SGK1
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Summary
SGK1 (serum/glucocorticoid regulated kinase 1, HGNC:10810) is a protein-coding gene on chromosome 6q23.2, encoding Serine/threonine-protein kinase Sgk1 (O00141). Serine/threonine-protein kinase which is involved in the regulation of a wide variety of ion channels, membrane transporters, cellular enzymes, transcription factors, neuronal excitability, cell growth, proliferation, survival, migration and apoptosis. In precision oncology, SGK1 Overexpression is associated with resistance to Alpelisib in Breast Cancer (CIViC Level B); 1 further curated variant–drug associations are listed below.
This gene encodes a serine/threonine protein kinase that plays an important role in cellular stress response. This kinase activates certain potassium, sodium, and chloride channels, suggesting an involvement in the regulation of processes such as cell survival, neuronal excitability, and renal sodium excretion. High levels of expression of this gene may contribute to conditions such as hypertension and diabetic nephropathy. Several alternatively spliced transcript variants encoding different isoforms have been noted for this gene.
Source: NCBI Gene 6446 — RefSeq curated summary.
At a glance
- GWAS associations: 17
- Clinical variants (ClinVar): 81 total — 1 likely-pathogenic
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- Precision-oncology evidence (CIViC): 2 curated variant–drug associations
- Cancer driver (intOGen): activating (oncogene-like) across 4 cancer types
- MANE Select transcript:
NM_001143676
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:10810 |
| Approved symbol | SGK1 |
| Name | serum/glucocorticoid regulated kinase 1 |
| Location | 6q23.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000118515 |
| Ensembl biotype | protein_coding |
| OMIM | 602958 |
| Entrez | 6446 |
Gene structure
Transcript identifiers
Ensembl transcripts: 31 — 15 retained_intron, 11 protein_coding, 5 protein_coding_CDS_not_defined
ENST00000237305, ENST00000367855, ENST00000367857, ENST00000367858, ENST00000413996, ENST00000460769, ENST00000461976, ENST00000472859, ENST00000473704, ENST00000474427, ENST00000475719, ENST00000475882, ENST00000477460, ENST00000484353, ENST00000485771, ENST00000489458, ENST00000490149, ENST00000524387, ENST00000524764, ENST00000524929, ENST00000525700, ENST00000525877, ENST00000528577, ENST00000530421, ENST00000531575, ENST00000531782, ENST00000532021, ENST00000532856, ENST00000533224, ENST00000534658, ENST00000944482
RefSeq mRNA: 5 — MANE Select: NM_001143676
NM_001143676, NM_001143677, NM_001143678, NM_001291995, NM_005627
CCDS: CCDS47476, CCDS47477, CCDS47478, CCDS5170, CCDS78184
Canonical transcript exons
ENST00000367858 — 14 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001445793 | 134317392 | 134318112 |
| ENSE00003459946 | 134171637 | 134171732 |
| ENSE00003470842 | 134171023 | 134171178 |
| ENSE00003538253 | 134170826 | 134170915 |
| ENSE00003538880 | 134174511 | 134174586 |
| ENSE00003539710 | 134207356 | 134207431 |
| ENSE00003554684 | 134169256 | 134170435 |
| ENSE00003572454 | 134173274 | 134173357 |
| ENSE00003580144 | 134173023 | 134173154 |
| ENSE00003595366 | 134172662 | 134172774 |
| ENSE00003631036 | 134172193 | 134172316 |
| ENSE00003632299 | 134173462 | 134173566 |
| ENSE00003656301 | 134174005 | 134174080 |
| ENSE00003685714 | 134261933 | 134262148 |
Expression profiles
Bgee: expression breadth ubiquitous, 299 present calls, max score 99.60.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 143.7802 / max 3666.2799, expressed in 1809 samples.
FANTOM5 promoters (31 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 75647 | 123.7557 | 1802 |
| 75651 | 6.8093 | 653 |
| 75650 | 5.3452 | 1341 |
| 75649 | 1.1726 | 551 |
| 75681 | 1.1179 | 189 |
| 75678 | 0.6272 | 130 |
| 75682 | 0.5203 | 114 |
| 75680 | 0.5100 | 120 |
| 75652 | 0.4945 | 156 |
| 75659 | 0.4196 | 96 |
Top tissues by expression
302 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| palpebral conjunctiva | UBERON:0001812 | 99.60 | gold quality |
| eye | UBERON:0000970 | 99.44 | gold quality |
| right lung | UBERON:0002167 | 99.39 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 99.39 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 99.27 | gold quality |
| gingival epithelium | UBERON:0001949 | 99.20 | gold quality |
| parietal pleura | UBERON:0002400 | 99.20 | gold quality |
| cervix epithelium | UBERON:0004801 | 99.19 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 99.17 | gold quality |
| gingiva | UBERON:0001828 | 99.14 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 99.14 | gold quality |
| lower lobe of lung | UBERON:0008949 | 99.08 | gold quality |
| gall bladder | UBERON:0002110 | 98.94 | gold quality |
| pleura | UBERON:0000977 | 98.88 | gold quality |
| pigmented layer of retina | UBERON:0001782 | 98.88 | gold quality |
| retina | UBERON:0000966 | 98.86 | gold quality |
| olfactory bulb | UBERON:0002264 | 98.83 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 98.82 | gold quality |
| renal glomerulus | UBERON:0000074 | 98.78 | gold quality |
| upper leg skin | UBERON:0004262 | 98.70 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 98.68 | gold quality |
| nephron tubule | UBERON:0001231 | 98.63 | gold quality |
| left ovary | UBERON:0002119 | 98.59 | gold quality |
| medial globus pallidus | UBERON:0002477 | 98.57 | gold quality |
| pericardium | UBERON:0002407 | 98.56 | gold quality |
| kidney epithelium | UBERON:0004819 | 98.52 | gold quality |
| squamous epithelium | UBERON:0006914 | 98.51 | gold quality |
| parotid gland | UBERON:0001831 | 98.44 | gold quality |
| nasal cavity mucosa | UBERON:0001826 | 98.40 | gold quality |
| globus pallidus | UBERON:0001875 | 98.38 | gold quality |
Single-cell (SCXA)
Detected in 16 experiment(s), a significant marker in 15.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-10137 | yes | 1980.85 |
| E-HCAD-35 | yes | 85.06 |
| E-MTAB-6701 | yes | 75.80 |
| E-GEOD-125970 | yes | 67.10 |
| E-MTAB-10553 | yes | 45.80 |
| E-MTAB-6678 | yes | 42.46 |
| E-MTAB-10287 | yes | 37.62 |
| E-GEOD-84465 | yes | 37.49 |
| E-CURD-46 | yes | 33.96 |
| E-MTAB-9467 | yes | 27.98 |
| E-HCAD-9 | yes | 18.40 |
| E-HCAD-1 | yes | 17.43 |
| E-GEOD-135922 | yes | 7.24 |
| E-GEOD-130148 | yes | 6.28 |
| E-MTAB-8530 | no | 765.94 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): APC, AR, CTNNB1, EGR1, GATA2, GLI1, IRF6, MECP2, MYC, NFAT5, NFKB, NR3C1, NR3C2, OVOL1, PGR, POLR2A, PPARG, RELA, SP1, SP3, TCF7L2, TP53, TSC22D3
miRNA regulators (miRDB)
150 targeting SGK1, 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-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-29A-3P | 100.00 | 73.11 | 1835 |
| HSA-MIR-29B-3P | 100.00 | 73.18 | 1833 |
| HSA-MIR-29C-3P | 100.00 | 73.15 | 1833 |
| HSA-MIR-4668-3P | 100.00 | 68.74 | 2635 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| 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-4747-5P | 100.00 | 67.90 | 2681 |
| HSA-MIR-5196-5P | 100.00 | 67.98 | 2761 |
| HSA-MIR-6130 | 100.00 | 66.69 | 2012 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-4789-3P | 99.99 | 70.75 | 2484 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-6077 | 99.99 | 68.04 | 2299 |
| HSA-MIR-19A-3P | 99.98 | 75.33 | 2762 |
| HSA-MIR-19B-3P | 99.98 | 75.44 | 2754 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-32-5P | 99.98 | 75.21 | 1964 |
| HSA-MIR-92A-3P | 99.98 | 75.21 | 1960 |
| HSA-MIR-92B-3P | 99.98 | 75.25 | 1955 |
| HSA-MIR-25-3P | 99.98 | 74.60 | 1817 |
| HSA-MIR-363-3P | 99.98 | 74.72 | 1821 |
| HSA-MIR-367-3P | 99.98 | 74.83 | 1819 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
Literature-anchored findings (GeneRIF, showing 40)
- Excessive transcription of the human serum and glucocorticoid dependent kinase hSGK1 in lung fibrosis (PMID:12077559)
- single nucleotide polymorphisms of SGK linked to variations in blood pressure (PMID:12215463)
- Glucocorticoidss stimulate sgk1 expression in human epithelial cells via activation of a GRE in the 5’-flanking region of sgk1. (PMID:12376324)
- 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)
- Sgk is a positive regulator of sodium transport. (PMID:12417559)
- Glomerulonephritis leads to glomerular and in some cases to epithelial up-regulation of hSGK1 transcription. (PMID:12435876)
- NHERF2 and SGK1 interact to enhance ROMK1 activity by enhancing abundance of channel protein in cell membrane, allowing integration of genomic regulation and activation of SGK1 and NHERF2 in control of ROMK1 activity and renal K(+) excretion. (PMID:12444200)
- The stimulating effect of SGK1 on the Xenopus oocyte Na(+)/K(+)-ATPase is mimicked by the isoforms SGK2 and SGK3. (PMID:12590200)
- 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)
