SHBG
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Also known as ABPTEBGMGC126834MGC138391
Summary
SHBG (sex hormone binding globulin, HGNC:10839) is a protein-coding gene on chromosome 17p13.1, encoding Sex hormone-binding globulin (P04278). Functions as an androgen transport protein, but may also be involved in receptor mediated processes.
This gene encodes a steroid binding protein that was first described as a plasma protein secreted by the liver but is now thought to participate in the regulation of steroid responses. The encoded protein transports androgens and estrogens in the blood, binding each steroid molecule as a dimer formed from identical or nearly identical monomers. Polymorphisms in this gene have been associated with polycystic ovary syndrome and type 2 diabetes mellitus. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 6462 — RefSeq curated summary.
At a glance
- GWAS associations: 33
- Clinical variants (ClinVar): 62 total
- Druggable target: yes — 30 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001040
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:10839 |
| Approved symbol | SHBG |
| Name | sex hormone binding globulin |
| Location | 17p13.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | ABP, TEBG, MGC126834, MGC138391 |
| Ensembl gene | ENSG00000129214 |
| Ensembl biotype | protein_coding |
| OMIM | 182205 |
| Entrez | 6462 |
Gene structure
Transcript identifiers
Ensembl transcripts: 27 — 23 protein_coding, 2 nonsense_mediated_decay, 1 retained_intron, 1 TEC
ENST00000340624, ENST00000380450, ENST00000416273, ENST00000441599, ENST00000570353, ENST00000570527, ENST00000570547, ENST00000571153, ENST00000572182, ENST00000572262, ENST00000574539, ENST00000575314, ENST00000575618, ENST00000575729, ENST00000575903, ENST00000576152, ENST00000576478, ENST00000576728, ENST00000576747, ENST00000576830, ENST00000624152, ENST00000856862, ENST00000856863, ENST00000856864, ENST00000856865, ENST00000856866, ENST00000856867
RefSeq mRNA: 8 — MANE Select: NM_001040
NM_001040, NM_001146279, NM_001146280, NM_001146281, NM_001289113, NM_001289114, NM_001289115, NM_001289116
CCDS: CCDS11117, CCDS54082, CCDS54083, CCDS58513, CCDS73961, CCDS73962
Canonical transcript exons
ENST00000380450 — 8 exons
| Exon | Start | End |
|---|---|---|
| ENSE00002663943 | 7630135 | 7630283 |
| ENSE00003465540 | 7630680 | 7630869 |
| ENSE00003485100 | 7633204 | 7633372 |
| ENSE00003601548 | 7632752 | 7632959 |
| ENSE00003606133 | 7630416 | 7630507 |
| ENSE00003641466 | 7631879 | 7632015 |
| ENSE00003648709 | 7631200 | 7631361 |
| ENSE00003682683 | 7631589 | 7631748 |
Expression profiles
Bgee: expression breadth ubiquitous, 162 present calls, max score 89.19.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.3340 / max 90.1901, expressed in 86 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 159282 | 0.2147 | 35 |
| 159281 | 0.1193 | 49 |
Top tissues by expression
292 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right lobe of liver | UBERON:0001114 | 89.19 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 88.78 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 84.39 | gold quality |
| liver | UBERON:0002107 | 83.79 | gold quality |
| right testis | UBERON:0004534 | 78.09 | gold quality |
| left testis | UBERON:0004533 | 77.20 | gold quality |
| testis | UBERON:0000473 | 74.33 | gold quality |
| hair follicle | UBERON:0002073 | 71.56 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 71.49 | gold quality |
| duodenum | UBERON:0002114 | 70.55 | gold quality |
| adrenal tissue | UBERON:0018303 | 70.38 | gold quality |
| cervix epithelium | UBERON:0004801 | 70.15 | gold quality |
| right adrenal gland | UBERON:0001233 | 70.01 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 69.94 | gold quality |
| Brodmann (1909) area 10 | UBERON:0013541 | 68.89 | gold quality |
| triceps brachii | UBERON:0001509 | 68.76 | gold quality |
| gluteal muscle | UBERON:0002000 | 68.63 | gold quality |
| squamous epithelium | UBERON:0006914 | 68.59 | gold quality |
| jejunal mucosa | UBERON:0000399 | 68.47 | gold quality |
| left adrenal gland | UBERON:0001234 | 67.91 | gold quality |
| oocyte | CL:0000023 | 67.18 | gold quality |
| adrenal cortex | UBERON:0001235 | 67.12 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 67.07 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 66.57 | gold quality |
| epithelium of esophagus | UBERON:0001976 | 66.43 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 66.34 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 66.32 | gold quality |
