STK24

Summary

STK24 (serine/threonine kinase 24, HGNC:11403) is a protein-coding gene on chromosome 13q32.2, encoding Serine/threonine-protein kinase 24 (Q9Y6E0). Serine/threonine-protein kinase that acts on both serine and threonine residues and promotes apoptosis in response to stress stimuli and caspase activation.

This gene encodes a serine/threonine protein kinase that functions upstream of mitogen-activated protein kinase (MAPK) signaling. The encoded protein is cleaved into two chains by caspases; the N-terminal fragment (MST3/N) translocates to the nucleus and promotes programmed cells death. There is a pseudogene for this gene on chromosome X. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 8428 — RefSeq curated summary.

At a glance

• GWAS associations: 20
• Clinical variants (ClinVar): 57 total
• Druggable target: yes — 18 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001032296

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11403
Approved symbol	STK24
Name	serine/threonine kinase 24
Location	13q32.2
Locus type	gene with protein product
Status	Approved
Aliases	MST-3, MST3, MST3B, STK3, STE20
Ensembl gene	ENSG00000102572
Ensembl biotype	protein_coding
OMIM	604984
Entrez	8428

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 10 protein_coding, 2 protein_coding_CDS_not_defined

ENST00000376547, ENST00000376554, ENST00000397517, ENST00000418038, ENST00000444574, ENST00000481288, ENST00000491878, ENST00000539966, ENST00000871799, ENST00000937323, ENST00000937324, ENST00000937325

RefSeq mRNA: 3 — MANE Select: NM_001032296 NM_001032296, NM_001286649, NM_003576

CCDS: CCDS32001, CCDS66573, CCDS9488

Canonical transcript exons

ENST00000539966 — 11 exons

Exon	Start	End
ENSE00000685167	98460372	98460440
ENSE00000685174	98461774	98461897
ENSE00000685183	98463691	98463836
ENSE00001007034	98457168	98457304
ENSE00001143743	98466376	98466561
ENSE00001621827	98474821	98474978
ENSE00001816526	98576745	98577107
ENSE00003474465	98482265	98482321
ENSE00003524685	98475250	98475358
ENSE00003596350	98519243	98519473
ENSE00003721017	98445185	98453209

Expression profiles

Bgee: expression breadth ubiquitous, 295 present calls, max score 99.89.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 66.1688 / max 362.6539, expressed in 1819 samples.

FANTOM5 promoters (13 alternative TSS)

Promoter ID	TPM avg	Samples expressed
137938	56.5719	1818
137939	4.6128	1610
137937	1.7773	1162
207084	1.4281	1014
137940	0.6624	334
137935	0.3434	159
137936	0.3270	144
137941	0.1669	58
137934	0.1146	46
137932	0.0598	25

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
secondary oocyte	CL:0000655	99.89	gold quality
esophagus squamous epithelium	UBERON:0006920	99.77	gold quality
amniotic fluid	UBERON:0000173	99.63	gold quality
pancreatic ductal cell	CL:0002079	99.62	gold quality
squamous epithelium	UBERON:0006914	99.62	gold quality
epithelium of esophagus	UBERON:0001976	99.59	gold quality
pigmented layer of retina	UBERON:0001782	99.56	gold quality
oocyte	CL:0000023	99.55	gold quality
gingival epithelium	UBERON:0001949	99.55	gold quality
endothelial cell	CL:0000115	99.52	gold quality
hair follicle	UBERON:0002073	99.43	gold quality
gingiva	UBERON:0001828	99.40	gold quality
tongue squamous epithelium	UBERON:0006919	99.38	gold quality
palpebral conjunctiva	UBERON:0001812	99.30	gold quality
cervix squamous epithelium	UBERON:0006922	99.22	gold quality
germinal epithelium of ovary	UBERON:0001304	99.17	gold quality
upper leg skin	UBERON:0004262	99.15	gold quality
jejunal mucosa	UBERON:0000399	99.14	gold quality
penis	UBERON:0000989	99.14	gold quality
oral cavity	UBERON:0000167	99.11	gold quality
skin of hip	UBERON:0001554	99.10	gold quality
epithelium of nasopharynx	UBERON:0001951	99.07	gold quality
parotid gland	UBERON:0001831	99.06	gold quality
pharyngeal mucosa	UBERON:0000355	99.04	gold quality
epithelial cell of pancreas	CL:0000083	98.95	gold quality
colonic mucosa	UBERON:0000317	98.95	gold quality
mucosa of sigmoid colon	UBERON:0004993	98.91	gold quality
lower esophagus mucosa	UBERON:0035834	98.89	gold quality
calcaneal tendon	UBERON:0003701	98.86	gold quality
tibia	UBERON:0000979	98.84	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-MTAB-6386	no	511.62
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

98 targeting STK24, 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-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-12118	100.00	65.88	1270
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-6891-5P	99.98	66.53	1372
HSA-MIR-3173-3P	99.98	66.49	1217
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-185-3P	99.95	67.01	1743
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-9718	99.94	68.91	918
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872

