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HSD17B2

gene
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Also known as HSD17SDR9C2

Summary

HSD17B2 (hydroxysteroid 17-beta dehydrogenase 2, HGNC:5211) is a protein-coding gene on chromosome 16q23.3, encoding 17-beta-hydroxysteroid dehydrogenase type 2 (P37059). Catalyzes the NAD-dependent oxidation of the highly active 17beta-hydroxysteroids, such as estradiol (E2), testosterone (T), and dihydrotestosterone (DHT), to their less active forms and thus regulates the biological potency of these steroids.

Enables estradiol 17-beta-dehydrogenase [NAD(P)+] activity and testosterone dehydrogenase (NAD+) activity. Involved in androgen metabolic process; estrogen biosynthetic process; and response to retinoic acid. Located in endoplasmic reticulum membrane.

Source: NCBI Gene 3294 — RefSeq curated summary.

At a glance

  • GWAS associations: 5
  • Clinical variants (ClinVar): 91 total
  • Druggable target: yes — 4 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_002153

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:5211
Approved symbolHSD17B2
Namehydroxysteroid 17-beta dehydrogenase 2
Location16q23.3
Locus typegene with protein product
StatusApproved
AliasesHSD17, SDR9C2
Ensembl geneENSG00000086696
Ensembl biotypeprotein_coding
OMIM109685
Entrez3294

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 11 protein_coding

ENST00000199936, ENST00000563491, ENST00000566213, ENST00000566838, ENST00000568090, ENST00000569351, ENST00000891334, ENST00000891335, ENST00000891336, ENST00000891337, ENST00000891338

RefSeq mRNA: 1 — MANE Select: NM_002153 NM_002153

CCDS: CCDS10936

Canonical transcript exons

ENST00000199936 — 5 exons

ExonStartEnd
ENSE000011038198209807582098534
ENSE000011038248209090282091039
ENSE000011038258207094282071127
ENSE000025985828203525382035689
ENSE000036524388206817082068382

Expression profiles

Bgee: expression breadth ubiquitous, 152 present calls, max score 98.79.

FANTOM5 (CAGE): breadth broad, TPM avg 5.9597 / max 372.0387, expressed in 480 samples.

FANTOM5 promoters (9 alternative TSS)

Promoter IDTPM avgSamples expressed
1552291.7502338
1552281.6438335
1552261.1142245
1552250.9020201
1552300.180171
1552240.142369
1552270.101541
1552230.091758
1552310.034010

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
jejunal mucosaUBERON:000039998.79gold quality
duodenumUBERON:000211498.41gold quality
mucosa of transverse colonUBERON:000499198.10gold quality
ileal mucosaUBERON:000033197.67gold quality
right lobe of liverUBERON:000111496.86gold quality
liverUBERON:000210796.50gold quality
rectumUBERON:000105295.43gold quality
placentaUBERON:000198794.13gold quality
colonic mucosaUBERON:000031794.09gold quality
mucosa of urinary bladderUBERON:000125993.54gold quality
mucosa of sigmoid colonUBERON:000499392.68gold quality
olfactory segment of nasal mucosaUBERON:000538691.13gold quality
gall bladderUBERON:000211089.11gold quality
pancreatic ductal cellCL:000207989.03silver quality
islet of LangerhansUBERON:000000688.06gold quality
urinary bladderUBERON:000125587.66gold quality
small intestineUBERON:000210886.97gold quality
small intestine Peyer’s patchUBERON:000345486.37gold quality
body of pancreasUBERON:000115085.98gold quality
pancreasUBERON:000126485.84gold quality
transverse colonUBERON:000115785.28gold quality
minor salivary glandUBERON:000183082.20gold quality
colonic epitheliumUBERON:000039781.77gold quality
epithelial cell of pancreasCL:000008381.50gold quality
saliva-secreting glandUBERON:000104479.79gold quality
intestineUBERON:000016079.00gold quality
lower esophagus mucosaUBERON:003583478.57gold quality
nasal cavity mucosaUBERON:000182678.19gold quality
mammalian vulvaUBERON:000099777.93gold quality
jejunumUBERON:000211577.44gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 5.

ExperimentMarker?Max mean expression
E-GEOD-111727yes1218.23
E-HCAD-11yes777.84
E-MTAB-6701yes69.96
E-HCAD-9yes7.93
E-ANND-3no0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CTNNB1, RARA, RXRA, SP1, SP2, SP3

Literature-anchored findings (GeneRIF, showing 39)

