ULK3

Summary

ULK3 (unc-51 like kinase 3, HGNC:19703) is a protein-coding gene on chromosome 15q24.1, encoding Serine/threonine-protein kinase ULK3 (Q6PHR2). Serine/threonine protein kinase that acts as a regulator of Sonic hedgehog (SHH) signaling and autophagy.

Enables protein serine/threonine kinase activity. Involved in several processes, including fibroblast activation; protein autophosphorylation; and regulation of smoothened signaling pathway. Located in cytoplasm.

Source: NCBI Gene 25989 — RefSeq curated summary.

At a glance

• GWAS associations: 32
• Clinical variants (ClinVar): 113 total
• Druggable target: yes — 36 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001099436

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:19703
Approved symbol	ULK3
Name	unc-51 like kinase 3
Location	15q24.1
Locus type	gene with protein product
Status	Approved
Aliases	DKFZP434C131, FLJ90566
Ensembl gene	ENSG00000140474
Ensembl biotype	protein_coding
OMIM	613472
Entrez	25989

Gene structure

Transcript identifiers

Ensembl transcripts: 50 — 30 protein_coding, 11 retained_intron, 9 nonsense_mediated_decay

ENST00000440863, ENST00000561725, ENST00000562161, ENST00000562395, ENST00000563301, ENST00000564029, ENST00000564767, ENST00000565011, ENST00000565373, ENST00000565790, ENST00000565881, ENST00000566479, ENST00000566631, ENST00000567472, ENST00000568210, ENST00000568273, ENST00000568667, ENST00000568679, ENST00000568718, ENST00000569437, ENST00000569813, ENST00000570276, ENST00000631115, ENST00000647587, ENST00000894348, ENST00000894349, ENST00000894350, ENST00000894351, ENST00000894352, ENST00000894353, ENST00000894354, ENST00000894355, ENST00000894356, ENST00000894357, ENST00000894358, ENST00000894359, ENST00000894360, ENST00000894361, ENST00000926382, ENST00000926383, ENST00000926384, ENST00000926385, ENST00000926386, ENST00000967230, ENST00000967231, ENST00000967232, ENST00000967233, ENST00000967234, ENST00000967235, ENST00000967236

RefSeq mRNA: 4 — MANE Select: NM_001099436 NM_001099436, NM_001284364, NM_001284365, NM_001411082

CCDS: CCDS45305, CCDS76779, CCDS92044

Canonical transcript exons

ENST00000440863 — 16 exons

Exon	Start	End
ENSE00002616460	74843004	74843156
ENSE00003467966	74840234	74840316
ENSE00003468998	74839010	74839050
ENSE00003501623	74837751	74837798
ENSE00003509853	74836118	74837244
ENSE00003521150	74842075	74842195
ENSE00003534197	74840498	74840641
ENSE00003552393	74837369	74837435
ENSE00003563838	74839268	74839373
ENSE00003615440	74841405	74841509
ENSE00003636602	74838152	74838192
ENSE00003639794	74838643	74838745
ENSE00003674992	74842280	74842420
ENSE00003677123	74838266	74838344
ENSE00003691127	74839558	74839713
ENSE00003694320	74838440	74838504

Expression profiles

Bgee: expression breadth ubiquitous, 240 present calls, max score 98.70.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 14.4693 / max 142.0891, expressed in 1792 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
150932	14.2261	1792
150931	0.2432	113

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right hemisphere of cerebellum	UBERON:0014890	98.70	gold quality
cerebellar hemisphere	UBERON:0002245	98.64	gold quality
cerebellar cortex	UBERON:0002129	98.58	gold quality
cerebellum	UBERON:0002037	98.12	gold quality
lower esophagus mucosa	UBERON:0035834	97.17	gold quality
skin of leg	UBERON:0001511	96.96	gold quality
skin of abdomen	UBERON:0001416	96.59	gold quality
right frontal lobe	UBERON:0002810	96.55	gold quality
adenohypophysis	UBERON:0002196	96.32	gold quality
small intestine Peyer’s patch	UBERON:0003454	96.06	gold quality
pituitary gland	UBERON:0000007	96.00	gold quality
esophagus mucosa	UBERON:0002469	95.90	gold quality
granulocyte	CL:0000094	95.89	gold quality
right uterine tube	UBERON:0001302	95.87	gold quality
upper arm skin	UBERON:0004263	95.82	gold quality
cortical plate	UBERON:0005343	95.75	gold quality
mucosa of transverse colon	UBERON:0004991	95.69	gold quality
metanephros cortex	UBERON:0010533	95.66	gold quality
right lobe of thyroid gland	UBERON:0001119	95.43	gold quality
apex of heart	UBERON:0002098	95.30	gold quality
transverse colon	UBERON:0001157	95.20	gold quality
Brodmann (1909) area 9	UBERON:0013540	95.19	gold quality
right adrenal gland cortex	UBERON:0035827	95.18	gold quality
right adrenal gland	UBERON:0001233	95.12	gold quality
left lobe of thyroid gland	UBERON:0001120	95.11	gold quality
spleen	UBERON:0002106	94.94	gold quality
small intestine	UBERON:0002108	94.67	gold quality
zone of skin	UBERON:0000014	94.58	gold quality
anterior cingulate cortex	UBERON:0009835	94.47	gold quality
minor salivary gland	UBERON:0001830	94.44	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	5.25

