 | does not affect localization at nucleus; when associated with a-250 and a-280. |
| 280 | does not affect localization at nucleus; when associated with a-250 and r-274. |
Function
Pathways and Gene Ontology
Reactome pathways
1 pathways
| ID | Pathway |
|---|---|
| R-HSA-8951664 | Neddylation |
MSigDB gene sets: 275 (showing top):
TGGTGCT_MIR29A_MIR29B_MIR29C, GCM_MAP4K4, MULLIGHAN_NPM1_SIGNATURE_3_UP, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, RORA1_01, AMIT_EGF_RESPONSE_60_HELA, ATACCTC_MIR202, GOBP_PROTEIN_NEDDYLATION, TGACCTY_ERR1_Q2, CACCAGC_MIR138, USF_C, SP1_Q2_01, SCHUHMACHER_MYC_TARGETS_UP, AAACCAC_MIR140
GO Biological Process (2): protein neddylation (GO:0045116), positive regulation of protein neddylation (GO:2000436)
GO Molecular Function (4): ubiquitin conjugating enzyme binding (GO:0031624), ubiquitin-like protein binding (GO:0032182), cullin family protein binding (GO:0097602), protein binding (GO:0005515)
GO Cellular Component (2): ubiquitin ligase complex (GO:0000151), nucleus (GO:0005634)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Post-translational protein modification | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein binding | 2 |
| protein modification by small protein conjugation | 1 |
| protein neddylation | 1 |
| positive regulation of protein modification by small protein conjugation or removal | 1 |
| regulation of protein neddylation | 1 |
| ubiquitin-like protein conjugating enzyme binding | 1 |
| binding | 1 |
| intracellular protein-containing complex | 1 |
| transferase complex | 1 |
| intracellular membrane-bounded organelle | 1 |
Protein interactions and networks
STRING
889 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| DCUN1D4 | CWH43 | Q9H720 | 581 |
| DCUN1D4 | OCIAD1 | Q9NX40 | 547 |
| DCUN1D4 | OCIAD2 | Q56VL3 | 507 |
| DCUN1D4 | FBXL13 | Q8NEE6 | 497 |
| DCUN1D4 | CUL3 | Q13618 | 477 |
| DCUN1D4 | LRRC66 | Q68CR7 | 475 |
| DCUN1D4 | SDAD1 | Q9NVU7 | 473 |
| DCUN1D4 | COPS2 | P61201 | 468 |
| DCUN1D4 | SPATA18 | Q8TC71 | 466 |
| DCUN1D4 | DCUN1D1 | Q96GG9 | 450 |
| DCUN1D4 | FBXL3 | Q9UKT7 | 442 |
| DCUN1D4 | FRYL | O94915 | 434 |
| DCUN1D4 | ARHGAP24 | Q8N264 | 417 |
| DCUN1D4 | A0A087WY85 | A0A087WY85 | 412 |
| DCUN1D4 | NFXL1 | Q6ZNB6 | 407 |
IntAct
10 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| DCUN1D4 | psi-mi:“MI:0915”(physical association) | 0.490 | |
| DDX21 | MED19 | psi-mi:“MI:2364”(proximity) | 0.480 |
| ECE1 | DCUN1D4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| DCUN1D4 | ARL4C | psi-mi:“MI:0914”(association) | 0.350 |
| DCUN1D4 | AFP | psi-mi:“MI:0914”(association) | 0.350 |
| NPM1 | SBNO1 | psi-mi:“MI:2364”(proximity) | 0.270 |
| VAV2 | DCUN1D4 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (54): CUL1 (Biochemical Activity), CUL2 (Biochemical Activity), CUL3 (Biochemical Activity), CUL4A (Biochemical Activity), CUL4B (Biochemical Activity), CUL5 (Biochemical Activity), DCUN1D4 (Co-fractionation), TOP3A (Co-fractionation), DCUN1D4 (Affinity Capture-MS), CUL1 (Affinity Capture-MS), CUL2 (Affinity Capture-MS), CUL3 (Affinity Capture-MS), CUL5 (Affinity Capture-MS), CAND1 (Affinity Capture-MS), RBX1 (Affinity Capture-MS)
ESM2 similar proteins: A4D161, B1AR13, D3ZV31, E1BBQ2, E1BGQ2, F1N2W9, O42148, O42224, O70524, O95453, P0C7P0, P56726, P97698, Q2T9V7, Q3UGM2, Q497H0, Q56K12, Q5RC51, Q5T6S3, Q5U2M7, Q5XII8, Q5ZIA0, Q60769, Q66J85, Q6DDJ3, Q6DJB3, Q6ZN54, Q7T0P6, Q7Z2E3, Q8BKW4, Q8BYN3, Q8CCA0, Q8IWR0, Q8K214, Q8K2I9, Q8NE86, Q8NFZ0, Q8TDW4, Q92564, Q96GD3