  • Purification, reconstitution, and steady-state kinetics of the trans-membrane 17 beta-hydroxysteroid dehydrogenase 2. (PMID:11940569)
  • Androgen inactivation in human lung fibroblasts: variations in levels of 17 beta-hydroxysteroid dehydrogenase type 2 (PMID:12161528)
  • the lower expression of type 2 17 beta-HSD mRNA in scalp hairs of untreated hirsute patients suggests androgen metabolism disturbances with predominance of more potent androgens (PMID:12957669)
  • 17HSD type 2 mRNA expression in gastric mucosa of children compared to adults may be associated with increased need for protection against the mucosal load of foreign substances. The downregulation may have relevance in the pathogenesis of gastric cancer. (PMID:14666693)
  • Aromatase mRNA was higher in epithelial than in stromal cells in eutopic and ectopic endometrium in endometriosis. 17betaHSD2 in epithelial cells was increased during secretory phases compared with late proliferative phase. (PMID:16595205)
  • HSD17B2 expression in endometrial epithelial cells, and, therefore, estrogen inactivation, is regulated by SP1 and SP3, which are downstream targets of progesterone-dependent paracrine signals originating from endometrial stromal cells. (PMID:16807381)
  • importance of 17HSD type 2 in breast cancer- cell lines & non-tumour breast cells; high or low expression of 17HSD type 2 affected oestradiol concentration significantly; response was dependent on endogenous expression of 17HSD type 1 (PMID:16954436)
  • Previously unknown polymorphism was found in exon four of HSD17B2. Polymorphism does not contribute to a higher risk of developing breast cancer. (PMID:17260097)
  • The expression of 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) in eutopic and ectopic endometrial tissues of women with endometriosis is reported. (PMID:17505937)
  • role for HSD17B2 in the action of retinoids, in addition to its oxidative HSD17B activity on sex steroids (PMID:17510238)
  • Data reported that a similar level of 17beta-hydroxysteroid dehydrogenase type 2 mRNA was found in Polycystic Ovary Syndrome and the control tissues. (PMID:17953976)
  • Overexpression in African-American breast cancer may contribute to the increased proportion of estrogen receptor-negative breast cancers and worse clinical outcome among African-American patients. (PMID:17993718)
  • The bone development in transgenic male mice ubiquitously expressing human HSD17B2, was studied. (PMID:18348690)
  • HSD17B2 germline mutations potentially involved in breast cancer predisposition. (PMID:18372405)
  • HSD17B2 mRNA is expressed in human skin, at higher levels in men than in women. Expression levels vary with skin sites. HSD17B2 levels are not altered by topical 17-beta-estradiol treatment. (PMID:18794456)
  • Higher mRNA levels of enzymes synthesizing and inactivating androgens are found in differentiated adipocytes, consistent with higher androgen-processing rates in these cells. (PMID:18984855)
  • 17beta-HSD type 2 was expressed in 20% of breast cancer specimens. decrease in 17beta-HSD type 2 expressions in breast cancer may play a role in the development &/or progression of cancer by modifying the intratumoral levels of estrogens & androgens. (PMID:18996480)
  • Data suggest that the 17HSD1/17HSD2 ratio might be useful as a predictive factor for tamoxifen treatment in ER-positive breast cancer patients. (PMID:19401349)
  • preference of 17betaHSD2 for E2 oxidation strongly resists alteration by genetic & metabolic means. Findings suggest additional structural features, beyond lack of a specific Arg residue, disfavor NADPH binding & thus support E2 oxidation by 17betaHSD2 (PMID:19556422)
  • BRCA1 and HSD17B2 genes may increase the risk of developing breast cancer via enhanced estradiol activity. (PMID:19729830)
  • HSD17B2 modulates estrogen-independent and estrogen-dependent action in transgenic female mice. (PMID:19797119)
  • Data show that steroidogenic enzymes (AKR1C3, HSD17B2, UGT2B15 and UGT2B17) and stem/progenitor cell markers CK5 and ABCG2 were upregulated in castration resistant prostate cancer. (PMID:21365123)
  • Data indicate that 17betaHSD2 expression is higher in HUAEC than in HUVEC; activity is higher in umbilical arteries near the placenta. These data are consistent with higher sex steroid inactivation in the arterial system of the foeto-placental unit. (PMID:21877158)
  • Single-nucleotide polymorphisms in HSD17B2, HSD17B3 and HSD17B1 are associated with plasma testosterone level and prostate cancer aggressiveness. (PMID:21900597)
  • no significant difference in the genotype and allele frequencies of rs8191246 between uterine leiomyoma cases and controls (PMID:22546946)
  • SNP variants in the 17beta-HSD2 and 17beta-HSD7 genes and 17beta-HSD7 copy number is associated with increased estradiol levels in breast cancer tissues. (PMID:24560990)
  • Single nucleotide polymorphism in HSD17B2 gene is associated with hepatocellular carcinoma. (PMID:24563232)
  • This study identified specific germline variations in estradiol metabolism-related pathways, namely CYP1B1, SULT2B1, and HSD17B2, as novel prognostic markers that are cumulatively associated with increased risk of prostate cancer progression (PMID:24682418)
  • overexpression of 17beta-HSD2 in sebocytes significantly increased the androstenedione production and markedly decreased the amounts of testosterone and dihydrotestosterone (PMID:24938708)
  • This study demonstrated that HSD17B2 transcript and protein levels are linked to some clinicopathological features in gastric cancer. (PMID:25776474)
  • High expression of either HSD17B2 or HMGCS2 predicted poor susceptibility of rectal cancer to preoperative chemoradiotherapy. (PMID:25929810)
  • Data indicate that conversion of testosterone to 4-dione detected in abdominal adipose tissue is caused by 17b-HSD type 2 which is localized in the vasculature of the adipose compartment. (PMID:26123590)
  • In both arm and subumbilical skin biopsy of patients with idiopathic hirsutism, there was an up-regulation of HSD17B2 mRNA expression. (PMID:26194504)
  • ATRA treatment decreased the mRNA expression of 17-beta-dehydrogenase 2 (HSD17B2) which converts estradiol into estrone in a dose-dependent manner (PMID:26228249)
  • Our findings suggested that CYP19A1 and HSD17B2 polymorphisms might be associated with circulating sex hormone levels in Japanese postmenopausal women, independent of current BMI. (PMID:26323233)
  • Our findings provide evidence of the clinical relevance, significance, and regulation of HSD17B2 in prostate cancer progression, which might provide new strategies for clinical management by targeting the functional silencing mechanisms of HSD17B2. (PMID:30228209)
  • Homology modeling meets site-directed mutagenesis: An ideal combination to elucidate the topology of 17beta-HSD2. (PMID:33246154)
  • A long non-coding RNA as a direct vitamin D target transcribed from the antisense strand of the human HSD17B2 locus. (PMID:35510872)
  • Single-cell RNA sequencing reveals that HSD17B2 in cancer-associated fibroblasts promotes the development and progression of castration-resistant prostate cancer. (PMID:37244445)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_reriohsd17b2ENSDARG00000045553
mus_musculusHsd17b2ENSMUSG00000031844
rattus_norvegicusHsd17b2ENSRNOG00000013982

