HSD11B1

Summary

HSD11B1 (hydroxysteroid 11-beta dehydrogenase 1, HGNC:5208) is a protein-coding gene on chromosome 1q32.2, encoding 11-beta-hydroxysteroid dehydrogenase 1 (P28845). Controls the reversible conversion of biologically active glucocorticoids such as cortisone to cortisol, and 11-dehydrocorticosterone to corticosterone in the presence of NADP(H).

The protein encoded by this gene is a microsomal enzyme that catalyzes the conversion of the stress hormone cortisol to the inactive metabolite cortisone. In addition, the encoded protein can catalyze the reverse reaction, the conversion of cortisone to cortisol. Too much cortisol can lead to central obesity, and a particular variation in this gene has been associated with obesity and insulin resistance in children. Mutations in this gene and H6PD (hexose-6-phosphate dehydrogenase (glucose 1-dehydrogenase)) are the cause of cortisone reductase deficiency. Alternate splicing results in multiple transcript variants encoding the same protein.

Source: NCBI Gene 3290 — RefSeq curated summary.

At a glance

• Gene–disease (curated): cortisone reductase deficiency 2 (Moderate, GenCC) — +1 more curated relationship
• GWAS associations: 1
• Clinical variants (ClinVar): 33 total — 2 pathogenic
• Phenotypes (HPO): 19
• Druggable target: yes — 13 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_005525

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:5208
Approved symbol	HSD11B1
Name	hydroxysteroid 11-beta dehydrogenase 1
Location	1q32.2
Locus type	gene with protein product
Status	Approved
Aliases	SDR26C1
Ensembl gene	ENSG00000117594
Ensembl biotype	protein_coding
OMIM	600713
Entrez	3290

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 6 protein_coding

ENST00000261465, ENST00000367027, ENST00000367028, ENST00000615289, ENST00000890352, ENST00000966146

RefSeq mRNA: 3 — MANE Select: NM_005525 NM_001206741, NM_005525, NM_181755

CCDS: CCDS1489

Canonical transcript exons

ENST00000367027 — 6 exons

Exon	Start	End
ENSE00000792110	209705811	209705941
ENSE00000792111	209706709	209706820
ENSE00000792112	209706943	209707128
ENSE00000792113	209732436	209732579
ENSE00001068294	209734304	209734929
ENSE00001443285	209704846	209705030

Expression profiles

Bgee: expression breadth ubiquitous, 233 present calls, max score 99.34.

FANTOM5 (CAGE): breadth broad, TPM avg 11.0995 / max 766.3118, expressed in 663 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
8348	8.9920	606
8350	1.5060	349
8349	0.4334	179
8346	0.1190	42
8347	0.0492	23

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
decidua	UBERON:0002450	99.34	gold quality
right lobe of liver	UBERON:0001114	98.82	gold quality
liver	UBERON:0002107	97.20	gold quality
islet of Langerhans	UBERON:0000006	94.42	gold quality
upper leg skin	UBERON:0004262	93.66	gold quality
right ovary	UBERON:0002118	93.24	gold quality
left ovary	UBERON:0002119	92.93	gold quality
urethra	UBERON:0000057	91.65	gold quality
right lung	UBERON:0002167	91.64	gold quality
stromal cell of endometrium	CL:0002255	91.24	gold quality
upper lobe of left lung	UBERON:0008952	91.01	gold quality
upper lobe of lung	UBERON:0008948	90.36	gold quality
skin of abdomen	UBERON:0001416	88.86	gold quality
upper arm skin	UBERON:0004263	88.64	gold quality
placenta	UBERON:0001987	87.92	gold quality
zone of skin	UBERON:0000014	87.84	gold quality
skin of leg	UBERON:0001511	87.78	gold quality
mammalian vulva	UBERON:0000997	87.44	gold quality
ovary	UBERON:0000992	86.53	gold quality
subcutaneous adipose tissue	UBERON:0002190	85.55	gold quality
adipose tissue	UBERON:0001013	84.76	gold quality
left coronary artery	UBERON:0001626	84.32	gold quality
metanephros cortex	UBERON:0010533	84.19	gold quality
calcaneal tendon	UBERON:0003701	83.93	gold quality
connective tissue	UBERON:0002384	83.87	gold quality
lung	UBERON:0002048	83.77	gold quality
smooth muscle tissue	UBERON:0001135	83.67	gold quality
prostate gland	UBERON:0002367	83.14	gold quality
coronary artery	UBERON:0001621	82.79	gold quality
mucosa of stomach	UBERON:0001199	82.72	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-CURD-7	yes	483.35
E-ENAD-21	yes	414.56
E-ANND-3	yes	19.94
E-MTAB-7249	yes	8.95
E-GEOD-83139	yes	6.92

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, CEBPB, CEBPG, GLI1, NFKB, NR1H3, NR3C1, PPARG, RELA, RXRA

miRNA regulators (miRDB)

46 targeting HSD11B1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-450B-5P	99.92	71.48	3175
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-LET-7A-2-3P	99.87	70.53	1921
HSA-MIR-579-3P	99.86	71.66	3628
HSA-LET-7G-3P	99.85	70.43	1929
HSA-MIR-664B-3P	99.84	71.65	3590
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-561-3P	99.64	70.90	3647
HSA-MIR-142-5P	99.48	70.92	2416
HSA-MIR-5590-3P	99.48	70.91	2429
HSA-MIR-582-5P	99.47	70.79	2635
HSA-MIR-513A-3P	99.39	70.63	3620
HSA-MIR-513C-3P	99.39	70.63	3620
HSA-MIR-3140-5P	99.39	69.04	1136
HSA-MIR-410-3P	99.27	69.98	2457
HSA-MIR-6797-3P	99.17	66.94	668
HSA-MIR-3606-3P	99.11	69.84	3254
HSA-MIR-376A-3P	99.06	69.17	1128
HSA-MIR-376B-3P	99.06	69.17	1128
HSA-MIR-330-5P	98.73	67.63	1788
HSA-MIR-4501	98.72	67.19	921
HSA-MIR-6796-3P	98.68	65.49	689
HSA-MIR-4700-5P	98.63	67.43	1915
HSA-MIR-6076	98.61	65.69	637

Literature-anchored findings (GeneRIF, showing 40)

