UBE2F

Summary

UBE2F (ubiquitin conjugating enzyme E2 F (putative), HGNC:12480) is a protein-coding gene on chromosome 2q37.3, encoding NEDD8-conjugating enzyme UBE2F (Q969M7). Accepts the ubiquitin-like protein NEDD8 from the UBA3-NAE1 E1 complex and catalyzes its covalent attachment to other proteins.

Enables NEDD8 conjugating enzyme activity. Involved in protein neddylation. Predicted to be active in cytosol and nucleus.

Source: NCBI Gene 140739 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 18 total — 2 pathogenic
• Druggable target: yes
• MANE Select transcript: NM_080678

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:12480
Approved symbol	UBE2F
Name	ubiquitin conjugating enzyme E2 F (putative)
Location	2q37.3
Locus type	gene with protein product
Status	Approved
Aliases	NCE2
Ensembl gene	ENSG00000184182
Ensembl biotype	protein_coding
OMIM	617700
Entrez	140739

Gene structure

Transcript identifiers

Ensembl transcripts: 51 — 38 protein_coding, 10 nonsense_mediated_decay, 3 retained_intron

ENST00000272930, ENST00000409332, ENST00000409633, ENST00000409953, ENST00000414443, ENST00000416292, ENST00000417231, ENST00000433241, ENST00000433568, ENST00000434137, ENST00000434655, ENST00000439338, ENST00000439780, ENST00000440223, ENST00000441728, ENST00000445676, ENST00000448502, ENST00000454786, ENST00000455999, ENST00000472479, ENST00000480828, ENST00000482096, ENST00000612130, ENST00000888988, ENST00000888989, ENST00000888990, ENST00000888991, ENST00000888992, ENST00000888993, ENST00000888994, ENST00000888995, ENST00000888996, ENST00000888997, ENST00000888998, ENST00000888999, ENST00000928512, ENST00000928513, ENST00000928514, ENST00000928515, ENST00000928516, ENST00000928517, ENST00000928518, ENST00000928519, ENST00000928520, ENST00000946655, ENST00000946656, ENST00000946657, ENST00000946658, ENST00000946659, ENST00000946660, ENST00000946661

RefSeq mRNA: 5 — MANE Select: NM_080678 NM_001278305, NM_001278306, NM_001278307, NM_001278308, NM_080678

CCDS: CCDS2523, CCDS63175, CCDS63176, CCDS63177

Canonical transcript exons

ENST00000272930 — 10 exons

Exon	Start	End
ENSE00001622711	238041288	238042782
ENSE00003490171	238032222	238032254
ENSE00003497317	237967014	237967132
ENSE00003518844	237994744	237994809
ENSE00003541831	238030556	238030613
ENSE00003574117	237973092	237973225
ENSE00003581620	237987963	237987992
ENSE00003593386	238025342	238025412
ENSE00003643362	238016566	238016633
ENSE00003690220	238035878	238035940

Expression profiles

Bgee: expression breadth ubiquitous, 256 present calls, max score 97.29.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.3969 / max 91.8919, expressed in 147 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
26313	25.1997	1815
26316	0.1845	80
26314	0.0761	35
26315	0.0680	28
26317	0.0470	8
26318	0.0213	2