Paralogs (25): HSD17B6 (ENSG00000025423), RDH11 (ENSG00000072042), HSD17B10 (ENSG00000072506), DHRS9 (ENSG00000073737), HSD17B14 (ENSG00000087076), DHRS12 (ENSG00000102796), HSDL1 (ENSG00000103160), HSD17B1 (ENSG00000108786), RDH10 (ENSG00000121039), HSD17B3 (ENSG00000130948), HSD17B7 (ENSG00000132196), HSD17B4 (ENSG00000133835), RDH5 (ENSG00000135437), RDH16 (ENSG00000139547), RDH12 (ENSG00000139988), HSD17B12 (ENSG00000149084), BDH1 (ENSG00000161267), DHRS3 (ENSG00000162496), SDR9C7 (ENSG00000170426), HSD17B13 (ENSG00000170509), SDR16C5 (ENSG00000170786), HSD11B2 (ENSG00000176387), WWOX (ENSG00000186153), HSD17B11 (ENSG00000198189), HSD17B8 (ENSG00000204228)

Protein

Protein identifiers

17-beta-hydroxysteroid dehydrogenase type 2 — P37059 (reviewed: P37059)

Alternative names: 20 alpha-hydroxysteroid dehydrogenase, E2DH, Estradiol 17-beta-dehydrogenase 2, Microsomal 17-beta-hydroxysteroid dehydrogenase, Short chain dehydrogenase/reductase family 9C member 2, Testosterone 17-beta-dehydrogenase

All UniProt accessions (6): P37059, H3BNN1, H3BQY3, H3BRZ6, H3BS44, H3BV42

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the NAD-dependent oxidation of the highly active 17beta-hydroxysteroids, such as estradiol (E2), testosterone (T), and dihydrotestosterone (DHT), to their less active forms and thus regulates the biological potency of these steroids. Oxidizes estradiol to estrone, testosterone to androstenedione, and dihydrotestosterone to 5alpha-androstan-3,17-dione. Also has 20-alpha-HSD activity.

Subunit / interactions. Homodimer.

Subcellular location. Endoplasmic reticulum membrane.

Tissue specificity. Expressed in placenta.

Similarity. Belongs to the short-chain dehydrogenases/reductases (SDR) family.

RefSeq proteins (1): NP_002144* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR002347SDR_famFamily
IPR020904Sc_DH/Rdtase_CSConserved_site
IPR036291NAD(P)-bd_dom_sfHomologous_superfamily

Pfam: PF00106

Enzyme classification (BRENDA):

  • EC 1.1.1.62 — 17beta-estradiol 17-dehydrogenase (BRENDA: 20 organisms, 283 substrates, 790 inhibitors, 95 Km, 44 kcat entries)

Substrate kinetics (BRENDA)

32 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

SubstrateKm (mM)Measurements
ESTRADIOL-17BETA0.0008–0.02514
ESTRONE—10
NADP+0.0001–99
17BETA-ESTRADIOL0.0006–0.0827
NADPH0.0003–0.167
ESTRADIOL0.0036–0.1186
TESTOSTERONE0.0071–0.2634
DEHYDROEPIANDROSTERONE0.0172–0.05983
5-ANDROSTENE-3BETA,17BETA-DIOL0.0066–0.00782
5ALPHA-DIHYDROTESTOSTERONE0.0067–0.1182
5BETA-PREGNAN-20ALPHA-OL-3-ONE0.0011–0.00332
DIHYDROTESTOSTERONE0.0043–0.0332
NAD+0.357–0.52
(S)-INDAN-1-OL0.5081
1-METHYL-6-DEHYDROESTRADIOL0.00851

Catalyzed reactions (Rhea), 4 shown:

