DYRK3

Summary

DYRK3 (dual specificity tyrosine phosphorylation regulated kinase 3, HGNC:3094) is a protein-coding gene on chromosome 1q32.1, encoding Dual specificity tyrosine-phosphorylation-regulated kinase 3 (O43781). Dual-specificity protein kinase that promotes disassembly of several types of membraneless organelles during mitosis, such as stress granules, nuclear speckles and pericentriolar material.

This gene product belongs to the DYRK family of dual-specificity protein kinases that catalyze autophosphorylation on serine/threonine and tyrosine residues. The members of this family share structural similarity, however, differ in their substrate specificity, suggesting their involvement in different cellular functions. The encoded protein has been shown to autophosphorylate on tyrosine residue and catalyze phosphorylation of histones H3 and H2B in vitro. Alternatively spliced transcript variants encoding different isoforms have been identified.

Source: NCBI Gene 8444 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 78 total
• Druggable target: yes — 16 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_003582

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3094
Approved symbol	DYRK3
Name	dual specificity tyrosine phosphorylation regulated kinase 3
Location	1q32.1
Locus type	gene with protein product
Status	Approved
Aliases	RED, REDK, hYAK3-2
Ensembl gene	ENSG00000143479
Ensembl biotype	protein_coding
OMIM	603497
Entrez	8444

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 5 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000367106, ENST00000367108, ENST00000367109, ENST00000441486, ENST00000489878, ENST00000649163

RefSeq mRNA: 2 — MANE Select: NM_003582 NM_001004023, NM_003582

CCDS: CCDS30999, CCDS31000

Canonical transcript exons

ENST00000367109 — 3 exons

Exon	Start	End
ENSE00001826413	206635536	206635780
ENSE00001863463	206647388	206655158
ENSE00003677693	206637650	206637761

Expression profiles

Bgee: expression breadth ubiquitous, 199 present calls, max score 92.63.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 12.1316 / max 467.2797, expressed in 1702 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter ID	TPM avg	Samples expressed
8123	10.1820	1683
8124	1.6528	813
8122	0.1818	43
8125	0.0397	3
8126	0.0251	6
8127	0.0241	6
8128	0.0183	6
8129	0.0079	2

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
type B pancreatic cell	CL:0000169	92.63	silver quality
left testis	UBERON:0004533	89.99	gold quality
olfactory bulb	UBERON:0002264	89.85	gold quality
right testis	UBERON:0004534	89.46	gold quality
diaphragm	UBERON:0001103	88.82	gold quality
testis	UBERON:0000473	87.75	gold quality
male germ cell	CL:0000015	87.57	silver quality
sperm	CL:0000019	86.89	silver quality
vena cava	UBERON:0004087	86.57	silver quality
cartilage tissue	UBERON:0002418	86.17	gold quality
adult organism	UBERON:0007023	85.52	gold quality
islet of Langerhans	UBERON:0000006	84.94	gold quality
stromal cell of endometrium	CL:0002255	84.40	gold quality
mucosa of paranasal sinus	UBERON:0005030	84.33	silver quality
apex of heart	UBERON:0002098	84.27	gold quality
mucosa of urinary bladder	UBERON:0001259	83.73	silver quality
heart left ventricle	UBERON:0002084	83.28	gold quality
cardiac ventricle	UBERON:0002082	83.13	gold quality
right atrium auricular region	UBERON:0006631	82.99	gold quality
gall bladder	UBERON:0002110	82.79	gold quality
cardiac atrium	UBERON:0002081	82.53	gold quality
hair follicle	UBERON:0002073	82.09	gold quality
epithelium of nasopharynx	UBERON:0001951	81.96	silver quality
heart	UBERON:0000948	81.90	gold quality
tongue squamous epithelium	UBERON:0006919	81.70	gold quality
superficial temporal artery	UBERON:0001614	81.04	gold quality
epithelium of mammary gland	UBERON:0003244	80.70	silver quality
mammary duct	UBERON:0001765	80.63	silver quality
smooth muscle tissue	UBERON:0001135	80.61	gold quality
cervix squamous epithelium	UBERON:0006922	80.38	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	7.97

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

31 targeting DYRK3, 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-3163	100.00	77.23	8605
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-374B-5P	99.90	69.98	2734
HSA-MIR-374A-5P	99.90	71.34	2923
HSA-MIR-466	99.67	70.85	2863
HSA-MIR-10393-5P	99.65	68.01	1368
HSA-MIR-5700	99.64	69.88	2280
HSA-MIR-657	99.48	66.02	848
HSA-MIR-4687-5P	99.14	66.26	488
HSA-MIR-3926	98.95	69.26	1438
HSA-MIR-129-1-3P	98.86	68.41	779
HSA-MIR-129-2-3P	98.86	68.41	779
HSA-MIR-4635	98.74	67.63	1339
HSA-MIR-330-5P	98.73	67.63	1788
HSA-MIR-4780	98.57	64.75	611
HSA-MIR-548S	98.50	67.17	1213
HSA-MIR-3187-5P	98.36	65.74	1776
HSA-MIR-326	98.25	66.44	1565
HSA-MIR-5087	98.01	69.09	965
HSA-MIR-1285-3P	97.72	67.02	1932
HSA-MIR-5189-5P	97.72	66.96	1814
HSA-MIR-6779-3P	97.51	65.82	789
HSA-MIR-612	97.26	65.95	1597
HSA-MIR-6860	97.21	66.31	1656
HSA-MIR-5694	97.06	67.70	682
HSA-MIR-27A-5P	97.01	65.63	528
HSA-MIR-192-5P	94.82	66.14	417