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): NCOR1

Literature-anchored findings (GeneRIF, showing 7)

• First named and identified as protein kinase of the ULK family (PMID:12471243)
• serine/threonine kinase ULK3 is involved in the SHH pathway as a positive regulator of GLI proteins (PMID:19878745)
• Dual function of UNC-51-like kinase 3 (Ulk3) in the Sonic hedgehog signaling pathway. (PMID:20643644)
• Structural and biochemical studies reveal an unusually tight interaction between ULK3 and IST1, an ESCRT-III subunit required for cytokinetic abscission. (PMID:26011858)
• Increased ULK3 also induces autophagy, which is unlinked from GLI and CAF activation. ULK3 upregulation occurs in the CAFs of several tumor types, and ULK3 silencing suppresses the tumor-enhancing properties of these cells. (PMID:28877478)
• Conformational plasticity of the ULK3 kinase domain. (PMID:34190988)
• The ULK3 kinase is a determinant of keratinocyte self-renewal and tumorigenesis targeting the arginine methylome. (PMID:36797248)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	ulk3	ENSDARG00000101661
mus_musculus	Ulk3	ENSMUSG00000032308
rattus_norvegicus	Ulk3	ENSRNOG00000038459
drosophila_melanogaster	Aduk	FBGN0037679

Paralogs (2): ULK2 (ENSG00000083290), ULK1 (ENSG00000177169)

Protein

Protein identifiers

Serine/threonine-protein kinase ULK3 — Q6PHR2 (reviewed: Q6PHR2)

Alternative names: Unc-51-like kinase 3

All UniProt accessions (8): Q6PHR2, H3BMW8, H3BP85, H3BPN6, H3BS27, H3BT78, H3BTS3, H3BV76

UniProt curated annotations — full annotation on UniProt →

Function. Serine/threonine protein kinase that acts as a regulator of Sonic hedgehog (SHH) signaling and autophagy. Acts as a negative regulator of SHH signaling in the absence of SHH ligand: interacts with SUFU, thereby inactivating the protein kinase activity and preventing phosphorylation of GLI proteins (GLI1, GLI2 and/or GLI3). Positively regulates SHH signaling in the presence of SHH: dissociates from SUFU, autophosphorylates and mediates phosphorylation of GLI2, activating it and promoting its nuclear translocation. Phosphorylates in vitro GLI2, as well as GLI1 and GLI3, although less efficiently. Also acts as a regulator of autophagy: following cellular senescence, able to induce autophagy.

Subunit / interactions. Interacts (via protein kinase domain) with SUFU.

Subcellular location. Cytoplasm.

Tissue specificity. Widely expressed. Highest levels observed in fetal brain. In adult tissues, high levels in brain, liver and kidney, moderate levels in testis and adrenal gland and low levels in heart, lung, stomach, thymus, prostate and placenta. In the brain, highest expression in the hippocampus, high levels also detected in the cerebellum, olfactory bulb and optic nerve. In the central nervous system, lowest levels in the spinal cord.

Post-translational modifications. Autophosphorylated. Autophosphorylation is blocked by interaction with SUFU.

Induction. Up-regulated during senescence.

Miscellaneous. May be produced at very low levels due to a premature stop codon in the mRNA, leading to nonsense-mediated mRNA decay. May be due to competing donor splice site.

Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family. APG1/unc-51/ULK1 subfamily.