- SGK-1 phosphorylation of Kir1.1 drives expression on the plasmalemma. The results suggest a possible molecular mechanism for aldosterone-dependent regulation of the secretory potassium channel in the kidney. (PMID:12684516)
- SN1 is a target for the ubiquitin ligase Nedd4-2, which is inactivated by the serum and glucocorticoid inducible kinase SGK1, its isoform SGK3, and protein kinase B. (PMID:12788082)
- up-regulation of SGK1 enhances cell surface epithelial sodium channel expression in collecting duct cells. (PMID:12923071)
- NHERF2, ROMK1, and SGK1 have roles in regulating protein abundance in the plasma membrane and K(+) current (PMID:14623317)
- SGK levels are increased in brains of Huntington’s disease patients; SGK phosphorylates huntingtin at serine 421, protecting striatal neurons against polyQ-huntingtin-induced toxicity. (PMID:14725621)
- SGK1 stimulates the NaPi IIb, at least in part, by phosphorylating and thereby inhibiting Nedd4-2 binding to its target. (PMID:15044175)
- Na+-coupled glucose transporter 1 (SGLT1) was regulated by neuronal cell expressed developmentally downregulated 4-2 (Nedd4-2) and serum- and glucocorticoid-inducible kinase 1 (SGK1) (PMID:15166308)
- cAMP-stimulated Na+ transport in H441 distal lung epithelial cells does not affect levels of this enzyme. (PMID:15208094)
- These findings argue against important role of coding regions of Sgk1 in blood pressure regulation and hypertension and in the hypertension-related progression of renal diseases. (PMID:15304560)
- cAMP regulates ENaC in part by phosphorylation and inhibition of Nedd4-2. Moreover, Nedd4-2 is a central convergence point for kinase regulation of Na(+) transport. (PMID:15328345)
- Sgk1 may modulate insulin action on the cotranslational glycosylation of glycoproteins (PMID:15342340)
- results identify NDRG1 and NDRG2 as physiological substrates for SGK1, and demonstrate that phosphorylation of NDRG1 by SGK1 primes it for phosphorylation by GSK3 (PMID:15461589)
- ClC-Ka/barttin channels are regulated by SGK1 and SGK3, which may thus participate in the regulation of transport in kidney and inner ear. (PMID:15496163)
- Nedd4-2 phosphorylation induces SGK ubiquitination and degradation (PMID:15576372)
- Co-expression of SGK1, but not of SGK2 or SGK3, increased Kv 4.3/KChIP2b channel currents. (PMID:15578212)
- demonstration of the significance of SGK1 and NHERF2 as TRPV5 modulators which are likely to participate in the regulation of calcium homeostasis by 1,25(OH)2D3 (PMID:15665527)
- SGK acts as an oncogene in breast cancer cells through activation of the IKK-NF-kappaB pathway, thereby preventing apoptosis. (PMID:15695387)
- SGK1 activation has a role in oncofetal fibronectin expression (PMID:15721303)
- In conclusion, the kinases SGK1 and SGK3 increase EAAT5 activity by increasing cell surface abundance of the carrier. (PMID:15737648)
- SGK1 and SGK3 increase SLC6A8 activity by increasing the maximal transport rate of the carrier. Deranged SGK1 and/or SGK3 dependent regulation of SLC6A8 may affect energy storage particularly in skeletal muscle, heart, and neurons (PMID:16036218)
- The effects of high glucose on proximal tubular cells proliferation, reduced apoptosis and increased NHE3 mRNA levels are mediated by EGFR-dependent up-regulation of SGK-1 (PMID:16105029)
- key role for sgk1 in the molecular pathway of cell death, in which sgk1 seems to exert a protective role. (PMID:16125969)
- SGK-1 risk carriers are at increased risk of hypertension and are more sensitive to the blood pressure elevating effects associated with hyperinsulinemia (PMID:16221215)
- SGK1 is upregulated in diabetic nephropathy and actively participates in the stimulation of matrix protein deposition in this common deleterious complication of diabetic hyperglycemia. (PMID:16301823)
- SGK1 regulates current amplitudes and kinetic properties of KCNQ4 channel activity, an effect sensitive to mutations in the SGK1 consensus sequence of the channel. (PMID:16301825)
- SGK1 regulates GLUT1 and may contribute to or account for the PI3 kinase-dependent but PKB-independent stimulation of GLUT1 by insulin. (PMID:16443776)
- constitutive ubiquitin-mediated degradation of SGK-1 is an important mechanism regulating its biological activity (PMID:16817852)
- SGK1 is targeted to the endoplasmic reticulum-associated ubiquitin-conjugation machinery by an amphipathic helix (PMID:16847254)
- Acute effect of glucocorticoids on NHE3 is mediated by a glucocorticoid receptor dependent mechanism that activates SGK1 in a nongenomic manner. (PMID:16971495)
- Incubation with glucose, the Ca2+-ionophore ionomycin and the cytokine TGF-beta1 were all found to evoke significant and time-dependent increases in both SGK1 and alphaENaC protein expression. (PMID:17170520)
- Our data do not support that SGK1 gene variations are disease-causing factors in genetically unexplained pseudohypoaldosteronism type 1. (PMID:17317952)
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Sgk1 | ENSMUSG00000019970 |
| rattus_norvegicus | Sgk1 | ENSRNOG00000011815 |
| drosophila_melanogaster | CG32944 | FBGN0052944 |
| drosophila_melanogaster | dop | FBGN0267390 |
| caenorhabditis_elegans | WBGENE00002192 | |
| caenorhabditis_elegans | wts-1 | WBGENE00007047 |
| caenorhabditis_elegans | WBGENE00010838 | |
| caenorhabditis_elegans | WBGENE00011992 |
Paralogs (13): MAST4 (ENSG00000069020), MAST2 (ENSG00000086015), MAST3 (ENSG00000099308), SGK2 (ENSG00000101049), SGK3 (ENSG00000104205), DMPK (ENSG00000104936), MAST1 (ENSG00000105613), MASTL (ENSG00000120539), LATS1 (ENSG00000131023), LATS2 (ENSG00000150457), STK32B (ENSG00000152953), STK32C (ENSG00000165752), STK32A (ENSG00000169302)
Protein
Protein identifiers
Serine/threonine-protein kinase Sgk1 — O00141 (reviewed: O00141)
Alternative names: Serum/glucocorticoid-regulated kinase 1
All UniProt accessions (6): E9PJN2, E9PP33, E9PR89, O00141, H0YCJ3, Q7Z3I4
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, cellular enzymes, transcription factors, neuronal excitability, cell growth, proliferation, survival, migration and apoptosis. Plays an important role in cellular stress response. Contributes to regulation of renal Na(+) retention, renal K(+) elimination, salt appetite, gastric acid secretion, intestinal Na(+)/H(+) exchange and nutrient transport, insulin-dependent salt sensitivity of blood pressure, salt sensitivity of peripheral glucose uptake, cardiac repolarization and memory consolidation. Up-regulates Na(+) channels: SCNN1A/ENAC, SCN5A and ASIC1/ACCN2, K(+) channels: KCNJ1/ROMK1, KCNA1-5, KCNQ1-5 and KCNE1, epithelial Ca(2+) channels: TRPV5 and TRPV6, chloride channels: BSND, CLCN2 and CFTR, glutamate transporters: SLC1A3/EAAT1, SLC1A2 /EAAT2, SLC1A1/EAAT3, SLC1A6/EAAT4 and SLC1A7/EAAT5, amino acid transporters: SLC1A5/ASCT2, SLC38A1/SN1 and SLC6A19, creatine transporter: SLC6A8, Na(+)/dicarboxylate cotransporter: SLC13A2/NADC1, Na(+)-dependent phosphate cotransporter: SLC34A2/NAPI-2B, glutamate receptor: GRIK2/GLUR6. Up-regulates carriers: SLC9A3/NHE3, SLC12A1/NKCC2, SLC12A3/NCC, SLC5A3/SMIT, SLC2A1/GLUT1, SLC5A1/SGLT1 and SLC15A2/PEPT2. Regulates enzymes: GSK3A/B, PMM2 and Na(+)/K(+) ATPase, and transcription factors: CTNNB1 and nuclear factor NF-kappa-B. Stimulates sodium transport into epithelial cells by enhancing the stability and expression of SCNN1A/ENAC. This is achieved by phosphorylating the NEDD4L ubiquitin E3 ligase, promoting its interaction with 14-3-3 proteins, thereby preventing it from binding to SCNN1A/ENAC and targeting it for degradation. Regulates store-operated Ca(+2) entry (SOCE) by stimulating ORAI1 and STIM1. Regulates KCNJ1/ROMK1 directly via its phosphorylation or indirectly via increased interaction with SLC9A3R2/NHERF2. Phosphorylates MDM2 and activates MDM2-dependent ubiquitination of p53/TP53. Phosphorylates MAPT/TAU and mediates microtubule depolymerization and neurite formation in hippocampal neurons. Phosphorylates SLC2A4/GLUT4 and up-regulates its activity. Phosphorylates APBB1/FE65 and promotes its localization to the nucleus. Phosphorylates MAPK1/ERK2 and activates it by enhancing its interaction with MAP2K1/MEK1 and MAP2K2/MEK2. Phosphorylates FBXW7 and plays an inhibitory role in the NOTCH1 signaling. Phosphorylates FOXO1 resulting in its relocalization from the nucleus to the cytoplasm. Phosphorylates FOXO3, promoting its exit from the nucleus and interference with FOXO3-dependent transcription. Phosphorylates BRAF and MAP3K3/MEKK3 and inhibits their activity. Phosphorylates SLC9A3/NHE3 in response to dexamethasone, resulting in its activation and increased localization at the cell membrane. Phosphorylates CREB1. Necessary for vascular remodeling during angiogenesis. Sustained high levels and activity may contribute to conditions such as hypertension and diabetic nephropathy. Isoform 2 exhibited a greater effect on cell plasma membrane expression of SCNN1A/ENAC and Na(+) transport than isoform 1.
