SGK2

Summary

SGK2 (serum/glucocorticoid regulated kinase 2, HGNC:13900) is a protein-coding gene on chromosome 20q13.12, encoding Serine/threonine-protein kinase Sgk2 (Q9HBY8). Serine/threonine-protein kinase which is involved in the regulation of a wide variety of ion channels, membrane transporters, cell growth, survival and proliferation.

This gene encodes a serine/threonine protein kinase. Although this gene product is similar to serum- and glucocorticoid-induced protein kinase (SGK), this gene is not induced by serum or glucocorticoids. This gene is induced in response to signals that activate phosphatidylinositol 3-kinase, which is also true for SGK. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 10110 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 82 total — 1 likely-pathogenic
• Druggable target: yes — 9 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_170693

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:13900
Approved symbol	SGK2
Name	serum/glucocorticoid regulated kinase 2
Location	20q13.12
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000101049
Ensembl biotype	protein_coding
OMIM	607589
Entrez	10110

Gene structure

Transcript identifiers

Ensembl transcripts: 21 — 17 protein_coding, 2 nonsense_mediated_decay, 2 retained_intron

ENST00000341458, ENST00000373077, ENST00000373100, ENST00000412111, ENST00000423407, ENST00000426287, ENST00000485914, ENST00000496343, ENST00000617268, ENST00000617358, ENST00000647716, ENST00000647834, ENST00000648083, ENST00000648530, ENST00000872540, ENST00000872541, ENST00000872542, ENST00000872543, ENST00000872544, ENST00000872545, ENST00000959623

RefSeq mRNA: 3 — MANE Select: NM_170693 NM_001199264, NM_016276, NM_170693

CCDS: CCDS13321

Canonical transcript exons

ENST00000373100 — 13 exons

Exon	Start	End
ENSE00000662177	43567068	43567117
ENSE00000662178	43567665	43567722
ENSE00000662179	43567916	43567999
ENSE00000662180	43569385	43569516
ENSE00000662181	43570617	43570729
ENSE00000662182	43571024	43571060
ENSE00001459462	43559027	43559159
ENSE00001659656	43576224	43576379
ENSE00001802219	43574909	43575004
ENSE00003500053	43579972	43580061
ENSE00003583106	43566473	43566531
ENSE00003786202	43572051	43572137
ENSE00003835959	43584852	43585627

Expression profiles

Bgee: expression breadth ubiquitous, 211 present calls, max score 97.26.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.3196 / max 54.2742, expressed in 63 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
184666	0.7512	108
184669	0.4979	72
184664	0.4477	81
184667	0.2568	59
184668	0.0442	25
209115	0.0185	9

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
mucosa of transverse colon	UBERON:0004991	97.26	gold quality
metanephros cortex	UBERON:0010533	96.93	gold quality
right lobe of liver	UBERON:0001114	95.31	gold quality
rectum	UBERON:0001052	94.41	gold quality
adult mammalian kidney	UBERON:0000082	93.38	gold quality
liver	UBERON:0002107	90.86	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	89.63	gold quality
renal medulla	UBERON:0000362	89.49	gold quality
transverse colon	UBERON:0001157	89.48	gold quality
kidney	UBERON:0002113	89.47	gold quality
duodenum	UBERON:0002114	89.22	gold quality
spinal cord	UBERON:0002240	88.05	gold quality
body of pancreas	UBERON:0001150	87.95	gold quality
cortex of kidney	UBERON:0001225	86.92	gold quality
nephron tubule	UBERON:0001231	86.27	silver quality
colonic mucosa	UBERON:0000317	85.67	gold quality
ileal mucosa	UBERON:0000331	85.58	gold quality
corpus callosum	UBERON:0002336	85.30	gold quality
jejunal mucosa	UBERON:0000399	85.06	gold quality
body of stomach	UBERON:0001161	85.05	gold quality
kidney epithelium	UBERON:0004819	84.07	silver quality
small intestine Peyer’s patch	UBERON:0003454	83.96	gold quality
mucosa of sigmoid colon	UBERON:0004993	83.69	gold quality
pancreas	UBERON:0001264	83.44	gold quality
small intestine	UBERON:0002108	83.44	gold quality
stomach	UBERON:0000945	83.36	gold quality
metanephros	UBERON:0000081	82.80	gold quality
right uterine tube	UBERON:0001302	82.38	gold quality
intestine	UBERON:0000160	81.70	gold quality
large intestine	UBERON:0000059	81.36	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	7.61