Isoforms (4)

UniProt ID	Names	Canonical?
Q6PHR2-1	1	yes
Q6PHR2-2	2
Q6PHR2-3	3
Q6PHR2-4	4

RefSeq proteins (4): NP_001092906, NP_001271293, NP_001271294, NP_001398011 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR007330	MIT_dom	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR036181	MIT_dom_sf	Homologous_superfamily
IPR045269	Atg1-like	Family

Pfam: PF00069, PF04212

Enzyme classification (BRENDA):

• EC 2.7.11.1 — non-specific serine/threonine protein kinase (BRENDA: 71 organisms, 682 substrates, 228 inhibitors, 23 Km, 6 kcat entries)

Substrate kinetics (BRENDA)

8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0007–0.64	11
KKRAARATSNVFA	0.013–0.045	3
PAH1 PHOSPHATIDATE PHOSPHATASE	0.0002	2
RRRLSSLRA	0.0036–0.0037	2
GTP	0.46	1
KKRAARASSNVFA	0.02	1
LYS-LYS-PHE-ASN-ARG-THR-LEU-SER-VAL-ALA	0.0093	1
MYELIN BASIC PROTEIN	0.145	1

Catalyzed reactions (Rhea), 2 shown:

• 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 (47 total): helix 14, strand 8, modified residue 5, splice variant 4, turn 4, domain 3, sequence variant 2, mutagenesis site 2, binding site 2, chain 1, sequence conflict 1, active site 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
4WZX	X-RAY DIFFRACTION	1.39
6FDY	X-RAY DIFFRACTION	1.7
6FDZ	X-RAY DIFFRACTION	2.55

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q6PHR2-F1	88.96	0.66

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): 137 (proton acceptor)

Ligand- & substrate-binding residues (2): 20–28; 44

Post-translational modifications (5): 384, 464, 176, 300, 350

Mutagenesis-validated functional residues (2):

Position	Phenotype
44	decreased kinase activity.
139	loss of kinase activity. does not promote gli1 nuclear localization.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-5632684	Hedgehog ‘on’ state

MSigDB gene sets: 106 (showing top): GOBP_REGULATION_OF_AUTOPHAGY, GOBP_VACUOLE_ORGANIZATION, GOBP_CELLULAR_SENESCENCE, GOBP_MACROAUTOPHAGY, GOBP_REGULATION_OF_CATABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_SMOOTHENED_SIGNALING_PATHWAY, GOBP_ORGANELLE_ASSEMBLY, GOBP_REGULATION_OF_SMOOTHENED_SIGNALING_PATHWAY, GOBP_SMOOTHENED_SIGNALING_PATHWAY, OZEN_MIR125B1_TARGETS, GOBP_POSITIVE_REGULATION_OF_SMOOTHENED_SIGNALING_PATHWAY, GOBP_PROTEIN_AUTOPHOSPHORYLATION, GOBP_AUTOPHAGOSOME_ORGANIZATION, GOBP_RESPONSE_TO_STARVATION, SENESE_HDAC3_TARGETS_DN

GO Biological Process (14): autophagosome assembly (GO:0000045), mitophagy (GO:0000423), autophagy (GO:0006914), smoothened signaling pathway (GO:0007224), regulation of autophagy (GO:0010506), piecemeal microautophagy of the nucleus (GO:0034727), response to starvation (GO:0042594), negative regulation of smoothened signaling pathway (GO:0045879), positive regulation of smoothened signaling pathway (GO:0045880), protein autophosphorylation (GO:0046777), reticulophagy (GO:0061709), fibroblast activation (GO:0072537), cellular senescence (GO:0090398), protein phosphorylation (GO:0006468)

GO Molecular Function (8): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (6): phagophore assembly site (GO:0000407), cytoplasm (GO:0005737), autophagosome (GO:0005776), cytosol (GO:0005829), phagophore assembly site membrane (GO:0034045), ciliary tip (GO:0097542)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Signaling by Hedgehog	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
macroautophagy	2
smoothened signaling pathway	2
regulation of smoothened signaling pathway	2
protein kinase activity	2
cytoplasm	2
Atg12 activating enzyme activity	1
protein-phosphatidylethanolamide deconjugating activity	1
Atg12 conjugating enzyme activity	1
Atg12 ligase activity	1
organelle assembly	1
Atg1/ULK1 kinase complex assembly	1
autophagosome organization	1
autophagy of mitochondrion	1
catabolic process	1
transmembrane transport	1
process utilizing autophagic mechanism	1
cell surface receptor signaling pathway	1
autophagy	1
regulation of catabolic process	1
microautophagy	1
nucleophagy	1
nucleus disassembly	1
response to stress	1
response to nutrient levels	1
negative regulation of signal transduction	1
positive regulation of signal transduction	1
protein phosphorylation	1
cell activation	1
cellular process	1
cellular response to stress	1
phosphorylation	1
protein modification process	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1