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
body of pancreas	UBERON:0001150	97.29	gold quality
pancreas	UBERON:0001264	96.37	gold quality
esophagus squamous epithelium	UBERON:0006920	96.13	gold quality
right atrium auricular region	UBERON:0006631	96.00	gold quality
cardiac atrium	UBERON:0002081	95.87	gold quality
leukocyte	CL:0000738	95.86	gold quality
epithelial cell of pancreas	CL:0000083	95.85	gold quality
monocyte	CL:0000576	95.81	gold quality
granulocyte	CL:0000094	95.80	gold quality
islet of Langerhans	UBERON:0000006	95.75	gold quality
amniotic fluid	UBERON:0000173	95.59	gold quality
pons	UBERON:0000988	95.38	gold quality
gastrocnemius	UBERON:0001388	95.37	gold quality
deltoid	UBERON:0001476	95.21	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	95.09	gold quality
blood	UBERON:0000178	95.04	gold quality
hindlimb stylopod muscle	UBERON:0004252	95.03	gold quality
heart	UBERON:0000948	94.87	gold quality
muscle of leg	UBERON:0001383	94.85	gold quality
heart left ventricle	UBERON:0002084	94.84	gold quality
hypothalamus	UBERON:0001898	94.77	gold quality
cardiac ventricle	UBERON:0002082	94.75	gold quality
spinal cord	UBERON:0002240	94.69	gold quality
myocardium	UBERON:0002349	94.69	gold quality
heart right ventricle	UBERON:0002080	94.61	gold quality
stromal cell of endometrium	CL:0002255	94.60	gold quality
lower esophagus mucosa	UBERON:0035834	94.50	gold quality
smooth muscle tissue	UBERON:0001135	94.49	gold quality
ascending aorta	UBERON:0001496	94.37	gold quality
cardiac muscle of right atrium	UBERON:0003379	94.34	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-MTAB-8142	yes	47.39
E-HCAD-13	yes	7.33
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

60 targeting UBE2F, 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-6740-5P	100.00	65.64	932
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-3658	99.96	73.87	4379
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-101-3P	99.94	75.03	2230
HSA-MIR-4778-3P	99.93	70.40	1818
HSA-MIR-10523-5P	99.91	69.22	2038
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-4698	99.84	71.41	4303
HSA-MIR-5010-3P	99.83	70.60	2357
HSA-MIR-6515-3P	99.82	68.19	1933
HSA-MIR-6844	99.82	70.69	2423
HSA-MIR-139-5P	99.80	69.50	1399
HSA-MIR-6817-3P	99.79	68.35	2126
HSA-MIR-6752-3P	99.72	66.71	1587
HSA-MIR-548AU-3P	99.70	68.22	1373
HSA-MIR-3059-5P	99.70	69.93	2491
HSA-MIR-580-3P	99.67	69.23	1841
HSA-MIR-1284	99.67	73.56	1353
HSA-MIR-586	99.65	70.40	2051
HSA-MIR-4756-3P	99.62	66.30	1319
HSA-MIR-5003-5P	99.61	69.13	1624
HSA-MIR-1252-3P	99.55	67.71	2862
HSA-MIR-17-3P	99.55	66.77	1311

Literature-anchored findings (GeneRIF, showing 5)

• Distinct preferences of UBC12 and UBE2F peptides for inhibiting different DCNLs, including the oncogenic DCNL1. (PMID:23201271)
• By ubiquitylating and degrading NOXA through activating CRL5, UBE2F selectively promotes lung cancer cell survival and could, therefore, serve as a novel cancer target (PMID:27591266)
• Study establishes a negative regulatory axis between two neddylation E2s with UBE2M ubiquitylating UBE2F, and two CRLs with CRL3 inactivating CRL5. (PMID:29932898)
• Induction of NEDD8-conjugating enzyme E2 UBE2F by platinum protects lung cancer cells from apoptosis and confers to platinum-insensitivity. (PMID:33184273)
• NEDD8-conjugating enzyme E2 UBE2F confers radiation resistance by protecting lung cancer cells from apoptosis. (PMID:34783226)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	ube2f	ENSDARG00000025754
mus_musculus	Ube2f	ENSMUSG00000034343
rattus_norvegicus	Ube2f	ENSRNOG00000019953
caenorhabditis_elegans	ubc-12	WBGENE00006707