Literature-anchored findings (GeneRIF, showing 23)

• Proteolytic activation of Mst3 by caspases. (PMID:12107159)
• Mst3 contains signals which may cooperate to control the subcellular distribution of Mst3. (PMID:15304321)
• Activation of NDR2 is a multistep process involving phosphorylation of the hydrophobic motif site Thr444/2 by MST3. (PMID:16314523)
• MST3 inhibits cell migration in a fashion dependent on autophosphorylation and may regulate paxillin phosphorylation through tyrosine phosphatase PTP-PEST (PMID:17046825)
• study demonstrated the essential role of Mst3, a human Ste20-like protein kinase, in the oxidative stress-induced apoptosis of trophoblasts of term placenta in normal spontaneous delivery (PMID:18040775)
• Our results reveal that H2O2-induced MST3-mediated cell death involves suppressing both a JNK survival pathway and up-regulation of HO-1. (PMID:19604147)
• The mammalian sterile 20-like serine/threonine protein kinase 3 (Mst3) plays an essential role in the staurosporine-induced apoptosis of HeLa cells. (PMID:19782762)
• five crystal structures of the catalytic domain of MST3 are presented, including a complex with ADP and manganese, a unique cofactor preferred by the enzyme, and a complex with adenine. (PMID:20124694)
• Mst3 is up-regulated and plays an important role in hypoxia-induced apoptosis of human trophoblasts. (PMID:21277991)
• Striatin orchestrates the regulation of Mst3 by PP2A. (PMID:21985334)
• mechanism of regulation of MST3 (PMID:22229648)
• results show that a STRADalpha-rac1-PAK1 pathway regulates cell polarity and invasion in LKB1-null cells. It also suggests that while the function of LKB1 and STRADalpha undoubtedly overlap, they may also have mutually exclusive roles (PMID:22493453)
• These data provide molecular understanding of the mechanism by which MO25 isoforms regulates the activity of STE20 family protein kinases. (PMID:23296203)
• This review notes that in the SOK1 and MST4 germinal center kinase III family of proteins, exon 1 encodes a 5’ untranslated region, but this is not the case for MST3. (PMID:23889253)
• This study demonistrated that MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development. (PMID:25456499)
• High MST3 expression is associated with breast cancer. (PMID:26910843)
• Aberrant STK24 expression was an independent prognostic indicator in lung adenocarcinoma patients. Its dysregulation was associated with its DNA copy number alteration and methylation. (PMID:29557182)
• Down-expression of MST3 in colorectal cancer cell lines enhanced their migration and invasion, but overexpression of MST3 could attenuate miR-222 overexpression in the promotion of migration and invasion in colorectal cell lines. (PMID:31034165)
• MST3 protein coats lipid droplets in human liver cells. Knockdown of MST3 attenuated lipid accumulation in human hepatocytes by stimulating beta-oxidation and triacylglycerol secretion while inhibiting fatty acid influx and lipid synthesis. MST3 expression was positively correlated with key features of NASH in human liver biopsies. (PMID:31173506)
• STK24 modulates excitatory synaptic transmission in epileptic hippocampal neurons. (PMID:32436359)
• Serine/threonine-protein kinase STK24 induces tumorigenesis by regulating the STAT3/VEGFA signaling pathway. (PMID:36720310)
• STE20-type kinases MST3 and MST4 promote the progression of hepatocellular carcinoma: Evidence from human cell culture and expression profiling of liver biopsies. (PMID:37490000)
• Protein Kinase STK24 Promotes Tumor Immune Evasion via the AKT-PD-L1 Axis. (PMID:38229183)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	stk24b	ENSDARG00000023878
danio_rerio	stk24a	ENSDARG00000100955
mus_musculus	Stk24	ENSMUSG00000063410
rattus_norvegicus	LOC134486345	ENSRNOG00000011511
drosophila_melanogaster	GckIII	FBGN0266465

Paralogs (35): MAP3K14 (ENSG00000006062), MAP4K3 (ENSG00000011566), MAP4K5 (ENSG00000012983), MAP2K3 (ENSG00000034152), SLK (ENSG00000065613), MAP4K4 (ENSG00000071054), STK10 (ENSG00000072786), PAK3 (ENSG00000077264), STRADB (ENSG00000082146), MAP3K1 (ENSG00000095015), STK4 (ENSG00000101109), PAK5 (ENSG00000101349), STK3 (ENSG00000104375), MAP4K1 (ENSG00000104814), MAP3K8 (ENSG00000107968), MAP2K6 (ENSG00000108984), NEK4 (ENSG00000114904), STK25 (ENSG00000115694), NRK (ENSG00000123572), PAK4 (ENSG00000130669), STK26 (ENSG00000134602), TAOK3 (ENSG00000135090), PAK6 (ENSG00000137843), MINK1 (ENSG00000141503), PAK1 (ENSG00000149269), TAOK2 (ENSG00000149930), TNIK (ENSG00000154310), TAOK1 (ENSG00000160551), MAP4K2 (ENSG00000168067), OXSR1 (ENSG00000172939), MAP3K19 (ENSG00000176601), PAK2 (ENSG00000180370), SBK2 (ENSG00000187550), STK39 (ENSG00000198648), STRADA (ENSG00000266173)