Subunit / interactions. Homodimer; disulfide-linked. Forms a trimeric complex with FBXW7 and NOTCH1. Interacts with MAPK3/ERK1, MAPK1/ERK2, MAP2K1/MEK1, MAP2K2/MEK2, NEDD4, NEDD4L, MAPT/TAU, MAPK7, CREB1, SLC9A3R2/NHERF2 and KCNJ1/ROMK1. Associates with the mammalian target of rapamycin complex 2 (mTORC2) via an interaction with MAPKAP1/SIN1.
Subcellular location. Cytoplasm. Nucleus. Endoplasmic reticulum membrane. Cell membrane. Mitochondrion Cell membrane.
Tissue specificity. Expressed in most tissues with highest levels in the pancreas, followed by placenta, kidney and lung. Isoform 2 is strongly expressed in brain and pancreas, weaker in heart, placenta, lung, liver and skeletal muscle.
Post-translational modifications. Regulated by phosphorylation. Activated by phosphorylation on Ser-422 by mTORC2, transforming it into a substrate for PDPK1 which phosphorylates it on Thr-256. Phosphorylation on Ser-397 and Ser-401 are also essential for its activity. Phosphorylation on Ser-78 by MAPK7 is required for growth factor-induced cell cycle progression. Ubiquitinated by NEDD4L; which promotes proteasomal degradation. Ubiquitinated by SYVN1 at the endoplasmic reticulum; which promotes rapid proteasomal degradation and maintains a high turnover rate in resting cells. Isoform 2 shows enhanced stability.
Activity regulation. Two specific sites, one in the kinase domain (Thr-256) and the other in the C-terminal regulatory region (Ser-422), need to be phosphorylated for its full activation. Phosphorylation at Ser-397 and Ser-401 are also essential for its activity. Activated by WNK1, WNK2, WNK3 and WNK4; which promote phosphorylation by mTORC2.
Domain organisation. Isoform 2 subcellular localization at the cell membrane and resistance to proteasomal degradation is mediated by the sequences within the first 120 amino acids.
Induction. Induced by a very large spectrum of stimuli distinct from glucocorticoids and serum. These include aldosterone, cell shrinkage, cell swelling, TGF-beta, ischemic injury of the brain, neuronal excitotoxicity memory consolidation, chronic viral hepatitis, DNA-damaging agents, vitamin D3 psychophysiological stress, iron, glucose, EDN1, CSF2, fibroblast growth factor, platelet-derived growth factor, phorbolesters, follicle-stimulating hormone, sorbitol, heat shock, oxidative stress, UV irradiation, and p53/TP53. Many of these stimuli are highly cell-specific, as is the case, for example for aldosterone, which has been found to stimulate its expression only in cells derived from aldosterone-responsive epithelia. Isoform 2 is not induced by glucocorticoids but by excessive extracellular glucose and by TGFB1, in cultured cells.
Miscellaneous. Produced by alternative promoter usage. Produced by alternative promoter usage. Produced by alternative splicing of isoform 1. Produced by alternative promoter usage.
Similarity. Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family.
Isoforms (5)
| UniProt ID | Names | Canonical? |
|---|---|---|
| O00141-1 | 1 | yes |
| O00141-2 | 2, Sgk1.1, Sgk1_v2 | |
| O00141-3 | 3, Sgk1.2 | |
| O00141-4 | 4 | |
| O00141-5 | 5 |
RefSeq proteins (5): NP_001137148, NP_001137149, NP_001137150, NP_001278924, NP_005618 (=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
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 (64 total): helix 14, strand 10, modified residue 7, mutagenesis site 7, sequence conflict 6, splice variant 4, domain 2, disulfide bond 2, sequence variant 2, region of interest 2, turn 2, binding site 2, chain 1, short sequence motif 1, compositionally biased region 1, active site 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2R5T | X-RAY DIFFRACTION | 1.9 |
| 7PUE | X-RAY DIFFRACTION | 2.51 |
| 3HDM | X-RAY DIFFRACTION | 2.6 |
| 3HDN | X-RAY DIFFRACTION | 3.1 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O00141-F1 | 80.55 | 0.57 |
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): 222 (proton acceptor)
Ligand- & substrate-binding residues (2): 104–112; 127
Post-translational modifications (7): 74, 78, 256, 369, 397, 401, 422
Disulfide bonds (2): 193, 258
Mutagenesis-validated functional residues (7):
| Position | Phenotype |
|---|---|
| 127 | abolishes enzymatic activity. |
| 256 | low activity. |
| 298 | abolishes interaction with nedd4 and nedd4l. |
| 422 | low activity. |
| 422 | 10-fold activation. |
Function
Pathways and Gene Ontology
Reactome pathways
19 pathways
| ID | Pathway |
|---|---|
| R-HSA-1257604 | PIP3 activates AKT signaling |
| R-HSA-2672351 | Stimuli-sensing channels |
| R-HSA-6804757 | Regulation of TP53 Degradation |
| R-HSA-8986944 | Transcriptional Regulation by MECP2 |
| R-HSA-9031628 | NGF-stimulated transcription |
| R-HSA-162582 | Signal Transduction |
| R-HSA-166520 | Signaling by NTRKs |
| R-HSA-187037 | Signaling by NTRK1 (TRKA) |
| R-HSA-198725 | Nuclear Events (kinase and transcription factor activation) |
| R-HSA-212436 | Generic Transcription Pathway |
| R-HSA-3700989 | Transcriptional Regulation by TP53 |
| R-HSA-382551 | Transport of small molecules |
| R-HSA-5633007 | Regulation of TP53 Activity |
| R-HSA-6806003 | Regulation of TP53 Expression and Degradation |
| R-HSA-73857 | RNA Polymerase II Transcription |
| R-HSA-74160 | Gene expression (Transcription) |
| R-HSA-9006925 | Intracellular signaling by second messengers |
| R-HSA-9006934 | Signaling by Receptor Tyrosine Kinases |
| R-HSA-983712 | Ion channel transport |
MSigDB gene sets: 680 (showing top):
GSE45365_NK_CELL_VS_CD8A_DC_MCMV_INFECTION_UP, AHRARNT_01, GOBP_MEMORY, TGGTGCT_MIR29A_MIR29B_MIR29C, BEGUM_TARGETS_OF_PAX3_FOXO1_FUSION_UP, GOBP_DIGESTION, BROWNE_HCMV_INFECTION_6HR_DN, GOBP_ACID_SECRETION, IIZUKA_LIVER_CANCER_EARLY_RECURRENCE, GOBP_COGNITION, HNF3ALPHA_Q6, GRUETZMANN_PANCREATIC_CANCER_DN, GOBP_BEHAVIOR, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS
GO Biological Process (19): regulation of cell growth (GO:0001558), protein phosphorylation (GO:0006468), sodium ion transport (GO:0006814), apoptotic process (GO:0006915), DNA damage response (GO:0006974), long-term memory (GO:0007616), regulation of blood pressure (GO:0008217), positive regulation of transporter activity (GO:0032411), intracellular signal transduction (GO:0035556), regulation of cell population proliferation (GO:0042127), regulation of apoptotic process (GO:0042981), neuron projection morphogenesis (GO:0048812), regulation of catalytic activity (GO:0050790), obsolete regulation of DNA-binding transcription factor activity (GO:0051090), regulation of gastric acid secretion (GO:0060453), renal sodium ion absorption (GO:0070294), regulation of signal transduction by p53 class mediator (GO:1901796), cellular response to aldosterone (GO:1904045), regulation of cell migration (GO:0030334)
GO Molecular Function (14): protein serine/threonine kinase activity (GO:0004674), protein serine/threonine/tyrosine kinase activity (GO:0004712), calcium channel regulator activity (GO:0005246), ATP binding (GO:0005524), potassium channel regulator activity (GO:0015459), sodium channel regulator activity (GO:0017080), chloride channel regulator activity (GO:0017081), 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), phosphatidylinositol binding (GO:0035091)