Paralogs (24): UBE2T (ENSG00000077152), UBE2A (ENSG00000077721), UBE2K (ENSG00000078140), CDC34 (ENSG00000099804), UBE2I (ENSG00000103275), UBE2W (ENSG00000104343), UBE2R2 (ENSG00000107341), UBE2S (ENSG00000108106), UBE2B (ENSG00000119048), UBE2G1 (ENSG00000132388), UBE2Z (ENSG00000159202), UBE2J2 (ENSG00000160087), AKTIP (ENSG00000166971), UBE2V2 (ENSG00000169139), UBE2C (ENSG00000175063), UBE2O (ENSG00000175931), UBE2U (ENSG00000177414), UBE2N (ENSG00000177889), UBE2G2 (ENSG00000184787), UBE2H (ENSG00000186591), UBE2J1 (ENSG00000198833), PEDS1 (ENSG00000240849), UBE2V1 (ENSG00000244687), UBE2NL (ENSG00000276380)

Protein

Protein identifiers

NEDD8-conjugating enzyme UBE2F — Q969M7 (reviewed: Q969M7)

Alternative names: NEDD8 carrier protein UBE2F, NEDD8 protein ligase UBE2F, NEDD8-conjugating enzyme 2, RING-type E3 NEDD8 transferase UBE2F, Ubiquitin-conjugating enzyme E2 F

All UniProt accessions (13): Q969M7, C9IZ93, C9J9P8, C9JF62, C9JFD2, C9JSK8, F2Z363, F8WB39, F8WCT3, F8WD80, F8WDQ9, F8WFB7, G5E9R6

UniProt curated annotations — full annotation on UniProt →

Function. Accepts the ubiquitin-like protein NEDD8 from the UBA3-NAE1 E1 complex and catalyzes its covalent attachment to other proteins. Together with the E3 ubiquitin ligase RNF7/RBX2, specifically neddylates cullin-5 (CUL5). Does not neddylate CUL1, CUL2, CUL3, CUL4A or CUL4B. Mediates neddylation of the CUL9-RBX1 complex. (Microbial infection) Following infection by HIV-1 virus, participates to HIV-1 Vif protein-mediated ubiquitination and degradation of APOBEC3G by mediating neddylation of cullin-5 (CUL5).

Subunit / interactions. Interacts with UBA3 and RBX2. Interacts (N-terminally acetylated form) with (via DCUN1 domain) DCUN1D1, DCUN1D2, DCUN1D3, DCUN1D4 and DCUN1D5.

Tissue specificity. Widely expressed (at protein level).

Post-translational modifications. The acetylation of Met-1 increases affinity for DCUN1D3 by about 2 orders of magnitude and is crucial for NEDD8 transfer to cullins.

Pathway. Protein modification; protein neddylation.

Similarity. Belongs to the ubiquitin-conjugating enzyme family. UBE2F subfamily.

Isoforms (7)

UniProt ID	Names	Canonical?
Q969M7-1	1	yes
Q969M7-2	2
Q969M7-3	3
Q969M7-4	4
Q969M7-5	5
Q969M7-6	6
Q969M7-7	7

RefSeq proteins (5): NP_001265234, NP_001265235, NP_001265236, NP_001265237, NP_542409* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000608	UBC	Domain
IPR016135	UBQ-conjugating_enzyme/RWD	Homologous_superfamily
IPR023313	UBQ-conjugating_AS	Active_site
IPR050113	Ub_conjugating_enzyme-E2-like	Family

Pfam: PF00179

Enzyme classification (BRENDA):

• EC 2.3.2.34 — E2 NEDD8-conjugating enzyme (BRENDA: 3 organisms, 20 substrates, 2 inhibitors, 0 Km, 0 kcat entries)

UniProt features (33 total): strand 10, splice variant 7, helix 7, turn 2, chain 1, domain 1, mutagenesis site 1, sequence conflict 1, region of interest 1, active site 1, modified residue 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
4GBA	X-RAY DIFFRACTION	2.4
3FN1	X-RAY DIFFRACTION	2.5
2EDI	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q969M7-F1	90.06	0.83

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): 116 (glycyl thioester intermediate)

Post-translational modifications (1): 1

Mutagenesis-validated functional residues (1):

Position	Phenotype
116	abolished nedd8 conjugating enzyme activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-8951664	Neddylation
R-HSA-983168	Antigen processing: Ubiquitination & Proteasome degradation