Protein interactions and networks

STRING

1390 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ULK3	SUFU	Q9UMX1	783
ULK3	ATG13	O75143	712
ULK3	ATG101	Q9BSB4	698
ULK3	GLI2	P10070	695
ULK3	GLI1	P08151	693
ULK3	RB1CC1	Q8TDY2	676
ULK3	GLI3	P10071	633
ULK3	KIF7	Q2M1P5	580
ULK3	SHH	Q15465	549
ULK3	ATG5	Q9H1Y0	531
ULK3	RPTOR	Q8N122	528
ULK3	ATG7	O95352	513
ULK3	ATG12	O94817	483
ULK3	PLEKHA7	Q6IQ23	479
ULK3	FAM219B	Q5XKK7	476

IntAct

45 interactions, top by confidence:

A	B	Type	Score
TRADD	TNF	psi-mi:“MI:0914”(association)	0.790
ULK3	FKBP5	psi-mi:“MI:0915”(physical association)	0.620
CDC37	ULK3	psi-mi:“MI:0915”(physical association)	0.560
ULK3	AIP	psi-mi:“MI:0914”(association)	0.530
ULK3	GOLGB1	psi-mi:“MI:0915”(physical association)	0.400
ULK3	CLTA	psi-mi:“MI:0915”(physical association)	0.400
CFTR	ULK3	psi-mi:“MI:0915”(physical association)	0.370
	PLK4	psi-mi:“MI:0914”(association)	0.350
	AURKA	psi-mi:“MI:0914”(association)	0.350
	GAK	psi-mi:“MI:0914”(association)	0.350
	SGK1	psi-mi:“MI:0914”(association)	0.350
	TBKBP1	psi-mi:“MI:0914”(association)	0.350
	AHRR	psi-mi:“MI:0914”(association)	0.350
TRAF2	UMAD1	psi-mi:“MI:0914”(association)	0.350
BIRC2	UMAD1	psi-mi:“MI:0914”(association)	0.350
RBCK1	UMAD1	psi-mi:“MI:0914”(association)	0.350
SHARPIN	MAP3K7	psi-mi:“MI:0914”(association)	0.350
TANK	CNOT1	psi-mi:“MI:0914”(association)	0.350
TNIP1	UMAD1	psi-mi:“MI:0914”(association)	0.350
TNIP2	CHUK	psi-mi:“MI:0914”(association)	0.350
TRADD	HNRNPCL2	psi-mi:“MI:0914”(association)	0.350
TRAF2	TMEM178B	psi-mi:“MI:0914”(association)	0.350
FADD	CHUK	psi-mi:“MI:0914”(association)	0.350
RBCK1	KHNYN	psi-mi:“MI:0914”(association)	0.350

BioGRID (71): ULK3 (Affinity Capture-RNA), AIP (Affinity Capture-MS), FKBP5 (Affinity Capture-MS), CDC37 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), FKBP5 (Affinity Capture-MS), AIP (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS), ULK3 (Affinity Capture-MS)

ESM2 similar proteins: A0A0U1RPR8, A0A7N9VSG0, D3ZGQ5, D3ZHP7, O08644, O09127, O15197, O43542, O73875, O73878, O75676, P0C0K6, P0C0K7, P21709, P23800, P29317, P29322, P41243, P51839, P51840, P52785, P54753, P54754, P54760, P54761, P55203, P57078, P97343, Q1KL86, Q3U3Q1, Q4V7Q6, Q5RCY1, Q5ZJH6, Q60750, Q62270, Q63285, Q6PHR2, Q7ZZC8, Q80YD6, Q86SG6

Diamond homologs: A1CHL6, A1CX69, A2QIL5, A6RYB8, A6ZU07, A7F0W2, A7KAL2, A7TIZ4, A8WYE4, B2DD29, D3ZHP7, D3ZML2, F4I1N8, F4IRW0, F4JBP3, I1RNG8, J4W0G2, O08678, O08679, O42844, O70405, O75385, O94547, P0CP70, P0CP71, P25323, P27448, P32562, P53104, P87248, P92937, Q03141, Q05512, Q0CLX3, Q0JI49, Q0UY20, Q10LQ2, Q19469, Q1DN93, Q23023

SIGNOR signaling

9 interactions.