• Effect of cellular differentiation on 11beta-hydroxysteroid dehydrogenase activity in the intestine (PMID:11755176)
• Human adrenal cortex and aldosterone secreting adenomas express both 11beta-hydroxysteroid dehydrogenase type 1 and type 2 genes. (PMID:11956655)
• 11beta-Hydroxysteroid dehydrogenase types 1 and 2 are up- and downregulated in cortisol-secreting adrenal adenomas. (PMID:12109593)
• cultured human ovarian surface epithelium (HOSE) cells express IL-1-responsive 11betaHSD1 mRNA (PMID:12202416)
• There is colocalization of 11beta-HSD1 and GR in the chorionic trophoblast. By binding to GR, glucocorticoids induce the expression of 11beta-HSD1 by a possible intracrine mechanism. (PMID:12390875)
• Acts as dehydrogenase inactivating cortisol to cortisone. 11beta-HSD1 dehydrogenase activity in “uncommitted” omental preadipocytes may provide autocrine mechanism to protect preadipocytes from differentiation, facilitating proliferation. (PMID:12530648)
• May regulate levels of glucocorticoids. Plasma cortisol levels could be predicted by a model incorporating adrenal HSD11B2 and tumor size. (PMID:12530692)
• Higher adipose 11-HSD1 activity is associated with features of metabolic syndrome. (PMID:12788882)
• Mutations in the genes encoding 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase interact to cause cortisone reductase deficiency. (PMID:12858176)
• 11beta-HSD1 activity may predict individual susceptibility to glucocorticoid-induced osteoporosis (PMID:12915682)
• idiopathic obesity is associated with transcriptional up-regulation of 11HSD1 in adipose tissue (PMID:12915696)
• glucocorticoids can positively induce 11beta-HSD1 expression in amnion fibroblasts, an effect further strengthened by proinflammatory cytokines. (PMID:12960005)
• increases in 11beta-HSD 1 expression/activity by intrauterine membranes during late gestation may result in increased potential for a local increase in fetal membranes should be considered as an extraadrenal source of cortisol during late gestation. (PMID:14557491)
• REVIEW: role in cortisol metabolism and visceral obesity (PMID:14682470)
• data suggest increased expression of the 11beta-HSD1 gene is associated with metabolic abnormalities in obese women and that increased expression may contribute to increased local conversion of cortisone to cortisol in adipose tissue of obese individuals (PMID:14742837)
• Data report on the in vitro oxysterol-metabolizing properties of human and rodent 11beta-hydroxysteroid dehydrogenase. (PMID:15095019)
• role of the N-terminal region on enzymatic activity and the relevance of 11beta-HSD1 orientation into the endoplasmic reticulum lumen (PMID:15152005)
• P.1088: “…genetic variations in the HSD11B1 gene were associated with Type 2 diabetes mellitus, plasma insulin concentrations and insulin action, independent of obesity.” (PMID:15156315)
• Decrease of 11betaHSD1 mRNA abundance and enzyme activity is associated with colorectal cancer (PMID:15172126)
• Decreased 11betaHSD1 activity and expression in obesity may act as a compensatory mechanism to enhance insulin sensitivity through a reduction in tissue-specific cortisol concentrations. (PMID:15181046)
• Hexose-6-phosphate dehydrogenase directly determines the reaction direction of 11beta-Hydroxysteroid dehydrogenase1 in intact cells as an oxoreductase. (PMID:15280030)
• The current study provides additional evidence that variability at the 11[beta]HSD1 gene begets the development of hypertension and that over the years changes in the environment have modified the effect of 11[beta]HSD1 on blood pressure in Pima Indians. (PMID:15452033)
• HIV patients treated with HAART showewd an increase in mRNA of this enzyme in adipose tissue, correlated with insulin resistance. (PMID:15455200)
• crystal structure of human 11beta-hydroxysteroid dehydrogenase type I (PMID:15513927)
• a molecular switch during osteoblast differentiation controls 11beta-Hydroxysteroid dehydrogenase expression and glucocorticoid synthesis (PMID:15591536)
• The portal vein delivers cortisol to the liver, and inhibition of 11HSD1 in visceral adipose tissue may be valuable in ameliorating insulin resistance in obesity. (PMID:15855321)
• monocyte-derived DCs are able to generate cortisol as a consequence of up-regulated 11beta-HSD1 expression. Immature DCs demonstrate selective enhancement of 11beta-HSD1 activity, leading to increased conversion of inactive cortisone to active cortisol. (PMID:15941907)
• 11beta-HSD1 has a role in the metabolism of xenobiotic carbonyl compounds. (PMID:16343739)
• Somatotropin treatment is able to decrease 11beta-HSD1 mRNA and increase 11beta-HSD2 and accordingly may be able to reduce the amount of locally produced cortisol in adipose tissue. (PMID:16368752)
• There was up-regulated expression of 11betaHSD-1 at menstruation and in first trimester decidua. (PMID:16406280)
• ER-lumenal orientation of 11beta-HSD1 is essential for the metabolism of the alternative substrate 7-ketocholesterol (7KC), a major cholesterol oxidation product found in atherosclerotic plaques and taken up from processed cholesterol-rich food. (PMID:16412558)
• cortisol up-regulates 11beta-HSD1 expression through induction of promoter activity, and the effect is enhanced by IL-1beta (PMID:16469798)
• The hydroxyl side chain of Y177 is likely involved with hyrogen bonding with the 3-hydroxy group of A ring of glycyrrhetinic acid. (PMID:16580270)
• is a steroid oxidoreductase able to use and produce 7alpha- and 7beta-hydroxy-DHEA through an oxidoreduction process generating the 7-oxo-DHEA intermediate (PMID:16603347)
• 11HSD1 is altered in a tissue-specific manner with reduced levels in liver but elevated levels in adipose tissue. Some polymorphisms have been demonstrated in intronic and upstream regions of the HSD11B1 gene. (PMID:16622297)
• Results strengthen the importance of 11beta-HSD-1 in obesity and its associated complications and suggest the need of clinical studies with specific 11beta-HSD-1 inhibitors. (PMID:16855188)
• the lack of increase of 11beta-HSD1 expression in Cushing’s syndrome could suggest downregulation of the enzyme as a result of long-term overstimulatio (PMID:16914598)
• Results suggest that gene expression modulation by glucocorticoids is under a decisive influence of target cell 11beta-hydroxysteroid dehydrogenase-1 that modulates the intracellular concentration of active glucocorticoids. (PMID:16996097)
• HSD11B1’s expression pattern in subcutaneous and omental adipose tissues. (PMID:17032748)
• Y280 is not involved in substrate binding but rather plays a selective role in inhibitor binding. The involvement of Y280 in inhibitor binding depends on the inhibitor chemical structure. (PMID:17306259)

Cross-species orthologs

17 orthologs

Organism	Symbol	Gene ID
danio_rerio	zgc:163083	ENSDARG00000099873
danio_rerio	zgc:92161	ENSDARG00000101749
danio_rerio	zgc:123284	ENSDARG00000102720
danio_rerio	zgc:112146	ENSDARG00000104829
mus_musculus	Hsd11b1	ENSMUSG00000016194
drosophila_melanogaster	CG7601	FBGN0027583
drosophila_melanogaster	CG31546	FBGN0051546
drosophila_melanogaster	CG31548	FBGN0051548
caenorhabditis_elegans		WBGENE00000970
caenorhabditis_elegans		WBGENE00000975
caenorhabditis_elegans		WBGENE00000981
caenorhabditis_elegans		WBGENE00000993
caenorhabditis_elegans		WBGENE00008985
caenorhabditis_elegans		WBGENE00008986
caenorhabditis_elegans		WBGENE00011424
caenorhabditis_elegans		WBGENE00022809
caenorhabditis_elegans		WBGENE00219274

Paralogs (13): RDH8 (ENSG00000080511), DHRS7 (ENSG00000100612), DHRS2 (ENSG00000100867), DHRS7B (ENSG00000109016), HSDL2 (ENSG00000119471), DHRS4 (ENSG00000157326), DHRS1 (ENSG00000157379), CBR1 (ENSG00000159228), CBR3 (ENSG00000159231), HSD11B1L (ENSG00000167733), DHRS7C (ENSG00000184544), DHRS4L2 (ENSG00000187630), DHRS11 (ENSG00000278535)

Protein

Protein identifiers

11-beta-hydroxysteroid dehydrogenase 1 — P28845 (reviewed: P28845)

Alternative names: 7-oxosteroid reductase, Corticosteroid 11-beta-dehydrogenase isozyme 1, Short chain dehydrogenase/reductase family 26C member 1

All UniProt accessions (4): A0A087WU76, A0A0A0MQV1, P28845, X5D2L1

UniProt curated annotations — full annotation on UniProt →

Function. Controls the reversible conversion of biologically active glucocorticoids such as cortisone to cortisol, and 11-dehydrocorticosterone to corticosterone in the presence of NADP(H). Participates in the corticosteroid receptor-mediated anti-inflammatory response, as well as metabolic and homeostatic processes. Plays a role in the secretion of aqueous humor in the eye, maintaining a normotensive, intraocular environment. Bidirectional in vitro, predominantly functions as a reductase in vivo, thereby increasing the concentration of active glucocorticoids. It has broad substrate specificity, besides glucocorticoids, it accepts other steroid and sterol substrates. Interconverts 7-oxo- and 7-hydroxy-neurosteroids such as 7-oxopregnenolone and 7beta-hydroxypregnenolone, 7-oxodehydroepiandrosterone (3beta-hydroxy-5-androstene-7,17-dione) and 7beta-hydroxydehydroepiandrosterone (3beta,7beta-dihydroxyandrost-5-en-17-one), among others. Catalyzes the stereo-specific conversion of the major dietary oxysterol, 7-ketocholesterol (7-oxocholesterol), into the more polar 7-beta-hydroxycholesterol metabolite. 7-oxocholesterol is one of the most important oxysterols, it participates in several events such as induction of apoptosis, accumulation in atherosclerotic lesions, lipid peroxidation, and induction of foam cell formation. Mediates the 7-oxo reduction of 7-oxolithocholate mainly to chenodeoxycholate, and to a lesser extent to ursodeoxycholate, both in its free form and when conjugated to glycine or taurine, providing a link between glucocorticoid activation and bile acid metabolism. Catalyzes the synthesis of 7-beta-25-dihydroxycholesterol from 7-oxo-25-hydroxycholesterol in vitro, which acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration.