GO Cellular Component (10): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), mitochondrion (GO:0005739), endoplasmic reticulum membrane (GO:0005789), cytosol (GO:0005829), plasma membrane (GO:0005886), nuclear speck (GO:0016607), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-14 pathways:
| Category | Pathways |
|---|---|
| Generic Transcription Pathway | 2 |
| Signal Transduction | 2 |
| Intracellular signaling by second messengers | 1 |
| Ion channel transport | 1 |
| Regulation of TP53 Expression and Degradation | 1 |
| Nuclear Events (kinase and transcription factor activation) | 1 |
| Signaling by Receptor Tyrosine Kinases | 1 |
| Signaling by NTRKs | 1 |
| Signaling by NTRK1 (TRKA) | 1 |
| RNA Polymerase II Transcription | 1 |
| Transcriptional Regulation by TP53 | 1 |
| Regulation of TP53 Activity | 1 |
| Gene expression (Transcription) | 1 |
| Transport of small molecules | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| ion channel regulator activity | 4 |
| cellular anatomical structure | 4 |
| protein kinase activity | 3 |
| intracellular membrane-bounded organelle | 3 |
| cytoplasm | 3 |
| intracellular anatomical structure | 2 |
| catalytic activity | 2 |
| cell growth | 1 |
| regulation of growth | 1 |
| regulation of cellular component organization | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| metal ion transport | 1 |
| programmed cell death | 1 |
| apoptotic signaling pathway | 1 |
| execution phase of apoptosis | 1 |
| cellular response to stress | 1 |
| memory | 1 |
| blood circulation | 1 |
| regulation of biological quality | 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 |
| apoptotic process | 1 |
| regulation of programmed cell death | 1 |
| neuron projection development | 1 |
| plasma membrane bounded cell projection morphogenesis | 1 |
| regulation of molecular function | 1 |
| gastric acid secretion | 1 |
| regulation of digestive system process | 1 |
| regulation of secretion | 1 |
| renal sodium ion transport | 1 |
| renal absorption | 1 |
| signal transduction by p53 class mediator | 1 |
| regulation of intracellular signal transduction | 1 |
| cellular response to mineralocorticoid stimulus | 1 |
| cellular response to alcohol | 1 |
Protein interactions and networks
STRING
3220 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| SGK1 | NEDD4L | Q96PU5 | 952 |
| SGK1 | TSC22D3 | Q99576 | 866 |
| SGK1 | MAPKAP1 | Q9BPZ7 | 851 |
| SGK1 | DEPTOR | Q8TB45 | 835 |
| SGK1 | FKBP5 | Q13451 | 826 |
| SGK1 | SCNN1B | P51168 | 802 |
| SGK1 | RICTOR | Q6R327 | 800 |
| SGK1 | FOXO3 | O43524 | 781 |
| SGK1 | SCNN1G | P51170 | 780 |
| SGK1 | KCNJ1 | P48048 | 770 |
| SGK1 | PRR5 | P85299 | 769 |
| SGK1 | MLST8 | Q9BVC4 | 746 |
| SGK1 | RPTOR | Q8N122 | 739 |
| SGK1 | MTOR | P42345 | 731 |
| SGK1 | SCNN1A | P37088 | 717 |
IntAct
83 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| TSC2 | SGK1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TSC2 | SGK1 | psi-mi:“MI:2364”(proximity) | 0.560 |
| SGK1 | MAL2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SGK1 | CETN3 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SGK1 | NDRG4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SGK1 | FKBP5 | psi-mi:“MI:0915”(physical association) | 0.560 |
| SGK1 | Wnk4 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.540 |
| Wnk4 | SGK1 | psi-mi:“MI:0915”(physical association) | 0.540 |
| SGK1 | RABAC1 | psi-mi:“MI:0915”(physical association) | 0.490 |
| RABAC1 | SGK1 | psi-mi:“MI:0915”(physical association) | 0.490 |
| CREB1 | SGK1 | psi-mi:“MI:0915”(physical association) | 0.490 |
| SGK1 | CREB1 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.490 |
| PDPK1 | SGK1 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.440 |
| SGK1 | GADD45G | psi-mi:“MI:0915”(physical association) | 0.440 |
| GADD45G | SGK1 | psi-mi:“MI:0403”(colocalization) | 0.440 |
| SGK1 | MAPT | psi-mi:“MI:0217”(phosphorylation reaction) | 0.440 |
| MTOR | SGK1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| SGK1 | ECH1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| HSP90AB1 | SGK1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| SGK1 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| SGK1 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| SGK1 | MAGEA1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| SGK1 | Rabac1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| SGK1 | Tmem109 | psi-mi:“MI:0915”(physical association) | 0.370 |
| SGK1 | TMEM184C | psi-mi:“MI:0915”(physical association) | 0.370 |
| SGK1 | psi-mi:“MI:0914”(association) | 0.350 | |
| SGK1 | HRAS | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (119): MAPT (Biochemical Activity), YWHAZ (Affinity Capture-Western), YWHAQ (Affinity Capture-Western), SGK1 (Affinity Capture-Western), SGK1 (Biochemical Activity), RPTOR (Affinity Capture-Western), MTOR (Affinity Capture-Western), AKT1S1 (Affinity Capture-Western), SGK1 (Affinity Capture-Western), CDKN1B (Biochemical Activity), SGK1 (Biochemical Activity), NDRG1 (Biochemical Activity), SGK1 (Biochemical Activity), NEDD4L (Biochemical Activity), ARL5B (Affinity Capture-MS)
ESM2 similar proteins: A0A509AKL0, A5K0N4, A8X6H1, A8X6H4, A8XNJ6, O00141, O61267, O64629, P05130, P05987, P09215, P20444, P21901, P23298, P24604, P24723, P28867, P42680, P54644, P62345, P81900, P90980, Q05655, Q0CIC7, Q13237, Q16974, Q25378, Q26619, Q2PJ68, Q4R633, Q54CY9, Q55GV3, Q5BKK4, Q5F3L1, Q5PU49, Q5Q0U5, Q61410, Q64595, Q64617, Q6GLY8
Diamond homologs: A1A4I4, A1Z7T0, A1Z9X0, A7MB74, A7MBL8, A8KBH6, A8WUG4, F1M7Y5, O00141, 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
SIGNOR signaling
71 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| SGK1 | “down-regulates activity” | MAP3K3 | phosphorylation |
| MAPK7 | up-regulates | SGK1 | phosphorylation |
| SGK1 | up-regulates | NEDD4L | phosphorylation |
| SGK1 | down-regulates | HTT | phosphorylation |
| SGK1 | up-regulates | NDRG2 | phosphorylation |
| SGK1 | down-regulates | NEDD4L | phosphorylation |
| SGK1 | down-regulates | MAPT | phosphorylation |
| SGK1 | down-regulates | NDRG1 | phosphorylation |
| SGK1 | up-regulates | FBXW7 | phosphorylation |
| MTOR | up-regulates | SGK1 | phosphorylation |
| SGK1 | down-regulates | CDKN1B | phosphorylation |
| SGK1 | “down-regulates activity” | CDKN1B | phosphorylation |
| SGK1 | up-regulates | NDRG1 | phosphorylation |
| mTORC2 | up-regulates | SGK1 | phosphorylation |
| SGK1 | “down-regulates activity” | FOXO3 | phosphorylation |
| PDPK1 | up-regulates | SGK1 | phosphorylation |
| SGK1 | “up-regulates activity” | NR3C1 | phosphorylation |
| SGK1 | down-regulates | GLI1 | binding |
| SGK1 | down-regulates | SMO | binding |
| SGK1 | “down-regulates activity” | NEDD4L | phosphorylation |
Disease & clinical
Cancer significance
From intOGen — cancer-driver classification: activating (oncogene-like) across 4 cancer types — DLBCLNOS, MLYM, NHL, PRCC.