A	Effect	B	Mechanism
ULK3	“up-regulates activity”	ULK3	phosphorylation
ULK3	“up-regulates activity”	GLI1	phosphorylation
ULK3	“up-regulates activity”	GLI2	phosphorylation
ULK3	“up-regulates activity”	GLI3	phosphorylation
ULK3	“down-regulates activity”	IST1	phosphorylation
ULK3	“down-regulates activity”	CHMP4C	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 42 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
TNFR1-induced proapoptotic signaling	7	99.2×	6e-11
TNFR1-induced NF-kappa-B signaling pathway	8	86.7×	6e-12
TNF signaling	6	81.9×	6e-09
RIPK1-mediated regulated necrosis	5	73.7×	4e-07
Regulation of necroptotic cell death	5	70.8×	4e-07
Regulation of TNFR1 signaling	8	57.8×	7e-11
Ub-specific processing proteases	5	8.6×	4e-03

GO biological processes:

GO term	Partners	Fold	FDR
canonical NF-kappaB signal transduction	9	86.8×	3e-13
tumor necrosis factor-mediated signaling pathway	5	43.5×	1e-05
negative regulation of canonical NF-kappaB signal transduction	9	40.7×	2e-10
cellular response to tumor necrosis factor	5	21.5×	2e-04
positive regulation of canonical NF-kappaB signal transduction	11	21.0×	4e-10
defense response to virus	6	10.9×	5e-04
inflammatory response	6	6.0×	8e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	79
Likely benign	6
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

2466 predictions. Top by Δscore:

Variant	Effect	Δscore
15:74837241:CAAG:C	acceptor_gain	1.0000
15:74837367:A:AC	donor_gain	1.0000
15:74837368:C:CC	donor_gain	1.0000
15:74837368:CAG:C	donor_gain	1.0000
15:74838260:CCTCA:C	donor_loss	1.0000
15:74838261:CTCAC:C	donor_loss	1.0000
15:74838262:TCA:T	donor_loss	1.0000
15:74838263:CACCT:C	donor_loss	1.0000
15:74838264:A:AC	donor_gain	1.0000
15:74838265:C:CA	donor_loss	1.0000
15:74838265:C:CC	donor_gain	1.0000
15:74838265:CCTG:C	donor_gain	1.0000
15:74838340:TCCTC:T	acceptor_gain	1.0000
15:74838341:CCTCC:C	acceptor_gain	1.0000
15:74838342:CTC:C	acceptor_gain	1.0000
15:74838343:TC:T	acceptor_gain	1.0000
15:74838344:CC:C	acceptor_gain	1.0000
15:74838345:C:CC	acceptor_gain	1.0000
15:74838348:C:CT	acceptor_gain	1.0000
15:74838349:A:T	acceptor_gain	1.0000
15:74838352:C:CT	acceptor_gain	1.0000
15:74838352:C:T	acceptor_gain	1.0000
15:74838354:C:CT	acceptor_gain	1.0000
15:74838437:AAC:A	donor_loss	1.0000
15:74838439:C:CT	donor_loss	1.0000
15:74838503:CT:C	acceptor_gain	1.0000
15:74838505:C:CC	acceptor_gain	1.0000
15:74838510:A:AC	acceptor_gain	1.0000
15:74838642:CCT:C	donor_gain	1.0000
15:74838746:CTGTA:C	acceptor_loss	1.0000

AlphaMissense

3056 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
15:74842391:C:A	K44N	1.000
15:74842391:C:G	K44N	1.000
15:74840513:C:A	G200W	0.999
15:74840522:A:G	W197R	0.999
15:74840522:A:T	W197R	0.999
15:74840640:G:C	D157E	0.999
15:74840640:G:T	D157E	0.999
15:74840641:T:A	D157V	0.999
15:74841457:C:A	K139N	0.999
15:74841457:C:G	K139N	0.999
15:74841459:T:C	K139E	0.999
15:74841463:A:C	D137E	0.999
15:74841463:A:T	D137E	0.999
15:74842173:A:G	L89P	0.999
15:74842326:A:G	L66P	0.999
15:74842337:C:A	E62D	0.999
15:74842337:C:G	E62D	0.999
15:74842393:T:C	K44E	0.999
15:74842395:A:T	I43K	0.999
15:74842398:G:T	A42D	0.999
15:74839638:G:T	R258S	0.998
15:74840513:C:G	G200R	0.998
15:74840513:C:T	G200R	0.998
15:74840520:C:A	W197C	0.998
15:74840520:C:G	W197C	0.998
15:74840629:G:T	A161E	0.998
15:74840641:T:G	D157A	0.998
15:74841405:C:G	D157H	0.998
15:74841461:A:G	L138P	0.998
15:74841464:T:A	D137V	0.998