Subunit / interactions. Homodimer.

Subcellular location. Endoplasmic reticulum membrane.

Tissue specificity. Widely expressed, highest expression in liver, lower in testis, ovary, lung, foreskin fibroblasts, and much lower in kidney. Expressed in liver (at protein level). Expressed in the basal cells of the corneal epithelium and in the ciliary nonpigmented epithelium (both at mRNA and at protein level).

Post-translational modifications. Glycosylated.

Disease relevance. Cortisone reductase deficiency 2 (CORTRD2) [MIM:614662] An autosomal dominant error of cortisone metabolism characterized by a failure to regenerate cortisol from cortisone, resulting in increased cortisol clearance, activation of the hypothalamic- pituitary axis and ACTH-mediated adrenal androgen excess. Clinical features include hyperandrogenism resulting in hirsutism, oligo- amenorrhea, and infertility in females and premature pseudopuberty in males. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. Hexose-6-phosphate dehydrogenase (H6PD) provides cosubstrate NADPH, and the glucose-6-phosphate transporter in the ER-membrane supplies the substrate for H6PDH, their activities stimulate the reduction of cortisone and abolish the oxidation of cortisol.

Pathway. Steroid metabolism.

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

RefSeq proteins (3): NP_001193670, NP_005516, NP_861420 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002347	SDR_fam	Family
IPR020904	Sc_DH/Rdtase_CS	Conserved_site
IPR036291	NAD(P)-bd_dom_sf	Homologous_superfamily
IPR051253	11-beta-HSD	Family

Pfam: PF00106

Enzyme classification (BRENDA):

• EC 1.1.1.146 — 11beta-hydroxysteroid dehydrogenase (BRENDA: 26 organisms, 286 substrates, 1331 inhibitors, 120 Km, 10 kcat entries)
• EC 1.1.1.B40 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
CORTISONE	0.0003–0.193	16
CORTISOL	0.0002–0.1	14
11BETA,17,21-TRIHYDROXY-PREGN-4-ENE-3,20-DIONE	0.0014–0.027	9
11BETA,21-DIHYDROXYPREGN-4-EN-3,20-DIONE	—	9
CORTICOSTERONE	0.0003–0.043	8
11-DEHYDROCORTICOSTERONE	0.0002–0.0073	7
17,21-DIHYDROXY-PREGN-4-ENE-3,11,20-TRIONE	0.0038–0.0095	6
NADP+	—	6
7BETA-HYDROXYCHOLESTEROL	0.0007–3.5	5
21-HYDROXY-PREGN-4-EN-3,11,20-TRIONE	0.0014–0.0028	4
7-OXOCHOLESTEROL	0.0004–0.0005	3
NADPH	0.0036–0.0037	3
11BETA-HYDROXYPROGESTERONE	—	2
11BETA-HYDROXYTESTOSTERONE	0.0001	2
5,5-DIMETHYL-3-(3-FLUORPHENYL)-4-(4-METHYLSULPHO	0.581–0.961	2

Catalyzed reactions (Rhea), 12 shown:

• an 11beta-hydroxysteroid + NADP(+) = an 11-oxosteroid + NADPH + H(+) (RHEA:11388)
• a 7beta-hydroxysteroid + NADP(+) = a 7-oxosteroid + NADPH + H(+) (RHEA:20233)
• corticosterone + NADP(+) = 11-dehydrocorticosterone + NADPH + H(+) (RHEA:42200)
• 7-oxolithocholate + NADPH + H(+) = ursodeoxycholate + NADP(+) (RHEA:47540)
• chenodeoxycholate + NADP(+) = 7-oxolithocholate + NADPH + H(+) (RHEA:53820)
• glycochenodeoxycholate + NADP(+) = 7-oxoglycolithocholate + NADPH + H(+) (RHEA:65056)
• taurochenodeoxycholate + NADP(+) = 7-oxotaurolithocholate + NADPH + H(+) (RHEA:65060)
• cortisone + NADPH + H(+) = cortisol + NADP(+) (RHEA:68616)
• 7-oxocholesterol + NADPH + H(+) = 7beta-hydroxycholesterol + NADP(+) (RHEA:68656)
• glycoursodeoxycholate + NADP(+) = 7-oxoglycolithocholate + NADPH + H(+) (RHEA:68976)
• tauroursodeoxycholate + NADP(+) = 7-oxotaurolithocholate + NADPH + H(+) (RHEA:68980)
• 7-oxopregnenolone + NADPH + H(+) = 7beta-hydroxypregnenolone + NADP(+) (RHEA:69436)

UniProt features (53 total): mutagenesis site 15, helix 15, strand 8, binding site 6, glycosylation site 3, topological domain 2, chain 1, sequence variant 1, transmembrane region 1, active site 1

Structure

Experimental structures (PDB)

42 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
1XU9	X-RAY DIFFRACTION	1.55
1XU7	X-RAY DIFFRACTION	1.8
3TFQ	X-RAY DIFFRACTION	1.8
2RBE	X-RAY DIFFRACTION	1.9
4C7K	X-RAY DIFFRACTION	1.91
4K1L	X-RAY DIFFRACTION	1.96
5PGY	X-RAY DIFFRACTION	2.07
2BEL	X-RAY DIFFRACTION	2.11
4C7J	X-RAY DIFFRACTION	2.16
3H6K	X-RAY DIFFRACTION	2.19
4HX5	X-RAY DIFFRACTION	2.19
4BB5	X-RAY DIFFRACTION	2.2
3BZU	X-RAY DIFFRACTION	2.25
2ILT	X-RAY DIFFRACTION	2.3
3FRJ	X-RAY DIFFRACTION	2.3
3HFG	X-RAY DIFFRACTION	2.3
3PDJ	X-RAY DIFFRACTION	2.3
3CH6	X-RAY DIFFRACTION	2.35
3CZR	X-RAY DIFFRACTION	2.35
4IJU	X-RAY DIFFRACTION	2.35
4IJV	X-RAY DIFFRACTION	2.35
4IJW	X-RAY DIFFRACTION	2.35
5PGU	X-RAY DIFFRACTION	2.35
5PGV	X-RAY DIFFRACTION	2.35
5PGW	X-RAY DIFFRACTION	2.37
5QII	X-RAY DIFFRACTION	2.45
3D4N	X-RAY DIFFRACTION	2.5
5PGX	X-RAY DIFFRACTION	2.5
3D5Q	X-RAY DIFFRACTION	2.55
4BB6	X-RAY DIFFRACTION	2.55

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P28845-F1	94.34	0.86

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): 183 (proton acceptor)

Ligand- & substrate-binding residues (6): 218–222; 41–67; 92–93; 119–121; 170; 183–187

Glycosylation sites (3): 123, 162, 207

Mutagenesis-validated functional residues (15):

Position	Phenotype
5–6	predominantly inverted topology. no effect on activity.
5–6	inverted topology. reduced vmax.
5	predominantly inverted topology. no effect on activity.
5	inverted topology. no effect on activity.
6	no effect on topology. increased km for corticosterone.
6	no effect on topology or activity.
18–21	no effect on topology. reduced vmax.
18–21	no effect on topology or activity.
19–21	no effect on topology. reduced vmax.
25–26	inverted topology. reduced vmax.
25–26	no effect on topology. reduced vmax.
25–26	reduced vmax.
25	no effect on activity.
26	no effect on activity.
35–36	complete loss of activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-194002	Glucocorticoid biosynthesis
R-HSA-9757110	Prednisone ADME

MSigDB gene sets: 403 (showing top): MODULE_93, CCAWYNNGAAR_UNKNOWN, GAANYNYGACNY_UNKNOWN, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GRAESSMANN_RESPONSE_TO_MC_AND_SERUM_DEPRIVATION_UP, MAZ_Q6, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, AP4_Q6, GGGTGGRR_PAX4_03, LEE_LIVER_CANCER_CIPROFIBRATE_DN, CAGCTG_AP4_Q5, AACWWCAANK_UNKNOWN, NKX61_01, CAIRO_HEPATOBLASTOMA_CLASSES_DN

