DUS2

Summary

DUS2 (dihydrouridine synthase 2, HGNC:26014) is a protein-coding gene on chromosome 16q22.1, encoding tRNA-dihydrouridine(20) synthase [NAD(P)+]-like (Q9NX74). Catalyzes the NADPH-dependent synthesis of dihydrouridine, a modified base found in the D-loop of most tRNAs.

This gene encodes a cytoplasmic protein that catalyzes the conversion of uridine residues to dihydrouridine in the D-loop of tRNA. The resulting modified bases confer enhanced regional flexibility to tRNA. The encoded protein may increase the rate of translation by inhibiting an interferon-induced protein kinase. This gene has been implicated in pulmonary carcinogenesis. Alternatively spliced transcript variants have been described for this gene.

Source: NCBI Gene 54920 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 70 total
• Druggable target: yes
• MANE Select transcript: NM_017803

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:26014
Approved symbol	DUS2
Name	dihydrouridine synthase 2
Location	16q22.1
Locus type	gene with protein product
Status	Approved
Aliases	FLJ20399, SMM1
Ensembl gene	ENSG00000167264
Ensembl biotype	protein_coding
OMIM	609707
Entrez	54920

Gene structure

Transcript identifiers

Ensembl transcripts: 54 — 51 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay

ENST00000358896, ENST00000432752, ENST00000561965, ENST00000562246, ENST00000564781, ENST00000564975, ENST00000565263, ENST00000565980, ENST00000566306, ENST00000567100, ENST00000568099, ENST00000569289, ENST00000570709, ENST00000571081, ENST00000575677, ENST00000576994, ENST00000859099, ENST00000859100, ENST00000859101, ENST00000859102, ENST00000859103, ENST00000859104, ENST00000859105, ENST00000859106, ENST00000859107, ENST00000859108, ENST00000859109, ENST00000859110, ENST00000859111, ENST00000859112, ENST00000859113, ENST00000859114, ENST00000914566, ENST00000914567, ENST00000914568, ENST00000914569, ENST00000914570, ENST00000914571, ENST00000914573, ENST00000914575, ENST00000914576, ENST00000914577, ENST00000914578, ENST00000914579, ENST00000914580, ENST00000914581, ENST00000970018, ENST00000970019, ENST00000970020, ENST00000970021, ENST00000970022, ENST00000970023, ENST00000970024, ENST00000970025

RefSeq mRNA: 3 — MANE Select: NM_017803 NM_001271762, NM_001271763, NM_017803

CCDS: CCDS10859, CCDS61970

Canonical transcript exons

ENST00000565263 — 17 exons

Exon	Start	End
ENSE00001516666	68025415	68025494
ENSE00001810734	68023284	68023351
ENSE00001822362	68078749	68079320
ENSE00003491546	68070134	68070220
ENSE00003497611	68074034	68074155
ENSE00003505791	68054574	68054617
ENSE00003525450	68076632	68076719
ENSE00003567043	68066566	68066636
ENSE00003579912	68070940	68071108
ENSE00003597822	68038006	68038149
ENSE00003626724	68049505	68049550
ENSE00003635036	68061066	68061113
ENSE00003657723	68066317	68066382
ENSE00003668558	68078445	68078518
ENSE00003691437	68075355	68075504
ENSE00003788831	68053564	68053655
ENSE00003790560	68056364	68056424

Expression profiles

Bgee: expression breadth ubiquitous, 236 present calls, max score 91.30.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 12.0726 / max 214.7140, expressed in 1787 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
154702	8.8492	1773
154701	3.0495	1491
154700	0.0909	11
154706	0.0423	14
154705	0.0406	20