Clinical variants and AI predictions
ClinVar
81 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 28 |
| Likely benign | 5 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 800349 | NM_001143676.3(SGK1):c.1379A>G (p.Asn460Ser) | Likely pathogenic |
SpliceAI
900 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 6:134170431:CCACT:C | acceptor_gain | 1.0000 |
| 6:134170432:CACT:C | acceptor_gain | 1.0000 |
| 6:134170432:CACTC:C | acceptor_gain | 1.0000 |
| 6:134170434:CT:C | acceptor_gain | 1.0000 |
| 6:134170435:TCTG:T | acceptor_loss | 1.0000 |
| 6:134170436:C:CC | acceptor_gain | 1.0000 |
| 6:134170436:C:T | acceptor_loss | 1.0000 |
| 6:134170437:T:A | acceptor_loss | 1.0000 |
| 6:134170438:G:C | acceptor_gain | 1.0000 |
| 6:134170442:C:CT | acceptor_gain | 1.0000 |
| 6:134170443:G:T | acceptor_gain | 1.0000 |
| 6:134170818:ATACT:A | donor_loss | 1.0000 |
| 6:134170820:ACTC:A | donor_loss | 1.0000 |
| 6:134170821:CTC:C | donor_loss | 1.0000 |
| 6:134170822:TCA:T | donor_loss | 1.0000 |
| 6:134170823:CA:C | donor_loss | 1.0000 |
| 6:134170824:A:AC | donor_gain | 1.0000 |
| 6:134170824:A:AT | donor_loss | 1.0000 |
| 6:134170825:C:A | donor_loss | 1.0000 |
| 6:134170825:C:CC | donor_gain | 1.0000 |
| 6:134170825:CCA:C | donor_gain | 1.0000 |
| 6:134170825:CCACA:C | donor_gain | 1.0000 |
| 6:134170912:CCAT:C | acceptor_gain | 1.0000 |
| 6:134170913:CAT:C | acceptor_gain | 1.0000 |
| 6:134170913:CATC:C | acceptor_gain | 1.0000 |
| 6:134170914:ATCTG:A | acceptor_loss | 1.0000 |
| 6:134170915:TC:T | acceptor_loss | 1.0000 |
| 6:134170916:C:CC | acceptor_gain | 1.0000 |
| 6:134170916:CTGTT:C | acceptor_loss | 1.0000 |
| 6:134170917:T:C | acceptor_loss | 1.0000 |
AlphaMissense
3509 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 6:134170301:A:C | F421L | 1.000 |
| 6:134170301:A:T | F421L | 1.000 |
| 6:134170302:A:G | F421S | 1.000 |
| 6:134170303:A:G | F421L | 1.000 |
| 6:134170310:G:C | F418L | 1.000 |
| 6:134170310:G:T | F418L | 1.000 |
| 6:134170311:A:G | F418S | 1.000 |
| 6:134170312:A:G | F418L | 1.000 |
| 6:134170397:A:C | F389L | 1.000 |
| 6:134170397:A:T | F389L | 1.000 |
| 6:134170398:A:G | F389S | 1.000 |
| 6:134170399:A:G | F389L | 1.000 |
| 6:134171066:A:G | L332P | 1.000 |
| 6:134171069:A:G | L331P | 1.000 |
| 6:134171146:C:A | M305I | 1.000 |
| 6:134171146:C:G | M305I | 1.000 |
| 6:134171146:C:T | M305I | 1.000 |
| 6:134171170:A:C | F297L | 1.000 |
| 6:134171170:A:T | F297L | 1.000 |
| 6:134171172:A:G | F297L | 1.000 |
| 6:134171172:A:T | F297I | 1.000 |
| 6:134171174:G:T | P296H | 1.000 |
| 6:134171650:A:C | M290R | 1.000 |
| 6:134171668:C:T | G284E | 1.000 |
| 6:134171669:C:G | G284R | 1.000 |
| 6:134171669:C:T | G284R | 1.000 |
| 6:134171673:G:C | C282W | 1.000 |
| 6:134171675:A:G | C282R | 1.000 |
| 6:134171676:C:A | W281C | 1.000 |
| 6:134171676:C:G | W281C | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000071493 (6:134263738 G>T), RS1000088374 (6:134301635 G>C,T), RS1000093736 (6:134307275 G>A), RS1000106332 (6:134219118 G>C), RS1000114897 (6:134215363 A>C,T), RS1000119177 (6:134214216 G>A,T), RS1000119535 (6:134227876 T>C), RS1000132917 (6:134174325 G>A,C), RS1000147595 (6:134307586 T>G), RS1000180293 (6:134314021 A>G), RS1000209038 (6:134264155 G>C), RS1000219694 (6:134194758 A>G), RS1000234069 (6:134314303 C>T), RS1000250736 (6:134194474 T>C), RS1000266092 (6:134221761 T>A)
Disease associations
OMIM: gene MIM:602958 | disease phenotypes: MIM:254500
GenCC curated gene-disease
Mondo (1): plasma cell myeloma (MONDO:0009693)
Orphanet (2): Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
17 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001538_30 | Immune reponse to smallpox (secreted IFN-alpha) | 4.000000e-07 |
| GCST002812_4 | Schizophrenia (inflammation and infection response interaction) | 8.000000e-06 |
| GCST003225_19 | Pelvic organ prolapse (moderate/severe) | 6.000000e-06 |
| GCST003225_5 | Pelvic organ prolapse (moderate/severe) | 4.000000e-06 |
| GCST003226_1 | Pelvic organ prolapse | 7.000000e-06 |
| GCST003226_7 | Pelvic organ prolapse | 2.000000e-06 |
| GCST004581_3 | Body mass index (smoking years interaction) | 2.000000e-06 |
| GCST006434_4 | Systolic blood pressure x alcohol consumption interaction (2df test) | 2.000000e-09 |
| GCST006988_119 | Blond vs. brown/black hair color | 2.000000e-08 |
| GCST010002_335 | Refractive error | 6.000000e-10 |
| GCST010796_2268 | Electrocardiogram morphology (amplitude at temporal datapoints) | 5.000000e-08 |
| GCST010796_2269 | Electrocardiogram morphology (amplitude at temporal datapoints) | 2.000000e-08 |
| GCST010796_2270 | Electrocardiogram morphology (amplitude at temporal datapoints) | 2.000000e-08 |
| GCST010796_2271 | Electrocardiogram morphology (amplitude at temporal datapoints) | 8.000000e-09 |
| GCST010796_2272 | Electrocardiogram morphology (amplitude at temporal datapoints) | 2.000000e-08 |
| GCST010796_2273 | Electrocardiogram morphology (amplitude at temporal datapoints) | 3.000000e-09 |
| GCST90000015_18 | Parkinson’s disease motor subtype (tremor to postural instability/gait difficulty score ratio) | 7.000000e-06 |
EFO canonical traits (9, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004645 | response to vaccine |
| EFO:0004873 | cytokine measurement |
| EFO:0007047 | Toxoplasma gondii seropositivity |
| EFO:0004340 | body mass index |
| EFO:0004329 | alcohol drinking |
| EFO:0006335 | systolic blood pressure |
| EFO:0003924 | hair color |
| EFO:0004327 | electrocardiography |
| EFO:0600011 | Parkinson’s disease symptom measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D009101 | Multiple Myeloma | C04.557.595.500; C14.907.454.460; C15.378.147.780.650; C15.378.463.515.460; C20.683.515.845; C20.683.780.650 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2343 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,624 (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 |
|---|---|---|---|
| CHEMBL3137336 | UPROSERTIB | 2 | 1,624 |
Clinical evidence (CIViC)
Drug × variant × indication: 2 predictive associations from 3 curated evidence items.