  • testosterone + NAD(+) = androst-4-ene-3,17-dione + NADH + H(+) (RHEA:14929)
  • 17beta-estradiol + NAD(+) = estrone + NADH + H(+) (RHEA:24612)
  • 17beta-hydroxy-5alpha-androstan-3-one + NAD(+) = 5alpha-androstan-3,17-dione + NADH + H(+) (RHEA:41992)
  • (20S)-hydroxypregn-4-en-3-one + NAD(+) = progesterone + NADH + H(+) (RHEA:42108)

UniProt features (6 total): binding site 2, chain 1, transmembrane region 1, active site 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P37059-F187.620.59

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): 232

Ligand- & substrate-binding residues (2): 82–111; 219

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

IDPathway
R-HSA-193144Estrogen biosynthesis

MSigDB gene sets: 151 (showing top): GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_UP, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, NKX25_02, GOBP_REGULATION_OF_HORMONE_LEVELS, TANG_SENESCENCE_TP53_TARGETS_UP, NKX61_01, GOMF_STEROID_DEHYDROGENASE_ACTIVITY_ACTING_ON_THE_CH_OH_GROUP_OF_DONORS_NAD_OR_NADP_AS_ACCEPTOR, GOBP_IN_UTERO_EMBRYONIC_DEVELOPMENT, YAGUE_PRETUMOR_DRUG_RESISTANCE_UP, GOBP_HORMONE_BIOSYNTHETIC_PROCESS, GOBP_STEROID_BIOSYNTHETIC_PROCESS, MODULE_99, GOBP_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, HP1SITEFACTOR_Q6, GOBP_ANDROGEN_METABOLIC_PROCESS

GO Biological Process (8): in utero embryonic development (GO:0001701), placenta development (GO:0001890), estrogen biosynthetic process (GO:0006703), steroid metabolic process (GO:0008202), androgen metabolic process (GO:0008209), response to retinoic acid (GO:0032526), lipid metabolic process (GO:0006629), steroid biosynthetic process (GO:0006694)

GO Molecular Function (6): estradiol 17-beta-dehydrogenase [NAD(P)+] activity (GO:0004303), 17-alpha,20-alpha-dihydroxypregn-4-en-3-one dehydrogenase [NAD(P)+] activity (GO:0047006), testosterone dehydrogenase (NAD+) activity (GO:0047035), protein binding (GO:0005515), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on the CH-OH group of donors, NAD or NADP as acceptor (GO:0016616)

GO Cellular Component (3): endoplasmic reticulum membrane (GO:0005789), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

CategoryPathways
Metabolism of steroid hormones1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
steroid metabolic process2
steroid dehydrogenase activity, acting on the CH-OH group of donors, NAD or NADP as acceptor2
chordate embryonic development1
animal organ development1
estrogen metabolic process1
hormone biosynthetic process1
steroid hormone biosynthetic process1
lipid metabolic process1
hormone metabolic process1
response to lipid1
response to oxygen-containing compound1
primary metabolic process1
lipid biosynthetic process1
17-beta-hydroxysteroid dehydrogenase (NAD+) activity1
binding1
catalytic activity1
oxidoreductase activity, acting on CH-OH group of donors1
organelle membrane1
nuclear outer membrane-endoplasmic reticulum membrane network1
endoplasmic reticulum subcompartment1
cytoplasm1
endomembrane system1
intracellular membrane-bounded organelle1
cellular anatomical structure1

Protein interactions and networks

STRING

1028 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
HSD17B2HSD17B1P14061986
HSD17B2HSD17B3P37058979
HSD17B2DHRS11Q6UWP2935
HSD17B2HSD17B4P51659928
HSD17B2AKR1C3P42330816
HSD17B2SRD5A1P18405775
HSD17B2CYP17A1P05093733
HSD17B2HSD3B2P26439701
HSD17B2CYP19A1P11511675
HSD17B2HSD3B1P14060648
HSD17B2STSP08842632
HSD17B2HSD17B7P56937629
HSD17B2CYP1A1P04798621
HSD17B2SULT1E1P49888582
HSD17B2SRD5A2P31213581

IntAct

7 interactions, top by confidence:

ABTypeScore
HSD17B2ERGIC2psi-mi:“MI:0915”(physical association)0.640
CFTRHSD17B2psi-mi:“MI:0915”(physical association)0.370
E5ESYT2psi-mi:“MI:0914”(association)0.350
HSD17B2ARL6IP5psi-mi:“MI:0914”(association)0.350
CDH5ESYT2psi-mi:“MI:2364”(proximity)0.270

BioGRID (13): ERGIC2 (Affinity Capture-MS), MBNL2 (Affinity Capture-MS), ERGIC2 (Affinity Capture-MS), HSD17B2 (Affinity Capture-MS), ERGIC2 (Affinity Capture-MS), IFITM3 (Affinity Capture-MS), ARL6IP5 (Affinity Capture-MS), TMEM109 (Affinity Capture-MS), INSR (Affinity Capture-MS), REEP6 (Affinity Capture-MS), REEP5 (Affinity Capture-MS), ERGIC3 (Affinity Capture-MS), HSD17B2 (PCA)