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	91.30	gold quality
left testis	UBERON:0004533	90.97	gold quality
right testis	UBERON:0004534	90.79	gold quality
monocyte	CL:0000576	90.58	gold quality
mononuclear cell	CL:0000842	90.48	gold quality
leukocyte	CL:0000738	90.27	gold quality
pancreatic ductal cell	CL:0002079	90.11	silver quality
blood	UBERON:0000178	89.31	gold quality
testis	UBERON:0000473	88.68	gold quality
spleen	UBERON:0002106	88.18	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	87.24	gold quality
tongue squamous epithelium	UBERON:0006919	85.99	gold quality
lymph node	UBERON:0000029	85.94	gold quality
lower esophagus mucosa	UBERON:0035834	85.53	gold quality
bone marrow cell	CL:0002092	85.36	gold quality
mucosa of transverse colon	UBERON:0004991	85.35	gold quality
type B pancreatic cell	CL:0000169	85.13	gold quality
esophagus mucosa	UBERON:0002469	84.24	gold quality
olfactory bulb	UBERON:0002264	84.23	gold quality
male germ cell	CL:0000015	83.99	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.90	gold quality
sperm	CL:0000019	83.82	gold quality
small intestine Peyer’s patch	UBERON:0003454	83.34	gold quality
bone marrow	UBERON:0002371	83.18	gold quality
skin of leg	UBERON:0001511	83.15	gold quality
vena cava	UBERON:0004087	83.05	silver quality
tonsil	UBERON:0002372	83.04	gold quality
skin of abdomen	UBERON:0001416	82.30	gold quality
gastrocnemius	UBERON:0001388	82.29	gold quality
vermiform appendix	UBERON:0001154	82.23	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	3.34

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

11 targeting DUS2, 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-367-3P	99.98	74.83	1819
HSA-MIR-32-5P	99.98	75.21	1964
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-3925-5P	99.21	67.90	1466
HSA-MIR-4478	99.07	65.16	2320
HSA-MIR-4755-3P	98.77	65.59	1915
HSA-MIR-668-3P	96.18	65.80	673

Literature-anchored findings (GeneRIF, showing 5)

• hDUS2 interacts with protein kinase PKR through its dsRNA binding/dimerization domain and inhibits its kinase activity. (PMID:18096616)
• crystals belonged to space group P2(1) and contained a single molecule of HsDus2L in the asymmetric unit (PMID:22442237)
• Here, the X-ray crystal structure of a construct of hDus2 encompassing the catalytic and tRNA-recognition domains (residues 1-340) determined at 1.9 A resolution is presented. (PMID:26143927)
• This is the first reported case of a tRNA-modifying enzyme (dihydrouridine synthase 2) carrying a dsRNA binding domain used to bind tRNAs. (PMID:26429968)
• we establish that while hDus2 dsRBD retains a conventional dsRNA recognition capability, the presence of an N-terminal extension appended to the canonical domain provides additional residues for binding tRNA in a structure-specific mode of action. (PMID:30605527)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	dus2	ENSDARG00000077607
mus_musculus	Dus2	ENSMUSG00000031901
rattus_norvegicus	Dus2	ENSRNOG00000019819
drosophila_melanogaster	Dus2	FBGN0030554
caenorhabditis_elegans	dus-2	WBGENE00013201

Paralogs (3): DUS4L (ENSG00000105865), DUS3L (ENSG00000141994), DUS1L (ENSG00000169718)

Protein

Protein identifiers

tRNA-dihydrouridine(20) synthase [NAD(P)+]-like — Q9NX74 (reviewed: Q9NX74)

Alternative names: Dihydrouridine synthase 2, Up-regulated in lung cancer protein 8, tRNA-dihydrouridine synthase 2-like

All UniProt accessions (13): E7EUN9, Q9NX74, H3BM64, H3BMK6, H3BQX4, H3BRI6, H3BSF3, H3BTR3, I3L0K0, I3L1K5, I3L4H0, I3L4Y9, J3QLD5

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the NADPH-dependent synthesis of dihydrouridine, a modified base found in the D-loop of most tRNAs. Specifically modifies U20 in cytoplasmic tRNAs. Activity depends on the presence of guanosine at position 19 in the tRNA substrate. Negatively regulates the activation of EIF2AK2/PKR.