Protein

Protein identifiers

Serine/threonine-protein kinase 24 — Q9Y6E0 (reviewed: Q9Y6E0)

Alternative names: Mammalian STE20-like protein kinase 3, STE20-like kinase MST3

All UniProt accessions (6): Q9Y6E0, B4DR80, H0Y630, Q5JV98, Q5JV99, Q5U0E6

UniProt curated annotations — full annotation on UniProt →

Function. Serine/threonine-protein kinase that acts on both serine and threonine residues and promotes apoptosis in response to stress stimuli and caspase activation. Mediates oxidative-stress-induced cell death by modulating phosphorylation of JNK1-JNK2 (MAPK8 and MAPK9), p38 (MAPK11, MAPK12, MAPK13 and MAPK14) during oxidative stress. Plays a role in a staurosporine-induced caspase-independent apoptotic pathway by regulating the nuclear translocation of AIFM1 and ENDOG and the DNase activity associated with ENDOG. Phosphorylates STK38L on ‘Thr-442’ and stimulates its kinase activity. In association with STK26 negatively regulates Golgi reorientation in polarized cell migration upon RHO activation. Also regulates cellular migration with alteration of PTPN12 activity and PXN phosphorylation: phosphorylates PTPN12 and inhibits its activity and may regulate PXN phosphorylation through PTPN12. May act as a key regulator of axon regeneration in the optic nerve and radial nerve. Part of the striatin-interacting phosphatase and kinase (STRIPAK) complexes. STRIPAK complexes have critical roles in protein (de)phosphorylation and are regulators of multiple signaling pathways including Hippo, MAPK, nuclear receptor and cytoskeleton remodeling. Different types of STRIPAK complexes are involved in a variety of biological processes such as cell growth, differentiation, apoptosis, metabolism and immune regulation.

Subunit / interactions. Monomer. Interacts with CTTNBP2NL. Interacts with RIPOR1 (via C-terminus); this interaction occurs in a PDCD10-dependent and Rho-independent manner. Interacts with PDCD10; this interaction is required for the association of STK24 with RIPOR1. Part of the core of STRIPAK complexes composed of PP2A catalytic and scaffolding subunits, the striatins (PP2A regulatory subunits), the striatin-associated proteins MOB4, STRIP1 and STRIP2, PDCD10 and members of the STE20 kinases, such as STK24 and STK26.

Subcellular location. Cytoplasm. Nucleus. Membrane.

Tissue specificity. Isoform A is ubiquitous. Isoform B is expressed in brain with high expression in hippocampus and cerebral cortex.

Post-translational modifications. Proteolytically processed by caspases during apoptosis. Proteolytic cleavage results in kinase activation, nuclear translocation of the truncated form (MST3/N) and the induction of apoptosis. Isoform B is activated by phosphorylation by PKA. Oxidative stress induces phosphorylation. Activated by autophosphorylation at Thr-190 and phosphorylation at this site is essential for its function. Manganese, magnesium and cobalt-dependent autophosphorylation is mainly on threonine residues while zinc-dependent autophosphorylation is on both serine and threonine residues.

Similarity. Belongs to the protein kinase superfamily. STE Ser/Thr protein kinase family. STE20 subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9Y6E0-1	B	yes
Q9Y6E0-2	A

RefSeq proteins (3): NP_001027467, NP_001273578, NP_003567 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR046409	PDC10_dimerisation_sf	Homologous_superfamily
IPR048288	PDCD10_N	Domain
IPR050629	STE20/SPS1-PAK	Family

Pfam: PF00069, PF20929

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 (59 total): helix 17, strand 12, binding site 5, modified residue 5, mutagenesis site 4, chain 3, turn 3, sequence variant 2, short sequence motif 2, site 1, splice variant 1, domain 1, region of interest 1, initiator methionine 1, active site 1

Structure

Experimental structures (PDB)