| Variant | Therapy | Indication | Effect | Level | CIViC |
|---|---|---|---|---|---|
| SGK1 Overexpression | Alpelisib | Breast Cancer | Resistance | CIViC B | EID1730 +1 |
| SGK1 Overexpression | SGK1-Inh + Alpelisib | Breast Cancer | Sensitivity/Response | CIViC D | EID1731 |
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 (5 total), top 5:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| compound 14n [PMID: 25589934] | Inhibition | 9.0 | pIC50 |
| Sanofi-14h | Inhibition | 8.0 | pIC50 |
| PO-322 | Inhibition | 7.27 | pIC50 |
| GSK650394 | Inhibition | 7.21 | pIC50 |
| EMD638683 | Inhibition | 5.52 | pIC50 |
Binding affinities (BindingDB)
571 measured of 661 human assays (661 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| N-[4-(3-amino-4-ethoxy-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-5-chloro-2,4-difluorobenzenesulfonamide | IC50 | 0.57 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 5-chloro-2-fluoro-N-[4-[4-(1-methylpiperidin-4-yl)oxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 0.59 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 5-chloro-N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-fluorobenzenesulfonamide | IC50 | 0.76 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[4-[[3-(aminomethyl)oxetan-3-yl]methoxy]-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]-2-chloro-5-methoxybenzenesulfonamide | IC50 | 0.85 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-5-chloro-2-fluorobenzenesulfonamide | IC50 | 1 nM | US-9221828: N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]sulfonamides as pharmaceuticals |
| 5-chloro-2-cyano-N-[4-[4-[(3-hydroxycyclohexyl)amino]-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.1 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-fluoro-5-methylbenzenesulfonamide | IC50 | 1.1 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-cyano-N-[4-[4-(3-fluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methylbenzenesulfonamide | IC50 | 1.1 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[6-[4-[(2,5-dichlorophenyl)sulfonylamino]phenyl]-1H-pyrazolo[3,4-d]pyrimidin-3-yl]cyclopropanecarboxamide | IC50 | 1.1 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-chloro-N-[4-(4-cyclopropyl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-5-methylbenzenesulfonamide | IC50 | 1.2 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-5-methyl-N-[4-(4-piperidin-3-yloxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | IC50 | 1.2 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-fluoro-5-methoxybenzenesulfonamide | IC50 | 1.3 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-cyano-N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methylbenzenesulfonamide | IC50 | 1.3 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 5-chloro-2-fluoro-N-[4-(3-methyl-4-piperidin-3-yloxy-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | IC50 | 1.3 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-cyano-N-[4-[4-(1-cyclopropylpiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[4,3-c]pyridin-6-yl]phenyl]-5-methylbenzenesulfonamide | IC50 | 1.3 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 5-chloro-2-fluoro-N-[4-[4-(3-hydroxypropylamino)-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.4 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-cyano-N-[4-[4-[(3-hydroxycyclohexyl)amino]-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methylbenzenesulfonamide | IC50 | 1.4 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-Chloro-N-[2-fluoro-4-(3-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-phenyl]-5-methoxy-benzenesulfonamide | IC50 | 1.4 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2,5-dichloro-N-[4-[4-(pyridin-4-ylmethylamino)-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(4-cyclopropyl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-2-fluoro-5-methoxybenzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-fluorobenzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-chloro-N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methoxybenzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2,5-difluoro-N-[4-[4-(3-fluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-amino-4-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-2-fluoro-5-methylbenzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-Amino-4-trifluoromethyl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-phenyl]-5-chloro-2-fluoro-benzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-amino-4-propoxy-1H-pyrazolo[4,3-c]pyridin-6-yl)phenyl]-5-chloro-2,4-difluorobenzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-N-[4-(4-methoxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl)phenyl]-5-methylbenzenesulfonamide | IC50 | 1.5 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[4-(azetidin-3-ylmethoxy)-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]-2,5-difluorobenzenesulfonamide | IC50 | 1.6 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-5-methyl-N-[4-(3-methyl-4-piperidin-3-yloxy-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | IC50 | 1.6 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-Amino-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-phenyl]-5-chloro-2,4-difluoro-benzenesulfonamide | IC50 | 1.6 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-Amino-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-phenyl]-5-chloro-2-cyano-benzenesulfonamide | IC50 | 1.6 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-amino-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-2-cyano-5-methylbenzenesulfonamide | IC50 | 1.6 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[6-[4-[(2,5-Dichlorophenyl)sulfonylamino]phenyl]-4-methyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl]tetrahydropyran-4-carboxamide | IC50 | 1.6 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-cyano-N-[4-[4-[(4-hydroxycyclohexyl)amino]-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methylbenzenesulfonamide | IC50 | 1.7 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-chloro-N-[4-[4-(4-hydroxycyclohexyl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methoxybenzenesulfonamide | IC50 | 1.7 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2,5-difluorobenzenesulfonamide | IC50 | 1.7 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-amino-1H-pyrazolo[4,3-c]pyridin-6-yl)phenyl]-2,5-dichlorobenzenesulfonamide | IC50 | 1.7 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-[3-amino-4-(trifluoromethyl)-1H-pyrazolo[4,3-c]pyridin-6-yl]phenyl]-2-cyano-5-methylbenzenesulfonamide | IC50 | 1.7 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| N-[4-(3-amino-4-ethoxy-1H-pyrazolo[4,3-c]pyridin-6-yl)phenyl]-2-fluoro-5-methoxybenzenesulfonamide | IC50 | 1.7 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-N-[4-[4-(3-fluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-N-[4-[4-[3-hydroxy-2-(hydroxymethyl)propoxy]-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methylbenzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2,5-dichloro-N-[2-fluoro-4-(3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 5-Chloro-2,4-difluoro-N-[4-(3-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-phenyl]-benzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-chloro-5-methoxy-N-[4-(4-methyl-1H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2,5-dichloro-N-[4-[3-methyl-4-(2,2,6,6-tetramethylpiperidin-4-yl)oxy-2H-pyrazolo[4,3-c]pyridin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-5-methoxy-N-[4-[3-methyl-4-(1,2,2,6,6-pentamethylpiperidin-4-yl)oxy-2H-pyrazolo[4,3-c]pyridin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.8 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2,3-dichloro-N-[4-(3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | IC50 | 1.9 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-N-[4-[4-(3-fluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methoxybenzenesulfonamide | IC50 | 1.9 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 2-fluoro-5-methyl-N-[4-[3-methyl-4-[(2-oxo-1H-pyridin-4-yl)oxy]-2H-pyrazolo[4,3-c]pyridin-6-yl]phenyl]benzenesulfonamide | IC50 | 1.9 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
| 5-chloro-2-cyano-N-[4-[4-(4-hydroxycyclohexyl)oxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | IC50 | 2 nM | US-9718825: N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals |
ChEMBL bioactivities
904 potent at pChembl≥5 of 915 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.24 | IC50 | 0.57 | nM | CHEMBL5863871 |
| 9.23 | IC50 | 0.59 | nM | CHEMBL5802087 |
| 9.12 | IC50 | 0.76 | nM | CHEMBL5085476 |
| 9.07 | IC50 | 0.85 | nM | CHEMBL5776800 |
| 9.00 | IC50 | 1 | nM | CHEMBL3092468 |
| 9.00 | IC50 | 1 | nM | CHEMBL3356029 |
| 9.00 | IC50 | 1 | nM | CHEMBL5093306 |
| 9.00 | IC50 | 1 | nM | CHEMBL5087657 |
| 9.00 | IC50 | 1 | nM | CHEMBL5075992 |
| 9.00 | IC50 | 1 | nM | CHEMBL5075362 |
| 9.00 | IC50 | 1 | nM | CHEMBL5074684 |
| 9.00 | IC50 | 1 | nM | CHEMBL5088069 |
| 9.00 | IC50 | 1 | nM | CHEMBL5087162 |
| 9.00 | IC50 | 1 | nM | CHEMBL5081869 |
| 9.00 | IC50 | 1 | nM | CHEMBL5083625 |
| 9.00 | IC50 | 1 | nM | CHEMBL5085476 |