GO Biological Process (4): steroid catabolic process (GO:0006706), lung development (GO:0030324), lipid metabolic process (GO:0006629), steroid metabolic process (GO:0008202)

GO Molecular Function (7): steroid binding (GO:0005496), protein homodimerization activity (GO:0042803), 7-beta-hydroxysteroid dehydrogenase (NADP+) activity (GO:0047022), NADP binding (GO:0050661), 11-beta-hydroxysteroid dehydrogenase (NADP+) activity (GO:0070524), cortisol dehydrogenase (NADP+) activity (GO:0102196), oxidoreductase activity (GO:0016491)

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

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Metabolism of steroid hormones	1
Drug ADME	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
steroid dehydrogenase activity, acting on the CH-OH group of donors, NAD or NADP as acceptor	2
steroid metabolic process	1
lipid catabolic process	1
respiratory tube development	1
animal organ development	1
respiratory system development	1
primary metabolic process	1
lipid metabolic process	1
lipid binding	1
identical protein binding	1
protein dimerization activity	1
adenyl nucleotide binding	1
11-beta-hydroxysteroid dehydrogenase (NADP+) activity	1
catalytic activity	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
cellular anatomical structure	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

3895 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
HSD11B1	H6PD	O95479	916
HSD11B1	NR3C1	P04150	852
HSD11B1	SRD5A1	P18405	820
HSD11B1	NR3C2	P08235	801
HSD11B1	POMC	P01189	767
HSD11B1	AKR1D1	P51857	753
HSD11B1	CYP17A1	P05093	701
HSD11B1	HPGD	P15428	680
HSD11B1	SULT2A1	Q06520	646
HSD11B1	CYP11B1	P15538	626
HSD11B1	HSD3B1	P14060	619
HSD11B1	ADIPOQ	Q15848	606
HSD11B1	SERPINA6	P08185	593
HSD11B1	CYP11A1	P05108	587
HSD11B1	SRD5A2	P31213	580

IntAct

8 interactions, top by confidence:

A	B	Type	Score
HSD11B1	HSD11B1	psi-mi:“MI:0915”(physical association)	0.400
GKAP1	HSD11B1	psi-mi:“MI:0915”(physical association)	0.370
HSD11B1	TMBIM6	psi-mi:“MI:0914”(association)	0.350
ATG16L1	ESYT2	psi-mi:“MI:0914”(association)	0.350
ATG16L1		psi-mi:“MI:0914”(association)	0.350
HSD11B1	TOR1A	psi-mi:“MI:0914”(association)	0.350
HSD11B1	ACSL4	psi-mi:“MI:0914”(association)	0.350

BioGRID (28): DAD1 (Affinity Capture-MS), TMX2 (Affinity Capture-MS), UGT8 (Affinity Capture-MS), TMBIM6 (Affinity Capture-MS), GLB1L2 (Affinity Capture-MS), CDC42SE2 (Affinity Capture-MS), RAB18 (Affinity Capture-MS), NHLRC3 (Affinity Capture-MS), TOR1A (Affinity Capture-MS), FAM69A (Affinity Capture-MS), TMX4 (Affinity Capture-MS), MANEA (Affinity Capture-MS), HSD11B1 (Affinity Capture-MS), UGT8 (Affinity Capture-MS), NPTX1 (Affinity Capture-MS)

ESM2 similar proteins: A0A140FAN3, A1L1W4, A5PJF6, A5PJJ7, A7LB59, A7LB60, F1QLP1, O16881, P0DKC5, P0DKC6, P0DKC7, P16232, P28845, P50172, P51975, P70385, Q02337, Q02338, Q09851, Q10130, Q29608, Q3SXM5, Q4V8B7, Q5M875, Q5R7K0, Q5XGF7, Q5ZJG8, Q5ZJZ5, Q6AYS8, Q6DCT3, Q6NRV4, Q6P3L6, Q6QA32, Q6QLL4, Q6R0J2, Q7T2D1, Q80XN0, Q80ZF7, Q8BTX9, Q8HZJ8

Diamond homologs: A0A017SEY2, A0A023I4F1, A0A0C6DRT7, A0A1B7YCL6, A0A2P1DP77, A0A345BJN5, A0A482ND39, A0A4P8DJW5, A0A5B8YU33, A0AAW1NHX6, A2RVM0, B2X050, B6H062, B6HLP6, B8M9L2, C8V3Y7, D7UQ42, F4JJR8, G1XTZ5, G3Y422, G4MVZ5, G9N4A1, G9N4A6, I1S2J3, O48741, O75828, O80333, P00335, P0DXW2, P15428, P16232, P19992, P21218, P28845, P42317, P50199, P50203, P51975, P70684, P9WEF8

SIGNOR signaling

2 interactions.

A	Effect	B	Mechanism
CEBPA	“up-regulates quantity by expression”	HSD11B1	“transcriptional regulation”
CEBPB	“up-regulates quantity by expression”	HSD11B1	“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	0
Uncertain significance	22
Likely benign	0
Benign	4

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
31588	NM_005525.4(HSD11B1):c.409C>T (p.Arg137Cys)	Pathogenic
31589	NM_005525.4(HSD11B1):c.561G>T (p.Lys187Asn)	Pathogenic

SpliceAI

663 predictions. Top by Δscore:

Variant	Effect	Δscore
1:209706703:CTGCA:C	acceptor_loss	1.0000
1:209706704:TGCA:T	acceptor_loss	1.0000
1:209706705:GCAG:G	acceptor_loss	1.0000
1:209706706:CAG:C	acceptor_loss	1.0000
1:209706707:AGGT:A	acceptor_gain	1.0000
1:209706708:G:GC	acceptor_loss	1.0000
1:209706708:GGT:G	acceptor_gain	1.0000
1:209706708:GGTG:G	acceptor_gain	1.0000
1:209706809:G:GT	donor_gain	1.0000
1:209706810:A:T	donor_gain	1.0000
1:209706817:ATGGG:A	donor_loss	1.0000
1:209706818:TGGGT:T	donor_loss	1.0000
1:209706819:GG:G	donor_gain	1.0000
1:209706820:GG:G	donor_gain	1.0000
1:209706820:GGTGA:G	donor_loss	1.0000
1:209706821:G:GG	donor_gain	1.0000
1:209706821:G:T	donor_loss	1.0000
1:209706822:T:A	donor_loss	1.0000
1:209706937:TTGCA:T	acceptor_loss	1.0000
1:209706938:TGCAG:T	acceptor_loss	1.0000
1:209706939:GCAG:G	acceptor_loss	1.0000
1:209706941:A:AG	acceptor_gain	1.0000
1:209706942:G:GG	acceptor_gain	1.0000
1:209706942:G:GT	acceptor_loss	1.0000
1:209707000:A:AG	acceptor_gain	1.0000
1:209707000:AT:A	acceptor_gain	1.0000
1:209707000:ATGAT:A	acceptor_gain	1.0000
1:209707001:T:G	acceptor_gain	1.0000
1:209707001:T:TA	acceptor_gain	1.0000
1:209707004:T:TA	acceptor_gain	1.0000

AlphaMissense

1920 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:209705838:T:A	V39D	0.994
1:209707047:A:C	S146R	0.994
1:209707049:T:A	S146R	0.994
1:209707049:T:G	S146R	0.994
1:209732480:T:C	F188L	0.993
1:209732482:T:A	F188L	0.993
1:209732482:T:G	F188L	0.993
1:209732474:A:C	S186R	0.992
1:209732476:C:A	S186R	0.992
1:209732476:C:G	S186R	0.992
1:209705883:T:C	L54P	0.991
1:209732557:T:G	C213W	0.991
1:209706958:T:C	L116P	0.990
1:209705843:G:T	G41W	0.988
1:209705855:G:A	G45R	0.988
1:209705855:G:C	G45R	0.988
1:209707128:G:T	G173W	0.988
1:209732484:C:A	A189D	0.988
1:209732555:T:C	C213R	0.988
1:209707040:C:A	N143K	0.987
1:209707040:C:G	N143K	0.987
1:209734365:T:G	C241W	0.987
1:209707119:T:C	S170P	0.986
1:209705849:A:C	S43R	0.985
1:209705851:C:A	S43R	0.985
1:209705851:C:G	S43R	0.985
1:209705915:G:C	A65P	0.985
1:209706958:T:A	L116H	0.985
1:209732472:C:A	A185E	0.985
1:209705844:G:A	G41E	0.984

dbSNP variants (sampled 300 via entrez): RS1000057637 (1:209716811 G>A), RS1000120915 (1:209698901 C>T), RS1000130845 (1:209709251 T>C), RS1000220437 (1:209698424 T>C), RS1000222065 (1:209722737 A>G), RS1000246186 (1:209715800 G>A), RS1000282 (1:209721440 T>C), RS1000283 (1:209721316 G>A), RS1000333505 (1:209728419 T>C), RS1000336465 (1:209701600 C>T), RS1000349996 (1:209710225 A>G), RS1000391167 (1:209709562 A>C,G), RS1000398570 (1:209710687 T>C), RS1000520538 (1:209698167 T>TTAGG), RS1000530707 (1:209695188 C>T)