40 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
3A7I	X-RAY DIFFRACTION	1.45
8QLT	X-RAY DIFFRACTION	1.47
3A7J	X-RAY DIFFRACTION	1.5
4QMT	X-RAY DIFFRACTION	1.5
4QMU	X-RAY DIFFRACTION	1.55
3A7F	X-RAY DIFFRACTION	1.55
4QMW	X-RAY DIFFRACTION	1.6
8QLS	X-RAY DIFFRACTION	1.61
4U8Z	X-RAY DIFFRACTION	1.63
8QLQ	X-RAY DIFFRACTION	1.64
8BZI	X-RAY DIFFRACTION	1.72
7B32	X-RAY DIFFRACTION	1.75
4QMQ	X-RAY DIFFRACTION	1.77
4W8D	X-RAY DIFFRACTION	1.77
4W8E	X-RAY DIFFRACTION	1.79
7B31	X-RAY DIFFRACTION	1.8
4QNA	X-RAY DIFFRACTION	1.85
8QLR	X-RAY DIFFRACTION	1.85
4QMM	X-RAY DIFFRACTION	1.85
4QMZ	X-RAY DIFFRACTION	1.88
4QML	X-RAY DIFFRACTION	1.88
4QMX	X-RAY DIFFRACTION	1.88
4QMS	X-RAY DIFFRACTION	1.88
4QMY	X-RAY DIFFRACTION	1.88
4QMO	X-RAY DIFFRACTION	1.9
7B33	X-RAY DIFFRACTION	1.9
3A7H	X-RAY DIFFRACTION	1.96
3CKW	X-RAY DIFFRACTION	1.96
3A7G	X-RAY DIFFRACTION	2
4QMP	X-RAY DIFFRACTION	2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y6E0-F1	78.38	0.50

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 (2): 325–326 (cleavage; by caspase-3, caspase-7 and caspase-8); 156 (proton acceptor)

Ligand- & substrate-binding residues (5): 112–114; 161; 174; 42–50; 65

Post-translational modifications (5): 18, 190, 320, 2, 4

Mutagenesis-validated functional residues (4):

Position	Phenotype
18	loss of phosphorylation by pka.
65	loss of activity and autophosphorylation.
190	loss of activity and autophosphorylation.
321	loss of proteolytic cleavage by caspases.

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-111465	Apoptotic cleavage of cellular proteins
R-HSA-75153	Apoptotic execution phase
R-HSA-109581	Apoptosis
R-HSA-5357801	Programmed Cell Death

MSigDB gene sets: 529 (showing top): GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_UP, GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, WENDT_COHESIN_TARGETS_UP, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GGGACCA_MIR133A_MIR133B, GOBP_EMBRYONIC_HEMOPOIESIS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_PROTEIN_LOCALIZATION_TO_CYTOSKELETON, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, FREAC2_01, TAATAAT_MIR126, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, GOBP_REGULATION_OF_DEVELOPMENTAL_GROWTH, KEGG_MAPK_SIGNALING_PATHWAY

GO Biological Process (11): protein phosphorylation (GO:0006468), signal transduction (GO:0007165), intrinsic apoptotic signaling pathway in response to oxidative stress (GO:0008631), cellular response to starvation (GO:0009267), negative regulation of cell migration (GO:0030336), cellular response to oxidative stress (GO:0034599), intracellular signal transduction (GO:0035556), protein autophosphorylation (GO:0046777), regulation of axon regeneration (GO:0048679), execution phase of apoptosis (GO:0097194), apoptotic process (GO:0006915)

GO Molecular Function (10): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), cadherin binding (GO:0045296), metal ion binding (GO:0046872), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (9): nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytoplasm (GO:0005737), Golgi apparatus (GO:0005794), cytosol (GO:0005829), membrane (GO:0016020), extracellular exosome (GO:0070062), FAR/SIN/STRIPAK complex (GO:0090443)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Apoptotic execution phase	1
Apoptosis	1
Programmed Cell Death	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
cellular process	2
intracellular anatomical structure	2
protein kinase activity	2
intracellular membrane-bounded organelle	2
nuclear lumen	2
cytoplasm	2
phosphorylation	1
protein modification process	1
cell communication	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
intrinsic apoptotic signaling pathway	1
cellular response to nutrient levels	1
cellular response to stress	1
response to starvation	1
cell migration	1
regulation of cell migration	1
negative regulation of cell motility	1
response to oxidative stress	1
cellular response to chemical stress	1
signal transduction	1
protein phosphorylation	1
axon regeneration	1
regulation of response to external stimulus	1
regulation of neuron projection regeneration	1
regulation of response to wounding	1
apoptotic process	1
bleb assembly	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	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
cell adhesion molecule binding	1
cation binding	1

Protein interactions and networks

STRING

1656 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
STK24	PDCD10	Q9BUL8	977
STK24	CDC42	P21181	946
STK24	CAB39	Q9Y376	905
STK24	SAV1	Q9H4B6	885
STK24	MOB4	Q9Y3A3	876
STK24	STK25	O00506	857
STK24	STRN	O43815	829
STK24	STRIP1	Q5VSL9	806
STK24	MOB1A	Q9H8S9	803
STK24	STRIP2	Q9ULQ0	767
STK24	STK26	Q9P289	707
STK24	MOB1B	Q7L9L4	677
STK24	CTTNBP2NL	Q9P2B4	667
STK24	SLC12A2	P55011	664
STK24	NCK1	P16333	664

IntAct

115 interactions, top by confidence:

A	B	Type	Score
PDCD10	STK25	psi-mi:“MI:0914”(association)	0.980
STK24	PDCD10	psi-mi:“MI:0915”(physical association)	0.950
PDCD10	STK24	psi-mi:“MI:0407”(direct interaction)	0.950
STK25	STRN	psi-mi:“MI:0914”(association)	0.900
STK24	STK25	psi-mi:“MI:0914”(association)	0.890
STRN3	STK25	psi-mi:“MI:0914”(association)	0.880
CTTNBP2NL	STK25	psi-mi:“MI:0914”(association)	0.880
STRN3	STRN	psi-mi:“MI:0914”(association)	0.880
STRN3	STRN	psi-mi:“MI:2364”(proximity)	0.880
STK24	STRN	psi-mi:“MI:0915”(physical association)	0.870
STK24	STRN	psi-mi:“MI:0914”(association)	0.870
STK26	STRN	psi-mi:“MI:0914”(association)	0.860
STRIP1	STK25	psi-mi:“MI:0914”(association)	0.840
MED17	MED19	psi-mi:“MI:0914”(association)	0.840
STRIP1	STK24	psi-mi:“MI:0915”(physical association)	0.740
MOB4	STK25	psi-mi:“MI:0914”(association)	0.730
SIKE1	STRN	psi-mi:“MI:0914”(association)	0.730
CTTNBP2NL	STK24	psi-mi:“MI:0915”(physical association)	0.710

BioGRID (270): PDCD10 (Two-hybrid), STK24 (Biochemical Activity), STK24 (Affinity Capture-MS), STK24 (Affinity Capture-MS), STK24 (Affinity Capture-MS), STK24 (Affinity Capture-MS), PDCD10 (Two-hybrid), STK24 (Affinity Capture-MS), STK24 (Affinity Capture-MS), STK24 (Co-fractionation), STK24 (Co-fractionation), STK24 (Co-fractionation), STK24 (Co-fractionation), TLK2 (Co-fractionation), STK24 (Two-hybrid)

ESM2 similar proteins: A0A1S4CGX4, A9RWC9, A9S5R3, A9SR33, O01775, O14047, O14733, O44408, O80396, P10506, P18652, P18654, P29678, P31938, P36506, P36507, P51812, Q01986, Q02750, Q03428, Q05116, Q08942, Q10664, Q13163, Q18846, Q1HG70, Q20347, Q21307, Q24324, Q4KSH7, Q4V3C8, Q5QN75, Q62862, Q63932, Q63980, Q7TPS0, Q8MXI4, Q91447, Q94A06, Q99JT2

Diamond homologs: A0A078CGE6, A0A194W8T8, A2AQW0, A2QHV0, A4K2M3, A4K2P5, A4K2Q5, A4K2S1, A4K2T0, A4K2W5, A4K2Y1, A7A1P0, A8XJW8, A9RVK2, A9SY39, B0LT89, B0XXN8, B5VNQ3, C4YRB7, E9Q3S4, F4HRJ4, G4N7X0, G4NDR3, H2L099, O00506, O14047, O14305, O22040, O22042, O24527, O54748, O61122, O61125, O81472, O95382, P0CY23, P0CY24, P23561, P27636, P28829

SIGNOR signaling

7 interactions.

A	Effect	B	Mechanism
STK24	up-regulates	STK38	phosphorylation
STK24	up-regulates	STK38L	phosphorylation
STK24	up-regulates	STK24	phosphorylation
STK24	“down-regulates activity”	PTPN12	phosphorylation
STK24	“up-regulates activity”	TAOK1	phosphorylation
PRKACA	unknown	STK24	phosphorylation
STK24	“up-regulates activity”	RAB8A	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 102 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.

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of hippo signaling	7	53.4×	3e-08
axonogenesis	6	10.5×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	35
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

7224 predictions. Top by Δscore:

Variant	Effect	Δscore
13:98446096:A:AC	acceptor_loss	1.0000
13:98446096:A:AG	acceptor_gain	1.0000
13:98446097:G:GT	acceptor_gain	1.0000
13:98446097:GA:G	acceptor_gain	1.0000
13:98446097:GAA:G	acceptor_gain	1.0000
13:98446097:GAATC:G	acceptor_gain	1.0000
13:98446201:ACCAG:A	donor_gain	1.0000
13:98446202:CCAG:C	donor_gain	1.0000
13:98446203:CAG:C	donor_gain	1.0000
13:98446203:CAGGT:C	donor_loss	1.0000
13:98446204:AG:A	donor_gain	1.0000
13:98446204:AGG:A	donor_loss	1.0000
13:98446205:GG:G	donor_gain	1.0000
13:98446205:GGTA:G	donor_loss	1.0000
13:98446206:G:GA	donor_loss	1.0000
13:98446206:G:GG	donor_gain	1.0000
13:98446663:CA:C	acceptor_loss	1.0000
13:98446664:A:AG	acceptor_gain	1.0000
13:98446665:G:GA	acceptor_gain	1.0000
13:98446665:GGA:G	acceptor_gain	1.0000
13:98446665:GGAC:G	acceptor_gain	1.0000
13:98446665:GGACA:G	acceptor_gain	1.0000
13:98457163:GTTAC:G	donor_loss	1.0000
13:98457164:TTAC:T	donor_loss	1.0000
13:98457165:TACCT:T	donor_loss	1.0000
13:98457166:A:AG	donor_loss	1.0000
13:98457167:C:CA	donor_loss	1.0000
13:98457167:CCT:C	donor_gain	1.0000
13:98457302:CAA:C	acceptor_gain	1.0000
13:98457303:AA:A	acceptor_gain	1.0000