ESM2 similar proteins: A0A193KX02, A0A397HK53, A1Y9I9, A4IG53, A5WWC6, B6CZ46, B6CZ56, B6CZ62, B8NR70, L0TAD5, O42898, P37059, P55205, P58781, P86243, Q0IIS3, Q0P464, Q28C60, Q28DI5, Q2KHV5, Q2VQV9, Q32LS6, Q3V1F8, Q4V339, Q5JTY5, Q5RIA9, Q5XI69, Q5XI79, Q66KL0, Q68EZ3, Q6DCK1, Q6GQ37, Q6PE54, Q6Q2C2, Q6TL19, Q7L592, Q7L5L3, Q8IUF1, Q8IX18, Q8NKC1

Diamond homologs: A0A097ZPE8, A0A0S2CGD3, A0A140FAN3, A0A144Y7G4, A0A162J3X8, A0A1U8QWA2, A0A1V0QSC6, A0A1W5SR39, A0QYC2, A4FUZ6, A4IGM4, A6SSW9, A7IQF2, A7IQH5, A7LB60, B6HV34, C0KTJ6, F1QWW8, G9FRD7, G9N4A9, O34782, O86034, P0A2D1, P0A2D2, P0DKC5, P0DKC6, P14802, P16544, P37059, P37440, P39831, P50171, P54554, P66778, P66780, P73574, P9WGS0, P9WGS1, P9WGS2, P9WGS3

SIGNOR signaling

2 interactions.

AEffectBMechanism
HSD17B2“up-regulates quantity”estrone“chemical modification”
HSD17B2“up-regulates quantity”17beta-estradiol“chemical modification”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance74
Likely benign10
Benign7

Top pathogenic / likely-pathogenic (0)

SpliceAI

1055 predictions. Top by Δscore:

VariantEffectΔscore
16:82070937:TCCAG:Tacceptor_loss1.0000
16:82070938:CCAGG:Cacceptor_loss1.0000
16:82070939:CAGG:Cacceptor_loss1.0000
16:82071059:TCACA:Tdonor_gain1.0000
16:82098068:A:AGacceptor_gain1.0000
16:82098070:CCCA:Cacceptor_loss1.0000
16:82098073:A:AGacceptor_gain1.0000
16:82098074:G:GGacceptor_gain1.0000
16:82098074:GAT:Gacceptor_gain1.0000
16:82068165:TGCA:Tacceptor_loss0.9900
16:82068166:GCAGG:Gacceptor_loss0.9900
16:82068167:CAGGT:Cacceptor_loss0.9900
16:82068168:A:ATacceptor_loss0.9900
16:82068168:AGGT:Aacceptor_gain0.9900
16:82068169:GGTG:Gacceptor_gain0.9900
16:82068337:A:Gdonor_gain0.9900
16:82068359:T:TAdonor_gain0.9900
16:82068378:CAGAG:Cdonor_loss0.9900
16:82068379:AGAG:Adonor_loss0.9900
16:82068380:GAG:Gdonor_gain0.9900
16:82068380:GAGG:Gdonor_loss0.9900
16:82068381:AGG:Adonor_loss0.9900
16:82068382:GGT:Gdonor_loss0.9900
16:82068383:G:Adonor_loss0.9900
16:82068384:T:Adonor_loss0.9900
16:82070940:A:AGacceptor_gain0.9900
16:82070941:G:GGacceptor_gain0.9900
16:82070941:GGACT:Gacceptor_gain0.9900
16:82091040:G:GGdonor_gain0.9900
16:82098069:C:Gacceptor_gain0.9900

AlphaMissense

2513 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
16:82071039:C:AN192K0.993
16:82071039:C:GN192K0.993
16:82090950:C:AA238D0.992
16:82091030:T:CF265L0.991
16:82091032:C:AF265L0.991
16:82091032:C:GF265L0.991
16:82070961:C:AN166K0.990
16:82070961:C:GN166K0.990
16:82071115:A:CS218R0.989
16:82071117:C:AS218R0.989
16:82071117:C:GS218R0.989
16:82071118:A:CS219R0.989
16:82071120:C:AS219R0.989
16:82071120:C:GS219R0.989
16:82071083:T:AL207H0.988
16:82090946:G:CA237P0.988
16:82090986:T:CL250P0.988
16:82035678:T:AV85D0.987
16:82071097:G:TG212W0.984
16:82070950:G:CA163P0.981
16:82090949:G:CA238P0.981
16:82071111:T:AN216K0.980
16:82071111:T:GN216K0.980
16:82090940:T:CS235P0.980
16:82068275:T:CL124S0.978
16:82071097:G:AG212R0.978
16:82071097:G:CG212R0.978
16:82068209:T:CL102P0.977
16:82071104:T:CL214P0.977
16:82071107:T:AV215E0.976

dbSNP variants (sampled 300 via entrez): RS1000024709 (16:82054886 C>A,G,T), RS1000054962 (16:82063624 C>T), RS1000132531 (16:82072189 G>A,C), RS1000201063 (16:82048193 T>A,C), RS1000237334 (16:82096662 G>A,T), RS1000269912 (16:82096868 A>G), RS1000330547 (16:82071790 T>C), RS1000335115 (16:82059723 G>A), RS1000359413 (16:82076353 C>T), RS1000382934 (16:82072001 C>G), RS1000419847 (16:82046062 T>C), RS1000438126 (16:82055089 T>C), RS1000446334 (16:82092133 C>T), RS1000522685 (16:82038426 T>C,G), RS1000537906 (16:82090227 T>C)