Disease associations

OMIM: gene MIM:600713 | disease phenotypes: MIM:258040, MIM:614662

GenCC curated gene-disease

Disease	Classification	Inheritance
cortisone reductase deficiency 2	Moderate	Autosomal dominant
cortisone reductase deficiency	Supportive	Autosomal dominant

Mondo (3): exstrophy-epispadias complex (MONDO:0017919), cortisone reductase deficiency 2 (MONDO:0013842), cortisone reductase deficiency (MONDO:0000193)

Orphanet (3): Exstrophy-epispadias complex (Orphanet:322), Cloacal exstrophy (Orphanet:93929), Hyperandrogenism due to cortisone reductase deficiency (Orphanet:168588)

HPO phenotypes

19 total (19 of 19 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000822	Hypertension
HP:0000826	Precocious puberty
HP:0000855	Insulin resistance
HP:0000858	Irregular menstruation
HP:0000956	Acanthosis nigricans
HP:0001513	Obesity
HP:0002900	Hypokalemia
HP:0003351	Decreased circulating renin concentration
HP:0003621	Juvenile onset
HP:0005616	Accelerated skeletal maturation
HP:0008258	Congenital adrenal hyperplasia
HP:0012411	Premature pubarche
HP:0012412	Premature adrenarche
HP:0025436	Elevated serum 11-deoxycortisol
HP:0030348	Increased circulating androgen concentration
HP:0031186	Abnormal circulating deoxycorticosterone level
HP:6000185	Low tetrahydrocortisol (THF) plus 5-alpha-THF/tetrahydrocortisone (THE) ratio
HP:6001080	Reduced urine tetrahydrocortisol plus 5-alpha-THF to tetrahydrocortisone ratio

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST004866_6	Alopecia areata	2.000000e-06

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C536447	Cortisone reductase deficiency (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3542430 (PROTEIN FAMILY), CHEMBL4235 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

13 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 447,660 (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
CHEMBL35	FUROSEMIDE	4	224,045
CHEMBL499915	CARBENOXOLONE	4	3,947
CHEMBL140	CURCUMIN	3	93,882
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	22,804
CHEMBL169	URSOLIC ACID	2	20,825
CHEMBL1761322	MK-0736	2	115
CHEMBL2153191	AZD-4017	2	187
CHEMBL230006	ENOXOLONE	2	24,361
CHEMBL3669417	BI-187004	2	45
CHEMBL4301600	BMS-823778 FREE BASE	2	24
CHEMBL441687	GLYCYRRHIZIN	2	57,389
CHEMBL4086816	BMS-816336	1
CHEMBL4297286	HSD-016	1	36

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

PharmGKB clinical annotations

3 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs4844880	Metabolism/PK	3	tacrolimus	Kidney Transplantation
rs846908	Metabolism/PK	3	tacrolimus	Kidney Transplantation
rs846910	Metabolism/PK	3	tacrolimus	Kidney Transplantation

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs846908	HSD11B1	3	1.75	1	tacrolimus
rs846910	HSD11B1	3	1.75	1	tacrolimus
rs4844880	HSD11B1	3	2.25	1	tacrolimus

GtoPdb / IUPHAR curated pharmacology

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

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

Most potent curated ligand interactions (7 total), top 7:

Ligand	Action	Affinity	Parameter
AZD4017	Inhibition	8.7	pIC50
BMS-823778	Inhibition	8.64	pIC50
INCB13739	Inhibition	8.49	pIC50
ABT-384	Inhibition	8.05	pKi
AZD8329	Inhibition	8.05	pIC50
UE2343	Inhibition	7.62	pIC50
enoxolone	Inhibition	7.54	pIC50

Binding affinities (BindingDB)