dbSNP variants (sampled 300 via entrez): RS1000002101 (15:74840877 C>A,T), RS1000445894 (15:74839816 T>C), RS1001813679 (15:74844831 G>C), RS1002150646 (15:74843489 C>T), RS1002531826 (15:74843230 C>G), RS1002540106 (15:74843093 C>A,T), RS1003055289 (15:74837326 C>T), RS1003412816 (15:74837554 TGAGA>T,TGAGAGAGA), RS1003563529 (15:74841461 AG>A), RS1003609345 (15:74837082 G>A,T), RS1003684241 (15:74836828 G>A), RS1004061279 (15:74839306 T>G), RS1004677749 (15:74837600 AAGAG>A,AAG,AAGAGAG), RS1004890489 (15:74839399 G>A,T), RS1005027668 (15:74837821 TGGGTGTG>T)

Disease associations

OMIM: gene MIM:613472 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

32 associations (top):

Study	Trait	p-value
GCST000396_3	Diastolic blood pressure	2.000000e-10
GCST001032_3	Caffeine consumption	6.000000e-07
GCST001215_2	Coffee consumption	7.000000e-09
GCST001227_6	Systolic blood pressure	6.000000e-23
GCST001228_18	Diastolic blood pressure	3.000000e-26
GCST002004_8	Adverse response to chemotherapy (neutropenia/leucopenia) (carboplatin)	4.000000e-06
GCST003273_19	Diastolic blood pressure	5.000000e-06
GCST004633_34	Neutrophil percentage of white cells	2.000000e-10
GCST004776_66	Systolic blood pressure	2.000000e-12
GCST004777_53	Diastolic blood pressure	6.000000e-16
GCST006187_40	Diastolic blood pressure (cigarette smoking interaction)	8.000000e-33
GCST006187_41	Diastolic blood pressure (cigarette smoking interaction)	5.000000e-30
GCST006188_44	Systolic blood pressure (cigarette smoking interaction)	1.000000e-28
GCST006188_45	Systolic blood pressure (cigarette smoking interaction)	4.000000e-23
GCST006190_2	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	8.000000e-21
GCST006190_53	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	1.000000e-21
GCST006192_50	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	5.000000e-15
GCST006192_73	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	1.000000e-12
GCST006193_35	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	2.000000e-24
GCST006193_74	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	4.000000e-24
GCST006195_17	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	1.000000e-16
GCST006195_66	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	3.000000e-15
GCST006231_65	Mean arterial pressure	2.000000e-15
GCST006258_52	Diastolic blood pressure	1.000000e-18
GCST006259_11	Systolic blood pressure	3.000000e-16
GCST007094_195	Diastolic blood pressure	3.000000e-29
GCST007098_37	Diastolic blood pressure	4.000000e-06
GCST007098_38	Diastolic blood pressure	5.000000e-06
GCST007099_204	Systolic blood pressure	1.000000e-16
GCST008489_23	Celiac disease	3.000000e-08

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0006336	diastolic blood pressure
EFO:0004330	coffee consumption
EFO:0006335	systolic blood pressure
EFO:0007990	neutrophil percentage of leukocytes
EFO:0006527	smoking status measurement
EFO:0006340	mean arterial pressure
EFO:0004509	hemoglobin measurement
EFO:0007993	lymphocyte percentage of leukocytes

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5047 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

36 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 359,464 (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
CHEMBL1078178	MOMELOTINIB	4	3,481
CHEMBL1171837	PONATINIB	4	8,955
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1789941	RUXOLITINIB	4	11,547
CHEMBL2028663	DABRAFENIB	4	12,430
CHEMBL2103743	TOFACITINIB CITRATE	4	1,672
CHEMBL221959	TOFACITINIB	4	10,408
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL5416410	DASATINIB	4	655
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL601719	CRIZOTINIB	4	14,403
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL274654	ORANTINIB	3	3,596
CHEMBL31965	CANERTINIB	3	8,083
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL1230609	FORETINIB	2
CHEMBL1721885	SU-014813	2
CHEMBL1922094	APITOLISIB	2
CHEMBL475251	R-406	2
CHEMBL482968	ENMD-2076	2
CHEMBL495727	AT-9283	2
CHEMBL572878	TOZASERTIB	2
CHEMBL1908397	KW-2449	1
CHEMBL2041933	AZD-7762	1