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

27 targeting SGK2, 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-3148	99.97	75.06	6478
HSA-MIR-6079	99.84	68.54	1170
HSA-MIR-4713-5P	99.78	67.80	1794
HSA-MIR-6745	99.74	65.33	1321
HSA-MIR-646	99.68	67.84	1645
HSA-MIR-466	99.67	70.85	2863
HSA-MIR-875-3P	99.63	69.47	2548
HSA-MIR-298	99.63	67.56	1916
HSA-MIR-6132	99.60	65.83	1554
HSA-MIR-6836-5P	99.60	65.62	1538
HSA-MIR-671-5P	99.52	67.11	1277
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-4786-3P	99.36	68.35	1390
HSA-MIR-1912-3P	99.32	67.40	936
HSA-MIR-6828-5P	99.31	69.21	1433
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-1295B-5P	99.03	67.50	810
HSA-MIR-4490	98.51	68.47	943
HSA-MIR-7843-3P	98.31	67.94	803
HSA-MIR-3130-5P	98.14	66.00	711
HSA-MIR-4483	98.09	64.12	1642
HSA-MIR-376C-3P	97.63	68.88	1263
HSA-MIR-4482-5P	97.53	65.68	598
HSA-MIR-921	97.09	66.45	562
HSA-MIR-215-3P	97.02	68.01	1209
HSA-MIR-6782-5P	96.45	64.42	612
HSA-MIR-1293	96.16	64.69	916

Literature-anchored findings (GeneRIF, showing 12)

• Powerful stimulating effect of all three isoforms of SGK on K(+) channels. Those effects may participate in regulation of epithelial transport, cell proliferation, and neuromuscular excitability. (PMID:12397388)
• All three members of the SGK family of kinases SGK1-3 and protein kinase B stimulate the slowly activating K(+) channel KCNE1/KCNQ1. The kinases may thus participate in the regulation of KCNE1-dependent transport and excitability. (PMID:12634932)
• Co-expression of SGK1, but not of SGK2 or SGK3, increased Kv 4.3/KChIP2b channel currents. (PMID:15578212)
• Glucocorticoid inducible kinase isoforms SGK1-3 are novel potent stimulators of Slc6a19 and may thus participate in the regulation of neutral amino acid transport in vivo. (PMID:20511718)
• Activation of hepatocyte pregnane X receptor is mediated through serum- and glucocorticoid-regulated kinase (SGK)2. (PMID:24204015)
• SGK2 stimulated hOAT4 transport activity by abrogating the inhibitory effect of Nedd4-2 on the transporter. (PMID:26740304)
• Loss of the paternally derived allele of the imprinted SGK2 gene is associated with Shwachman-Diamond syndrome. (PMID:27553422)
• These findings suggest that SGK2 promotes hepatocellular carcinoma progression and mediates glycogen synthase kinase 3 beta/beta-catenin signaling in hepatocellular carcinoma cells. (PMID:28639896)
• SGK2 promotes renal cancer progression via enhancing ERK 1/2 and AKT phosphorylation. (PMID:31002126)
• SGK2 is overexpressed in colon cancer and promotes epithelial-mesenchymal transition in colon cancer cells. (PMID:32565024)
• Serum- and glucocorticoid- inducible kinase 2, SGK2, is a novel autophagy regulator and modulates platinum drugs response in cancer cells. (PMID:32848212)
• SGK2 promotes prostate cancer metastasis by inhibiting ferroptosis via upregulating GPX4. (PMID:36720852)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	sgk2a	ENSDARG00000063370
mus_musculus	Sgk2	ENSMUSG00000017868
rattus_norvegicus	Sgk2	ENSRNOG00000033573
caenorhabditis_elegans		WBGENE00004789