AlphaMissense

2828 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
13:98463826:G:T	A277D	1.000
13:98463834:T:A	R274S	1.000
13:98463834:T:G	R274S	1.000
13:98463835:C:G	R274T	1.000
13:98463836:T:C	R274G	1.000
13:98466395:A:C	L267W	1.000
13:98466397:A:C	C266W	1.000
13:98466398:C:T	C266Y	1.000
13:98466399:A:G	C266R	1.000
13:98466473:A:G	F241S	1.000
13:98466476:A:G	L240S	1.000
13:98466524:A:G	L224P	1.000
13:98466526:T:A	E223D	1.000
13:98466526:T:G	E223D	1.000
13:98466534:C:G	A221P	1.000
13:98466536:G:T	T220K	1.000
13:98466539:A:T	I219K	1.000
13:98466542:C:A	G218V	1.000
13:98466542:C:T	G218D	1.000
13:98466543:C:G	G218R	1.000
13:98466545:A:G	L217P	1.000
13:98466548:G:A	S216F	1.000
13:98466549:A:G	S216P	1.000
13:98466550:C:A	W215C	1.000
13:98466550:C:G	W215C	1.000
13:98466551:C:G	W215S	1.000
13:98466552:A:G	W215R	1.000
13:98466552:A:T	W215R	1.000
13:98466557:T:A	D213V	1.000
13:98466557:T:C	D213G	1.000

dbSNP variants (sampled 300 via entrez): RS1000019651 (13:98487685 T>C), RS1000038193 (13:98524870 C>T), RS1000040500 (13:98490196 G>C), RS1000075643 (13:98482675 C>T), RS1000116776 (13:98554219 T>A), RS1000212394 (13:98460088 T>C), RS1000217719 (13:98493258 G>A), RS1000218556 (13:98458543 G>A), RS1000231911 (13:98449599 A>C), RS1000284675 (13:98453348 A>G), RS1000312956 (13:98575975 G>A,T), RS1000325903 (13:98462795 C>T), RS1000341321 (13:98540156 A>G), RS1000348019 (13:98559347 T>A), RS1000390962 (13:98564969 C>T)

Disease associations

OMIM: gene MIM:604984 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

20 associations (top):

Study	Trait	p-value
GCST000785_12	Longevity	1.000000e-06
GCST001342_9	Alzheimer’s disease	4.000000e-06
GCST002045_1	Educational attainment	8.000000e-08
GCST002598_68	Educational attainment	3.000000e-07
GCST004136_18	Methadone dose in opioid dependence	3.000000e-06
GCST004401_1	Reading disability or specific language impairment (pleiotropy)	7.000000e-06
GCST007324_152	Adventurousness	9.000000e-13
GCST007325_284	General risk tolerance (MTAG)	1.000000e-12
GCST007709_123	General factor of neuroticism	4.000000e-10
GCST007709_125	General factor of neuroticism	3.000000e-08
GCST008357_30	Mood instability	9.000000e-09
GCST008647_42	Urinary sodium excretion	2.000000e-09
GCST009524_307	Household income (MTAG)	1.000000e-09
GCST009524_310	Household income (MTAG)	2.000000e-09
GCST009524_5	Household income (MTAG)	5.000000e-10
GCST009524_61	Household income (MTAG)	9.000000e-11
GCST010244_111	Triglyceride levels	8.000000e-09
GCST010988_475	Adult body size	2.000000e-09
GCST011377_6	Shoulder impingement or rotator cuff tear	3.000000e-08
GCST90000514_21	Gastroesophageal reflux disease	2.000000e-11

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0004784	self reported educational attainment
EFO:0007907	methadone dose measurement
EFO:0008579	risk-taking behaviour
EFO:0007660	neuroticism measurement
EFO:0008475	mood instability measurement
EFO:0009282	sodium measurement
EFO:0009695	household income
EFO:0004530	triglyceride measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5082 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

18 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 136,106 (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
CHEMBL180022	NERATINIB	4	9,404
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL576982	QUIZARTINIB	4	4,432
CHEMBL1088752	LOSMAPIMOD	3	865
CHEMBL2105728	CRENOLANIB	3	2,167
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL1721885	SU-014813	2	363
CHEMBL3039525	GOLVATINIB	2	535
CHEMBL572878	TOZASERTIB	2	2,998
CHEMBL607707	PELITINIB	2	6,340
CHEMBL1908397	KW-2449	1	622
CHEMBL3128043	PF-03758309	1	233
CHEMBL4289017	PF-03814735	1	537
CHEMBL574738	AST-487	1	451

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs58896682	FARP1, STK24		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — YSK subfamily

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
bosutinib	Inhibition	8.41	pIC50

Binding affinities (BindingDB)

7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Staurosporine	KD	1.7 nM
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril	KD	520 nM
N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide	KD	1100 nM
5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide	KD	2600 nM
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b	KD	3100 nM
(E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)but-2-enamide	KD	3500 nM
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	KD	3500 nM

ChEMBL bioactivities

107 potent at pChembl≥5 of 115 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.48	IC50	3.34	nM	STAUROSPORINE
8.47	IC50	3.4	nM	STAUROSPORINE
8.41	IC50	3.9	nM	BOSUTINIB
8.37	IC50	4.32	nM	STAUROSPORINE
8.19	Kd	6.5	nM	NERATINIB
8.15	IC50	7	nM	NERATINIB
8.00	IC50	10	nM	HESPERADIN
8.00	EC50	10	nM	CHEMBL5571948
7.96	Kd	11	nM	LOSMAPIMOD
7.93	IC50	11.8	nM	STAUROSPORINE
7.75	Kd	18	nM	CHEMBL4554938
7.72	Kd	19	nM	PF-03814735
7.70	EC50	20	nM	CHEMBL5571159
7.64	EC50	23	nM	CHEMBL5569777
7.60	Kd	25	nM	BOSUTINIB
7.57	EC50	27	nM	CHEMBL5565155
7.48	EC50	33	nM	CHEMBL5590480
7.47	EC50	34	nM	CHEMBL5594538
7.38	EC50	42	nM	CHEMBL5567421
7.37	IC50	43	nM	CHEMBL3770443
7.35	IC50	44.8	nM	CHEMBL4554938
7.32	EC50	48	nM	CHEMBL5575508
7.26	EC50	55	nM	CHEMBL5565155
7.25	EC50	56	nM	CHEMBL5566570
7.24	Kd	57	nM	CRENOLANIB
7.24	EC50	57	nM	CHEMBL5573797
7.24	EC50	57	nM	CHEMBL5572995
7.22	EC50	60	nM	CHEMBL5555859
7.20	Kd	63	nM	SUNITINIB
7.10	EC50	80	nM	CHEMBL5562742
7.09	EC50	81	nM	CHEMBL5573797
7.04	EC50	92	nM	CHEMBL5567287
7.03	IC50	94	nM	BAY-3827
7.00	Kd	100	nM	SU-014813
6.96	EC50	110	nM	CHEMBL5562742
6.96	Kd	110	nM	NINTEDANIB
6.94	EC50	115	nM	CHEMBL5573230
6.92	Kd	120	nM	STAUROSPORINE
6.92	EC50	120	nM	STAUROSPORINE
6.85	EC50	140	nM	STAUROSPORINE
6.79	EC50	163	nM	CHEMBL5590631
6.75	EC50	178	nM	CHEMBL5566570
6.75	Kd	180	nM	JNJ-7706621
6.68	Kd	207	nM	GOLVATINIB
6.66	EC50	221	nM	CHEMBL5567421
6.64	Kd	230	nM	GILTERITINIB
6.61	EC50	244	nM	CHEMBL5589642
6.60	EC50	251	nM	CHEMBL3818046
6.56	EC50	278	nM	CHEMBL5567028
6.55	EC50	280	nM	CHEMBL1235645