| small intestine | UBERON:0002108 | 66.09 | gold quality |
| esophagus squamous epithelium | UBERON:0006920 | 65.86 | gold quality |
| adrenal gland | UBERON:0002369 | 65.57 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.94 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): ESR1, HNF4A, HNF4G, ID1, MSC, NR3C1, NR5A1, PAX1, PPARG, SCX, TBP, USF1, USF2
Literature-anchored findings (GeneRIF, showing 40)
- A (TAAAA)(n) pentanucleotide repeat, located within an alu sequence at the 5’ boundary of the human SHBG promoter, influences its transcriptional activity in association with downstream elements, including an SP1-binding site (PMID:11473114)
- observations are consistent with the hypothesis that SHBG, destined to participate in signaling at the cell membrane, is locally regulated and produced (PMID:12015315)
- Data suggest that O-glycosylation of sex hormone-binding gllobulin is essential for SHBG binding to a membrane receptor that is responsible for inhibiting the estradiol-induced proliferation of MCF-7 breast cancer cells. (PMID:12039072)
- 2.35 A and 1.7 A crystal structures of the amino-terminal LG domain of SHBG. Resolution of a disordered region at the entrance of the human sex hormone-binding globulin steroid-binding site. (PMID:12054810)
- binds steroid ligands in specific orientations producing distinct changes in protein conformation (PMID:12065592)
- serum concentrations are elevated in kwashiorkor and anorexia nervosa but not in marasmus; marker of nutritional status in anorexia nervosa and kwashiorkor (PMID:12081841)
- polymorphisms in familial and sporadic breast cancer (PMID:12151349)
- Results describe the crystal structure of human sex hormone-binding globulin in complex with 2-methoxyestradiol. (PMID:12228253)
- Data show that human sex hormone-binding globulin (SHBG) transcripts containing an alternative exon 1 sequence are located specifically in the testicular germ cells of transgenic mice, whereas murine SHBG transcripts are confined to Sertoli cells. (PMID:12235141)
- SHBG and sex steroids showed a negative correlation with serum lipids considered a cardiovascular risk (PMID:12603009)
- study shows that for patients with polycystic ovary syndrome, sex hormone-binding globulin is an integrated marker of insulin resistance that may be of use to identify insulin-resistant individuals for targeted treatment (PMID:12679434)
- sex-hormone-binding globulin has a role in modulating tyrosinase activity at the posttranslational level through the cell membrane signaling pathway of melanocytes (PMID:12753385)
- Plasma SHBG level may represent significant predictor of metabolic syndrome in men and premenopausal women. (PMID:12800098)
- first-trimester sex hormone binding globulin levels were lower among women in whom gestational diabetes mellitus subsequently developed (PMID:12861158)
- IGFBP-1 and SHBG are equally sensitive to ambient insulin concentrations in human hepatoma cell cultures, and the production of both proteins is also attenuated by the IGFs. (PMID:14568572)
- Novel (TAAAA)n allele found in low frequency, mainly in controls. May be genetic contribution to decreased SHBG levels frequently seen in polycystic ovary syndrome(PCOS). May act as susceptibility gene, genetic link for origin. (PMID:14671199)
- May be a marker for insulin resistance in type 2 diabetes. (PMID:14694008)
- Polymorphism(s) within coding sequence and, potentially, in regulatory sequence of SHBG gene are associated with circulating SHBG levels and may represent part of genetic background of sex steroid hormone activity. (PMID:14764814)
- Low total testosterone and SHBG levels independently predict development of the metabolic syndrome and diabetes in middle-aged men. (PMID:15111517)
- SHBG androgen sensitivity test is a simple diagnostic tool for the detection of androgen receptor malfunction in gonadal dysgenesis. (PMID:15146368)
- SHBG may play a key role in male patients with idiopathic or secondary osteoporosis. (PMID:15193539)
- Serum SHBG appeared to be an independent positive predictor of bone turnover rate, which also positively associated with serum 25-hydroxyvitamin-D levels. (PMID:15292305)
- USF transcription factors repress SHBG transcription in Sertoli cells through an interaction with FP4 within its proximal promoter (PMID:15574421)
- SHBG interacts with cell membranes and causes inhibition of the anti-apoptotic effect of estradiol. (PMID:15664449)