Disease associations

OMIM: gene MIM:109685 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

StudyTraitp-value
GCST004744_25Lung adenocarcinoma6.000000e-06
GCST008170_5Thyroglobulin plasma levels3.000000e-06
GCST009391_1455Metabolite levels6.000000e-06
GCST009391_1465Metabolite levels5.000000e-06
GCST009391_1469Metabolite levels1.000000e-06

EFO canonical traits (4, from GWAS)

EFO IDTrait name
EFO:0010050thyroglobulin measurement
EFO:0010405triacylglycerol 48:2 measurement
EFO:0010406triacylglycerol 48:3 measurement
EFO:0010407triacylglycerol 48:4 measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2789 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 238,593 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL140CURCUMIN393,882
CHEMBL50QUERCETIN374,559
CHEMBL44GENISTEIN244,212
CHEMBL150KAEMPFEROL125,940

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 1.-.-.- Oxidoreductases

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

LigandActionAffinityParameter
compound 24 [PMID: 31343176]Inhibition8.21pIC50

Binding affinities (BindingDB)

72 measured of 85 human assays (85 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
3-methoxy-5-(6-methoxynaphthalen-2-yl)-N-phenylbenzamideIC507 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
N-[2-methoxy-4-(6-methoxynaphthalen-2-yl)phenyl]acetamideIC5010 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
6-(3-hydroxyphenyl)-1-(4-morpholin-4-ylphenyl)naphthalen-2-olIC5020 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
4-[4-[2-hydroxy-6-(3-hydroxyphenyl)naphthalen-1-yl]anilino]-4-oxobutanoic acidIC5020 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
N-[3-[2-hydroxy-6-(3-hydroxyphenyl)naphthalen-1-yl]phenyl]methanesulfonamideIC5023 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
(E)-3-[3-methoxy-5-(6-methoxynaphthalen-2-yl)phenyl]-N-methylprop-2-enamideIC5030 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
US8546392, 68IC5039 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
N-[3-[2-hydroxy-6-(3-hydroxyphenyl)naphthalen-1-yl]phenyl]acetamideIC5040 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
3-[3-methoxy-5-(6-methoxynaphthalen-2-yl)phenyl]-N-methylpropanamideIC5050 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
3-methoxy-5-(6-methoxynaphthalen-2-yl)-N-methylbenzamideIC5050 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
4-[2-(3-hydroxyphenyl)-1,3-thiazol-5-yl]phenolIC5050 nM
3-[5-(4-hydroxyphenyl)thiophen-2-yl]phenolIC5069 nM
ethyl (E)-3-[2-methoxy-6-(3-methoxyphenyl)naphthalen-1-yl]prop-2-enoateIC5070 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
3-[4-(4-hydroxyphenyl)thiophen-2-yl]phenolIC5077 nM
3-[2-methoxy-6-(3-methoxyphenyl)naphthalen-1-yl]-N-(1,3-thiazol-2-yl)benzenesulfonamideIC5090 nMUS-8546392: 17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
3-[5-(3-hydroxyphenyl)pyridin-2-yl]phenolIC50101 nM
4-[4-(3-hydroxyphenyl)thiophen-2-yl]phenolIC50151 nM
3-[5-(3-hydroxyphenyl)-1,2,4-thiadiazol-3-yl]phenolIC50169 nM
3-[5-(3-hydroxyphenyl)thiophen-2-yl]phenolIC50173 nM
3-[4-(3-hydroxyphenyl)phenyl]phenolIC50173 nM
3-[4-(3-hydroxyphenyl)thiophen-2-yl]phenolIC50185 nM
cid_269792IC50201 nM
3-[2-(3-hydroxyphenyl)-1,3-thiazol-5-yl]phenolIC50243 nM
4,6-dichloro-5-hydroxy-N-[1-methyl-4-[[2-(trifluoromethyl)phenyl]methylcarbamoyl]pyrazol-3-yl]pyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-5-hydroxy-N-[1-methyl-3-[[2-(trifluoromethoxy)phenyl]methylcarbamoyl]pyrazol-4-yl]pyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-5-hydroxy-N-[1-methyl-5-[[2-(trifluoromethoxy)phenyl]methylcarbamoyl]pyrazol-4-yl]pyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
3-[(3,5-dichloro-4-hydroxybenzoyl)amino]-1-methyl-N-[[2-(trifluoromethyl)phenyl]methyl]pyrazole-4-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
3-[(3,5-dichloro-4-hydroxybenzoyl)amino]-1-phenyl-N-[[2-(trifluoromethyl)phenyl]methyl]pyrazole-4-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-5-hydroxy-N-[8-methyl-4-oxo-3-[[2-(trifluoromethyl)phenyl]methyl]-1,2,3-benzotriazin-5-yl]pyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-N-[8-fluoro-4-oxo-3-[[2-(trifluoromethyl)phenyl]methyl]-1,2,3-benzotriazin-5-yl]-5-hydroxypyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
3,5-dichloro-N-[2,8-dimethyl-4-oxo-3-[2-[2-(trifluoromethyl)phenyl]cyclobutyl]quinazolin-5-yl]-4-hydroxybenzamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-N-[1-ethyl-2,4-dioxo-3-[[2-(trifluoromethyl)phenyl]methyl]quinazolin-5-yl]-5-hydroxypyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-N-[8-fluoro-1-methyl-2,4-dioxo-3-[[2-(trifluoromethyl)phenyl]methyl]quinazolin-5-yl]-5-hydroxypyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-5-hydroxy-N-[1-methyl-2,4-dioxo-3-[[2-(trifluoromethyl)phenyl]methyl]quinazolin-5-yl]pyridine-2-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
5-[(3,5-dichloro-4-hydroxybenzoyl)amino]-2-methyl-N-[[2-(trifluoromethoxy)phenyl]methyl]-1,3-thiazole-4-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
5-[(4,6-dichloro-5-hydroxypyridine-2-carbonyl)amino]-2-methyl-N-[[2-(trifluoromethoxy)phenyl]methyl]-1,3-thiazole-4-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
5-[(4,6-dichloro-5-hydroxypyridine-2-carbonyl)amino]-N-[1-[2-(trifluoromethyl)phenyl]cyclopropyl]-1,3-thiazole-4-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
5-[(4,6-dichloro-5-hydroxypyridine-2-carbonyl)amino]-N-methyl-N-[[2-(trifluoromethyl)phenyl]methyl]-1,3-thiazole-4-carboxamideIC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
5-(4,6-dichloro-5-IC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
5-(3,5-dichloro-4-IC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
N-(adamantan-1-ylmethyl)-5-IC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
N-(benzo[d][1,3]dioxol-5-IC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
N-(chroman-4-yl)-5-(4,6-IC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF
4,6-dichloro-5-hydroxy-N-(1-IC50300 nMUS-20250100993: 2-SUBSTITUTED THIAZOLE HSD17B13 INHIBITORS AND USES THEREOF