Diamond homologs: A4IHK8, Q1RMX9, Q4V8B2, Q54GP1, Q5ADL9, Q5E9V1, Q5PPL2, Q5R9G1, Q5RDF9, Q5RHX6, Q5ZKU1, Q60YT5, Q6C0B6, Q6DFA1, Q6PH85, Q86JM4, Q8BZJ7, Q8CCA0, Q8IWE4, Q8K0V2, Q8T8S1, Q92564, Q96GG9, Q9BTE7, Q9CXV9, Q9QZ73, Q9U3C8, Q9VUQ8, Q9VWB1, Q5AWS1, Q8WZK4, Q9MBG8, Q4PF67, Q12395, Q750Y3, P0CN06, P0CN07, Q6FJR2
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
38 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 23 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2547 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 4:51843264:GTCA:G | donor_gain | 1.0000 |
| 4:51843268:G:GG | donor_gain | 1.0000 |
| 4:51863434:A:AG | acceptor_gain | 1.0000 |
| 4:51863435:A:G | acceptor_gain | 1.0000 |
| 4:51863436:G:GA | acceptor_gain | 1.0000 |
| 4:51863436:GA:G | acceptor_gain | 1.0000 |
| 4:51863436:GAT:G | acceptor_gain | 1.0000 |
| 4:51863436:GATT:G | acceptor_gain | 1.0000 |
| 4:51863436:GATTT:G | acceptor_gain | 1.0000 |
| 4:51863503:AGCTG:A | donor_gain | 1.0000 |
| 4:51863504:GCTG:G | donor_gain | 1.0000 |
| 4:51863504:GCTGG:G | donor_gain | 1.0000 |
| 4:51863505:CTG:C | donor_gain | 1.0000 |
| 4:51863505:CTGG:C | donor_loss | 1.0000 |
| 4:51863507:GGT:G | donor_loss | 1.0000 |
| 4:51863508:G:GG | donor_gain | 1.0000 |
| 4:51863508:G:T | donor_loss | 1.0000 |
| 4:51863509:T:G | donor_loss | 1.0000 |
| 4:51874270:GGAA:G | acceptor_gain | 1.0000 |
| 4:51874382:A:G | donor_gain | 1.0000 |
| 4:51877754:A:AG | acceptor_gain | 1.0000 |
| 4:51877755:A:G | acceptor_gain | 1.0000 |
| 4:51877761:A:AG | acceptor_gain | 1.0000 |
| 4:51877761:AGCAT:A | acceptor_gain | 1.0000 |
| 4:51877762:G:GA | acceptor_gain | 1.0000 |
| 4:51877762:GC:G | acceptor_gain | 1.0000 |
| 4:51877762:GCA:G | acceptor_gain | 1.0000 |
| 4:51877762:GCAT:G | acceptor_gain | 1.0000 |
| 4:51877762:GCATG:G | acceptor_gain | 1.0000 |
| 4:51877851:GCAG:G | donor_gain | 1.0000 |
AlphaMissense
1953 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 4:51877829:C:G | C106W | 1.000 |
| 4:51877836:T:A | W109R | 1.000 |
| 4:51877836:T:C | W109R | 1.000 |
| 4:51886607:T:C | F128S | 1.000 |
| 4:51886609:T:C | C129R | 1.000 |
| 4:51886610:G:A | C129Y | 1.000 |
| 4:51886611:T:G | C129W | 1.000 |
| 4:51886631:C:A | P136Q | 1.000 |
| 4:51891770:T:A | L142H | 1.000 |
| 4:51891770:T:C | L142P | 1.000 |
| 4:51891779:C:A | A145D | 1.000 |
| 4:51891794:C:A | A150E | 1.000 |
| 4:51891805:G:C | G154R | 1.000 |
| 4:51891806:G:A | G154D | 1.000 |
| 4:51891812:T:C | F156S | 1.000 |
| 4:51891826:T:A | W161R | 1.000 |
| 4:51891826:T:C | W161R | 1.000 |
| 4:51891827:G:C | W161S | 1.000 |
| 4:51891828:G:C | W161C | 1.000 |
| 4:51891828:G:T | W161C | 1.000 |
| 4:51891835:G:A | G164R | 1.000 |
| 4:51891835:G:C | G164R | 1.000 |
| 4:51891836:G:A | G164E | 1.000 |
| 4:51899290:T:C | L176P | 1.000 |
| 4:51899352:T:G | Y197D | 1.000 |
| 4:51899361:G:C | A200P | 1.000 |
| 4:51899362:C:A | A200E | 1.000 |
| 4:51899364:T:C | F201L | 1.000 |
| 4:51899366:T:A | F201L | 1.000 |
| 4:51899366:T:G | F201L | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000039344 (4:51839338 G>A,T), RS1000043555 (4:51879269 T>G), RS1000111279 (4:51914646 G>A,T), RS1000149939 (4:51884917 G>A,T), RS1000163884 (4:51915016 G>A), RS1000214392 (4:51833139 T>C), RS1000227149 (4:51898585 A>G), RS1000258977 (4:51902584 C>G,T), RS1000372477 (4:51874562 C>T), RS1000379244 (4:51851133 G>T), RS1000500826 (4:51897486 C>G,T), RS1000508924 (4:51884628 C>T), RS1000517338 (4:51901617 C>G,T), RS1000569997 (4:51901892 G>A,T), RS1000589095 (4:51857463 C>G,T)