- Estimation of genetic and nongenetic influences on endogenous sex hormones (testosterone, estradiol, estrone, and SHBG) in a large sample of 532 adult white mono- and dizygotic male twins (PMID:15755867)
- Intrahepatic cholestasis of pregnancy is associated with blunted responses of SHBG to oral estrogen. (PMID:15784702)
- Interacts with prostatic proteins in a yeast two-hybrid system. (PMID:15862967)
- TAAAA repeat polymorphism in the promoter region provides evidence for a possible association of SHBG gene with age at menarche. (PMID:15879463)
- Finds variant SHBG Asn allele (Asp327Asn) associated with reduced breast cancer risk in postmenopausal women [OR, 0.73; 95% CI (95% CI), 0.53-0.99], but not in premenopausal women [OR, 1.03; 95% CI, 0.82-1.27). (PMID:15894658)
- SHBG-immunoreactive neurons were observed in the supraoptic nucleus, the suprachiasmatic nucleus, the bed nucleus of the stria terminalis, paraventricular nucleus, arcuate nucleus, the perifornical region and the medial preoptic area in human brains. (PMID:16155373)
- Data show that some special genotypes and low serum SHBG levels may be associated with PCOS and its glucose metabolic status, but both SHBG gene polymorphism genotype and serum SHBG are not good indicators to find out the PCOS individual at high risk. (PMID:16331562)
- Low SHBG and/or androgen deficiency may provide early warning signs for cardiovascular risk and an opportunity for early intervention in nonobese men. (PMID:16394089)
- SHBG may have a role in cardiovascular disease in women with polycystic ovary syndrome (PMID:16757555)
- Polymorphisms in the SHBG promoter predict serum levels of SHBG, androgens, and glucuronidated androgen metabolites, and hip Bone Mineral Density in men. (PMID:16926255)
- A study evaluating testosterone and estradiol (E2) levels among women in relation to 5 single nucleotide polymorphisms (SNPs) of the aromatase (CYP 19) gene in women of 4 ethnic/racial groups is presented. (PMID:16949385)
- Although certain parameters of insulin status and serum SHBG demonstrated statistically significant correlation coefficients, these relationships are weak and SHBG cannot be used as a predictor of insulin resistance. (PMID:17027360)
- The present study demonstrated a time and operation effect decline in plasma DHEAS levels. In contrast, the time x operation interaction on SHBG levels exhibited an increase toward postoperative day 7. (PMID:17027364)
- SHBG, but not CYP17, CYP1B1, or COMT polymorphisms are associated with different sex hormone levels in post-menopausal breast cancer survivors (PMID:17077994)
- the (TAAAA)(n) SHBG gene polymorphism might have a role in serum SHBG expression and in hyperandrogenaemic clinical presentation of PCOS (PMID:17189294)
- D327N polymorphism of the SHBG gene does not influence susceptibility to polycystic ovary syndrome (PMID:17258903)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Shbg | ENSMUSG00000005202 |
| rattus_norvegicus | Shbg | ENSRNOG00000011357 |
Paralogs (1): PROS1 (ENSG00000184500)
Protein
Protein identifiers
Sex hormone-binding globulin — P04278 (reviewed: P04278)
Alternative names: Sex steroid-binding protein, Testis-specific androgen-binding protein, Testosterone-estradiol-binding globulin, Testosterone-estrogen-binding globulin
All UniProt accessions (14): P04278, A0A0C4DGN2, B0FWH5, B0FWH6, B0FWH7, I3L0M1, I3L145, I3L1C1, I3L1G4, I3L1J1, I3L2F1, I3L2X4, I3L4B9, I3L4D0
UniProt curated annotations — full annotation on UniProt →
Function. Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone, and 17-beta-estradiol. Regulates the plasma metabolic clearance rate of steroid hormones by controlling their plasma concentration.
Subunit / interactions. Homodimer.
Subcellular location. Secreted.
Tissue specificity. Isoform 1 and isoform 2 are present in liver and testis.
Post-translational modifications. Variant Asn-356 contains one N-linked (GlcNAc…) at position 356.
Isoforms (5)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P04278-1 | 1, SHBG, SHBGr-1 | yes |
| P04278-2 | 2, Sex hormone binding globulin-gene-related protein (SHBGgrp), SHBGr-2 | |
| P04278-3 | 3 | |
| P04278-4 | 4 | |
| P04278-5 | 5 |
RefSeq proteins (8): NP_001031, NP_001139751, NP_001139752, NP_001139753, NP_001276042, NP_001276043, NP_001276044, NP_001276045 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001791 | Laminin_G | Domain |
| IPR013320 | ConA-like_dom_sf | Homologous_superfamily |
| IPR051145 | GAS-SHBG-PROS | Family |
Pfam: PF00054
UniProt features (43 total): strand 16, splice variant 5, helix 5, sequence variant 4, sequence conflict 3, glycosylation site 3, domain 2, disulfide bond 2, signal peptide 1, chain 1, turn 1
Structure
Experimental structures (PDB)
13 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 1D2S | X-RAY DIFFRACTION | 1.55 |
| 1F5F | X-RAY DIFFRACTION | 1.7 |
| 1KDK | X-RAY DIFFRACTION | 1.7 |
| 6PYA | X-RAY DIFFRACTION | 1.71 |
| 6PYF | X-RAY DIFFRACTION | 1.73 |
| 1LHW | X-RAY DIFFRACTION | 1.75 |
| 6ULB | X-RAY DIFFRACTION | 1.75 |
| 1LHU | X-RAY DIFFRACTION | 1.8 |
| 6PYB | X-RAY DIFFRACTION | 1.8 |
| 1LHN | X-RAY DIFFRACTION | 2 |
| 1LHO | X-RAY DIFFRACTION | 2 |
| 1LHV | X-RAY DIFFRACTION | 2 |
| 1KDM | X-RAY DIFFRACTION | 2.35 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P04278-F1 | 86.03 | 0.71 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (2): 193–217, 362–390
Glycosylation sites (3): 36, 380, 396
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 70 (showing top):
MODULE_16, MODULE_404, MODULE_118, MODULE_379, ACEVEDO_LIVER_TUMOR_VS_NORMAL_ADJACENT_TISSUE_DN, CAIRO_HEPATOBLASTOMA_DN, MODULE_88, MODULE_242, MODULE_104, MODULE_55, GOMF_STEROID_BINDING, MODULE_23, MODULE_7, GOMF_LIPID_BINDING, MODULE_181
GO Biological Process (0):
GO Molecular Function (4): steroid binding (GO:0005496), androgen binding (GO:0005497), protein binding (GO:0005515), lipid binding (GO:0008289)
GO Cellular Component (2): extracellular region (GO:0005576), extracellular exosome (GO:0070062)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| binding | 2 |
| lipid binding | 1 |
| hormone binding | 1 |
| cellular anatomical structure | 1 |
| extracellular vesicle | 1 |
Protein interactions and networks
STRING
1440 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| SHBG | ALB | P02768 | 996 |
| SHBG | SERPINA6 | P08185 | 952 |
| SHBG | INS | P01308 | 881 |
| SHBG | IGF1 | P01343 | 860 |
| SHBG | PRL | P01236 | 822 |
| SHBG | ADIPOQ | Q15848 | 817 |
| SHBG | AMH | P03971 | 792 |
| SHBG | NRXN2 | Q9P2S2 | 791 |
| SHBG | LEP | P41159 | 763 |
| SHBG | CYP19A1 | P11511 | 763 |
| SHBG | SERPINA7 | P05543 | 753 |
| SHBG | NRXN1 | Q9ULB1 | 740 |
| SHBG | ESR2 | Q92731 | 732 |
| SHBG | GNRH1 | P01148 | 720 |
| SHBG | CRP | P02741 | 719 |
IntAct
6 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| TMEM236 | SHBG | psi-mi:“MI:0915”(physical association) | 0.400 |
| Trappc8 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| psi-mi:“MI:0914”(association) | 0.350 | ||
| GRB2 | SHBG | psi-mi:“MI:0915”(physical association) | 0.000 |
| CLEC4G | SHBG | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (62): SHBG (Affinity Capture-MS), CNTNAP3B (Affinity Capture-MS), GNB2 (Affinity Capture-MS), SHBG (Affinity Capture-MS), SHBG (Negative Genetic), SHBG (Negative Genetic), SHBG (Proximity Label-MS), SHBG (Two-hybrid), SHBG (Two-hybrid), ASB16-AS1 (Two-hybrid), FYTTD1 (Two-hybrid), HYI (Two-hybrid), RMND5B (Two-hybrid), CECR5 (Two-hybrid), AKR1B1 (Two-hybrid)
ESM2 similar proteins: A0A140LHF2, A0EQL2, D3YZF7, D7PDD4, O15533, O55237, O70394, O70540, O95866, P04278, P05111, P07994, P08689, P0C6B3, P0DP72, P15196, P17490, P18627, P40238, P55101, P60882, P97497, Q00657, Q08351, Q14393, Q14773, Q16671, Q3SWY4, Q5BK54, Q5NKT8, Q5TJE4, Q61790, Q61826, Q62588, Q6PZD2, Q6UVK1, Q6UWB1, Q7Z7M0, Q7Z7M1, Q86VR7
Diamond homologs: A0EQL2, P04278, P08689, P15196, P97497, Q0V8T5, Q0V8T8, Q62588, Q8WYK1, Q96NU0, Q99P47, D0PRN3, O54991, P33450, P78357, Q0V8T7, Q3KN41, Q9BZ76, Q9C0A0, Q0V8T0, Q61001
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
62 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 46 |
| Likely benign | 9 |
| Benign | 6 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1753 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 17:7626611:CCAC:C | acceptor_gain | 1.0000 |
| 17:7626612:CAC:C | acceptor_gain | 1.0000 |
| 17:7626612:CACC:C | acceptor_gain | 1.0000 |
| 17:7626613:ACC:A | acceptor_loss | 1.0000 |
| 17:7626615:C:CC | acceptor_gain | 1.0000 |
| 17:7626615:CT:C | acceptor_loss | 1.0000 |
| 17:7626616:T:G | acceptor_loss | 1.0000 |
| 17:7626928:G:C | donor_gain | 1.0000 |
| 17:7626990:C:A | donor_gain | 1.0000 |
| 17:7627242:T:TC | acceptor_gain | 1.0000 |
| 17:7627244:G:GC | acceptor_gain | 1.0000 |
| 17:7627248:C:CT | acceptor_gain | 1.0000 |
| 17:7627604:T:TA | donor_gain | 1.0000 |
| 17:7630252:G:T | donor_gain | 1.0000 |
| 17:7630508:G:GG | donor_gain | 1.0000 |
| 17:7630866:CCAG:C | donor_loss | 1.0000 |
| 17:7630869:GG:G | donor_loss | 1.0000 |
| 17:7631195:TGCA:T | acceptor_loss | 1.0000 |
| 17:7631198:A:AG | acceptor_gain | 1.0000 |
| 17:7631198:AGGT:A | acceptor_gain | 1.0000 |
| 17:7631199:G:GG | acceptor_gain | 1.0000 |
| 17:7631199:GGT:G | acceptor_gain | 1.0000 |
| 17:7631199:GGTG:G | acceptor_gain | 1.0000 |
| 17:7614448:TCAC:T | donor_loss | 0.9900 |
| 17:7614449:CACCT:C | donor_loss | 0.9900 |
| 17:7614450:ACC:A | donor_loss | 0.9900 |
| 17:7626610:GCCAC:G | acceptor_gain | 0.9900 |
| 17:7626611:CCACC:C | acceptor_gain | 0.9900 |
| 17:7626613:AC:A | acceptor_gain | 0.9900 |
| 17:7626614:CC:C | acceptor_gain | 0.9900 |
AlphaMissense
2577 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 17:7630863:G:C | W129C | 0.986 |
| 17:7630863:G:T | W129C | 0.986 |
| 17:7630861:T:A | W129R | 0.976 |
| 17:7630861:T:C | W129R | 0.976 |
| 17:7630693:T:C | F73L | 0.966 |
| 17:7630695:T:A | F73L | 0.966 |
| 17:7630695:T:G | F73L | 0.966 |
| 17:7631630:G:C | W199C | 0.961 |
| 17:7631630:G:T | W199C | 0.961 |
| 17:7630763:T:C | F96S | 0.959 |
| 17:7631736:T:C | F235L | 0.959 |
| 17:7631738:C:A | F235L | 0.959 |
| 17:7631738:C:G | F235L | 0.959 |
| 17:7630762:T:C | F96L | 0.956 |
| 17:7630764:T:A | F96L | 0.956 |
| 17:7630764:T:G | F96L | 0.956 |
| 17:7630775:T:C | L100P | 0.952 |
| 17:7630720:G:A | G82R | 0.947 |
| 17:7630720:G:C | G82R | 0.947 |
| 17:7630864:C:G | H130D | 0.944 |
| 17:7631628:T:A | W199R | 0.943 |
| 17:7631628:T:C | W199R | 0.943 |
| 17:7630778:G:C | R101P | 0.934 |
| 17:7630703:G:C | R76P | 0.933 |
| 17:7630784:G:T | G103V | 0.931 |
| 17:7631737:T:C | F235S | 0.930 |
| 17:7630802:T:C | L109P | 0.928 |
| 17:7630823:T:C | L116P | 0.928 |
| 17:7632919:G:C | W340C | 0.926 |
| 17:7632919:G:T | W340C | 0.926 |
dbSNP variants (sampled 300 via entrez): RS1000223321 (17:7633722 C>G), RS1000274522 (17:7620869 G>A), RS1000367065 (17:7629760 T>C), RS1000959745 (17:7632280 A>T), RS1000978984 (17:7614497 C>A,G,T), RS1001096819 (17:7614285 G>A,C), RS1001098626 (17:7621258 A>C), RS1001483022 (17:7628374 C>T), RS1001755466 (17:7615838 A>G), RS1001823863 (17:7616962 T>C), RS1001984611 (17:7615514 G>A), RS1002100618 (17:7615436 T>A,G), RS1002107677 (17:7617433 T>A), RS1002214784 (17:7622758 G>A,T), RS1002236681 (17:7632986 T>A,C,G)
Disease associations
OMIM: gene MIM:182205 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
33 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000189_33 | Protein quantitative trait loci | 3.000000e-07 |
| GCST001264_1 | Testosterone levels | 1.000000e-41 |
| GCST001264_2 | Testosterone levels | 2.000000e-22 |
| GCST001554_1 | Sex hormone-binding globulin levels | 2.000000e-16 |
| GCST001612_12 | Sex hormone-binding globulin levels | 2.000000e-106 |
| GCST001612_24 | Sex hormone-binding globulin levels | 2.000000e-55 |
| GCST001612_25 | Sex hormone-binding globulin levels | 3.000000e-46 |
| GCST001612_26 | Sex hormone-binding globulin levels | 1.000000e-24 |
| GCST001612_27 | Sex hormone-binding globulin levels | 2.000000e-21 |
| GCST001612_28 | Sex hormone-binding globulin levels | 1.000000e-07 |
| GCST001612_8 | Sex hormone-binding globulin levels | 4.000000e-80 |
| GCST001612_9 | Sex hormone-binding globulin levels | 6.000000e-30 |
| GCST001653_1 | Androgen levels | 6.000000e-08 |
| GCST001653_3 | Androgen levels | 1.000000e-12 |
| GCST001653_5 | Androgen levels | 1.000000e-11 |
| GCST001653_6 | Androgen levels | 9.000000e-10 |
| GCST002195_6 | Hormone measurements | 1.000000e-08 |
| GCST002195_7 | Hormone measurements | 5.000000e-19 |
| GCST002925_8 | Sex hormone levels | 1.000000e-15 |
| GCST004621_186 | Red cell distribution width | 7.000000e-09 |
| GCST006979_802 | Heel bone mineral density | 1.000000e-14 |
| GCST007929_53 | Medication use (calcium channel blockers) | 5.000000e-09 |
| GCST009158_28 | Uterine fibroids | 7.000000e-31 |
| GCST010002_119 | Refractive error | 3.000000e-22 |
| GCST010703_158 | Brain morphology (MOSTest) | 3.000000e-09 |
| GCST010989_19 | Body size at age 10 | 4.000000e-09 |
| GCST90020024_510 | A body shape index | 2.000000e-10 |
| GCST90020025_1299 | Waist-to-hip ratio adjusted for BMI | 3.000000e-10 |
| GCST90020025_1300 | Waist-to-hip ratio adjusted for BMI | 1.000000e-15 |
| GCST90020027_546 | Waist-hip index | 2.000000e-11 |
EFO canonical traits (12, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004696 | sex hormone-binding globulin measurement |
| EFO:0004908 | testosterone measurement |
| EFO:0004909 | dihydrotestosterone measurement |
| EFO:0004730 | hormone measurement |
| EFO:0009188 | Red cell distribution width |
| EFO:0009270 | heel bone mineral density |
| EFO:0009930 | Calcium channel blocker use measurement |
| EFO:0004346 | neuroimaging measurement |
| EFO:0009819 | comparative body size at age 10, self-reported |
| EFO:0007789 | BMI-adjusted waist circumference |
| EFO:0007788 | BMI-adjusted waist-hip ratio |
| EFO:0004697 | estradiol measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3305 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
30 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538,597 (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 |
|---|---|---|---|
| CHEMBL103 | PROGESTERONE | 4 | 162,141 |
| CHEMBL1162 | NORETHINDRONE | 4 | 91,150 |
| CHEMBL135 | ESTRADIOL | 4 | 123,080 |
| CHEMBL1395 | METHYLTESTOSTERONE | 4 | 486,600 |
| CHEMBL1405 | ESTRONE | 4 | 36,722 |
| CHEMBL1479 | DANAZOL | 4 | 16,256 |
| CHEMBL1531 | ETONOGESTREL | 4 | 4,893 |
| CHEMBL1533 | DESOGESTREL | 4 | 9,566 |
| CHEMBL193482 | ESTRIOL | 4 | 21,295 |
| CHEMBL2107797 | NORGESTREL | 4 | 10,747 |
| CHEMBL258918 | MESTEROLONE | 4 | 2,485 |
| CHEMBL386630 | TESTOSTERONE | 4 | 129,997 |
| CHEMBL389621 | HYDROCORTISONE | 4 | 207,645 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4 | 40,543 |
| CHEMBL717 | MEDROXYPROGESTERONE ACETATE | 4 | 51,452 |
| CHEMBL90593 | PRASTERONE | 4 | 23,422 |
| CHEMBL110739 | CORTICOSTERONE | 3 | 28,274 |
| CHEMBL1499 | CORTISONE | 3 | 79,011 |
| CHEMBL241694 | ETHISTERONE | 3 | 3,833 |
| CHEMBL757 | NANDROLONE | 3 | 9,485 |
| CHEMBL1868702 | GESTRINONE | 2 | |
| CHEMBL253144 | CORTODOXONE | 2 | |
| CHEMBL259548 | BOLASTERONE | 2 | |
| CHEMBL261514 | MESTANOLONE | 2 | |
| CHEMBL273453 | ALDOSTERONE | 2 | |
| CHEMBL27769 | STANOLONE | 2 | |
| CHEMBL282575 | ESTRADIOL BENZOATE | 2 | |
| CHEMBL299613 | 2-METHOXYESTRADIOL | 2 | |
| CHEMBL44 | GENISTEIN | 2 | |
| CHEMBL253363 | PREGNENOLONE | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
1 measured of 1 human assays (1 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 4-((1S,2S,5S,6S,9R)-5-Hydroxymethyl-6,8,9-trimethyl-3-oxa-bicyclo[3.3.1]non-7-en-2-yl)-2-methoxy-phenol | IC50 | 22400 nM |
ChEMBL bioactivities
93 potent at pChembl≥5 of 103 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.74 | Kd | 0.182 | nM | STANOLONE |
| 9.74 | Kd | 0.182 | nM | CHEMBL260202 |
| 9.60 | Kd | 0.2512 | nM | MESTEROLONE |
| 9.54 | Kd | 0.2884 | nM | CHEMBL259126 |
| 9.38 | Kd | 0.4169 | nM | CHEMBL411053 |
| 9.32 | Kd | 0.4786 | nM | CHEMBL265926 |
| 9.31 | Kd | 0.4898 | nM | CHEMBL265925 |
| 9.20 | Kd | 0.631 | nM | TESTOSTERONE |
| 9.17 | Kd | 0.6761 | nM | ANDROSTENEDIOL |
| 9.12 | Kd | 0.7586 | nM | CHEMBL260660 |
| 9.11 | Kd | 0.7762 | nM | ANDROSTANDIOL |
| 9.08 | Kd | 0.8318 | nM | 2-METHOXYESTRADIOL |
| 9.07 | Kd | 0.8511 | nM | CHEMBL260659 |
| 9.05 | Kd | 0.8913 | nM | CHEMBL261866 |
| 9.05 | Kd | 0.8913 | nM | CHEMBL408707 |
| 9.00 | Kd | 1 | nM | CHEMBL195836 |
| 9.00 | Kd | 1 | nM | CHEMBL261643 |
| 8.91 | Kd | 1.23 | nM | NORGESTREL |
| 8.91 | Kd | 1.23 | nM | CHEMBL410519 |
| 8.83 | Kd | 1.479 | nM | ESTRADIOL |
| 8.81 | Kd | 1.549 | nM | MESTANOLONE |
| 8.80 | Kd | 1.585 | nM | CHEMBL408973 |
| 8.78 | Kd | 1.66 | nM | ETHISTERONE |
| 8.76 | Kd | 1.738 | nM | CHEMBL223967 |
| 8.76 | Kd | 1.738 | nM | BOLASTERONE |
| 8.71 | Kd | 1.95 | nM | CHEMBL359619 |
| 8.62 | Kd | 2.399 | nM | CHEMBL121458 |
| 8.62 | Kd | 2.399 | nM | EQUILENIN |
| 8.57 | Kd | 2.692 | nM | CHEMBL265942 |
| 8.51 | Kd | 3.09 | nM | EQUILIN |
| 8.51 | Kd | 3.09 | nM | CHEMBL259599 |
| 8.46 | Kd | 3.467 | nM | CHEMBL411731 |
| 8.46 | Kd | 3.467 | nM | CHEMBL430043 |
| 8.43 | Kd | 3.715 | nM | METHYLTESTOSTERONE |
| 8.42 | IC50 | 3.8 | nM | STANOLONE |
| 8.36 | Kd | 4.365 | nM | CHEMBL409895 |
| 8.36 | Kd | 4.365 | nM | CHEMBL260639 |
| 8.36 | Kd | 4.365 | nM | CHEMBL260641 |
| 8.36 | Kd | 4.365 | nM | CHEMBL260640 |
| 8.36 | Kd | 4.365 | nM | CHEMBL411730 |
| 8.30 | Kd | 5.012 | nM | CHEMBL261406 |
| 8.27 | Kd | 5.37 | nM | CHEMBL261407 |
| 8.23 | Kd | 5.888 | nM | ETONOGESTREL |
| 8.23 | Kd | 5.888 | nM | CHEMBL406406 |
| 8.20 | Kd | 6.31 | nM | DANAZOL |
| 8.18 | Kd | 6.607 | nM | ESTRONE |
| 8.11 | Kd | 7.762 | nM | GESTRINONE |
| 7.97 | Kd | 10.72 | nM | NORETHINDRONE |
| 7.92 | Kd | 12.02 | nM | CHEMBL411316 |
| 7.88 | Kd | 13.18 | nM | CHEMBL409084 |
PubChem BioAssay actives
93 with measured affinity, of 320 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 |
|---|---|---|---|---|
| (5S,8R,9S,10S,13S,14S,17S)-17-hydroxy-10,13-dimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0002 | uM |
| (5S,8R,9S,10S,13S,14S,17R)-17-ethynyl-17-hydroxy-10,13-dimethyl-2,4,5,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0002 | uM |
| (1S,5S,8R,9S,10S,13S,14S,17S)-17-hydroxy-1,10,13-trimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0003 | uM |
| (3S,8R,9S,10R,13S,14S,17S)-13-methyl-1,2,3,4,7,8,9,10,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0003 | uM |
| (5S,7R,8R,9S,10S,13S,14S,17S)-17-hydroxy-7,10,13-trimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0004 | uM |
| (8R,9S,10R,13S,14S,17S)-17-hydroxy-4,10,13-trimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0005 | uM |
| (8R,9S,13S,14S,17S)-2-iodo-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0005 | uM |
| Testosterone | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0006 | uM |
| (3S,8R,9S,10R,13S,14S,17S)-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0007 | uM |
| (3R,5S,8R,9S,10S,13S,14S,17S)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0008 | uM |
| (13S,14S,17S)-13-methyl-11,12,14,15,16,17-hexahydrocyclopenta[a]phenanthrene-2,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0008 | uM |
| (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0008 | uM |
| (5S,7R,8R,9S,10S,13S,14S,17S)-17-hydroxy-7,10,13,17-tetramethyl-2,4,5,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0009 | uM |
| (7R,8R,9R,10R,13S,17S)-17-hydroxy-7,13-dimethyl-2,6,7,8,9,10,11,12,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0009 | uM |
| (5S,6S,8R,9S,10R,13S,14S,17S)-6-fluoro-17-hydroxy-10,13-dimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0009 | uM |
| (3S,8R,9S,10R,13S,14S,17S)-10,13-dimethyl-2,3,6,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0010 | uM |
| (3S,5S,7R,8R,9S,10S,13S,14S,17S)-7,10,13-trimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0010 | uM |
| (3S,8R,9S,10R,13S,14S,17R)-17-ethynyl-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0012 | uM |
| (8R,9S,10R,13S,14S)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0012 | uM |
| (5S,8R,9S,10S,13S,14S,17S)-17-hydroxy-10,13,17-trimethyl-2,4,5,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0015 | uM |
| Estradiol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0015 | uM |
| (5S,8S,9R,10S,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-11-methylidene-2,4,5,6,7,8,9,10,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0016 | uM |
| (7R,8R,9S,10R,13S,14S,17S)-17-hydroxy-7,10,13,17-tetramethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0017 | uM |
| (8R,9S,13S,14S,17S)-13-methyl-8,9,11,12,14,15,16,17-octahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0017 | uM |
| (8R,9S,10R,13S,14S,17R)-17-ethynyl-17-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0017 | uM |
| (7R,8R,9S,10R,13S,14S,17S)-17-hydroxy-7,10,13-trimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0019 | uM |
| (9S,13S,14S,17S)-13-methyl-6,9,11,12,14,15,16,17-octahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0024 | uM |
| (13S,14S)-3-hydroxy-13-methyl-12,14,15,16-tetrahydro-11H-cyclopenta[a]phenanthren-17-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0024 | uM |
| (7R,8R,9S,10R,13S,14S,17S)-17-hydroxy-7,10,13,17-tetramethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0027 | uM |
| (9S,13S,14S)-3-hydroxy-13-methyl-9,11,12,14,15,16-hexahydro-6H-cyclopenta[a]phenanthren-17-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0031 | uM |
| (7R,8S,9R,10S,13S,14S,17S)-9-fluoro-17-hydroxy-7,10,13-trimethyl-2,6,7,8,11,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0031 | uM |
| (7R,8R,9R,10S,13S,14S,17S)-17-hydroxy-7,13-dimethyl-2,4,5,6,7,8,9,10,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0035 | uM |
| (3S,5S,7R,8R,9S,10S,13S,14S,17S)-7,10,13,17-tetramethyl-1,2,3,4,5,6,7,8,9,11,12,14,15,16-tetradecahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0035 | uM |
| Methyltestosterone | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0037 | uM |
| (7R,8R,9S,10R,13S,14S,17S)-17-hydroxy-7,10,13-trimethyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0044 | uM |
| (8R,9R,10S,13S,14S,17S)-17-hydroxy-13-methyl-2,4,5,6,7,8,9,10,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0044 | uM |
| (8R,9S,10R,13S,14S)-10,13,17-trimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0044 | uM |
| (6S,8R,9S,10R,13S,14S,17S)-17-hydroxy-6,10,13-trimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0044 | uM |
| (5S,8R,9S,10S,13S,14S,17R)-17-ethynyl-3,3-difluoro-10,13-dimethyl-2,4,5,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0044 | uM |