Subunit / interactions. Interacts with EPRS1. Interacts (via DRBM domain) with PRKRA and EIF2AK2/PKR (via DRBM 1 domain).

Subcellular location. Cytoplasm. Endoplasmic reticulum.

Tissue specificity. Weak expression in heart, placenta and skeletal muscle. Up-regulated in most lung cancer cells (at protein level).

Activity regulation. Inhibited by canertinib, PD 168393, AST-1306 and PF-6274484.

Domain organisation. Efficient dihydrouridine synthesis requires the presence of both the catalytic domain and the C-terminal RNA-binding DRBM domain.

Similarity. Belongs to the Dus family. Dus2 subfamily.

RefSeq proteins (3): NP_001258691, NP_001258692, NP_060273* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR013785	Aldolase_TIM	Homologous_superfamily
IPR014720	dsRBD_dom	Domain
IPR018517	tRNA_hU_synthase_CS	Conserved_site
IPR035587	DUS-like_FMN-bd	Domain
IPR044463	DUS2_DSRM	Domain
IPR052582	tRNA-DUS-like	Family

Pfam: PF00035, PF01207

Enzyme classification (BRENDA):

• EC 1.3.1.91 — tRNA-dihydrouridine20 synthase [NAD(P)+] (BRENDA: 4 organisms, 19 substrates, 0 inhibitors, 1 Km, 1 kcat entries)

Catalyzed reactions (Rhea), 1 shown:

• 5,6-dihydrouridine(20) in tRNA + NADP(+) = uridine(20) in tRNA + NADPH + H(+) (RHEA:53336)

UniProt features (74 total): helix 22, strand 17, mutagenesis site 11, binding site 7, turn 6, region of interest 5, modified residue 2, chain 1, domain 1, compositionally biased region 1, active site 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
4WFT	X-RAY DIFFRACTION	1.7
5OC4	X-RAY DIFFRACTION	1.71
5OC5	X-RAY DIFFRACTION	1.89
4XP7	X-RAY DIFFRACTION	1.9
6EZA	X-RAY DIFFRACTION	2
6EZC	X-RAY DIFFRACTION	2
6F00	X-RAY DIFFRACTION	2.16
6EI8	X-RAY DIFFRACTION	2.25
6EZB	X-RAY DIFFRACTION	2.25
4WFS	X-RAY DIFFRACTION	2.68
5OC6	X-RAY DIFFRACTION	3.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NX74-F1	87.81	0.76

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 (proton donor)

Ligand- & substrate-binding residues (7): 43; 87; 155; 183; 214–216; 242–243; 18–20

Post-translational modifications (2): 445, 488

Mutagenesis-validated functional residues (11):

Position	Phenotype
294	increased affinity for trna and increased dihydrouridine synthesis; when associated with k-305.
305	increased affinity for trna and increased dihydrouridine synthesis; when associated with k-294.
361–362	decreased affinity for trna.
367	mildly decreased affinity for trna.
371	strongly decreased affinity for trna.
372	mildly decreased affinity for trna.
379	mildly decreased affinity for trna.
397	mildly decreased affinity for trna.
417	mildly decreased affinity for trna.
419	decreased affinity for trna. strongly decreased affinity for trna; when associated with a-420.
420	decreased affinity for trna. strongly decreased affinity for trna; when associated with a-419.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-6782315	tRNA modification in the nucleus and cytosol
R-HSA-9833482	PKR-mediated signaling

MSigDB gene sets: 150 (showing top): WANG_CLIM2_TARGETS_UP, chr16q22, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_THE_CH_CH_GROUP_OF_DONORS, GOBP_TRNA_METABOLIC_PROCESS, SENESE_HDAC1_AND_HDAC2_TARGETS_DN, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM, GOBP_RNA_MODIFICATION, DOANE_RESPONSE_TO_ANDROGEN_DN, CREB_Q2_01, GOBP_DEFENSE_RESPONSE_TO_VIRUS, GOBP_TRNA_PROCESSING, CREBP1CJUN_01, GOBP_RESPONSE_TO_VIRUS, REACTOME_METABOLISM_OF_RNA