Disease associations
OMIM: gene MIM:612977 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST006088_36 | Familial squamous cell lung carcinoma | 4.000000e-07 |
| GCST008058_1 | Estimated glomerular filtration rate | 4.000000e-10 |
| GCST008059_248 | Estimated glomerular filtration rate | 2.000000e-10 |
| GCST008163_485 | Height | 1.000000e-06 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006953 | family history of lung cancer |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4295914 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
2 potent at pChembl≥5 of 3 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 6.09 | Ki | 807 | nM | CHEMBL4592844 |
| 6.09 | Ki | 810 | nM | CHEMBL4592844 |
PubChem BioAssay actives
2 with measured affinity, of 6 total; 1 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 |
|---|---|---|---|---|
| 4-(4-methylphenyl)-2-prop-2-ynylsulfanyl-6-(1,3-thiazol-2-ylsulfanyl)pyrimidine-5-carbonitrile | 1599586: Binding affinity to N-terminal GST tagged recombinant DCN4 (unknown origin) (102 to 292 residues) expressed in Escherichia coli BL21(DE3) assessed as reduction in DCN1/FAM-labelled N-terminal acetylated UBE2M (1 to 21 residues) protein-protein interaction after 30 mins by HTRF assay | ki | 0.8070 | uM |
CTD chemical–gene interactions
41 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, decreases expression, affects expression, increases methylation | 7 |
| trichostatin A | affects cotreatment, decreases expression | 3 |
| potassium chromate(VI) | affects cotreatment, decreases expression | 2 |
| Phenylmercuric Acetate | affects cotreatment, decreases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| FR900359 | decreases phosphorylation | 1 |
| dicrotophos | decreases expression | 1 |
| methylmercuric chloride | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| salinomycin | decreases expression | 1 |
| beta-lapachone | decreases expression | 1 |
| sodium arsenite | decreases expression | 1 |
| epigallocatechin gallate | decreases expression, affects cotreatment | 1 |
| chromium hexavalent ion | decreases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, decreases expression | 1 |
| dorsomorphin | affects cotreatment, decreases expression | 1 |
| bisphenol S | affects cotreatment, increases expression | 1 |
| jinfukang | decreases expression | 1 |
| picoxystrobin | increases expression | 1 |
| PCI 5002 | affects cotreatment, increases expression | 1 |
| Temozolomide | decreases expression | 1 |
| Zoledronic Acid | increases expression | 1 |
| Vorinostat | increases expression | 1 |
| Panobinostat | affects cotreatment, decreases expression | 1 |
| Acetaminophen | decreases expression | 1 |
| Dexamethasone | increases expression, affects cotreatment | 1 |
| Indomethacin | affects cotreatment, increases expression | 1 |
| Methyl Methanesulfonate | decreases expression | 1 |
| Phthalic Acids | increases methylation | 1 |
ChEMBL screening assays
5 unique, capped per target: 5 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4222551 | Binding | Inhibition of human DCN4-mediated cullin neddylation assessed as reduction in transfer of fluorescein-5-maleimide-tagged NEDD8 from N-terminally acetylated human UBE2M to CUL2-CTD at 50 uM measured for 1 min by pulse-chase assay | Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation. — J Med Chem |
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.