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs2290573	Efficacy	3	imatinib	Chronic myelogenous leukemia;BCR-ABL1 positive

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2290573	ULK3	3	2.50	1	imatinib

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Unc-51-like kinase (ULK) family

ChEMBL bioactivities

69 potent at pChembl≥5 of 69 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.92	IC50	1.2	nM	STAUROSPORINE
8.92	Kd	1.2	nM	STAUROSPORINE
8.49	IC50	3.21	nM	STAUROSPORINE
8.38	IC50	4.2	nM	STAUROSPORINE
8.31	Kd	4.9	nM	LESTAURTINIB
8.22	Kd	6	nM	GILTERITINIB
8.15	Kd	7.1	nM	R-406
7.96	Kd	11	nM	TAE-684
7.85	Kd	14	nM	CHEMBL4576489
7.80	Kd	16	nM	CHEMBL4465866
7.72	Kd	19	nM	PF-03814735
7.45	Kd	35.61	nM	CHEMBL5653589
7.38	Kd	42	nM	SUNITINIB
7.38	Kd	42	nM	SU-014813
7.35	Kd	45	nM	AT-9283
7.24	Kd	57	nM	AST-487
7.22	Kd	60	nM	NINTEDANIB
7.11	ED50	78.44	nM	CHEMBL5653589
6.97	Kd	107	nM	K-252A
6.92	Kd	120	nM	KW-2449
6.77	Kd	170	nM	DOVITINIB
6.67	Kd	212	nM	LESTAURTINIB
6.57	Kd	272	nM	R-406
6.54	Kd	291	nM	MOMELOTINIB
6.54	Kd	290	nM	FEDRATINIB
6.53	Kd	297	nM	XL-019
6.51	Kd	310	nM	TOZASERTIB
6.46	IC50	343	nM	CHEMBL5079601
6.36	Kd	433	nM	SU-014813
6.35	Kd	450	nM	FORETINIB
6.34	Kd	460	nM	BOSUTINIB
6.32	Kd	474	nM	CHEMBL3688339
6.32	Kd	476	nM	ENMD-2076
6.31	Kd	492	nM	XL-228
6.21	Kd	612	nM	CHEMBL3699142
6.20	Kd	626	nM	PF-03758309
6.18	Kd	655	nM	Cerdulatinib Hydrochloride
6.17	Kd	670	nM	AXITINIB
6.14	Kd	721	nM	APITOLISIB
6.10	Kd	801	nM	CYC-116
6.05	Kd	900	nM	CHEMBL1908395
6.04	Kd	920	nM	ERLOTINIB
6.02	IC50	946	nM	CHEMBL4446892
6.01	Kd	968	nM	DOVITINIB
6.00	IC50	1000	nM	TP-030-1
6.00	IC50	1000	nM	TP-030-2
6.00	IC50	1000	nM	TP-030n
5.98	Kd	1046	nM	KW-2449
5.95	Kd	1125	nM	SUNITINIB
5.93	Kd	1167	nM	CHEMBL3990456