MSigDB gene sets: 171 (showing top): REACTOME_ADAPTIVE_IMMUNE_SYSTEM, REACTOME_CLASS_I_MHC_MEDIATED_ANTIGEN_PROCESSING_PRESENTATION, REACTOME_ANTIGEN_PROCESSING_UBIQUITINATION_PROTEASOME_DEGRADATION, CGGAARNGGCNG_UNKNOWN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GOBP_PROTEIN_NEDDYLATION, GGGTGGRR_PAX4_03, MARTINEZ_RB1_TARGETS_DN, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GARY_CD5_TARGETS_DN, BIOCARTA_PARKIN_PATHWAY, GATA1_04, GATA1_03, TATA_C, DODD_NASOPHARYNGEAL_CARCINOMA_UP

GO Biological Process (6): post-translational protein modification (GO:0043687), protein neddylation (GO:0045116), protein polyubiquitination (GO:0000209), proteasome-mediated ubiquitin-dependent protein catabolic process (GO:0043161), innate immune response (GO:0045087), defense response to virus (GO:0051607)

GO Molecular Function (8): ATP binding (GO:0005524), NEDD8 transferase activity (GO:0019788), NEDD8 conjugating enzyme activity (GO:0061654), nucleotide binding (GO:0000166), ubiquitin-protein transferase activity (GO:0004842), protein binding (GO:0005515), transferase activity (GO:0016740), NEDD8 ligase activity (GO:0061663)

GO Cellular Component (2): nucleus (GO:0005634), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Post-translational protein modification	1
Class I MHC mediated antigen processing & presentation	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
ubiquitin-like protein transferase activity	2
NEDD8 transferase activity	2
protein modification process	1
protein modification by small protein conjugation	1
protein ubiquitination	1
ubiquitin-dependent protein catabolic process	1
proteasomal protein catabolic process	1
immune response	1
defense response to symbiont	1
defense response	1
response to virus	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
ubiquitin-like protein conjugating enzyme activity	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
binding	1
catalytic activity	1
ubiquitin-like protein ligase activity	1
intracellular membrane-bounded organelle	1
cytoplasm	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1042 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
UBE2F	RNF7	Q9UBF6	978
UBE2F	UBA3	Q8TBC4	922
UBE2F	NAE1	Q13564	917
UBE2F	NEDD8	Q15843	901
UBE2F	DCUN1D1	Q96GG9	860
UBE2F	CUL5	Q93034	828
UBE2F	RBX1	P62877	772
UBE2F	SENP8	Q96LD8	771
UBE2F	CUL1	Q13616	704
UBE2F	CAND1	Q86VP6	639
UBE2F	CUL2	Q13617	599
UBE2F	COPS5	Q92905	598
UBE2F	CUL4A	Q13619	588
UBE2F	CUL4B	Q13620	584
UBE2F	CUL3	Q13618	568

IntAct

18 interactions, top by confidence:

A	B	Type	Score
PAX6	UBE2F	psi-mi:“MI:0915”(physical association)	0.560
LCN2	UBE2F	psi-mi:“MI:0915”(physical association)	0.560
UBE2F	GNB2	psi-mi:“MI:0915”(physical association)	0.560
UBE2F	TYK2	psi-mi:“MI:0915”(physical association)	0.370
UBE2F	EIF2B4	psi-mi:“MI:0915”(physical association)	0.370
UBE2F	UBA3	psi-mi:“MI:0915”(physical association)	0.370
PRAME	UBE2F	psi-mi:“MI:0915”(physical association)	0.370
UBE2F	WDR77	psi-mi:“MI:0915”(physical association)	0.370
RNF34	UBE2F	psi-mi:“MI:0915”(physical association)	0.370
CUL9	NVL	psi-mi:“MI:0914”(association)	0.350
STAT1	UBE2F	psi-mi:“MI:0915”(physical association)	0.000
UBE2F	PAX6	psi-mi:“MI:0915”(physical association)	0.000
UBE2F	LCN2	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (54): CUL1 (Biochemical Activity), UBE2F (Reconstituted Complex), UBE2F (Biochemical Activity), UBE2F (Biochemical Activity), UBE2F (Reconstituted Complex), UBE2F (Co-fractionation), UBE2F (Reconstituted Complex), UBE2F (Reconstituted Complex), UBE2F (Affinity Capture-Western), UBE2F (Reconstituted Complex), UBE2F (Reconstituted Complex), UBE2F (Reconstituted Complex), UBE2F (Two-hybrid), UBE2F (Two-hybrid), UBE2F (Positive Genetic)