Literature-anchored findings (GeneRIF, showing 13)

• DYRK3 has roles in kinase activation, binding to CREB, and hematopoietic progenitor cell survival (PMID:12356771)
• DYRK3, expression is strong in erythroid cells and testis, but is also detected in adult kidney and liver (PMID:15607427)
• DYRK3 dual-specificity kinase attenuates erythropoiesis during anemia (PMID:18854306)
• DYRK1A and DYRK3 promote cell survival through phosphorylation and activation of SIRT1. (PMID:20167603)
• the lipid raft-dependent endocytosis process mediates C. neoformans internalization into HBMEC and the CD44 protein of the hosts, cytoskeleton, and intracellular kinase-DYRK3 are involved in this process (PMID:21693704)
• Study identified the dual specificity tyrosine-phosphorylation-regulated kinase 3 (DYRK3) as a protein with the ability to condense P-granule-like speckles in the cytosol and to prevent stress granule dissolution via its N-terminal domain when it is in a kinase-inactive form. (PMID:23415227)
• Study shows that the auto-phosphorylation of S350 of DYRK3 stabilizes the protein and positively regulates the functional activity. The S350 residue is located between N-lobe and C-lobe and its auto-phosphorylation mediates hydrogen bond interactions with many nearby residues from C-lobe domain and alphaC-helix to stabilize overall structure. (PMID:29634919)
• a mechanism in which the dilution of phase-separating proteins during nuclear-envelope breakdown and the DYRK3-dependent degree of their solubility combine to allow cells to dissolve and condense several membraneless organelles during mitosis (PMID:29973724)
• Dual Specificity Kinase DYRK3 Promotes Aggressiveness of Glioblastoma by Altering Mitochondrial Morphology and Function. (PMID:33804169)
• Protein quality control of DYRK family protein kinases by the Hsp90-Cdc37 molecular chaperone. (PMID:34147560)
• DYRK3 contributes to differentiation and hypoxic control in neuroblastoma. (PMID:34171798)
• Dual-Specificity, Tyrosine Phosphorylation-Regulated Kinases (DYRKs) and cdc2-Like Kinases (CLKs) in Human Disease, an Overview. (PMID:34205123)
• Dual-specificity kinase DYRK3 phosphorylates p62 at the Thr-269 residue and promotes melanoma progression. (PMID:38519031)

Cross-species orthologs

7 orthologs

Organism	Symbol	Gene ID
danio_rerio	dyrk3	ENSDARG00000070600
mus_musculus	Dyrk3	ENSMUSG00000016526
rattus_norvegicus	Dyrk3	ENSRNOG00000004870
drosophila_melanogaster	mnb	FBGN0259168
caenorhabditis_elegans		WBGENE00003149
caenorhabditis_elegans		WBGENE00013727
caenorhabditis_elegans		WBGENE00185089

Paralogs (12): DYRK4 (ENSG00000010219), CLK1 (ENSG00000013441), HIPK2 (ENSG00000064393), DYRK1B (ENSG00000105204), HIPK3 (ENSG00000110422), CLK4 (ENSG00000113240), DYRK2 (ENSG00000127334), DYRK1A (ENSG00000157540), HIPK4 (ENSG00000160396), HIPK1 (ENSG00000163349), CLK2 (ENSG00000176444), CLK3 (ENSG00000179335)

Protein

Protein identifiers

Dual specificity tyrosine-phosphorylation-regulated kinase 3 — O43781 (reviewed: O43781)