ChEMBL bioactivities

669 potent at pChembl≥5 of 762 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.70IC500.2nMCHEMBL4457145
9.70IC500.2nMCHEMBL4529443
9.49IC500.32nMCHEMBL4293115
9.40IC500.4nMCHEMBL4546082
9.40IC500.4nMCHEMBL4464314
9.22IC500.6nMCHEMBL4513439
9.20IC500.63nMCHEMBL4295076
9.07IC500.85nMCHEMBL4276934
9.05IC500.9nMCHEMBL4574253
9.00IC501nMCHEMBL4585585
8.96IC501.1nMCHEMBL4293119
8.96IC501.1nMCHEMBL4284771
8.96IC501.1nMCHEMBL4287575
8.96IC501.1nMCHEMBL4466918
8.92IC501.2nMCHEMBL4441152
8.89IC501.3nMCHEMBL4286251
8.89IC501.3nMCHEMBL4292910
8.85IC501.4nMCHEMBL4092593
8.85IC501.4nMCHEMBL4459275
8.85IC501.4nMCHEMBL4552641
8.80IC501.6nMCHEMBL4283851
8.74IC501.8nMCHEMBL4283199
8.74IC501.8nMCHEMBL4450585
8.70IC502nMCHEMBL4285743
8.66IC502.2nMCHEMBL4276985
8.64IC502.3nMCHEMBL4290218
8.64IC502.3nMCHEMBL4291052
8.62IC502.4nMCHEMBL4285743
8.59IC502.6nMCHEMBL4291714
8.57IC502.7nMCHEMBL3629589
8.57IC502.7nMCHEMBL4286141
8.54IC502.9nMCHEMBL4447938
8.54IC502.9nMCHEMBL4443578
8.51IC503.1nMCHEMBL4286097
8.47IC503.4nMCHEMBL4277596
8.47IC503.4nMCHEMBL4584616
8.44IC503.6nMCHEMBL4450450
8.43IC503.7nMCHEMBL3629588
8.42IC503.8nMCHEMBL4282320
8.40IC504nMCHEMBL4279043
8.39IC504.1nMCHEMBL4088890
8.39IC504.1nMCHEMBL4519484
8.36IC504.4nMCHEMBL4278956
8.36IC504.4nMCHEMBL4462505
8.35IC504.5nMCHEMBL4282780
8.32IC504.8nMCHEMBL4439604
8.28IC505.2nMCHEMBL4289526
8.28IC505.2nMCHEMBL4470668
8.27IC505.4nMCHEMBL4280913
8.27IC505.4nMCHEMBL4277362

PubChem BioAssay actives

649 with measured affinity, of 1566 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.