ESM2 similar proteins: A2VDY4, A2Z5S8, A7SM54, A8Q8J2, A8XAF4, A9UR29, B0WVC4, B3MC02, B3NPZ0, B3RTL9, B4H538, B4HSI1, B4J9W6, B4KQQ4, B4LL39, B4MIX7, B4P6S9, B4QHD6, C3ZDX5, O01757, O76808, P27008, P27967, P27969, P42747, Q03598, Q0ZB76, Q178A5, Q1RMW1, Q1ZXC9, Q28X71, Q32L27, Q42540, Q5RHR0, Q7K1Z5, Q7PND3, Q7TSS2, Q7YQJ9, Q7Z7E8, Q8K224

Diamond homologs: A0A1B0GUS4, A3KN22, A5PKP9, D3ZDK2, O00103, O00762, O13685, O74196, O74549, P0CS16, P0CS17, P15731, P15732, P21734, P25867, P35128, P35129, P35130, P35131, P35132, P35133, P35134, P35135, P42746, P43102, P46595, P49459, P51668, P52478, P52490, P52491, P52492, P61077, P61078, P61079, P61080, P61081, P61082, P62837, P62838

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
pevonedistat	“down-regulates quantity”	UBE2F	“chemical inhibition”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	0
Uncertain significance	16
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
147844	GRCh38/hg38 2q37.2-37.3(chr2:235028429-242066108)x1	Pathogenic
3148868	GRCh37/hg19 2q37.1-37.3(chr2:235267074-242782258)x1	Pathogenic

SpliceAI

2264 predictions. Top by Δscore:

Variant	Effect	Δscore
2:237973087:TTCA:T	acceptor_loss	1.0000
2:237973088:TCA:T	acceptor_loss	1.0000
2:237973089:CA:C	acceptor_loss	1.0000
2:237973089:CAGG:C	acceptor_loss	1.0000
2:237973090:A:AG	acceptor_gain	1.0000
2:237973090:AG:A	acceptor_gain	1.0000
2:237973090:AGG:A	acceptor_gain	1.0000
2:237973091:G:GA	acceptor_gain	1.0000
2:237973091:G:GT	acceptor_gain	1.0000
2:237973091:GG:G	acceptor_gain	1.0000
2:237973091:GGG:G	acceptor_gain	1.0000
2:237973091:GGGT:G	acceptor_gain	1.0000
2:237973091:GGGTA:G	acceptor_gain	1.0000
2:237973225:GGTA:G	donor_loss	1.0000
2:237973225:GGTAA:G	donor_loss	1.0000
2:237973226:GT:G	donor_loss	1.0000
2:237973227:T:A	donor_loss	1.0000
2:238035875:AAG:A	acceptor_gain	1.0000
2:238041270:A:AG	acceptor_gain	1.0000
2:237973082:T:A	acceptor_gain	0.9900
2:237973089:CAGGG:C	acceptor_gain	0.9900
2:237973205:G:GT	donor_gain	0.9900
2:237987961:A:AG	acceptor_gain	0.9900
2:237987962:G:GG	acceptor_gain	0.9900
2:237987993:G:GG	donor_gain	0.9900
2:238016564:A:AG	acceptor_gain	0.9900
2:238016565:G:GG	acceptor_gain	0.9900
2:238016565:GATGA:G	acceptor_gain	0.9900
2:238017850:G:GT	donor_gain	0.9900
2:238017850:G:T	donor_gain	0.9900