GO Biological Process (3): tRNA dihydrouridine synthesis (GO:0002943), antiviral innate immune response (GO:0140374), tRNA processing (GO:0008033)

GO Molecular Function (11): tRNA binding (GO:0000049), double-stranded RNA binding (GO:0003725), protein kinase inhibitor activity (GO:0004860), FMN binding (GO:0010181), tRNA dihydrouridine synthase activity (GO:0017150), flavin adenine dinucleotide binding (GO:0050660), NADPH binding (GO:0070402), tRNA-dihydrouridine20 synthase activity (GO:0102264), RNA binding (GO:0003723), protein binding (GO:0005515), oxidoreductase activity (GO:0016491)

GO Cellular Component (4): cytoplasm (GO:0005737), mitochondrion (GO:0005739), endoplasmic reticulum (GO:0005783), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
tRNA processing	1
Antimicrobial mechanism of IFN-stimulated genes	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
anion binding	3
cytoplasm	3
RNA binding	2
cellular anatomical structure	2
intracellular membrane-bounded organelle	2
tRNA modification	1
innate immune response	1
defense response to virus	1
RNA processing	1
tRNA metabolic process	1
protein kinase activity	1
kinase inhibitor activity	1
protein kinase regulator activity	1
ribonucleotide binding	1
tRNA dihydrouridine synthesis	1
RNA dihydrouridine synthase activity	1
catalytic activity, acting on a tRNA	1
nucleotide binding	1
NADP binding	1
tRNA dihydrouridine synthase activity	1
nucleic acid binding	1
binding	1
catalytic activity	1
intracellular anatomical structure	1
endomembrane system	1

Protein interactions and networks

STRING

1882 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DUS2	EPRS1	P07814	918
DUS2	TRMT1	Q9NXH9	644
DUS2	TRMT5	Q32P41	643
DUS2	TRUB1	Q8WWH5	629
DUS2	TRIT1	Q9H3H1	614
DUS2	DDX28	Q9NUL7	592
DUS2	TRMT10A	Q8TBZ6	548
DUS2	TRMT61A	Q96FX7	532
DUS2	COMTD1	Q86VU5	530
DUS2	DTWD2	Q8NBA8	530
DUS2	TRMT44	Q8IYL2	514
DUS2	DTWD1	Q8N5C7	512
DUS2	BUD13	Q9BRD0	504
DUS2	GTPBP3	Q969Y2	491
DUS2	MAP6D1	Q9H9H5	489

IntAct

15 interactions, top by confidence:

A	B	Type	Score
KANSL1	PHF20L1	psi-mi:“MI:0914”(association)	0.530
NS	DUS2	psi-mi:“MI:0915”(physical association)	0.370
DUS2	NS1	psi-mi:“MI:0915”(physical association)	0.370
DUS2	NS	psi-mi:“MI:0915”(physical association)	0.370
NECTIN2	DUS2	psi-mi:“MI:0915”(physical association)	0.370
DUS2	SMN1	psi-mi:“MI:0915”(physical association)	0.370
DUS2	TK1	psi-mi:“MI:0915”(physical association)	0.370
JUN		psi-mi:“MI:0914”(association)	0.350
SSB	RPS3A	psi-mi:“MI:0914”(association)	0.350
KANSL1	ECI2	psi-mi:“MI:0914”(association)	0.350

BioGRID (27): DUS2 (Affinity Capture-MS), DUS2 (Affinity Capture-MS), DUS2 (Affinity Capture-MS), DUS2 (Two-hybrid), DUS2 (Two-hybrid), PRKRA (Two-hybrid), EIF2AK2 (Two-hybrid), DUS2 (Reconstituted Complex), DUS2 (Reconstituted Complex), EIF2AK2 (Affinity Capture-Western), PRKRA (Affinity Capture-Western), DUS2 (Affinity Capture-MS), DUS2 (Co-fractionation), DUS2 (Co-fractionation), DUS2 (Co-fractionation)

ESM2 similar proteins: A2VE14, A5PLN9, B1WC68, D3Z7P3, O54865, O89050, O94925, P13264, P16068, P20595, P38024, P51583, P97834, Q02153, Q0VCB2, Q0VCJ8, Q13042, Q13098, Q3TIR1, Q4R4U1, Q4ZHR9, Q5F450, Q5M887, Q5NVN7, Q5R5F8, Q5RB35, Q5RB59, Q5RBN9, Q5RKN4, Q5ZJB7, Q5ZMH6, Q67FW5, Q6AXQ0, Q6NRT5, Q86TJ2, Q8R349, Q8VH37, Q91YQ7, Q99LD4, Q99PV3

Diamond homologs: A3LUK5, A5DBS1, O25427, O27281, O52532, O52533, O52536, O52539, O67533, O68273, O83945, O95620, P0A2R6, P0A2R7, P0ABT5, P0ABT6, P0ABT7, P0CN28, P0CN29, P33371, P37567, P41504, P44606, P44965, P45672, P9WNS6, P9WNS7, Q06063, Q08111, Q09504, Q1RH84, Q28BT8, Q3KRC5, Q3SWF0, Q4UNJ4, Q50049, Q54CU9, Q55724, Q68XZ3, Q6CWM0

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	69
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

5819 predictions. Top by Δscore:

Variant	Effect	Δscore
16:67989319:TCA:T	donor_loss	1.0000
16:67989320:CACT:C	donor_loss	1.0000
16:67989321:A:AC	donor_gain	1.0000
16:67989321:AC:A	donor_loss	1.0000
16:67989322:C:CT	donor_gain	1.0000
16:67989322:CTTG:C	donor_gain	1.0000
16:67989394:GTGAT:G	acceptor_gain	1.0000
16:67989395:TGAT:T	acceptor_gain	1.0000
16:67989396:GAT:G	acceptor_gain	1.0000
16:67989398:TCTG:T	acceptor_loss	1.0000
16:67989399:C:CC	acceptor_gain	1.0000
16:67989399:CTGG:C	acceptor_loss	1.0000
16:67990132:C:CC	acceptor_gain	1.0000
16:67991008:A:C	acceptor_gain	1.0000
16:67991880:C:CA	donor_gain	1.0000
16:67991975:CAGAG:C	acceptor_gain	1.0000
16:67991980:C:CC	acceptor_gain	1.0000
16:67992060:CTAC:C	donor_loss	1.0000
16:67992062:ACCTT:A	donor_loss	1.0000
16:67992063:C:CT	donor_loss	1.0000
16:67992189:CAGAA:C	acceptor_gain	1.0000
16:68038002:TCAG:T	acceptor_loss	1.0000
16:68038004:A:AG	acceptor_gain	1.0000
16:68038004:A:G	acceptor_loss	1.0000
16:68038004:AG:A	acceptor_gain	1.0000
16:68038005:G:GA	acceptor_gain	1.0000
16:68038005:GG:G	acceptor_gain	1.0000
16:68038005:GGC:G	acceptor_gain	1.0000
16:68038005:GGCT:G	acceptor_gain	1.0000
16:68038149:GGTAA:G	donor_loss	1.0000

AlphaMissense

3192 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
16:68038106:G:C	R28T	0.999
16:68038106:G:T	R28M	0.999
16:68038107:G:C	R28S	0.999
16:68038107:G:T	R28S	0.999
16:68056394:C:A	N113K	0.999
16:68056394:C:G	N113K	0.999
16:68056401:T:C	C116R	0.999
16:68066361:C:G	C154W	0.999
16:68066627:T:A	V182D	0.999
16:68066636:G:C	R185T	0.999
16:68070134:G:C	R185S	0.999
16:68070134:G:T	R185S	0.999
16:68038139:T:A	V39D	0.998
16:68053615:G:C	R75P	0.998
16:68056390:T:A	V112D	0.998
16:68066359:T:C	C154R	0.998
16:68066636:G:T	R185M	0.998
16:68074069:G:C	K282N	0.998
16:68074069:G:T	K282N	0.998
16:68076658:C:A	P370H	0.998
16:68078482:T:A	V403D	0.998
16:68038114:G:C	A31P	0.997
16:68054574:G:A	G89R	0.997
16:68054574:G:C	G89R	0.997
16:68054574:G:T	G89W	0.997
16:68056392:A:G	N113D	0.997
16:68056398:G:C	G115R	0.997
16:68061075:G:A	G127R	0.997
16:68061075:G:C	G127R	0.997
16:68066360:G:A	C154Y	0.997

dbSNP variants (sampled 300 via entrez): RS1000021461 (16:68064558 C>A,T), RS1000061433 (16:68074901 G>T), RS1000088000 (16:68066011 A>G), RS1000134505 (16:68074675 G>A), RS1000135250 (16:68029207 A>C), RS1000160049 (16:68045667 G>A), RS1000209731 (16:68048192 T>A), RS1000263589 (16:68045214 A>G), RS1000288415 (16:68031761 C>T), RS1000321413 (16:68055330 A>C,T), RS1000445110 (16:68031467 A>G,T), RS1000473246 (16:68048605 G>A,T), RS1000495184 (16:68037073 T>C), RS1000499244 (16:68064050 A>G), RS1000550224 (16:68046732 G>A)

Disease associations

OMIM: gene MIM:609707 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST002539_84	Schizophrenia	2.000000e-08
GCST006803_42	Schizophrenia	4.000000e-08
GCST010002_113	Refractive error	2.000000e-14
GCST010083_349	Hemoglobin levels	9.000000e-12
GCST90002381_92	Eosinophil count	7.000000e-13

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004509	hemoglobin measurement
EFO:0004842	eosinophil count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3879825 (SINGLE PROTEIN)

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

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
5.80	IC50	1600	nM	CHEMBL3883534

PubChem BioAssay actives

1 with measured affinity, of 1 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
N-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]prop-2-enamide	1337178: Inhibition of PF-06422899 binding to recombinant C-terminal FLAG-tagged DUS2L (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay	ic50	1.6000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects expression, decreases expression	2
TAK-243	increases sumoylation	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
bisphenol A	affects cotreatment, increases methylation	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
CGP 52608	affects binding, increases reaction	1
Arsenic Trioxide	decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Acrolein	affects cotreatment, increases oxidation, increases abundance	1
Air Pollutants	affects cotreatment, increases abundance, increases oxidation	1
Atrazine	decreases expression	1
Benzo(a)pyrene	increases methylation	1
Cadmium	increases abundance, increases expression	1
Doxorubicin	decreases expression	1
Ethyl Methanesulfonate	decreases expression	1
Methyl Methanesulfonate	decreases expression	1
Ozone	increases oxidation, increases abundance, affects cotreatment	1
Thiram	decreases expression	1
Tobacco Smoke Pollution	affects expression	1
Tretinoin	decreases expression	1
Urethane	decreases expression	1
Aflatoxin B1	increases methylation	1
Cadmium Chloride	increases abundance, increases expression	1
Copper Sulfate	decreases expression	1
Lactic Acid	decreases expression	1
Acrylamide	decreases expression	1
Volatile Organic Compounds	affects cotreatment, increases oxidation	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3877215	Binding	Inhibition of PF-06422899 binding to recombinant C-terminal FLAG-tagged DUS2L (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay	Non-kinase targets of protein kinase inhibitors. — Nat Rev Drug Discov

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_E0U0	Ubigene Hep G2 DUS2 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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