| (8S,9S,13S,14S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-ol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0050 | uM |
| (3R,5S,7R,8S,9R,10S,13S,14S,17R)-13-ethyl-17-ethynyl-7-methyl-11-methylidene-1,2,3,4,5,6,7,8,9,10,12,14,15,16-tetradecahydrocyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0054 | uM |
| (8S,9R,10S,13S,14S,17S)-9-fluoro-17-hydroxy-10,13,17-trimethyl-2,6,7,8,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthrene-3,11-dione | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0059 | uM |
| Etonogestrel | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0059 | uM |
| Danazol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0063 | uM |
| Estrone | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0066 | uM |
| (8S,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,14,15,16-octahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0078 | uM |
| Norethindrone | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0107 | uM |
| (8R,9S,10R,13S,14S,16R,17R)-16,17-dihydroxy-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0120 | uM |
| (3S,8S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-10-methyl-11-methylidene-2,3,6,7,8,9,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-3,17-diol | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0132 | uM |
| prasterone | 318680: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | kd | 0.0144 | uM |
CTD chemical–gene interactions
124 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Ethinyl Estradiol | affects binding, affects cotreatment, increases expression | 9 |
| bisphenol A | affects response to substance, increases secretion, affects binding, decreases expression, decreases secretion | 5 |
| Estradiol | increases expression, increases reaction, affects binding, affects expression | 5 |
| Tamoxifen | affects binding, increases expression | 4 |
| Benzo(a)pyrene | decreases expression, decreases methylation, increases expression | 3 |
| Testosterone | affects binding, increases expression | 3 |
| Aflatoxin B1 | decreases expression, decreases methylation, increases expression | 3 |
| Levonorgestrel | affects binding, affects cotreatment, increases expression | 3 |
| propylparaben | affects binding, decreases secretion | 2 |
| methylparaben | affects binding, decreases secretion | 2 |
| o,p’-DDT | affects binding, decreases reaction | 2 |
| norgestimate | affects cotreatment, increases expression | 2 |
| sodium arsenite | increases expression | 2 |
| mono-benzyl phthalate | increases secretion, decreases secretion, increases abundance, increases expression | 2 |
| Dibutyl Phthalate | affects binding, increases abundance, increases expression, increases secretion | 2 |
| Mitotane | increases expression, increases reaction, affects binding | 2 |
| Quercetin | affects binding, increases expression | 2 |
| Dihydrotestosterone | affects binding, decreases reaction | 2 |
| Toremifene | affects binding, increases expression | 2 |
| Genistein | affects binding, increases expression | 2 |
| Raloxifene Hydrochloride | increases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| 2-hydroxyestradiol | increases expression | 1 |
| 3-deoxyestrone | affects binding | 1 |
| 2,4,6-tribromophenol | increases expression | 1 |
| dioxybenzone | affects binding | 1 |
| naringenin | affects binding | 1 |
| diethyl phthalate | affects binding | 1 |
| tetramethrin | affects binding | 1 |
| triclocarban | decreases secretion | 1 |
ChEMBL screening assays
34 unique, capped per target: 26 binding, 7 admet, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1025919 | Binding | Binding affinity to SHBG | Lignans interfering with 5 alpha-dihydrotestosterone binding to human sex hormone-binding globulin. — J Nat Prod |
| CHEMBL1037223 | ADMET | Binding affinity to human sex hormone binding globulin after 30 mins by size-exclusion HPLC analysis | Radiolabeled 5-iodo-3’-O-(17beta-succinyl-5alpha-androstan-3-one)-2’-deoxyuridine and its 5’-monophosphate for imaging and therapy of androgen receptor-positive cancers: synthesis and biological evaluation. — J Med Chem |
| CHEMBL847537 | Functional | Inhibition of hSHBG (human sex hormone binding globulin ) | A novel, nonsteroidal inhibitor of androgen binding to the rat androgen binding protein: diethyl [[[3-(2,6-dimethyl-4-pyridinyl)-4-fluorophenyl]amino]methylene] propanedioate. — J Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): uterine corpus leiomyoma