1695 measured of 1759 human assays (1759 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[[1-[[(2-fluorophenyl)sulfonyl-methylamino]methyl]cyclopropanecarbonyl]amino]adamantane-1-carboxamide	IC50	0.02 nM	US-9464044: Compound having ability to inhibit 11Beta-HSD1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient
(2R)-N-(adamantan-2-yl)-1-(cyclopentylmethyl)pyrrolidine-2-carboxamide	IC50	0.03 nM
(2R)-N-(adamantan-2-yl)-1-(2-methylpropyl)pyrrolidine-2-carboxamide	IC50	0.03 nM
(2R)-N-(adamantan-2-yl)-1-(cyclobutylmethyl)pyrrolidine-2-carboxamide	IC50	0.03 nM
(2R)-N-(adamantan-2-yl)-1-[(4-cyanophenyl)methyl]pyrrolidine-2-carboxamide	IC50	0.03 nM
(2R)-N-(adamantan-2-yl)-1-[(1-hydroxycyclohexyl)methyl]pyrrolidine-2-carboxamide	IC50	0.03 nM
4-[[2-[3-methyl-1,1-dioxo-6-(2,4,6-trichlorophenyl)-1,2,6-thiadiazinan-2-yl]acetyl]amino]adamantane-1-carboxamide	IC50	0.1 nM	US-9073906: Sulfamide derivative having an adamantyl group and its pharmaceutically acceptable salt
pyridine amide, 30	IC50	0.1 nM
CHEMBL3609877	IC50	0.1 nM
CHEMBL2152223	IC50	0.1 nM
4-[[1-[(3-chlorophenyl)sulfonyl-methylamino]cyclopropanecarbonyl]amino]adamantane-1-carboxamide	IC50	0.12 nM	US-9464044: Compound having ability to inhibit 11Beta-HSD1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient
4-[[2-[1,1-dioxo-6-(2,4,6-trichlorophenyl)-1,2,6-thiadiazinan-2-yl]acetyl]amino]adamantane-1-carboxamide	IC50	0.2 nM	US-9073906: Sulfamide derivative having an adamantyl group and its pharmaceutically acceptable salt
CHEMBL3608403	IC50	0.2 nM
[3-[1-(3-fluoro-4-pyridin-3-ylphenyl)cyclopropyl]-8-methyl-6,9-dihydro-5H-[1,2,4]triazolo[4,3-d][1,4]thiazepin-8-yl]methanol	IC50	0.3 nM	US-8927536: Tetrahydrothiazepine derivative
4-[[1-[[(3-chloro-2-fluorophenyl)sulfonylamino]methyl]cyclopropanecarbonyl]amino]adamantane-1-carboxamide	IC50	0.3 nM	US-9464044: Compound having ability to inhibit 11Beta-HSD1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient
CHEMBL3608400	IC50	0.3 nM
(6S)-6-(2-hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(2-oxo-1H-pyridin-4-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-one	IC50	0.31 nM	US-8575157
(2R)-N-(adamantan-2-yl)-1-(cyclohexylmethyl)pyrrolidine-2-carboxamide	IC50	0.32 nM
(2R)-N-(adamantan-2-yl)-1-(2,2,2-trifluoroethyl)pyrrolidine-2-carboxamide	IC50	0.32 nM
(2R)-N-(adamantan-2-yl)-1-(3,3,3-trifluoropropyl)pyrrolidine-2-carboxamide	IC50	0.32 nM
(2R)-N-(adamantan-2-yl)-1-[(4-chlorophenyl)methyl]pyrrolidine-2-carboxamide	IC50	0.32 nM
(2R)-N-(adamantan-2-yl)-1-[(3-cyanophenyl)methyl]pyrrolidine-2-carboxamide	IC50	0.32 nM
(2R)-N-(adamantan-2-yl)-1-[(1-hydroxycyclopentyl)methyl]pyrrolidine-2-carboxamide	IC50	0.34 nM
4-[[2-[(2,6-difluorophenyl)sulfonylamino]-2-methylpropanoyl]amino]adamantane-1-carboxamide	IC50	0.36 nM	US-9464044: Compound having ability to inhibit 11Beta-HSD1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient
4-[[2-[1,1-dioxo-7-(2,4,6-trichlorophenyl)-1,2,7-thiadiazepan-2-yl]acetyl]amino]adamantane-1-carboxamide	IC50	0.4 nM	US-9073906: Sulfamide derivative having an adamantyl group and its pharmaceutically acceptable salt
4-[[1-[(1-methylindol-7-yl)sulfonylamino]cyclopropanecarbonyl]amino]adamantane-1-carboxamide	IC50	0.4 nM	US-9464044: Compound having ability to inhibit 11Beta-HSD1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient
CHEMBL2152217	IC50	0.4 nM
CHEMBL3127857	IC50	0.4 nM
CHEMBL3127868	IC50	0.43 nM
(5-carbamoyl-2-adamantyl) (3R)-3-(7-chloro-2-oxo-3H-benzimidazol-1-yl)pyrrolidine-1-carboxylate	IC50	0.46 nM	US-9163012: Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
2-adamantyl (2R)-2-[4-(1-methyl-2-oxo-4-pyridinyl)-1,3-thiazol-2-yl]pyrrolidine-1-carboxylate	IC50	0.47 nM	US-9163012: Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
(6S)-6-(2-hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(6-oxo-1-propan-2-ylpyridazin-3-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-one	IC50	0.49 nM	US-8592410: Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1
spiro-carboxamide scaffold, 13	IC50	0.5 nM
N-(adamantan-2-yl)-7-bromo-3-(carbamoylmethyl)-2,3-dihydrospiro[indene-1,4’-piperidine]-1’-carboxamide	IC50	0.5 nM
(6S)-6-(4-fluorophenyl)-3-[(1S)-1-[4-(4-fluorophenyl)phenyl]ethyl]-6-(2-hydroxyethyl)-1,3-oxazinan-2-one	IC50	0.51 nM	US-8598163: Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
2-adamantyl 3-(5-chloropyrimidin-2-yl)pyrrolidine-1-carboxylate	IC50	0.52 nM	US-9163012: Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
(5-carbamoyl-2-adamantyl) (3S)-3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]pyrrolidine-1-carboxylate	IC50	0.54 nM	US-9163012: Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
3-[(6R)-3-[(1S)-1-[4-(4-fluorophenyl)phenyl]ethyl]-2-oxo-6-phenyl-1,3-oxazinan-6-yl]propanamide	IC50	0.55 nM	US-8598163: Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
(R)-3-(3-Trifluoromethyl-pyridin-2-ylamino)-pyrrolidine-1-carboxylic acid 5-carbamoyl-adamantan-2-yl ester	IC50	0.55 nM
(6R)-3-[(1S)-1-[4-(4-fluorophenyl)phenyl]ethyl]-6-(3-hydroxypropyl)-6-phenyl-1,3-oxazinan-2-one	IC50	0.55 nM	US-8598163: Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
3-[(6R)-6-(4-fluorophenyl)-2-oxo-3-[(1S)-1-[4-(6-oxo-1H-pyridin-3-yl)phenyl]ethyl]-1,3-oxazinan-6-yl]-2,2-dimethylpropanenitrile	IC50	0.58 nM	US-8575157
N-{4-[(1-cyanocyclopropyl)methyl]cyclohexyl}-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide	IC50	0.6 nM
4-[[2-[(2-fluorophenyl)sulfonylamino]-2-methylpropanoyl]amino]adamantane-1-carboxamide	IC50	0.6 nM	US-9464044: Compound having ability to inhibit 11Beta-HSD1 enzyme or pharmaceutically acceptable salt thereof, method for producing same, and pharmaceutical composition containing same as active ingredient
CHEMBL4071232	IC50	0.6 nM
2,2-dimethyl-3-[(6R)-3-[(1S)-1-[4-(1-methyl-2-oxo-4-pyridinyl)phenyl]ethyl]-2-oxo-6-phenyl-1,3-oxazinan-6-yl]propanenitrile	IC50	0.61 nM	US-8575157
(S)-3-(3-Trifluoromethyl-pyridin-2-ylamino)-pyrrolidine-1-carboxylic acid 5-carbamoyl-adamantan-2-yl ester	IC50	0.63 nM
(6R)-6-(2,2-dimethylbut-3-ynyl)-3-[(1S)-1-[4-(6-oxo-1H-pyridin-3-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-one	IC50	0.65 nM	US-8575157
(5-carbamoyl-2-adamantyl) (3S)-3-(7-chloro-3-methyl-2-oxobenzimidazol-1-yl)pyrrolidine-1-carboxylate	IC50	0.67 nM	US-9163012: Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
(R)-3-(6-Trifluoromethyl-pyridin-2-ylamino)-pyrrolidine-1-carboxylic acid 5-carbamoyl-adamantan-2-yl ester	IC50	0.67 nM
(5-carbamoyl-2-adamantyl) (3S)-3-[(3,5-difluoro-2-pyridinyl)oxy]pyrrolidine-1-carboxylate	IC50	0.68 nM	US-9163012: Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1

ChEMBL bioactivities

4794 potent at pChembl≥5 of 4881 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.70	IC50	0.02	nM	CHEMBL3897844
10.70	IC50	0.02	nM	CHEMBL5289716
10.52	EC50	0.03	nM	CHEMBL2377209
10.52	IC50	0.03	nM	CHEMBL1096870
10.52	IC50	0.03	nM	CHEMBL1098130
10.52	IC50	0.03	nM	CHEMBL1098131
10.52	IC50	0.03	nM	CHEMBL1098145
10.52	IC50	0.03	nM	CHEMBL1096451
10.00	IC50	0.1	nM	CHEMBL2152223
10.00	IC50	0.1	nM	CHEMBL3609877
10.00	IC50	0.1	nM	CHEMBL3663670
9.96	IC50	0.11	nM	CHEMBL1081251
9.92	IC50	0.12	nM	CHEMBL3961200
9.70	IC50	0.2	nM	CHEMBL3608403
9.70	IC50	0.2	nM	CHEMBL3663666
9.70	IC50	0.2	nM	CHEMBL512355
9.55	IC50	0.28	nM	CHEMBL497748
9.52	IC50	0.3	nM	CHEMBL3608400
9.52	IC50	0.3	nM	CHEMBL3681931
9.52	IC50	0.3	nM	CHEMBL3895758
9.52	IC50	0.3	nM	CHEMBL4073961
9.51	IC50	0.31	nM	CHEMBL3664636
9.49	IC50	0.32	nM	CHEMBL1097177
9.49	IC50	0.32	nM	CHEMBL1097178
9.49	IC50	0.32	nM	CHEMBL1097827
9.49	IC50	0.32	nM	CHEMBL1097828
9.49	IC50	0.32	nM	CHEMBL1098159
9.48	IC50	0.33	nM	CHEMBL1080752
9.47	IC50	0.34	nM	CHEMBL494180
9.47	IC50	0.34	nM	CHEMBL1095787
9.44	IC50	0.36	nM	CHEMBL3963976
9.40	IC50	0.4	nM	CHEMBL2152217
9.40	IC50	0.4	nM	CHEMBL3127857
9.40	IC50	0.4	nM	CHEMBL3127854
9.40	IC50	0.4	nM	CHEMBL3287025
9.40	IC50	0.4	nM	CHEMBL3608401
9.40	IC50	0.4	nM	CHEMBL3639625
9.40	IC50	0.4	nM	CHEMBL3899122
9.40	IC50	0.4	nM	CHEMBL4101787
9.40	IC50	0.4	nM	CHEMBL522964
9.40	IC50	0.4	nM	CHEMBL1269895
9.40	IC50	0.4	nM	CHEMBL1829761
9.37	IC50	0.43	nM	CHEMBL3127868
9.35	IC50	0.45	nM	CHEMBL3127856
9.34	IC50	0.46	nM	CHEMBL4109576
9.33	IC50	0.47	nM	CHEMBL4108485
9.31	IC50	0.49	nM	CHEMBL3127855
9.31	IC50	0.49	nM	CHEMBL3645514
9.30	IC50	0.5	nM	CHEMBL3318967
9.30	IC50	0.5	nM	CHEMBL4075869