PubChem BioAssay actives

99 with measured affinity, of 1043 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	1612682: Inhibition of human MST3 using MBP as substrate by [gamma-33P]-ATP assay	ic50	0.0033	uM
Bosutinib	507440: Inhibition of STK24	ic50	0.0039	uM
Neratinib	624917: Binding constant for MST3 kinase domain	kd	0.0065	uM
N-[2-hydroxy-3-[C-phenyl-N-[4-(piperidin-1-ylmethyl)phenyl]carbonimidoyl]-1H-indol-5-yl]ethanesulfonamide	2090802: Inhibition of MST3 (unknown origin)	ic50	0.0100	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-[4-fluoro-3-(hydroxymethyl)anilino]pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0100	uM
6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide	1425180: 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	0.0110	uM
4-[(2,9-dimethyl-8-oxo-6-thia-2,9,12,14-tetrazatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-13-yl)amino]benzenesulfonamide	2189142: Binding affinity to MST3 (unknown origin) assessed as dissociation constant	kd	0.0180	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	1425180: 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
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-[4-(3-hydroxypropyl)anilino]pyrido[2,3-d]pyrimidin-7-one	2090814: Inhibition of MST3 (unknown origin) expressed in intact HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0200	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(4-hydroxyanilino)pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0230	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(3-morpholin-4-ylpropylamino)pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0270	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(3-piperazin-1-ylpropylamino)pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0330	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(3-hydroxy-4-methylanilino)pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0340	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0420	uM
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	1280636: Inhibition of human recombinant MST3	ic50	0.0430	uM
8-[(4-aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0480	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-[3-(2-oxopyrrolidin-1-yl)propylamino]pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0560	uM
1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine	1425180: 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	0.0570	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(1,3-dihydroxypropan-2-ylamino)pyrido[2,3-d]pyrimidin-7-one	2090814: Inhibition of MST3 (unknown origin) expressed in intact HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0570	uM
8-(4-aminobutyl)-2-[3-(4-aminophenyl)propylamino]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0570	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-8-(2-piperidin-4-ylethyl)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0600	uM
Sunitinib	435532: Binding constant for MST3 kinase domain	kd	0.0630	uM
2,4,5,8,14,16,23-heptazatetracyclo[13.7.1.13,6.017,22]tetracosa-1(23),3,6(24),15,17,19,21-heptaen-7-one	2093081: Binding affinity to C-terminal full length human MST3 expressed in permeabilized HEK293T cells incubated for 2 hrs by NanoBRET assay	ec50	0.0800	uM
8-(5-aminopentyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.0920	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	435532: Binding constant for MST3 kinase domain	kd	0.1000	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	624917: Binding constant for MST3 kinase domain	kd	0.1100	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(2-methoxy-4-morpholin-4-ylanilino)pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.1150	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(2-hydroxy-5-methoxyanilino)pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.1630	uM
4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide	435532: Binding constant for MST3 kinase domain	kd	0.1800	uM
1-N’-[2-fluoro-4-[[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]-4-pyridinyl]oxy]phenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide	1425180: 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	0.2070	uM
Gilteritinib	1425180: 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	0.2300	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(4-hydroxybutyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.2440	uM
8-(3-aminopropyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.2510	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.2780	uM
2-[4-[[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]phenyl]acetonitrile	2093081: Binding affinity to C-terminal full length human MST3 expressed in permeabilized HEK293T cells incubated for 2 hrs by NanoBRET assay	ec50	0.2800	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(2-hydroxyethyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.2880	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(5-hydroxypentyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.3160	uM
8-(4-aminobutyl)-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-[2-methyl-5-(trifluoromethyl)anilino]pyrido[2,3-d]pyrimidin-7-one	2090815: Inhibition of MST3 (unknown origin) expressed in lysed HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.3670	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	1425180: 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	0.3690	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(3-hydroxypropyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.3820	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(2-methoxyethyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.4200	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	435532: Binding constant for MST3 kinase domain	kd	0.4300	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	1526175: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged STK24 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.4360	uM
2,4,5,8,15,17,24-heptazatetracyclo[14.7.1.13,6.018,23]pentacosa-1(24),3,6(25),16,18,20,22-heptaen-7-one	2093081: Binding affinity to C-terminal full length human MST3 expressed in permeabilized HEK293T cells incubated for 2 hrs by NanoBRET assay	ec50	0.4500	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(3-methoxypropyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.5940	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-(4-methoxybutyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.6140	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	507634: Binding affinity to MST3	kd	0.7600	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	1526175: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged STK24 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.7670	uM
6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-8-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one	2090806: Inhibition of MST3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 20 hrs by NanoBRET assay	ec50	0.7750	uM
2,4,5,8,16,18,25-heptazapentacyclo[15.7.1.13,6.111,15.019,24]heptacosa-1(25),3,6(27),11(26),12,14,17,19,21,23-decaen-7-one	2093081: Binding affinity to C-terminal full length human MST3 expressed in permeabilized HEK293T cells incubated for 2 hrs by NanoBRET assay	ec50	0.9200	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, affects cotreatment, decreases methylation	3
Arsenic Trioxide	increases expression, affects cotreatment	2
Benzo(a)pyrene	affects methylation	2
Tamoxifen	affects expression, affects cotreatment, decreases expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression	2
Raloxifene Hydrochloride	affects expression, affects cotreatment, decreases expression	2
bisphenol F	increases expression	1
cinnamaldehyde	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
sodium arsenite	decreases expression, increases abundance	1
perfluorooctane sulfonic acid	increases expression	1
CGP 52608	affects binding, increases reaction	1
bisphenol S	decreases methylation	1
bisphenol AF	increases expression	1
Temozolomide	decreases expression	1
Sunitinib	increases expression	1
Fulvestrant	affects cotreatment, decreases methylation	1
Acetaminophen	increases expression	1
Air Pollutants	affects expression, increases abundance	1
Arsenic	decreases expression, increases abundance	1
Chelating Agents	affects binding, increases expression	1
Copper	affects binding, increases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Estradiol	affects expression	1
Hydrogen Peroxide	affects cotreatment, increases expression	1
Ivermectin	decreases expression	1
Ozone	affects expression, increases abundance	1
Phenobarbital	affects expression	1
Selenium	increases expression	1

ChEMBL screening assays

314 unique, capped per target: 314 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1041151	Binding	Residual activity of MST3 at 1 uM by microplate scintillation counting	Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization. — Bioorg Med Chem

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1CP	Abcam A-431 STK24 KO	Cancer cell line	Female

Clinical trials (associated diseases)

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