Alternative names: Regulatory erythroid kinase

All UniProt accessions (3): O43781, A0A3B3ISB2, Q5SY34

UniProt curated annotations — full annotation on UniProt →

Function. Dual-specificity protein kinase that promotes disassembly of several types of membraneless organelles during mitosis, such as stress granules, nuclear speckles and pericentriolar material. Dual-specificity tyrosine-regulated kinases (DYRKs) autophosphorylate a critical tyrosine residue in their activation loop and phosphorylate their substrate on serine and threonine residues. Acts as a central dissolvase of membraneless organelles during the G2-to-M transition, after the nuclear-envelope breakdown: acts by mediating phosphorylation of multiple serine and threonine residues in unstructured domains of proteins, such as SRRM1 and PCM1. Does not mediate disassembly of all membraneless organelles: disassembly of P-body and nucleolus is not regulated by DYRK3. Dissolution of membraneless organelles at the onset of mitosis is also required to release mitotic regulators, such as ZNF207, from liquid-unmixed organelles where they are sequestered and keep them dissolved during mitosis. Regulates mTORC1 by mediating the dissolution of stress granules: during stressful conditions, DYRK3 partitions from the cytosol to the stress granule, together with mTORC1 components, which prevents mTORC1 signaling. When stress signals are gone, the kinase activity of DYRK3 is required for the dissolution of stress granule and mTORC1 relocation to the cytosol: acts by mediating the phosphorylation of the mTORC1 inhibitor AKT1S1, allowing full reactivation of mTORC1 signaling. Also acts as a negative regulator of EPO-dependent erythropoiesis: may place an upper limit on red cell production during stress erythropoiesis. Inhibits cell death due to cytokine withdrawal in hematopoietic progenitor cells. Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1: this in turn inhibits p53/TP53 activity and apoptosis.

Subunit / interactions. Interacts with SIRT1.

Subcellular location. Nucleus. Cytoplasm. Nucleus speckle. Cytoplasmic granule. Cytoskeleton. Microtubule organizing center. Centrosome.

Tissue specificity. Isoform 1: Highly expressed in testis and in hematopoietic tissue such as fetal liver, and bone marrow. Isoform 1: Predominant form in fetal liver and bone marrow. Isoform 1: Present at low levels in heart, pancreas, lymph node and thymus. Isoform 2: Highly expressed in testis and in hematopoietic tissue such as fetal liver, and bone marrow. Isoform 2: Predominant form in testis. Isoform 2: Present at low levels in heart, pancreas, lymph node and thymus.

Post-translational modifications. Ubiquitinated at anaphase by the anaphase-promoting complex (APC/C), leading to its degradation by the proteasome. Protein kinase activity is activated following autophosphorylation at Tyr-369. Autophosphorylation at Ser-350 stabilizes the protein and enhances the protein kinase activity.

Activity regulation. Protein kinase activity is activated following autophosphorylation at Tyr-369. Inhibited by harmine, an ATP competitive inhibitor. Inhibited by small-compound GSK-626616.

Domain organisation. The N-terminal domain, which is intrinsically disordered, is required for stress granule localization.

Induction. By EPO/erythropoietin.

Similarity. Belongs to the protein kinase superfamily. CMGC Ser/Thr protein kinase family. MNB/DYRK subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
O43781-1	1, Long	yes
O43781-2	2, Short

RefSeq proteins (2): NP_001004023, NP_003573* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR042521	DYRK	Homologous_superfamily
IPR050494	Ser_Thr_dual-spec_kinase	Family

Pfam: PF00069

Enzyme classification (BRENDA):

• EC 2.7.12.1 — dual-specificity kinase (BRENDA: 51 organisms, 125 substrates, 188 inhibitors, 14 Km, 10 kcat entries)

Substrate kinetics (BRENDA)

2 substrates with measured Km, best-characterized 2. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.019–0.1185	7
HISTONE H1	0.006–0.012	5

Catalyzed reactions (Rhea), 3 shown:

• L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)
• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (55 total): helix 19, strand 9, turn 7, mutagenesis site 4, binding site 3, modified residue 2, splice variant 2, sequence conflict 2, chain 1, domain 1, sequence variant 1, region of interest 1, short sequence motif 1, compositionally biased region 1, active site 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
5Y86	X-RAY DIFFRACTION	1.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O43781-F1	76.21	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.

Catalytic / active sites (1): 335 (proton acceptor)

Ligand- & substrate-binding residues (3): 215–223; 238; 288–291

Post-translational modifications (2): 369, 350

Mutagenesis-validated functional residues (4):

Position	Phenotype
238	kinase dead; induces formation of stress granules-like in absence of stress. impaired dissolution of membraneless organe
350	decreased stability of the protein.
350	phosphomimetic mutant; increased stability of the protein.
470–474	abolishes localization to the nucleus, leading to impaired dissolution of nuclear speckles during mitosis.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 236 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_MYELOID_CELL_HOMEOSTASIS, MODULE_64, GOBP_ERYTHROCYTE_HOMEOSTASIS, GOBP_CELL_CYCLE_PHASE_TRANSITION, GAUSSMANN_MLL_AF4_FUSION_TARGETS_G_DN, GOCC_MICROTUBULE_ORGANIZING_CENTER, GOBP_REGULATION_OF_DNA_DAMAGE_RESPONSE_SIGNAL_TRANSDUCTION_BY_P53_CLASS_MEDIATOR, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, GOBP_REGULATION_OF_CELL_CYCLE_G2_M_PHASE_TRANSITION, NIKOLSKY_BREAST_CANCER_1Q32_AMPLICON, GOBP_POSITIVE_REGULATION_OF_CELL_CYCLE_G2_M_PHASE_TRANSITION, MODULE_75, ATF1_Q6, SASSON_RESPONSE_TO_FORSKOLIN_DN

GO Biological Process (11): protein phosphorylation (GO:0006468), erythrocyte differentiation (GO:0030218), nuclear speck organization (GO:0035063), stress granule disassembly (GO:0035617), negative regulation of apoptotic process (GO:0043066), negative regulation of DNA damage response, signal transduction by p53 class mediator (GO:0043518), cell division (GO:0051301), regulation of cellular response to stress (GO:0080135), positive regulation of cell cycle G2/M phase transition (GO:1902751), organelle disassembly (GO:1903008), regulation of TORC1 signaling (GO:1903432)

GO Molecular Function (12): magnesium ion binding (GO:0000287), protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), protein serine/threonine/tyrosine kinase activity (GO:0004712), protein tyrosine kinase activity (GO:0004713), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), metal ion binding (GO:0046872)

GO Cellular Component (9): pericentriolar material (GO:0000242), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), cytoskeleton (GO:0005856), cytoplasmic stress granule (GO:0010494), nuclear speck (GO:0016607), centrosome (GO:0005813)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein kinase activity	4
cellular anatomical structure	4
phosphorylation	1
protein modification process	1
myeloid cell differentiation	1
erythrocyte homeostasis	1
nuclear body organization	1
protein-RNA complex disassembly	1
organelle disassembly	1
apoptotic process	1
regulation of apoptotic process	1
negative regulation of programmed cell death	1
DNA damage response, signal transduction by p53 class mediator	1
regulation of DNA damage response, signal transduction by p53 class mediator	1
negative regulation of signal transduction by p53 class mediator	1
cellular process	1
cellular response to stress	1
regulation of cellular process	1
regulation of response to stress	1
cell cycle G2/M phase transition	1
positive regulation of cell cycle phase transition	1
regulation of cell cycle G2/M phase transition	1
organelle organization	1
cellular component disassembly	1
regulation of TOR signaling	1
TORC1 signaling	1
metal ion binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
cation binding	1
centrosome	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

988 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DYRK3	H2BC21	Q16778	517
DYRK3	GATA1	P15976	515
DYRK3	G3BP1	Q13283	406
DYRK3	MKRN2OS	H3BPM6	400
DYRK3	LNX1	Q8TBB1	389
DYRK3	PNRC1	Q12796	381
DYRK3	RPS19BP1	Q86WX3	376
DYRK3	EPB42	P16452	363
DYRK3	AKT1S1	Q96B36	352
DYRK3	ARHGEF10L	Q9HCE6	343
DYRK3	CADPS	Q9ULU8	337
DYRK3	DCAF7	P61962	333
DYRK3	EEF2	P13639	330
DYRK3	SLC13A5	Q86YT5	325
DYRK3	TIA1	P31483	323

IntAct

10 interactions, top by confidence:

A	B	Type	Score
ZNRD2	CCDC85C	psi-mi:“MI:0914”(association)	0.530
Ogn	DYRK3	psi-mi:“MI:0407”(direct interaction)	0.440
DYRK3	PKM	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
SIRT1	DYRK3	psi-mi:“MI:0915”(physical association)	0.400
DYRK3	SORL1	psi-mi:“MI:0915”(physical association)	0.400
NEK4	E2F8	psi-mi:“MI:0914”(association)	0.350
DYRK3	EIF3F	psi-mi:“MI:0914”(association)	0.350
FTL		psi-mi:“MI:0914”(association)	0.350
DYRK3	PRNP	psi-mi:“MI:0407”(direct interaction)	0.000

BioGRID (46): DYRK3 (Reconstituted Complex), Sirt1 (Biochemical Activity), DYRK3 (Affinity Capture-MS), DYRK3 (Affinity Capture-MS), DYRK3 (Two-hybrid), DYRK3 (Affinity Capture-MS), DYRK3 (Affinity Capture-MS), DYRK3 (Reconstituted Complex), EIF3F (Affinity Capture-MS), HSPB1 (Affinity Capture-MS), EIF2S1 (Affinity Capture-MS), TPM3 (Affinity Capture-MS), TPM2 (Affinity Capture-MS), SNRPB2 (Affinity Capture-MS), TPM1 (Affinity Capture-MS)

ESM2 similar proteins: B3WFY8, O35831, O43781, P20793, P20794, P23293, P39073, P83101, Q00537, Q03407, Q03957, Q04859, Q4R6S5, Q4R7T5, Q501Q9, Q5R754, Q5SN53, Q5U4C9, Q5VN19, Q5XIT0, Q5ZCI1, Q5ZIU3, Q62726, Q63686, Q67C40, Q6BV06, Q6CR51, Q6CRA9, Q6FKC6, Q6FQ83, Q6Z8C8, Q753D9, Q75D46, Q75KK8, Q8K0D0, Q8W4J2, Q922Y0, Q92630, Q92772, Q96WV9

Diamond homologs: A4L9P5, A8WJR8, A8X4H1, A8X5H5, B3WFY8, G5EDB2, O14132, O23145, O43781, O55076, O76039, O88850, O88904, P14680, P18265, P18431, P20911, P22518, P24941, P43288, P43289, P48963, P49657, P49759, P49840, P50613, P51136, P51567, P51568, P51952, P83102, Q00526, Q03147, Q04859, Q07538, Q08DZ2, Q09690, Q09815, Q0IJ08, Q10156

SIGNOR signaling

6 interactions.