| 9.00 | IC50 | 1 | nM | CHEMBL5070612 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5775294 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5966376 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5780093 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL5913005 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL5898456 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL5943271 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5988036 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5768922 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5081869 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL6065816 |
| 8.85 | IC50 | 1.4 | nM | CHEMBL5911107 |
| 8.85 | IC50 | 1.4 | nM | CHEMBL5765800 |
| 8.85 | IC50 | 1.4 | nM | CHEMBL5746702 |
| 8.83 | IC50 | 1.47 | nM | STAUROSPORINE |
| 8.82 | IC50 | 1.5 | nM | CHEMBL3355031 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL5785037 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL5958106 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL5982568 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL5837773 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL6003000 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL5789079 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL6056857 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL5838749 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5846227 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5994877 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5086929 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5082336 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5844362 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL6031107 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL5865409 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL5893172 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL5905959 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL5894177 |
PubChem BioAssay actives
324 with measured affinity, of 1494 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 |
|---|---|---|---|---|
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2,5-dichlorothiophene-3-sulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2-chlorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2,5-dichlorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2-fluoro-5-(trifluoromethyl)benzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2-fluorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2,5-difluorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2-chloro-5-methoxybenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-5-bromo-2-chlorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-5-chloro-2-fluorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0010 | uM |
| 5-chloro-N-[4-[4-(3,3-difluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-fluorobenzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 5-chloro-2-fluoro-N-[4-(3-methyl-4-piperidin-3-yloxy-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 5-chloro-2-fluoro-N-[4-[4-[3-hydroxy-2-(hydroxymethyl)propoxy]-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-[(3R)-pyrrolidin-3-yl]-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 5-chloro-2-fluoro-N-[4-(3-methyl-4-piperidin-4-yloxy-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 5-chloro-2-fluoro-N-[4-[4-(3-fluoropiperidin-4-yl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| N-(2-aminoethyl)-6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-(1H-1,2,4-triazol-5-ylmethyl)-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-(2-hydroxyethyl)-N-methyl-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-(1,3-oxazol-4-ylmethyl)-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-(1H-imidazol-2-ylmethyl)-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-(1-methylazetidin-3-yl)-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 5-chloro-2-fluoro-N-[4-[3-methyl-4-[(1-propan-2-ylazetidin-3-yl)methoxy]-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| N-[1-(cyclopropylmethyl)pyrrolidin-3-yl]-6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-[(1-ethylpyrrolidin-3-yl)methyl]-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-[1-(2-hydroxyethyl)pyrrolidin-3-yl]-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| 6-[4-[(2,3-dichlorophenyl)sulfonylamino]phenyl]-N-(1-methylpyrrolidin-3-yl)-1H-pyrazolo[5,4-b]pyridine-4-carboxamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| N-[4-[4-[[3-(aminomethyl)oxetan-3-yl]methoxy]-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-chloro-2-fluorobenzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-5-chloro-2-fluorobenzenesulfonamide | 1056407: Inhibition of recombinant human SGK-1 expressed in baculovirus expression system using (5(6)-carboxyfluorescein)-RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay | ic50 | 0.0010 | uM |
| 5-chloro-2-fluoro-N-[4-[4-(4-hydroxycyclohexyl)oxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0010 | uM |
| N-[4-[4-(3-aminopropoxy)-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]-2,5-dichlorobenzenesulfonamide | 1177119: Inhibition of SGK1 (unknown origin) assessed as substrate phosphorylation | ic50 | 0.0012 | uM |
| 2,5-dichloro-N-[4-(3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]benzenesulfonamide | 1177119: Inhibition of SGK1 (unknown origin) assessed as substrate phosphorylation | ic50 | 0.0012 | uM |
| 5-chloro-2-cyano-N-[4-[4-(4-hydroxycyclohexyl)oxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1177119: Inhibition of SGK1 (unknown origin) assessed as substrate phosphorylation | ic50 | 0.0015 | uM |
| 2-fluoro-N-[4-[4-(4-hydroxycyclohexyl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-5-methoxybenzenesulfonamide | 1177119: Inhibition of SGK1 (unknown origin) assessed as substrate phosphorylation | ic50 | 0.0015 | uM |
| 2-fluoro-N-[4-(4-methoxy-1H-pyrazolo[5,4-d]pyrimidin-6-yl)phenyl]-5-methylbenzenesulfonamide | 1177119: Inhibition of SGK1 (unknown origin) assessed as substrate phosphorylation | ic50 | 0.0015 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 2151341: Inhibition of SGK1 (unknown origin) in the presence of [33P]ATP by kinase hotspot assay | ic50 | 0.0015 | uM |
| N-[4-(3-amino-4-cyclopropyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl)phenyl]-2-cyano-5-methoxybenzenesulfonamide | 1177119: Inhibition of SGK1 (unknown origin) assessed as substrate phosphorylation | ic50 | 0.0015 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-2,3-dichlorobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0020 | uM |
| N-[4-(3-amino-1H-indazol-6-yl)phenyl]-5-chloro-2-cyanobenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0020 | uM |
| 5-chloro-2-fluoro-N-[4-[4-(4-hydroxycyclohexyl)oxy-3-methyl-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0020 | uM |
| 5-chloro-2-fluoro-N-[4-[3-methyl-4-(morpholin-2-ylmethoxy)-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0020 | uM |
| 5-chloro-2-fluoro-N-[4-[3-methyl-4-(1,2,2,6,6-pentamethylpiperidin-4-yl)oxy-2H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0020 | uM |
| 2,3-dichloro-N-[4-[4-(piperazine-1-carbonyl)-1H-pyrazolo[5,4-b]pyridin-6-yl]phenyl]benzenesulfonamide | 1821042: Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 10 uM ATP and measured after 60 mins by microfluidics assay | ic50 | 0.0020 | uM |
| N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-cyano-5-methoxybenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0020 | uM |
| N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2-fluoro-5-methoxybenzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0020 | uM |
| N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)-2-fluorophenyl]-5-chloro-2-fluorobenzenesulfonamide | 1056407: Inhibition of recombinant human SGK-1 expressed in baculovirus expression system using (5(6)-carboxyfluorescein)-RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay | ic50 | 0.0020 | uM |
| N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)-2-fluorophenyl]-2,5-dichlorobenzenesulfonamide | 1056407: Inhibition of recombinant human SGK-1 expressed in baculovirus expression system using (5(6)-carboxyfluorescein)-RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay | ic50 | 0.0020 | uM |
| 2,5-dichloro-N-[4-(3-methyl-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]benzenesulfonamide | 1177297: Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP | ic50 | 0.0020 | uM |
| 2-fluoro-5-methyl-N-[4-(3-methyl-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]benzenesulfonamide | 1056407: Inhibition of recombinant human SGK-1 expressed in baculovirus expression system using (5(6)-carboxyfluorescein)-RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay | ic50 | 0.0020 | uM |
| 2-chloro-5-methoxy-N-[4-(3-methyl-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]benzenesulfonamide | 1056407: Inhibition of recombinant human SGK-1 expressed in baculovirus expression system using (5(6)-carboxyfluorescein)-RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay | ic50 | 0.0020 | uM |
CTD chemical–gene interactions
164 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Estradiol | decreases expression, decreases reaction, affects reaction, increases expression, affects cotreatment | 11 |
| Benzo(a)pyrene | decreases expression, increases expression, affects methylation | 8 |