PubChem BioAssay actives

3485 with measured affinity, of 4691 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
(2R)-N-(2-adamantyl)-1-(cyclopentylmethyl)pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	<0.0001	uM
3-[[1-[[(2-fluorophenyl)sulfonyl-methylamino]methyl]cyclopropanecarbonyl]amino]adamantane-1-carboxamide	1941895: Inhibition of human 11beta-HSD1 in liver microsome incubated for 24 hrs by LC-MS analysis	ic50	<0.0001	uM
(2R)-N-(2-adamantyl)-1-(2-methylpropyl)pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	<0.0001	uM
(2R)-N-(2-adamantyl)-1-(cyclobutylmethyl)pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	<0.0001	uM
(2R)-N-(2-adamantyl)-1-[(4-cyanophenyl)methyl]pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	<0.0001	uM
(2R)-N-(2-adamantyl)-1-[(1-hydroxycyclohexyl)methyl]pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	<0.0001	uM
4-(4-cyanophenyl)-N-quinolin-2-ylbenzenesulfonamide	744020: Inhibition of 11beta-HSD1 in human HEK293 cells	ec50	<0.0001	uM
4-[[2-[(2-chloro-4-fluorophenyl)sulfonylamino]-2-methylpropanoyl]amino]adamantane-1-carboxamide	1242250: Inhibition of human 11beta-HSD1	ic50	0.0001	uM
(3,3-dimethylpiperidin-1-yl)-[6-(3-fluoro-4-methylphenyl)-2-pyridinyl]methanone	1799207: Scintillation Proximity Assay (SPA) from Article 10.1016/j.bmcl.2008.04.069: “Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.”	ic50	0.0001	uM
(1S,4S)-2-(4-tert-butylphenyl)sulfonyl-5-methyl-2,5-diazabicyclo[2.2.1]heptane	466259: Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay	ic50	0.0001	uM
(2R)-1-(3-chloro-2-methylphenyl)sulfonyl-N-(5-hydroxy-2-adamantyl)-2-methylpyrrolidine-2-carboxamide	692678: Inhibition of human 11betaHSD1 by scintillation proximity assay	ic50	0.0001	uM
N-[4-(2-cyanoethyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide	339318: Inhibition of 11beta-HSD1 in human adipocytes	ic50	0.0002	uM
4-[[2-[(3,5-dichlorophenyl)sulfonylamino]-2-methylpropanoyl]amino]adamantane-1-carboxamide	1242250: Inhibition of human 11beta-HSD1	ic50	0.0002	uM
(2R)-N-(2-adamantyl)-1-(cyclohexylmethyl)pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	0.0003	uM
4-[[2-[(2,5-dichlorophenyl)sulfonylamino]-2-methylpropanoyl]amino]adamantane-1-carboxamide	1242250: Inhibition of human 11beta-HSD1	ic50	0.0003	uM
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-1,2,4-triazol-3-yl]phenol	404225: Inhibition of human 11beta HSD1 by SPA assay	ic50	0.0003	uM
(1S,4S)-2-[4-(2,2-dimethylpropyl)phenyl]sulfonyl-5-methyl-2,5-diazabicyclo[2.2.1]heptane	466259: Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay	ic50	0.0003	uM
(2R)-N-(2-adamantyl)-1-(2,2,2-trifluoroethyl)pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	0.0003	uM
(2R)-N-(2-adamantyl)-1-(3,3,3-trifluoropropyl)pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	0.0003	uM
(2R)-N-(2-adamantyl)-1-[(4-chlorophenyl)methyl]pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	0.0003	uM
(2R)-N-(2-adamantyl)-1-[(3-cyanophenyl)methyl]pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	0.0003	uM
(2R)-N-(2-adamantyl)-1-[(1-hydroxycyclopentyl)methyl]pyrrolidine-2-carboxamide	480484: Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay	ic50	0.0003	uM
2-[2-(4-fluorophenyl)-2-adamantyl]-1-pyrrolidin-1-ylethanone	1448522: Inhibition of 11beta-HSD1 in human microsomes using [3H]cortisone as substrate preincubated for 10 mins followed by substrate addition measured after 4 hrs by SPA	ic50	0.0003	uM
3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-1,2,4-triazole	404225: Inhibition of human 11beta HSD1 by SPA assay	ic50	0.0003	uM
1,1,1-trifluoro-2-[4-[(2R)-2-methyl-4-[(1-pyridin-4-ylcyclopropyl)methyl]piperazin-1-yl]sulfonylphenyl]propan-2-ol	394980: Inhibition of full length human recombinant 11beta-HSD1 expressed in baculovirus insect cell system assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH	ic50	0.0004	uM
(5-carbamoyl-2-adamantyl) (3R)-3-[(3-cyano-2-pyridinyl)amino]pyrrolidine-1-carboxylate	527512: Inhibition of 11betaHSD1 in human platelet assessed as [3H]-cortisone to [3H]-cortisol by microscintillation plate reader	ic50	0.0004	uM
(6R)-3-[(1S)-1-[4-(4-fluorophenyl)phenyl]ethyl]-6-(3-hydroxypropyl)-6-phenyl-1,3-oxazinan-2-one	618804: Inhibition of 11 beta-HSD1 in differentiated human adipocytes assessed as conversion of [3H]-cortisone to [3H]-cortisol after 10 mins by HPLC	ic50	0.0004	uM
(6R)-6-(3-hydroxypropyl)-6-phenyl-3-[(1S)-1-(4-pyridin-4-ylphenyl)ethyl]-1,3-oxazinan-2-one	1453852: Inhibition of 11beta-HSD1 in human omental adipocytes using [3H]cortisone as substrate preincubated for 1 hr followed by substrate addition measured after 3 to 4 hrs by scintillation proximity assay	ic50	0.0004	uM
(3S)-1-(3-chloro-2-methylphenyl)sulfonyl-N-[(1R,2S,4R)-1,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl]piperidine-3-carboxamide	692678: Inhibition of human 11betaHSD1 by scintillation proximity assay	ic50	0.0004	uM
4-[[2-[(2,6-difluorophenyl)sulfonylamino]-2-methylpropanoyl]amino]adamantane-1-carboxamide	1242250: Inhibition of human 11beta-HSD1	ic50	0.0004	uM
4-cyclopropyl-2-(cyclopropylmethoxy)-N-(5-hydroxy-2-adamantyl)-1,3-thiazole-5-carboxamide	1074503: Inhibition of recombinant human 11beta-HSD1 using cortisone/[3H]-cortisone as substrate after 5 hrs by reverse-phase HPLC analysis	ic50	0.0004	uM
N-(5-hydroxy-2-adamantyl)-2-methoxy-4-[(2R)-oxolan-2-yl]-1,3-thiazole-5-carboxamide	1074503: Inhibition of recombinant human 11beta-HSD1 using cortisone/[3H]-cortisone as substrate after 5 hrs by reverse-phase HPLC analysis	ic50	0.0004	uM
N-(5-hydroxy-2-adamantyl)-2-[(2S)-1-methoxypropan-2-yl]oxy-4-[(2R)-oxolan-2-yl]-1,3-thiazole-5-carboxamide	1074503: Inhibition of recombinant human 11beta-HSD1 using cortisone/[3H]-cortisone as substrate after 5 hrs by reverse-phase HPLC analysis	ic50	0.0004	uM
2-(3-cyanocyclobutyl)oxy-N-(5-hydroxy-2-adamantyl)-4-[(2R)-oxolan-2-yl]-1,3-thiazole-5-carboxamide	1074503: Inhibition of recombinant human 11beta-HSD1 using cortisone/[3H]-cortisone as substrate after 5 hrs by reverse-phase HPLC analysis	ic50	0.0004	uM
(3S)-1-(3-chloro-2-methylphenyl)sulfonyl-N-[(1S,2S,4S)-1,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl]piperidine-3-carboxamide	1151397: Inhibition of human 11beta-HSD1	ic50	0.0004	uM
1,1,1-trifluoro-2-[4-[(2R)-2-methyl-4-[(1-pyridin-3-ylcyclopropyl)methyl]piperazin-1-yl]sulfonylphenyl]propan-2-ol	394980: Inhibition of full length human recombinant 11beta-HSD1 expressed in baculovirus insect cell system assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH	ic50	0.0005	uM
1,1,1-trifluoro-2-[4-[(2R)-2-methyl-4-[(1-pyridin-3-ylcyclobutyl)methyl]piperazin-1-yl]sulfonylphenyl]propan-2-ol	394980: Inhibition of full length human recombinant 11beta-HSD1 expressed in baculovirus insect cell system assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH	ic50	0.0005	uM