Paralogs (13): MAST4 (ENSG00000069020), MAST2 (ENSG00000086015), MAST3 (ENSG00000099308), SGK3 (ENSG00000104205), DMPK (ENSG00000104936), MAST1 (ENSG00000105613), SGK1 (ENSG00000118515), MASTL (ENSG00000120539), LATS1 (ENSG00000131023), LATS2 (ENSG00000150457), STK32B (ENSG00000152953), STK32C (ENSG00000165752), STK32A (ENSG00000169302)

Protein

Protein identifiers

Serine/threonine-protein kinase Sgk2 — Q9HBY8 (reviewed: Q9HBY8)

Alternative names: Serum/glucocorticoid-regulated kinase 2

All UniProt accessions (9): Q9HBY8, A0A0G2JNI2, A0A3B3IRL0, A0A3B3IRX6, A0A3B3IT40, A0A3B3IUG0, F2Z3C8, Q5H8Y5, X6R8H3

UniProt curated annotations — full annotation on UniProt →

Function. Serine/threonine-protein kinase which is involved in the regulation of a wide variety of ion channels, membrane transporters, cell growth, survival and proliferation. Up-regulates Na(+) channels: SCNN1A/ENAC, K(+) channels: KCNA3/Kv1.3, KCNE1 and KCNQ1, amino acid transporter: SLC6A19, glutamate transporter: SLC1A6/EAAT4, glutamate receptors: GRIA1/GLUR1 and GRIK2/GLUR6, Na(+)/H(+) exchanger: SLC9A3/NHE3, and the Na(+)/K(+) ATPase.

Subcellular location. Cytoplasm. Nucleus.

Tissue specificity. Highly expressed in liver, kidney and pancreas, and at lower levels in brain.

Post-translational modifications. Activated by phosphorylation on Ser-356 by an unknown kinase (may be mTORC2 but not confirmed), transforming it into a substrate for PDPK1 which then phosphorylates it on Thr-193.

Activity regulation. Two specific sites, one in the kinase domain (Thr-193) and the other in the C-terminal regulatory region (Ser-356), need to be phosphorylated for its full activation.

Similarity. Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q9HBY8-2	1, alpha	yes
Q9HBY8-1	2, beta
Q9HBY8-3	3

RefSeq proteins (3): NP_001186193, NP_057360, NP_733794* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR000961	AGC-kinase_C	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR017892	Pkinase_C	Domain

Pfam: PF00069, PF00433

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 (22 total): modified residue 5, sequence variant 3, sequence conflict 3, domain 2, splice variant 2, binding site 2, chain 1, mutagenesis site 1, region of interest 1, short sequence motif 1, active site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9HBY8-F1	88.10	0.72

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): 159 (proton acceptor)

Ligand- & substrate-binding residues (2): 41–49; 64

Post-translational modifications (5): 334, 356, 357, 10, 193

Mutagenesis-validated functional residues (1):

Position	Phenotype
356	increased activation.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-2672351	Stimuli-sensing channels
R-HSA-382551	Transport of small molecules
R-HSA-983712	Ion channel transport

MSigDB gene sets: 93 (showing top): GOBP_POSITIVE_REGULATION_OF_TRANSPORTER_ACTIVITY, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GOBP_GROWTH, HNF1_Q6, CAGCTG_AP4_Q5, GOBP_POSITIVE_REGULATION_OF_MOLECULAR_FUNCTION, RGTTAMWNATT_HNF1_01, BLALOCK_ALZHEIMERS_DISEASE_UP, TGACATY_UNKNOWN, HNF1_C, GFI1_01, BASAKI_YBX1_TARGETS_DN, HNF1_01, GOBP_POSITIVE_REGULATION_OF_TRANSPORT, GOBP_REGULATION_OF_TRANSPORT

GO Biological Process (6): regulation of cell growth (GO:0001558), protein phosphorylation (GO:0006468), positive regulation of transporter activity (GO:0032411), intracellular signal transduction (GO:0035556), regulation of cell population proliferation (GO:0042127), response to oxidative stress (GO:0006979)

GO Molecular Function (10): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), potassium channel regulator activity (GO:0015459), sodium channel regulator activity (GO:0017080), 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 (4): nucleoplasm (GO:0005654), cytosol (GO:0005829), nucleus (GO:0005634), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Ion channel transport	1
Transport of small molecules	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
intracellular anatomical structure	2
protein kinase activity	2
ion channel regulator activity	2
cell growth	1
regulation of growth	1
regulation of cellular component organization	1
phosphorylation	1
protein modification process	1
transporter activity	1
positive regulation of molecular function	1
positive regulation of transport	1
signal transduction	1
cell population proliferation	1
regulation of cellular process	1
response to stress	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
potassium channel activity	1
sodium channel activity	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
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
nuclear lumen	1
cytoplasm	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

1498 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SGK2	TP53	P04637	485
SGK2	NR1I2	O75469	448
SGK2	IGF1	P01343	445
SGK2	L3MBTL1	Q9Y468	426
SGK2	G6PC3	Q9BUM1	381
SGK2	NENF	Q9UMX5	364
SGK2	TBC1D16	Q8TBP0	346
SGK2	NEDD4L	Q96PU5	340
SGK2	PROCA1	Q8NCQ7	337
SGK2	ADCY10	Q96PN6	332
SGK2	ESPN	B1AK53	331
SGK2	G6PC1	P35575	328
SGK2	OSBPL3	Q9H4L5	320
SGK2	GPR21	Q99679	320
SGK2	TSC2	P49815	306

IntAct

8 interactions, top by confidence:

A	B	Type	Score
SGK2	HSP90AB1	psi-mi:“MI:0915”(physical association)	0.670
SGK2	HSP90AA1	psi-mi:“MI:0914”(association)	0.530
SGK2	DAPK1	psi-mi:“MI:0407”(direct interaction)	0.440
SGK2	IL3RA	psi-mi:“MI:0915”(physical association)	0.370
SGK2	DDX5	psi-mi:“MI:0914”(association)	0.350
SGK3	AIP	psi-mi:“MI:0914”(association)	0.350
SGK2	AIP	psi-mi:“MI:0914”(association)	0.350

BioGRID (50): CCT3 (Affinity Capture-MS), CCT4 (Affinity Capture-MS), CCT5 (Affinity Capture-MS), CCT6A (Affinity Capture-MS), CCT7 (Affinity Capture-MS), CCT8 (Affinity Capture-MS), DDX5 (Affinity Capture-MS), FKBP5 (Affinity Capture-MS), ILF3 (Affinity Capture-MS), TCP1 (Affinity Capture-MS), SGK2 (Affinity Capture-RNA), SGK2 (Reconstituted Complex), SGK2 (Affinity Capture-MS), PMM2 (Two-hybrid), HIRIP3 (Two-hybrid)

ESM2 similar proteins: A7MB74, A8XJQ6, A8XNJ6, O00141, O55173, O75582, P05986, P10665, P10666, P18652, P18653, P18654, P21901, P51812, Q02111, Q04759, Q05655, Q06226, Q12706, Q15349, Q15418, Q2PJ68, Q4R633, Q5BKK4, Q5F3L1, Q5PU49, Q5Q0U5, Q5R4K3, Q5R7A7, Q63531, Q6GLY8, Q6GPN6, Q6PFQ0, Q6U1I9, Q7JP68, Q7TPS0, Q7ZTW4, Q8C050, Q8R4U9, Q8R4V0

Diamond homologs: A1A4I4, A1Z7T0, A1Z9X0, A7MBL8, A8KBH6, A8WUG4, F1M7Y5, O08874, O19111, O42632, P04409, P05126, P05128, P05129, P05130, P05696, P05771, P05772, P09215, P09216, P09217, P10102, P10829, P10830, P13677, P13678, P16054, P17252, P20444, P23298, P24583, P24723, P28867, P31748, P31749, P31750, P31751, P34722, P34885, P36582

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
PDPK1	up-regulates	SGK2	phosphorylation
SGK2	“down-regulates activity”	FOXO3	phosphorylation
SGK2	“down-regulates activity”	FOXO	phosphorylation
PDPK1	“up-regulates activity”	SGK2	phosphorylation
“2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid”	“down-regulates activity”	SGK2	“chemical inhibition”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	60
Likely benign	3
Benign	3

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
1183962	NM_170693.3(SGK2):c.380G>A (p.Arg127Gln)	Likely pathogenic

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

2417 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
20:43572070:A:T	D177V	1.000
20:43567956:C:A	A62E	0.999
20:43567963:G:C	K64N	0.999
20:43567963:G:T	K64N	0.999
20:43570729:G:T	R158M	0.999
20:43571026:A:C	D159A	0.999
20:43571026:A:T	D159V	0.999
20:43572069:G:C	D177H	0.999
20:43572070:A:C	D177A	0.999
20:43572070:A:G	D177G	0.999
20:43572071:T:A	D177E	0.999
20:43572071:T:G	D177E	0.999
20:43567682:T:C	F35S	0.998
20:43567961:A:C	K64Q	0.998
20:43567961:A:G	K64E	0.998
20:43569407:G:C	R84P	0.998
20:43569463:T:C	F103L	0.998
20:43569465:C:A	F103L	0.998
20:43569465:C:G	F103L	0.998
20:43570678:C:A	A141D	0.998
20:43570729:G:C	R158T	0.998
20:43571026:A:G	D159G	0.998
20:43571027:T:A	D159E	0.998
20:43571027:T:G	D159E	0.998
20:43571042:C:A	N164K	0.998
20:43571042:C:G	N164K	0.998
20:43572052:G:A	G171E	0.998
20:43572083:C:G	C181W	0.998
20:43574963:T:A	W218R	0.998
20:43574963:T:C	W218R	0.998

dbSNP variants (sampled 300 via entrez): RS1000185640 (20:43561770 T>G), RS1000198552 (20:43567539 G>A,T), RS1000231614 (20:43584646 G>C), RS1000370024 (20:43581166 T>C), RS1000454472 (20:43561781 G>A,T), RS1000512596 (20:43580463 C>T), RS1001020949 (20:43580098 G>A), RS1001069870 (20:43579703 C>T), RS1001077387 (20:43572725 A>G), RS1001268222 (20:43573162 C>G,T), RS1001330441 (20:43579643 A>G), RS1001392261 (20:43578816 G>A), RS1001573071 (20:43571520 T>A,G), RS1001634354 (20:43585545 C>A), RS1001642220 (20:43579205 C>T)

Disease associations

OMIM: gene MIM:607589 | disease phenotypes: MIM:114500

GenCC curated gene-disease

Mondo (1): colorectal cancer (MONDO:0005575)

Orphanet (1): NON RARE IN EUROPE: Colorectal cancer (Orphanet:466667)

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST003518_11	Daytime sleep phenotypes	5.000000e-06
GCST012053_10	Weight	7.000000e-07

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0007828	daytime rest measurement
EFO:0004338	body weight

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5794 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

9 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 20,878 (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
CHEMBL38380	FASUDIL	3	11,953
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL1967878	CENISERTIB	2	358
CHEMBL1980297	ILORASERTIB	2	581
CHEMBL565612	SOTRASTAURIN	2	1,355
CHEMBL1084546	PF-00562271	1	399
CHEMBL1969664	AZD-1080	1	600
CHEMBL1980391	RG-1530	1	37
CHEMBL482967	CYC-116	1	651

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — SGK family

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
GSK650394	Inhibition	6.99	pIC50
compound 14n [PMID: 25589934]	Inhibition	6.89	pIC50

ChEMBL bioactivities

273 potent at pChembl≥5 of 273 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.10	Ki	7.943	nM	CHEMBL1980995
7.82	IC50	15.2	nM	STAUROSPORINE
7.82	IC50	15.1	nM	STAUROSPORINE
7.80	Ki	15.85	nM	CHEMBL1973540
7.78	IC50	16.5	nM	STAUROSPORINE
7.70	Ki	19.95	nM	CHEMBL1965845
7.70	Ki	19.95	nM	CHEMBL1998121
7.68	IC50	21	nM	CHEMBL5082336
7.60	Ki	25.12	nM	CHEMBL2001751
7.40	Ki	39.81	nM	CHEMBL1969502
7.30	Ki	50.12	nM	CHEMBL1997534
7.30	Ki	50.12	nM	CHEMBL1970903
7.30	Ki	50.12	nM	CHEMBL1966524
7.30	Ki	50.12	nM	CHEMBL1966628
7.20	Ki	63.1	nM	CHEMBL1975128
7.20	Ki	63.1	nM	CHEMBL1998159
7.20	Ki	63.1	nM	CHEMBL1999931
7.10	Ki	79.43	nM	CHEMBL1991063
7.00	Ki	100	nM	CHEMBL1969042
7.00	Ki	100	nM	CHEMBL2003638
6.99	IC50	103	nM	GSK-650394
6.90	Ki	125.9	nM	CHEMBL1982957
6.90	Ki	125.9	nM	CHEMBL1999811
6.89	IC50	128	nM	CHEMBL3092468
6.80	IC50	160	nM	GSK-650394
6.80	Ki	158.5	nM	CHEMBL1986943
6.80	Ki	158.5	nM	CHEMBL1988608
6.80	Ki	158.5	nM	CHEMBL1976090
6.80	Ki	158.5	nM	CHEMBL2006933
6.80	Ki	158.5	nM	CHEMBL1974870
6.70	Ki	199.5	nM	GSK-269962A
6.70	Ki	199.5	nM	CHEMBL1241473
6.70	Ki	199.5	nM	CHEMBL1970217
6.70	Ki	199.5	nM	CHEMBL244378
6.60	Ki	251.2	nM	BAY-549
6.60	Ki	251.2	nM	CYC-116
6.60	Ki	251.2	nM	SP-600125
6.60	Ki	251.2	nM	CHEMBL1966343
6.60	Ki	251.2	nM	CHEMBL1982711
6.60	Ki	251.2	nM	CHEMBL1976240
6.60	Ki	251.2	nM	CHEMBL1682345
6.50	Ki	316.2	nM	CHEMBL1986263
6.50	Ki	316.2	nM	CHEMBL2004934
6.50	Ki	316.2	nM	CHEMBL1969049
6.50	Ki	316.2	nM	CHEMBL1989646
6.50	Ki	316.2	nM	CHEMBL1965836
6.50	Ki	316.2	nM	CHEMBL1992342
6.50	Ki	316.2	nM	CHEMBL1972346
6.50	Ki	316.2	nM	CHEMBL1990254
6.50	Ki	316.2	nM	CHEMBL1990885

PubChem BioAssay actives

8 with measured affinity, of 1231 total; 6 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	2198412: Inhibition of human SGK2 using KGSGSGRPRTSSFAEG as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radiometric Hot-SpotSM Kinase assay	ic50	0.0151	uM
N-[4-(3-amino-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-5-chloro-2-cyanobenzenesulfonamide	1821045: Inhibition of human SGK2 in presence 500 uM presence of ATP	ic50	0.0210	uM
N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-5-chloro-2-fluorobenzenesulfonamide	1177302: Inhibition of human SGK2 in presence of 500 uM ATP	ic50	0.1280	uM
N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2,3-dichlorobenzenesulfonamide	1177302: Inhibition of human SGK2 in presence of 500 uM ATP	ic50	0.9240	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	1526184: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged SGK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	1.2210	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	1526184: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged SGK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	1.7710	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression, increases expression, increases methylation	7
Valproic Acid	affects cotreatment, decreases expression, increases expression	4
sodium arsenite	increases expression, decreases expression	2
Acetaminophen	decreases expression	2
Nickel	decreases expression	2
Rifampin	increases expression, affects binding, increases reaction, affects expression, affects reaction (+2 more)	2
Cyclosporine	increases expression, decreases expression	2
Aflatoxin B1	affects expression, increases expression	2
aristolochic acid I	increases expression	1
dicrotophos	increases expression	1
methylmercuric chloride	decreases expression	1
azoxystrobin	affects expression	1
CGP 52608	affects binding, increases reaction	1
K 7174	decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
clothianidin	decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
licochalcone B	increases expression	1
jinfukang	affects cotreatment, increases expression	1
picoxystrobin	decreases expression	1
(+)-JQ1 compound	decreases expression	1
Atorvastatin	affects cotreatment, increases expression	1
Troglitazone	increases expression	1
Fluvastatin	affects cotreatment, increases expression	1
Ampicillin	decreases expression	1
Arsenic	affects methylation	1
Barium	decreases reaction, increases transport	1
Cisplatin	affects cotreatment, increases expression	1
Diethylhexyl Phthalate	decreases expression	1
Doxorubicin	increases expression	1

ChEMBL screening assays

195 unique, capped per target: 194 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1022317	Binding	Inhibition of SGK2 at 100 nM relative to control	Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases. — J Med Chem
CHEMBL1963793	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: SGK	PubChem BioAssay data set

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00114829	PHASE4	UNKNOWN	Preoperative Assessment of Colon Tumor
NCT00114842	PHASE4	COMPLETED	Magnetic Resonance (MR) Colonography With Fecal Tagging
NCT00114946	PHASE4	TERMINATED	A Study to Compare Two Avastin-Based Treatment Regimens for the Treatment of Metastatic Colorectal Cancer
NCT00122720	PHASE4	COMPLETED	The Effect of Darbepoetin Upon Rehabilitation for Colorectal Cancer Surgery
NCT00129870	PHASE4	TERMINATED	CONCEPT: Comparison of Oxaliplatin vs Conventional Methods With Calcium/Magnesium in First-Line Metastatic Colorectal Cancer
NCT00138060	PHASE4	COMPLETED	Toxicity/Benefit Ratio Optimization of Chemotherapy in Colorectal Cancer (CRC) Patients by Determination of Individual Genotypic Determinants
NCT00216424	PHASE4	TERMINATED	Capecitabine (Xeloda) and Radiation for Patients With Rectosigmoid Carcinoma
NCT00327093	PHASE4	TERMINATED	Elaboration of a Model for Predicting Efficacy of Monoclonal Antibodies (Cetuximab and Bevacizumab) in Patients With Colorectal Cancer and Liver Metastases
NCT00332943	PHASE4	COMPLETED	MR Colonography With Fecal Tagging. Barium vs. BariumFerumoxsil
NCT00441311	PHASE4	COMPLETED	Dissemination of Colorectal Cancer Screening to Primary Care Physicians
NCT00460837	PHASE4	WITHDRAWN	Comparison of Bowel Preparation in Virtual Colonoscopy (VC) - Patient Experience
NCT00473980	PHASE4	COMPLETED	Preoperative Non-steroidal Anti-inflammatory Drugs(NSAID) to Colorectal Cancer Patients
NCT00488904	PHASE4	COMPLETED	Omega-3 Fatty Acids and Postoperative Complications After Colorectal Surgery
NCT00496678	PHASE4	COMPLETED	Trial of Patient Navigation-Activation
NCT00502671	PHASE4	COMPLETED	A Study of Xeloda (Capecitabine) as Adjuvant Monotherapy in Patients With Colon Cancer.
NCT00559676	PHASE4	COMPLETED	Study of Biomarkers in Patients Undergoing Chemotherapy for Metastatic Colorectal Cancer
NCT00577031	PHASE4	COMPLETED	OBELIX Study: A Study of Avastin (Bevacizumab) in Combination With XELOX in Patients With Metastatic Cancer of the Colon or Rectum.
NCT00626054	PHASE4	COMPLETED	Comparison of Two Methods of Administration of a PEG Solution
NCT00812864	PHASE4	COMPLETED	Pharmacokinetic Study of Capecitabine in Elderly Cancer Patient (≥ 75 Years)
NCT00868569	PHASE4	UNKNOWN	Transhepatic Arterial Chemotherapy (TAC) Versus Transcatheter Arterial Chemoembolization (TACE) Plus Folfox4 as the Treatment of Unresectable Liver Metastasis of Colorectal Cancer
NCT00868816	PHASE4	COMPLETED	Oxaliplatine Based Adjuvant Chemotherapy for Stage II/III Colorectal Cancer: 8 Cycles Versus 12 Cycles
NCT00874406	PHASE4	UNKNOWN	Preoperative Transhepatic Arterial Chemotherapy (TAC) in the Treatment of Liver Metastasis of Resectable Colorectal Cancer
NCT00928928	PHASE4	COMPLETED	Oxidative Stress Markers in Open and Laparoscopic Colectomy for Cancer
NCT00942461	PHASE4	COMPLETED	Inflammatory Response in Laparoscopic and Open Colectomy
NCT01023633	PHASE4	UNKNOWN	OPTIMOX1 in Chinese mCRC Patients
NCT01271582	PHASE4	UNKNOWN	Investigation of Association Between UGT1A1 Polymorphisms and Irinotecan Toxicity in Korean Patients
NCT01315990	PHASE4	UNKNOWN	FOLFIRI in Combination With Cetuximab in the First-line Treatment of Metastatic Colorectal Cancer Including a Regular Dermal Prophylaxis to Prevent Acneiforme Follicular Exanthema
NCT01493713	PHASE4	COMPLETED	Correlation Between RECIST, Morphologic Response by CT- Histopathologic Response in Hepatic Metastasis Secondary to Colorectal Cancer
NCT01609660	PHASE4	COMPLETED	Impact of Probiotics on the Intestinal Microbiota
NCT01641458	PHASE4	COMPLETED	Pharmacology-driven Dosing of Fluoropyrimidines in Cancer Patients
NCT01689792	PHASE4	COMPLETED	A Multi-centre Study Comparing the Polyp Detection Rate of Two Different Types of Bowel Preparation: a 2-litre Solution (MOVIPREP®) Versus a Hyperosmotic and Stimulant Combined Low Volume Bowel Preparation (Sodium Picosulfate and Magnesium Citrate)
NCT01695772	PHASE4	COMPLETED	A Study of Bevacizumab Plus 5-Flurouracil (5-FU) Based Doublet Chemotherapy as Neoadjuvant Therapy for Participants With Previously Untreated Unresectable Liver-Only Metastases From Colorectal Cancer
NCT01695863	PHASE4	COMPLETED	Efficacy and Patient Satisfaction of Miralax and Gatorade Versus Movi Prep
NCT01706822	PHASE4	TERMINATED	Radial Reload Laparoscopic LAR Case Series
NCT01740947	PHASE4	TERMINATED	Does Administration of Antibiotics in Patients Undergoing Surgery for Colorectal Cancer Result in Less Complications and Better Prognosis?
NCT01831310	PHASE4	COMPLETED	Nutrition for Colorectal Cancer Patients and Neutrophil Functions
NCT01841294	PHASE4	UNKNOWN	NK Activity Modulation Induced by Intravenous Lidocaine During Colorectal Laparoscopic Surgery
NCT01959061	PHASE4	UNKNOWN	Efficacy and Safety of Raltitrexed-based Transarterial Chemoembolisation(TACE)for Colorectal Cancer Liver Metastases
NCT02032953	PHASE4	UNKNOWN	Enhancing the Anabolic Effect of Perioperative Nutrition With Insulin While Maintaining Normoglycemia
NCT02567331	PHASE4	COMPLETED	A Study of Capecitabine (Xeloda) in Patients With Metastatic Colorectal Cancer