AlphaMissense

1210 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:238016593:T:C	F81S	1.000
2:238025372:T:A	W105R	1.000
2:238025372:T:C	W105R	1.000
2:238025397:G:T	G113V	1.000
2:238030590:T:A	W130R	1.000
2:238030590:T:C	W130R	1.000
2:238030592:G:C	W130C	1.000
2:238030592:G:T	W130C	1.000
2:237973217:T:A	L37H	0.999
2:237994795:T:C	L67P	0.999
2:238016592:T:C	F81L	0.999
2:238016594:T:A	F81L	0.999
2:238016594:T:G	F81L	0.999
2:238016599:T:C	F83S	0.999
2:238016611:T:A	V87D	0.999
2:238025346:C:A	P96H	0.999
2:238025357:T:C	C100R	0.999
2:238025359:C:G	C100W	0.999
2:238025373:G:C	W105S	0.999
2:238025374:G:C	W105C	0.999
2:238025374:G:T	W105C	0.999
2:238025375:C:G	H106D	0.999
2:238025376:A:G	H106R	0.999
2:238025377:C:A	H106Q	0.999
2:238025377:C:G	H106Q	0.999
2:238025379:C:A	P107H	0.999
2:238025383:C:A	N108K	0.999
2:238025383:C:G	N108K	0.999
2:238025385:T:A	I109N	0.999
2:238025396:G:T	G113W	0.999

dbSNP variants (sampled 300 via entrez): RS1000011574 (2:237984385 T>C), RS1000012568 (2:238026050 T>G), RS1000024575 (2:238023706 C>A), RS1000061179 (2:237991405 A>G), RS1000071563 (2:237986080 C>A,T), RS1000172493 (2:238005359 G>A), RS1000182761 (2:238033233 G>A), RS1000234342 (2:238037887 G>A,C), RS1000243194 (2:237997135 G>A), RS1000284078 (2:237998759 C>G), RS1000348959 (2:238003294 T>A,C,G), RS1000367139 (2:238041656 G>A), RS1000473128 (2:238032161 G>T), RS1000510188 (2:238036996 A>G), RS1000512673 (2:238018556 G>C)

Disease associations

OMIM: gene MIM:617700 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST008153_10	Lean body mass	3.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004995	lean body mass

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523422 (SINGLE PROTEIN)

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

Binding affinities (BindingDB)

66 measured of 103 human assays (103 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]-3-fluorobenzamide	IC50	3.2 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(2,6-difluorophenyl)ethynyl]-7-[(1R,4R,5S)-4,5-dihydroxy-3-[(sulfamoylamino)methyl]cyclopent-2-en-1-yl]pyrrolo[2,3-d]pyrimidine	IC50	3.3 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-(3-hydroxy-1-piperidyl)phenyl]ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	3.5 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-fluoro-6-methoxy-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	3.5 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-[(3R)-3-fluoropyrrolidin-1-yl]phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	4 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-(4-hydroxy-1-piperidyl)phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	4.2 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-(4-oxo-1-piperidyl)phenyl]ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	4.3 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]-5-[2-(1,1-dioxo-2,3-dihydrobenzothiophen-7-yl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	4.3 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-[2-ethylsulfonyl-6-fluoro-4-[(3R)-3-hydroxypyrrolidin-1-yl]phenyl]ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	4.4 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(2,6-difluoro-4-hydroxy-phenyl)ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	4.5 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(5-benzyloxypyrimidin-2-yl)ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	5.1 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-[(3S)-3-fluoropyrrolidin-1-yl]phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	5.1 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-fluoro-6-isopropoxy-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	5.3 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
8-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]quinoline	IC50	5.4 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(3-fluoro-2,5-dimethoxy-4-pyridyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	5.6 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
2-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]benzenesulfonamide	IC50	5.6 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(4-cyano-2,6-difluoro-phenyl)ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	5.8 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-[(3S)-3-hydroxypyrrolidin-1-yl]phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	6.2 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[4-(azetidin-1-yl)-2,6-difluoro-phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	6.8 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-[4-[2-[4-amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]-3,5-difluoro-phenyl]morpholine	IC50	7.6 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
1-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]isoquinoline	IC50	7.8 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-fluoro-6-methylsulfanyl-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	8.5 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-(triazol-2-ylmethoxy)phenyl]ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	8.5 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-(pyrazol-1-ylmethoxy)phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	8.9 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]-5-[2-(2-ethylsulfonyl-6-fluoro-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	9 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(4-amino-2-fluoro-phenyl)ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	9.1 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]-5-[2-(1,1-dioxo-3,4-dihydro-2H-thiochromen-8-yl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	9.1 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
8-[2-[4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]quinoline	IC50	9.2 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2,6-dimethoxyphenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	9.6 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
2-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]-3-fluoro-benzenesulfonamide	IC50	9.7 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-ethylsulfanylphenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	10 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-[4-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]-3,5-difluoro-phenyl]thiomorpholine	IC50	11 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
8-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2.3-d]pyrimidin-5-yl]ethynyl]-7-methoxyquinoline	IC50	11 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-methylsulfanylphenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	11 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-[4-(ethylamino)-2,6-difluoro-phenyl]ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	12 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
MLN4924	IC50	12 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-ethylsulfonyl-6-fluoro-4-pyrrolidin-1-yl-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	13 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]-5-[2-(2-fluoro-6-methoxy-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	13 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-[2,6-difluoro-4-(4-methylpiperazin-1-yl)phenyl]ethynyl]-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidine	IC50	13 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
8-[4-[2-[4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]-3-ethoxy-5-fluoro-phenyl]-3-oxa-8-azabicyclo[3,2,1]octane	IC50	13 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(3-fluoro-5-methoxy-4-pyridyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	14 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(3,5-difluoro-2-methoxy-4-pyridyl)ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	14 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-(2-indan-1-ylethynyl)pyrrolo[2,3-d]pyrimidine	IC50	15 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-5-[2-(2,4-difluoro-3-pyridyl) ethynyl]-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidine	IC50	15 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-[4-[2-[4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]-3-ethoxy-5-fluoro-phenyl]morpholine	IC50	15 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-ethoxy-6-methoxy-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	16 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
3-[[4-[2-[4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]pyrrolo[2,3-d]pyrimidin-5-yl]ethynyl]phenoxy]methyl]benzamide	IC50	18 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(1,1-dioxo-3,4-dihydro-2H-thiochromen-8-yl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	19 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
4-Amino-7-[(1R,2S,3R,4R)-2,3-dihydroxy-4-[(sulfamoylamino)methyl]cyclopentyl]-5-[2-(2-ethylsulfanyl-6-fluoro-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine	IC50	19 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
[(2R,3S,5R)-5-[4-amino-5-[1-[(3,4-dimethylphenyl)methyl]pyrazol-4-yl]pyrrolo[2,3-d]pyrimidin-7-yl]-3-hydroxyoxolan-2-yl]methyl sulfamate	IC50	19 nM	US-10174040: Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Tretinoin	decreases expression	2
salinomycin	decreases expression	1
trichostatin A	affects expression	1
arsenite	decreases methylation	1
chloropicrin	decreases expression	1
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	decreases reaction, increases expression	1
Sunitinib	increases expression	1
Atrazine	decreases expression	1
Vehicle Emissions	decreases reaction, increases expression	1
Carbamazepine	affects expression	1
Tobacco Smoke Pollution	increases expression	1
Cyclosporine	increases expression	1
Acrylamide	increases expression	1
Particulate Matter	decreases reaction, 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
CHEMBL4316377	Binding	Inhibition of UBE2F in human A549 cells assessed as decrease in Cullin5-Nedd8 adduct level at 50 uM measured after 6 to 12 hrs by Western blot analysis	Discovery of candesartan cilexetic as a novel neddylation inhibitor for suppressing tumor growth. — Eur J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B2K4	Abcam HeLa UBE2F KO	Cancer cell line	Female
CVCL_TV67	HAP1 UBE2F (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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