[4-[cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-(4-fluorophenyl)cyclohexyl]methyl carbamate	550524: Inhibition of human full length 11beta-HSD1 assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay	ic50	0.0005	uM
2-azaspiro[4.5]decan-2-yl-(1-phenylcyclopropyl)methanone	1799039: 11beta-HSD1 Homogeneous Time-Resolved Fluorescence (HTRF) Assay from Article 10.1016/j.bmcl.2009.02.123: “Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.”	ic50	0.0005	uM
N-(2-adamantyl)-1-(2-amino-2-oxoethyl)-4-bromospiro[1,2-dihydroindene-3,4’-piperidine]-1’-carboxamide	458823: Inhibition of human recombinant 11beta-HSD1 expressed in CHO cells assessed as conversion of [3H]cortisone to [3H]cortisol by SPA	ic50	0.0005	uM
(5-carbamoyl-2-adamantyl) (3S)-3-[[3-(trifluoromethyl)-2-pyridinyl]amino]pyrrolidine-1-carboxylate	527512: Inhibition of 11betaHSD1 in human platelet assessed as [3H]-cortisone to [3H]-cortisol by microscintillation plate reader	ic50	0.0005	uM
(6S)-3-[(1S)-1-[4-(4-fluorophenyl)phenyl]ethyl]-6-(2-hydroxyethyl)-6-phenyl-1,3-oxazinan-2-one	618803: Inhibition of human 11 beta-HSD1 expressed in CHO cells assessed as conversion of [3H]cortisone to [3H]cortisol after 1 hr by scintillation proximity assay	ic50	0.0005	uM
(6S)-6-(4-fluorophenyl)-3-[(1S)-1-[4-(4-fluorophenyl)phenyl]ethyl]-6-(2-hydroxyethyl)-1,3-oxazinan-2-one	618803: Inhibition of human 11 beta-HSD1 expressed in CHO cells assessed as conversion of [3H]cortisone to [3H]cortisol after 1 hr by scintillation proximity assay	ic50	0.0005	uM
3-[3-[1-(4-chlorophenyl)cyclopropyl]-[1,2,4]triazolo[4,3-a]pyridin-8-yl]-3-methylbutan-1-ol	1532963: Inhibition of recombinant human 11beta-HSD1 expressed in HEK293 cell microsomes using [3H]cortisone as substrate after 4 hrs by homogeneous immuno-radiometric scintillation proximity assay	ic50	0.0005	uM
3-[1-(4-chlorophenyl)cyclopropyl]-8-[2-(trifluoromethoxy)phenoxy]-[1,2,4]triazolo[4,3-a]pyridine	1185112: Inhibition of human recombinant 11beta-HSD-1 expressed in HEK293 EBNA cells using [3H]-cortisone and NADPH by scintillation proximity assay	ic50	0.0005	uM
(6R)-3-[(1S)-1-[4-(5-fluoro-3-pyridinyl)phenyl]ethyl]-6-(3-hydroxypropyl)-6-phenyl-1,3-oxazinan-2-one	1453851: Inhibition of human 11beta-HSD1 expressed in CHO cell microsomes using [3H]cortisone as substrate preincubated with substrate for 10 mins followed by enzyme addition measured after 90 mins by microbeta scintillation proximity assay	ic50	0.0005	uM
N-(5-hydroxy-2-adamantyl)-2-(2-methoxyethoxy)-4-[(2R)-oxolan-2-yl]-1,3-thiazole-5-carboxamide	1074503: Inhibition of recombinant human 11beta-HSD1 using cortisone/[3H]-cortisone as substrate after 5 hrs by reverse-phase HPLC analysis	ic50	0.0005	uM
2-[2-(4-fluorophenyl)-2-adamantyl]-1-[3-(hydroxymethyl)azetidin-1-yl]ethanone	1448522: Inhibition of 11beta-HSD1 in human microsomes using [3H]cortisone as substrate preincubated for 10 mins followed by substrate addition measured after 4 hrs by SPA	ic50	0.0006	uM
N-[4-[(1-cyanocyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide	1798885: 11beta-HSD1 SPA Assay from Article 10.1016/j.bmcl.2009.01.058: “Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.”	ic50	0.0006	uM
1,1,1-trifluoro-2-[4-[(2R)-2-methyl-4-[(1-pyridin-4-ylcyclobutyl)methyl]piperazin-1-yl]sulfonylphenyl]propan-2-ol	394980: Inhibition of full length human recombinant 11beta-HSD1 expressed in baculovirus insect cell system assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH	ic50	0.0006	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Hydrocortisone	affects oxidation, increases reaction, increases chemical synthesis, increases metabolic processing, increases oxidation (+7 more)	10
bisphenol A	increases expression, affects binding, affects cotreatment, decreases activity, increases activity (+3 more)	7
Cortisone	affects cotreatment, increases activity, increases chemical synthesis, increases oxidation, increases expression (+6 more)	5
Dexamethasone	increases activity, increases expression, affects reaction, decreases reaction, affects cotreatment (+1 more)	4
Tobacco Smoke Pollution	affects expression, decreases expression, increases expression	4
benzamide	decreases activity	3
bisphenol S	increases expression, affects cotreatment	3
Rosiglitazone	decreases expression, decreases reaction, increases activity, affects cotreatment	3
Benzo(a)pyrene	decreases expression, increases methylation	3
Progesterone	affects cotreatment, decreases reaction, increases expression, increases reaction, increases reduction	3
Testosterone	decreases reaction, increases reduction, increases activity, increases expression, affects binding (+1 more)	3
Mifepristone	affects expression, affects reaction, affects binding, decreases activity, decreases reaction (+2 more)	3
Aflatoxin B1	affects expression, decreases expression	3
sodium arsenite	decreases expression, increases expression	2
perfluorooctane sulfonic acid	decreases reaction, increases expression, decreases activity, decreases expression	2
Chenodeoxycholic Acid	increases chemical synthesis, increases reduction, decreases activity	2
Estradiol	affects binding, affects cotreatment, increases expression	2
Methotrexate	decreases expression, increases expression	2
NADP	increases oxidation, increases reduction, affects binding, increases activity	2
Tetrachlorodibenzodioxin	decreases expression	2
1-Methyl-3-isobutylxanthine	affects cotreatment, decreases expression, increases expression, decreases reaction	2
Isotretinoin	decreases expression	2
Cadmium Chloride	increases expression	2
lead acetate	increases expression	1
dioctyl adipate	decreases activity	1
4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone	decreases reaction, increases reduction	1
mono-(2-ethylhexyl)phthalate	increases expression	1
sulforaphane	increases activity, affects binding, decreases activity, decreases reaction	1
tetrabromobisphenol A	decreases activity	1
7-ketolithocholic acid	increases reduction, increases chemical synthesis	1

ChEMBL screening assays

311 unique, capped per target: 308 binding, 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1012778	Binding	Inhibition of human recombinant 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone by scintillation proximity assay	Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model. — J Med Chem
CHEMBL859753	Functional	In vivo inhibition of 11beta-HSD1 at 1 h (10 mg/kg, po) assessed by extent of cortisone to cortisol conversion	Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome. — Bioorg Med Chem Lett

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT04760028	PHASE4	COMPLETED	Study on the Influencing Factors of Electroencephalogram Parameters Under Anesthesia
NCT06106425	Not specified	UNKNOWN	Diagnostic and Prognostic Criteria of EEG in Neonatal Convulsions at Assiut University Children Hospital