A	Effect	B	Mechanism
DYRK3	down-regulates	AKT1S1	phosphorylation
DYRK3	down-regulates	mTORC1	phosphorylation
DYRK3	“down-regulates activity”	NCOA3	phosphorylation
ATF4	“down-regulates quantity by repression”	DYRK3	“transcriptional regulation”
DYRK3	“down-regulates activity”	AKT1S1	phosphorylation
DYRK3	“up-regulates activity”	SIRT1	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	70
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

664 predictions. Top by Δscore:

Variant	Effect	Δscore
1:206635697:C:G	donor_gain	1.0000
1:206636954:G:GT	donor_gain	1.0000
1:206636961:A:T	donor_gain	1.0000
1:206636964:GAGAA:G	donor_gain	1.0000
1:206636966:G:GT	donor_gain	1.0000
1:206636966:GAA:G	donor_gain	1.0000
1:206636969:G:GG	donor_gain	1.0000
1:206637647:TAG:T	acceptor_loss	1.0000
1:206637648:AGGTT:A	acceptor_gain	1.0000
1:206637649:G:GA	acceptor_loss	1.0000
1:206637649:GGTTG:G	acceptor_gain	1.0000
1:206637762:G:GG	donor_gain	1.0000
1:206647384:A:AG	acceptor_gain	1.0000
1:206647384:ATAG:A	acceptor_loss	1.0000
1:206647385:T:G	acceptor_gain	1.0000
1:206647385:TAGAT:T	acceptor_loss	1.0000
1:206647386:A:AG	acceptor_gain	1.0000
1:206647386:AGAT:A	acceptor_gain	1.0000
1:206647387:G:GA	acceptor_gain	1.0000
1:206647387:GA:G	acceptor_gain	1.0000
1:206647387:GAT:G	acceptor_gain	1.0000
1:206647387:GATG:G	acceptor_gain	1.0000
1:206647387:GATGA:G	acceptor_gain	1.0000
1:206635590:TCGA:T	donor_gain	0.9900
1:206635635:GGC:G	donor_gain	0.9900
1:206635636:GC:G	donor_gain	0.9900
1:206635636:GCG:G	donor_gain	0.9900
1:206635638:G:GG	donor_gain	0.9900
1:206635778:G:GT	donor_gain	0.9900
1:206635820:G:GT	donor_gain	0.9900

AlphaMissense

3875 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:206647856:T:C	F220L	1.000
1:206647858:T:A	F220L	1.000
1:206647858:T:G	F220L	1.000
1:206647912:A:C	K238N	1.000
1:206647912:A:T	K238N	1.000
1:206648202:A:C	D335A	1.000
1:206648202:A:T	D335V	1.000
1:206648262:A:T	D355V	1.000
1:206648263:C:A	D355E	1.000
1:206648263:C:G	D355E	1.000
1:206647821:G:C	R208P	0.999
1:206647860:G:A	G221E	0.999
1:206647905:C:A	A236D	0.999
1:206647908:T:C	L237P	0.999
1:206647910:A:G	K238E	0.999
1:206647911:A:T	K238I	0.999
1:206647977:T:C	L260P	0.999
1:206648036:T:C	F280L	0.999
1:206648038:C:A	F280L	0.999
1:206648038:C:G	F280L	0.999
1:206648040:G:C	R281P	0.999
1:206648202:A:G	D335G	0.999
1:206648203:T:A	D335E	0.999
1:206648203:T:G	D335E	0.999
1:206648209:G:C	K337N	0.999
1:206648209:G:T	K337N	0.999
1:206648216:A:C	N340H	0.999
1:206648216:A:G	N340D	0.999
1:206648217:A:C	N340T	0.999
1:206648217:A:G	N340S	0.999

dbSNP variants (sampled 300 via entrez): RS1000775981 (1:206649305 G>A), RS1001050177 (1:206637124 A>G), RS1001223845 (1:206651104 C>G), RS1001668757 (1:206643031 G>A,T), RS1002000921 (1:206644631 C>T), RS1002086409 (1:206650180 C>T), RS1002327920 (1:206638284 T>G), RS1002597011 (1:206637880 G>T), RS1003072831 (1:206639740 G>A,C), RS1003788189 (1:206646469 A>G), RS1003842324 (1:206640331 C>T), RS1003858119 (1:206633586 C>A,T), RS1004497064 (1:206652005 C>T), RS1004827708 (1:206653398 C>A,T), RS1005002325 (1:206646827 C>T)

Disease associations

OMIM: gene MIM:603497 | 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
GCST90002392_249	Mean corpuscular volume	3.000000e-13

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4575 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

16 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 230,515 (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
CHEMBL1173055	RUCAPARIB	4	7,009
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL5416410	DASATINIB	4	655
CHEMBL140	CURCUMIN	3	93,882
CHEMBL223360	LINIFANIB	3	3,925
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	22,804
CHEMBL1230165	SILMITASERTIB	2	593
CHEMBL1614713	CC-401	2	389
CHEMBL1738757	REBASTINIB	2	1,478
CHEMBL565612	SOTRASTAURIN	2	1,355
CHEMBL1969664	AZD-1080	1	600
CHEMBL269538	HARMINE	1	4,346
CHEMBL4784318	CIRTUVIVINT	1	34
CHEMBL482767	SNS-314	1	336
CHEMBL5426285	5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)-	1	4

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

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Dyrk2 subfamily

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
compound 1a [PMID: 24900749]	Inhibition	7.15	pIC50
compound 20 [PMID: 30998356]	Inhibition	6.98	pIC50
compound 3b [PMID: 23454515]	Inhibition	6.74	pIC50
kinase inhibitor 2 [PMID: 30199702]	Inhibition	6.42	pIC50

ChEMBL bioactivities

598 potent at pChembl≥5 of 602 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.98	IC50	0.104	nM	CHEMBL4546504
9.00	IC50	1	nM	CHEMBL3728543
9.00	IC50	1	nM	CHEMBL3728359
8.70	IC50	2	nM	CHEMBL5422486
8.30	Ki	5.012	nM	CHEMBL1986943
8.30	Ki	5.012	nM	CHEMBL1974870
8.10	Ki	7.943	nM	CHEMBL1997129
8.10	Ki	7.943	nM	CHEMBL2006439
8.10	Ki	7.943	nM	CHEMBL2001751
8.00	IC50	10	nM	CHEMBL3730504
8.00	IC50	10	nM	CHEMBL5200518
8.00	IC50	10	nM	CHEMBL5404416
8.00	IC50	10	nM	CHEMBL5416942
8.00	Ki	10	nM	CHEMBL1964290
8.00	Ki	10	nM	CHEMBL1973098
8.00	Ki	10	nM	CHEMBL1965660
8.00	Ki	10	nM	CHEMBL1991063
7.98	IC50	10.4	nM	CHEMBL393525
7.94	IC50	11.4	nM	STAUROSPORINE
7.92	IC50	12	nM	CHEMBL5438158
7.85	IC50	14	nM	CHEMBL5195216
7.85	IC50	14	nM	CHEMBL5405059
7.85	IC50	14	nM	CHEMBL5414801
7.80	IC50	16	nM	CHEMBL5412565
7.80	Ki	15.85	nM	CHEMBL1981079
7.79	IC50	16.42	nM	STAUROSPORINE
7.76	IC50	17.48	nM	CHEMBL5574295
7.72	IC50	19	nM	CHEMBL5091238
7.71	IC50	19.5	nM	STAUROSPORINE
7.70	IC50	19.83	nM	CHEMBL5091238
7.69	IC50	20.6	nM	ABEMACICLIB
7.68	IC50	21.1	nM	CHEMBL3894571
7.66	IC50	22	nM	CHEMBL5422654
7.64	IC50	22.7	nM	CHEMBL5081787
7.63	IC50	23.5	nM	CHEMBL5279705
7.62	IC50	24	nM	CHEMBL5417147
7.62	IC50	24	nM	CHEMBL5418722
7.62	IC50	24	nM	CHEMBL5409574
7.60	IC50	25	nM	CHEMBL5179655
7.60	Ki	25.12	nM	CHEMBL1967887
7.55	IC50	28	nM	CHEMBL5441121
7.52	IC50	30	nM	CHEMBL3589674
7.52	IC50	30	nM	CHEMBL5088687
7.51	IC50	30.8	nM	SILMITASERTIB
7.50	Ki	31.62	nM	CHEMBL1965836
7.50	Ki	31.62	nM	CHEMBL259922
7.46	IC50	34.8	nM	STAUROSPORINE
7.46	IC50	35	nM	CHEMBL5396550
7.42	IC50	38	nM	CHEMBL5438293
7.42	IC50	38	nM	CHEMBL5438728

PubChem BioAssay actives

373 with measured affinity, of 1314 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
4-[[5-chloro-4-(4-hydroxy-4-methylcyclohexyl)oxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-N,N-dimethyl-3-[(2R)-1,1,1-trifluoropropan-2-yl]oxybenzamide	1551601: Inhibition of recombinant human full length GST-tagged DYRK3 expressed in baculovirus expression system by Z’-LYTE assay	ic50	0.0001	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-[(3,5,7-trifluoro-1-adamantyl)imino]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0020	uM
2-(1-adamantylamino)-5-[(E)-benzimidazol-5-ylidenemethyl]-1H-imidazol-4-ol	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0100	uM
(4Z)-4-[(4-hydroxy-3-methoxyphenyl)methylidene]-2-[4-(4-methylpiperazin-1-yl)anilino]-1H-imidazol-5-one	1871889: Inhibition of GST-fused human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method	ic50	0.0100	uM
(4Z)-4-[(3-hydroxy-4-methoxyphenyl)methylidene]-2-[4-(4-methylpiperazin-1-yl)anilino]-1H-imidazol-5-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0100	uM
N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0104	uM
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	1715372: Inhibition of human DYRK3 using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay	ic50	0.0114	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-[(3-fluoro-1-adamantyl)imino]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0120	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-[(3-hydroxy-1-adamantyl)imino]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0140	uM
(4Z)-4-(1,4-benzodioxin-3-ylmethylidene)-2-[4-(4-methylpiperazin-1-yl)anilino]-1H-imidazol-5-one	1871889: Inhibition of GST-fused human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method	ic50	0.0140	uM
(4Z)-4-(2,3-dihydro-1,4-benzodioxin-6-ylmethylidene)-2-[4-(4-methylpiperazin-1-yl)anilino]-1H-imidazol-5-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0140	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-[[3-(dimethylamino)-1-adamantyl]imino]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0160	uM
(2S)-2-[[6-(6-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)quinazolin-4-yl]amino]-2-phenylethanol	2110573: Inhibition of DYRK3 (unknown origin) preincubated with enzyme for 10 mins followed by substrate and ATP addition measured after 60 mins by ADP-Glo reagent based assay	ic50	0.0175	uM
(5Z)-2-(1-adamantylimino)-5-(1,3-benzothiazol-6-ylmethylidene)imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0190	uM
Abemaciclib	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0206	uM
methyl 9-(2-fluoro-4-methoxyanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate	1714130: Inhibition of DYRK3 (unknown origin)	ic50	0.0211	uM
N-[3-[[(4Z)-4-(1,3-benzothiazol-6-ylmethylidene)-5-oxoimidazolidin-2-ylidene]amino]-1-adamantyl]acetamide	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0220	uM
(5Z)-2-(2,6-dichlorophenyl)imino-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidin-4-one	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0227	uM
4,14,15-trimethoxy-10-azatetracyclo[7.6.1.02,7.012,16]hexadeca-1(15),2(7),3,5,8,13-hexaen-11-one	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0235	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-[(3-methoxy-1-adamantyl)imino]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0240	uM
N-[3-[[(4Z)-4-(1,3-benzothiazol-6-ylmethylidene)-5-oxoimidazolidin-2-ylidene]amino]-1-adamantyl]cyclopropanecarboxamide	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0240	uM
N-[3-[[(4Z)-4-(1,3-benzothiazol-6-ylmethylidene)-5-oxoimidazolidin-2-ylidene]amino]-1-adamantyl]methanesulfonamide	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0240	uM
(4Z)-4-(1,3-benzodioxol-5-ylmethylidene)-2-[4-(4-methylpiperazin-1-yl)anilino]-1H-imidazol-5-one	1871889: Inhibition of GST-fused human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method	ic50	0.0250	uM
(5Z)-2-[(1S)-2-amino-1-phenylethyl]imino-5-(1,3-benzothiazol-6-ylmethylidene)imidazolidin-4-one;dihydrochloride	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0280	uM
10-chloro-2-(3-methoxyphenyl)-11H-indolo[3,2-c]quinoline-6-carboxylic acid	1232291: Inhibition of human recombinant DYRK3 expressed in Escherichia coli using RS peptide as substrate	ic50	0.0300	uM
5-(2-amino-4-pyridinyl)-N-[(3-fluoro-2-pyridinyl)methyl]-2-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine	1812165: Inhibition of DYRK3 (unknown origin) by TR FRET assay	ic50	0.0300	uM
5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0308	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-(3,3-difluorocycloheptyl)iminoimidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0350	uM
(5Z)-2-(2-amino-1-phenylethyl)imino-5-(1,3-benzothiazol-6-ylmethylidene)imidazolidin-4-one;dihydrochloride	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0380	uM
(5Z)-2-(1-adamantylimino)-5-(1,3-benzoxazol-6-ylmethylidene)imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0380	uM
(5Z)-2-(1-adamantylimino)-5-[(2-methylindazol-5-yl)methylidene]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0400	uM
N-[2-[2-aminoethyl(methyl)amino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide	1301619: Inhibition of Dyrk3 (unknown origin) by quantitative PCR	ic50	0.0400	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-(3-tricyclo[3.3.1.03,7]nonanylimino)imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0420	uM
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-[2-(methylamino)-1-phenylethyl]iminoimidazolidin-4-one;dihydrochloride	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0450	uM
(5Z)-2-(1-adamantylimino)-5-(1,3-benzodioxol-5-ylmethylidene)imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0470	uM
4-[6-[6-(propan-2-ylamino)indazol-1-yl]pyrazin-2-yl]benzoic acid	1391119: Inhibition of DYRK3 (unknown origin)	ic50	0.0540	uM
(4Z)-4-(1,3-benzothiazol-6-ylmethylidene)-2-[4-(4-methylpiperazin-1-yl)anilino]-1H-imidazol-5-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0580	uM
[3-[[(4Z)-4-(1,3-benzothiazol-6-ylmethylidene)-5-oxoimidazolidin-2-ylidene]amino]-1-adamantyl] acetate	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0600	uM
(5Z)-2-(1-adamantylimino)-5-[(3-methylbenzimidazol-5-yl)methylidene]imidazolidin-4-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0680	uM
N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-methylphenyl]acetamide	760570: Inhibition of Dyrk-3 (unknown origin)	ic50	0.0700	uM
4-[3-(4-hydroxyphenyl)-2H-pyrazolo[3,4-b]pyridin-5-yl]benzene-1,2-diol	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0719	uM
2-(1-adamantylamino)-5-[(E)-indazol-5-ylidenemethyl]-1H-imidazol-4-ol	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.0740	uM
(2S)-2-[[3-(3-chlorophenyl)imidazo[1,2-b]pyridazin-6-yl]amino]butan-1-ol	1459434: Inhibition of GST tagged recombinant human DYRK3 expressed in Escherichia coli using woodtide as substrate after 30 mins by [gamma-33P]ATP based scintillation counting analysis	ic50	0.0810	uM
(1Z)-1-(3-ethyl-5-hydroxy-1,3-benzothiazol-2-ylidene)propan-2-one	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.0826	uM
methyl 9-(2,4-dichloroanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate	1714130: Inhibition of DYRK3 (unknown origin)	ic50	0.0932	uM
4-[[4-cyclopentyloxy-5-(2-methyl-1,3-benzoxazol-6-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxy-N-methylbenzamide	1476574: Inhibition of human full length recombinant GST-tagged DYRK3 expressed in baculovirus by Z’-LYTE assay	ic50	0.0990	uM
N-[3-[6-[[(2S)-1-hydroxybutan-2-yl]amino]imidazo[1,2-b]pyridazin-3-yl]phenyl]acetamide	1459434: Inhibition of GST tagged recombinant human DYRK3 expressed in Escherichia coli using woodtide as substrate after 30 mins by [gamma-33P]ATP based scintillation counting analysis	ic50	0.1100	uM
ethyl 3-[6-[[(2S)-1-hydroxybutan-2-yl]amino]imidazo[1,2-b]pyridazin-3-yl]benzoate	1459434: Inhibition of GST tagged recombinant human DYRK3 expressed in Escherichia coli using woodtide as substrate after 30 mins by [gamma-33P]ATP based scintillation counting analysis	ic50	0.1100	uM
[2,7-dimethoxy-9-[[(3S)-pyrrolidin-3-yl]methylsulfanyl]acridin-4-yl]methanol	1947685: Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	ic50	0.1118	uM
(4Z)-4-(1,3-benzothiazol-6-ylmethylidene)-2-[[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]amino]-1H-imidazol-5-one	2010393: Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay	ic50	0.1120	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	decreases methylation, increases expression	3
Cisplatin	increases expression	3
Valproic Acid	increases expression, affects expression	3
sodium arsenite	decreases expression, increases expression	2
Air Pollutants	increases expression, affects expression, increases abundance	2
Smoke	decreases expression, increases expression	2
TL8-506	affects cotreatment, increases expression	1
bisphenol A	increases methylation, affects cotreatment	1
ethyl-p-hydroxybenzoate	decreases expression	1
trichostatin A	increases expression	1
zinc chromate	increases abundance, increases expression	1
5-iodotubercidin	decreases activity	1
S-(1,2-dichlorovinyl)cysteine	decreases reaction, increases expression	1
chromium hexavalent ion	increases abundance, increases expression	1
CGP 52608	affects binding, increases reaction	1
oxamflatin	increases expression	1
apicidin	increases expression	1
deguelin	decreases expression	1
2-palmitoylglycerol	increases expression	1
abrine	increases expression	1
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	decreases expression	1
(4-amino-1,4-dihydro-3-(2-pyridyl)-5-thioxo-1,2,4-triazole)copper(II)	increases expression	1
picoxystrobin	increases expression	1
NSC 689534	affects binding, increases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Temozolomide	decreases expression	1
Sunitinib	increases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Vorinostat	increases expression	1
Leflunomide	decreases expression	1

ChEMBL screening assays

230 unique, capped per target: 229 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1004124	Binding	Inhibition of DYRK3 at 1 uM relative to control	Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. — J Med Chem
CHEMBL1963773	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: DYRK3	PubChem BioAssay data set

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1QJ	Abcam HeLa DYRK3 KO	Cancer cell line	Female
CVCL_SL27	HAP1 DYRK3 (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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