| Valproic Acid | affects cotreatment, increases expression, affects expression, decreases expression | 8 |
| Tetrachlorodibenzodioxin | affects cotreatment, decreases expression, increases expression | 6 |
| bisphenol A | decreases methylation, increases expression, decreases reaction, affects expression, affects cotreatment (+2 more) | 5 |
| sodium arsenite | affects cotreatment, decreases expression, increases abundance, increases expression | 5 |
| Fulvestrant | decreases expression, decreases reaction, increases expression, affects cotreatment, affects methylation | 5 |
| Cyclosporine | decreases expression | 4 |
| trichostatin A | increases expression, affects cotreatment | 3 |
| Irinotecan | increases expression | 3 |
| Formaldehyde | increases expression | 3 |
| Cadmium Chloride | decreases expression, increases expression, increases phosphorylation, decreases reaction, affects cotreatment | 3 |
| Raloxifene Hydrochloride | affects cotreatment, increases expression, decreases expression, affects expression | 3 |
| Particulate Matter | increases abundance, affects cotreatment, decreases expression | 3 |
| lead acetate | decreases expression, affects cotreatment | 2 |
| ochratoxin A | decreases expression | 2 |
| potassium chromate(VI) | affects cotreatment, increases expression, decreases expression | 2 |
| nickel sulfate | increases expression | 2 |
| mercuric bromide | increases expression, affects cotreatment | 2 |
| chromium hexavalent ion | affects expression, increases abundance, increases expression | 2 |
| Arsenic Trioxide | increases expression | 2 |
| Arsenic | increases abundance, affects expression, affects cotreatment, decreases expression | 2 |
| Atrazine | increases expression, affects reaction | 2 |
| Copper | affects binding, increases expression | 2 |
| Dexamethasone | increases expression, decreases reaction | 2 |
| Ethyl Methanesulfonate | decreases expression, increases expression | 2 |
| Mestranol | affects reaction, increases expression | 2 |
| Ouabain | decreases reaction, increases transport, decreases expression | 2 |
| Phenylmercuric Acetate | affects cotreatment, increases expression | 2 |
| Progesterone | affects reaction, increases expression, decreases reaction | 2 |
ChEMBL screening assays
538 unique, capped per target: 535 binding, 2 admet, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1003328 | Binding | Inhibition of SGK1 at 1 uM relative to control | Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. — J Med Chem |
| CHEMBL4407586 | ADMET | Inhibition of recombinant human GST-tagged SGK catalytic domain (60 to 431 residues) expressed in baculovirus expression system at 25 uM using FRET-labeled Ser/Thr 06 peptide as substrate measured after 1 hr by Z’-lyte assay relative to con | Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase. — J Med Chem |
| CHEMBL5464247 | Functional | SGK1 degradation assay | Data for DCP probe SGK3-PROTAC1 |
Cellosaurus cell lines
7 cell lines: 6 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D8A5 | Ubigene A-549 SGK1 KO | Cancer cell line | Male |
| CVCL_D8V2 | Ubigene HCT 116 SGK1 KO | Cancer cell line | Male |
| CVCL_D9RI | Ubigene HEK293 SGK1 KO | Transformed cell line | Female |
| CVCL_E1CE | Ubigene SU-DHL-4 SGK1 KO | Cancer cell line | Male |
| CVCL_TK84 | HAP1 SGK1 (-) 1 | Cancer cell line | Male |
| CVCL_TK85 | HAP1 SGK1 (-) 2 | Cancer cell line | Male |
| CVCL_TK86 | HAP1 SGK1 (-) 3 | Cancer cell line | Male |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00029224 | PHASE4 | COMPLETED | Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions |
| NCT00104104 | PHASE4 | COMPLETED | A Multiple Myeloma Trial in Patients With Bone Metastases |
| NCT00211211 | PHASE4 | COMPLETED | FREE Study - Fracture Reduction Evaluation |
| NCT00242528 | PHASE4 | WITHDRAWN | Open-label Study, to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Bone Lesions Secondary to Multiple Myeloma. |
| NCT00257114 | PHASE4 | COMPLETED | Evaluation of VELCADE Given as Retreatment to Multiple Myeloma Patients for Efficacy, Safety and Tolerability |
| NCT00352703 | PHASE4 | COMPLETED | PROMPT - Palifermin in Reduction of Oral Mucositis in PBSC Transplantation |
| NCT00361140 | PHASE4 | COMPLETED | Busulfan Safety/Efficacy as Conditioning Prior to Hematopoietic Cell Transplantation (HCT) |
| NCT00622505 | PHASE4 | COMPLETED | Zoledronic Acid Treatment (Every 4 or 12 Weeks) to Prevent Skeletal Complications in Advanced Multiple Myeloma Participants |
| NCT00652041 | PHASE4 | COMPLETED | Bortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma |
| NCT00733538 | PHASE4 | COMPLETED | Stage I Multiple Myeloma Treatment |
| NCT01087008 | PHASE4 | COMPLETED | Zoledronic Acid in Patients With Multiple Myeloma and Asymptomatic Biochemical Relapse |
| NCT01249690 | PHASE4 | UNKNOWN | Efficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma |
| NCT01410929 | PHASE4 | WITHDRAWN | Evaluation of Vertebral Compression Fracture Fixation With RF Kyphoplasty in Patients With Multiple Myeloma |
| NCT01731886 | PHASE4 | COMPLETED | Lenalidomide and Dexamethasone With/Without Stem Cell Transplant in Patients With Multiple Myeloma |
| NCT01868828 | PHASE4 | UNKNOWN | A Study of PAD Versus Velcade, Cyclophosphamide and Dexamethasone (VCD) Treatment in Subjects With Multiple Myeloma |
| NCT02268890 | PHASE4 | COMPLETED | A Pharmacokinetic Study of Bortezomib in Taiwanese Participants With Multiple Myeloma |
| NCT02286830 | PHASE4 | COMPLETED | Prolonged Protection From Bone Disease in Multiple Myeloma |
| NCT02559154 | PHASE4 | UNKNOWN | Modified Bortezomib-based Combination Therapy for Multiple Myeloma |
| NCT02577783 | PHASE4 | UNKNOWN | PDD vs PAD to Treat Initially Diagnosed MM |
| NCT02773550 | PHASE4 | TERMINATED | Treatment With a Scheme With Low Doses of Bortezomib / Melphalan / Prednisone (MPV) in Patients With Multiple Myeloma |
| NCT02958969 | PHASE4 | COMPLETED | Apixaban for Primary Prevention of Venous Thromboembolism in Patients With Multiple Myeloma |
| NCT03173092 | PHASE4 | TERMINATED | A Study of Ixazomib (NINLARO®) in Combination With Lenalidomide and Dexamethasone (IRD) for the Treatment of Participants With Multiple Myeloma (MM) |
| NCT03619252 | PHASE4 | COMPLETED | Pneumococcal Vaccination of Multiple Myeloma Patients on Novel Agents |
| NCT03768960 | PHASE4 | COMPLETED | A Study of DARZALEX (Daratumumab) In Indian Participants With Relapsed and Refractory Multiple Myeloma, Whose Prior Therapy Included a Proteasome Inhibitor and an Immunomodulatory Agent |
| NCT03829371 | PHASE4 | ACTIVE_NOT_RECRUITING | STUDY COMPARING TWO STANDARD TREATMENTS IN AUTOLOGOUS STEM CELL TRANSPLANTATION INELIGIBLE POPULATION AFFECTED BY MULTIPLE MYELOMA |
| NCT03908138 | PHASE4 | UNKNOWN | RDD Versus VDD in Newly Diagnosed Patients With Multiple Myeloma |
| NCT04217967 | PHASE4 | COMPLETED | Ixazomib, Lenalidomide, and Combination for Maintenance in NDMM Patients |
| NCT04952766 | PHASE4 | COMPLETED | Study Evaluating SARS-CoV-2 (COVID-19) Humoral Response After BNT162b2 Vaccine in Immunocompromised Adults Compared to Healthy Adults |
| NCT04989140 | PHASE4 | UNKNOWN | Study of Pomalidomide, Oral Dexamethasone and Ixazomib in Patients With Relapsed MM Who Have Received Lenalidomide |
| NCT05183139 | PHASE4 | WITHDRAWN | A Multicenter In-class Transition Study of Ixazomib Combined With Pomalidomide and Dexamethasone or With Lenalidomide and Dexamethasone in Adults With Relapsed/Refractory Multiple Myeloma |
| NCT05201781 | PHASE4 | RECRUITING | A Long-term Study for Participants Previously Treated With Ciltacabtagene Autoleucel |
| NCT05429515 | PHASE4 | NOT_YET_RECRUITING | Effect of HFR-SUPRA in the Treatment of Multiple Myeloma-related Acute Kidney Injury |
| NCT05511428 | PHASE4 | COMPLETED | Home Based Daratumumab Administration for Patients With Multiple Myeloma |
| NCT05545202 | PHASE4 | UNKNOWN | A Randomized, Comparative, Double-blind Trial of Pentaisomaltose and Dimethyl Sulphoxide for Cryoprotection of Hematopoietic Stem Cells in Subjects With Multiple Myeloma or Malignant Lymphoma With a Need for Autologous Transplantation |
| NCT05555329 | PHASE4 | COMPLETED | Alternative Dosing Scheme of Pomalidomide 4 mg Every Other Day Versus Pomalidomide 2 mg and 4 mg Every Day; the POMAlternative Study |
| NCT05722405 | PHASE4 | RECRUITING | Ixazomib Plus Low-dose Lenalidomide Versus Ixazomib Alone for Maintenance Treatment of High Risk Multiple Myeloma |
| NCT05855122 | PHASE4 | UNKNOWN | Safety and ASCT-related Symptom Burden Optimization of Tocilizumab in ASCT Following HD Melphalan Conditioning for Multiple Myeloma Patients |
| NCT05944783 | PHASE4 | NOT_YET_RECRUITING | Bioequivalence Studies of Dasatinib 100 Mg |
| NCT06057402 | PHASE4 | RECRUITING | Elranatamab Post Trial Access Study for Participants With Multiple Myeloma (MM) |
| NCT06251076 | PHASE4 | RECRUITING | Plan Development for Giving Teclistamab in the Outpatient Setting |
Related Atlas pages
- Associated diseases: breast carcinoma
- Biomarker drugs (CIViC) (drugs whose response is associated with variants in this gene — CIViC predictive evidence, not targeting): Alpelisib
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): breast cancer, breast carcinoma, pelvic organ prolapse, plasma cell myeloma