PubChem BioAssay actives

63 with measured affinity, of 815 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
(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	1715128: Inhibition of human ULK3 using MBP as substrate by [gamma-33P]-ATP assay	ic50	0.0012	uM
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one	508128: Binding affinity to ULK3	kd	0.0049	uM
Gilteritinib	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0060	uM
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one	624818: Binding constant for ULK3 kinase domain	kd	0.0071	uM
5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine	624818: Binding constant for ULK3 kinase domain	kd	0.0110	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526258: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged ULK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0140	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526258: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged ULK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0160	uM
N-[2-[4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0190	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149730: Binding affinity to human ULK3 incubated for 45 mins by Kinobead based pull down assay	kd	0.0356	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	624818: Binding constant for ULK3 kinase domain	kd	0.0420	uM
Sunitinib	508128: Binding affinity to ULK3	kd	0.0420	uM
1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0450	uM
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea	624818: Binding constant for ULK3 kinase domain	kd	0.0570	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	624818: Binding constant for ULK3 kinase domain	kd	0.0600	uM
methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.1070	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	624818: Binding constant for ULK3 kinase domain	kd	0.1200	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	624818: Binding constant for ULK3 kinase domain	kd	0.1700	uM
Fedratinib	624818: Binding constant for ULK3 kinase domain	kd	0.2900	uM
Momelotinib	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2910	uM
N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2970	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	624818: Binding constant for ULK3 kinase domain	kd	0.3100	uM
N-[3-[[5-cyclopropyl-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]propyl]cyclobutanecarboxamide	1823792: Inhibition of full length recombinant human ULK3 using casein as substrate incubated for 40 mins in presence of [gamma-33P-ATP] by radiometric scintillation assay	ic50	0.3430	uM
1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide	624818: Binding constant for ULK3 kinase domain	kd	0.4500	uM
Bosutinib	624818: Binding constant for ULK3 kinase domain	kd	0.4600	uM
1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.4740	uM
6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.4760	uM
4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.4920	uM
3-[3-[N-[4-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.6120	uM
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.6260	uM
4-(cyclopropylamino)-2-[4-(4-ethylsulfonylpiperazin-1-yl)anilino]pyrimidine-5-carboxamide;hydrochloride	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.6550	uM
Axitinib	624818: Binding constant for ULK3 kinase domain	kd	0.6700	uM
(2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.7210	uM
4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.8010	uM
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride	624818: Binding constant for ULK3 kinase domain	kd	0.9000	uM
Erlotinib	624818: Binding constant for ULK3 kinase domain	kd	0.9200	uM
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide	1823792: Inhibition of full length recombinant human ULK3 using casein as substrate incubated for 40 mins in presence of [gamma-33P-ATP] by radiometric scintillation assay	ic50	0.9460	uM
2-amino-2-cyclohexyl-N-[2-(1-methylpyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]acetamide	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.1670	uM
Midostaurin	508128: Binding affinity to ULK3	kd	1.3000	uM
4-[[[5-bromo-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide	1823792: Inhibition of full length recombinant human ULK3 using casein as substrate incubated for 40 mins in presence of [gamma-33P-ATP] by radiometric scintillation assay	ic50	1.3710	uM
3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.4550	uM
Dabrafenib	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.4800	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149730: Binding affinity to human ULK3 incubated for 45 mins by Kinobead based pull down assay	kd	1.6085	uM
Ponatinib	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.7200	uM
3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide	1425209: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.7890	uM
Ruxolitinib	624818: Binding constant for ULK3 kinase domain	kd	2.4000	uM
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate	624818: Binding constant for ULK3 kinase domain	kd	4.6000	uM
N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide	624818: Binding constant for ULK3 kinase domain	kd	4.7000	uM
Vandetanib	624818: Binding constant for ULK3 kinase domain	kd	6.4000	uM
Tofacitinib	624818: Binding constant for ULK3 kinase domain	kd	6.4000	uM
Crizotinib	624818: Binding constant for ULK3 kinase domain	kd	6.7000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases abundance, increases expression	3
Valproic Acid	affects expression, decreases expression, increases methylation	2
aristolochic acid I	increases expression	1
FR900359	increases phosphorylation	1
bisphenol F	affects cotreatment, decreases expression	1
cobaltous chloride	decreases expression	1
perfluorooctanoic acid	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
di-n-butylphosphoric acid	affects expression	1
perfluorooctane sulfonic acid	decreases expression	1
CGP 52608	affects binding, increases reaction	1
perfluoro-n-nonanoic acid	decreases expression	1
corosolic acid	increases expression	1
perfluorohexanesulfonic acid	decreases expression	1
abrine	decreases expression	1
jinfukang	affects cotreatment, increases expression	1
Sunitinib	increases expression	1
Acetaminophen	increases expression	1
Amiodarone	increases expression	1
Arsenic	increases abundance, increases expression	1
Benzo(a)pyrene	increases methylation	1
Caffeine	decreases phosphorylation	1
Cisplatin	affects cotreatment, increases expression	1
Dexamethasone	affects cotreatment, decreases expression	1
Estradiol	affects cotreatment, decreases expression	1
Indomethacin	affects cotreatment, decreases expression	1
Smoke	decreases expression	1
Tretinoin	decreases expression	1
1-Methyl-3-isobutylxanthine	affects cotreatment, decreases expression	1

ChEMBL screening assays

199 unique, capped per target: 199 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1021463	Binding	Inhibition of ULK3 assessed as enzyme activity relative to control	Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). — J Med Chem

Cellosaurus cell lines

4 cell lines: 3 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B3KW	Abcam HEK293T ULK3 KO	Transformed cell line	Female
CVCL_TW34	HAP1 ULK3 (-) 1	Cancer cell line	Male
CVCL_TW35	HAP1 ULK3 (-) 2	Cancer cell line	Male
CVCL_TW36	HAP1 ULK3 (-) 3	Cancer cell line	Male

Clinical trials (associated diseases)

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