CompoundAssayTypeValueUnit
4-methyl-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0002uM
3-methyl-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0002uM
[5-(4-hydroxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0003uM
3-chloro-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0004uM
4-chloro-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0004uM
[5-(2-hydroxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0006uM
N-[2,4-difluoro-5-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]-4-fluorobenzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0006uM
(5-phenylthiophen-2-yl)-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0008uM
N-[3-[5-(2-chloro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0009uM
4-fluoro-N-[2-methyl-5-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0010uM
[5-(3-hydroxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0011uM
[5-(2-methoxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0011uM
[5-(1H-indol-4-yl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0011uM
2-cyano-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0011uM
4-fluoro-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0012uM
[5-(4-hydroxy-3,5-dimethylphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0013uM
[5-(1H-indol-5-yl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0013uM
[5-(2,4-difluorophenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0014uM
N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]-2-(trifluoromethyl)benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0014uM
3-cyano-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0014uM
[5-(3,5-dichloro-4-methoxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0016uM
[5-(3-methoxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0018uM
4-bromo-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]-2-(trifluoromethoxy)benzenesulfonamide1601559: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0018uM
N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]-2-(trifluoromethoxy)benzenesulfonamide1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0020uM
[5-(3-amino-4,5-difluorophenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0022uM
[5-(4-methoxy-3,5-dimethylphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0023uM
[5-(4-methoxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0023uM
[5-(3-chloro-4-hydroxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0026uM
N-[3-[5-(2,6-difluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]-1-methylimidazole-4-sulfonamide1252529: Inhibition of human placental microsomal 17beta HSD2 using unlabeled- and labelled [2,4,6,7-3H]-E2 as substrate incubated for 20 mins by HPLC analysisic500.0027uM
[5-(3-fluoro-4-hydroxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0027uM
4-fluoro-N-[2-fluoro-5-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0029uM
4-cyano-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0029uM
(5-quinolin-7-ylthiophen-2-yl)-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0031uM
[5-(3-amino-4-hydroxyphenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0034uM
6-chloro-N-[2,4-difluoro-5-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]pyridine-3-sulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0034uM
N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]methanesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0036uM
N-[3-[5-(2,6-difluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]pyridine-3-sulfonamide1252529: Inhibition of human placental microsomal 17beta HSD2 using unlabeled- and labelled [2,4,6,7-3H]-E2 as substrate incubated for 20 mins by HPLC analysisic500.0037uM
[5-(1H-indol-6-yl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0038uM
[5-(2-aminophenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0040uM
1-methyl-N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]imidazole-4-sulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0041uM
[2-[5-(2,6-difluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl] sulfamate1482689: Inhibition of human placental cytosolic 17beta-HSD2 using [3H]-E2/E2 substrate and NAD+ after 20 mins by HPLC based radio-detection methodic500.0041uM
[5-[3-(hydroxymethyl)phenyl]thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0044uM
4-fluoro-N-[4-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0044uM
N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]acetamide1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0045uM
N-[3-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]cyclopropanesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0048uM
[5-(3H-benzimidazol-5-yl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0052uM
4-cyano-N-[2,4-difluoro-5-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]benzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0052uM
[5-(3-aminophenyl)thiophen-2-yl]-(2,4,5-trifluoro-3-hydroxyphenyl)methanone1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0054uM
3-[5-(2,3,4-trifluoro-5-hydroxybenzoyl)thiophen-2-yl]benzamide1415113: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysisic500.0054uM
N-[2,3-difluoro-5-[5-(2,4,5-trifluoro-3-hydroxybenzoyl)thiophen-2-yl]phenyl]-4-fluorobenzenesulfonamide1564134: Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysisic500.0055uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Estradiolincreases expression, decreases expression, affects metabolic processing, increases chemical synthesis, affects binding (+2 more)6
Tetrachlorodibenzodioxinaffects expression, increases expression4
Cyclosporinedecreases expression4
bisphenol Aincreases expression, decreases expression, decreases reaction3
Acetaminophendecreases expression, increases expression3
Benzo(a)pyreneaffects methylation, decreases expression, increases expression, increases methylation3
Calcitriolincreases expression, increases reaction, affects cotreatment3
Progesteroneaffects cotreatment, increases expression, decreases expression3
Cadmium Chlorideincreases expression, decreases expression3
sodium arseniteaffects methylation, decreases expression2
(+)-JQ1 compoundaffects cotreatment, decreases expression2
Arsenicaffects methylation, increases abundance, increases expression2
Testosteroneaffects metabolic processing, affects cotreatment, increases expression2
Tobacco Smoke Pollutiondecreases expression, increases expression2
8-Bromo Cyclic Adenosine Monophosphatedecreases reaction, increases expression2
Aflatoxin B1affects expression, decreases methylation2
Particulate Matterincreases abundance, increases expression2
2-methoxyestronedecreases activity, increases chemical synthesis, increases metabolic processing1
2,4,6-tribromophenoldecreases expression1
methyleugenoldecreases expression1
lead acetateincreases expression1
sodium arsenateincreases abundance, increases expression1
acetoacetyl CoAaffects binding1
decabromobiphenyl etherdecreases expression1
1’-hydroxyestragoleincreases oxidation1
3,4-dichloroanilineincreases expression1
beta-lapachoneincreases expression1
zinc chromateincreases abundance, increases expression1
dienogestdecreases expression1
cupric chlorideincreases expression1

ChEMBL screening assays

113 unique, capped per target: 109 binding, 2 admet, 2 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1032439BindingInhibition of human placental microsomal 17beta-HSD2Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). — J Med Chem
CHEMBL4051804ADMETInhibition of human placental cytosolic 17beta-HSD2 using [3H]-E2/E2 substrate and NAD+ after 20 mins by HPLC based radio-detection methodFirst Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases. — J Med Chem
CHEMBL864129FunctionalInhibition of 17-beta HSD2 in MDA-MB231cells at 10 uMModification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. — J Med Chem

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 81

This page pulls from 81 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot