Ethisterone

Summary

Ethisterone (CHEMBL241694) is a phase-3 clinical-stage small-molecule progestin (ATC G03DC04); indicated across 2 conditions.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: G03DC04
• Indications: 2 conditions
• Chemistry: 312.4 Da · C21H28O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL241694
Name	Ethisterone
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5284557
ChEBI	CHEBI:34749
ATC	G03DC04
Molecular formula	C21H28O2
Molecular weight	312.4
InChIKey	CHNXZKVNWQUJIB-CEGNMAFCSA-N

SMILES: C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@]4(C#C)O)C

IUPAC name: (8R,9S,10R,13S,14S,17R)-17-ethynyl-17-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one

ChEBI definition: A 17β-hydroxy steroid that is testosterone in which the 17β hydrogen is replaced by an ethynyl group. Ethisterone was the first orally active progestin and is a metabolite of danazol.

Pharmacological roles (ChEBI): progestin.

Other ChEBI roles (chemical / environmental): drug metabolite.

Also known as: Ethisterone, Etisterona, NSC-9565, Ora-lutin, Pranone, Syngestrotabs, Trosinone, ethisterone, SID26748742, SID855561, SID56422131, ETHISTERONE

Patent coverage: 1,153 distinct patent families (3,833 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Survival motor neuron protein, Prelamin-A/C, Androgen receptor, Glucocorticoid receptor, Estrogen receptor, Progesterone receptor, Menin/Histone-lysine N-methyltransferase MLL, Androgen receptor, Sex hormone-binding globulin, Tyrosinase.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 12 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SHBG	8.78	Kd	1.66	nM	CHEMBL_ACT_2155731
LMNA	8.35	Potency	4.5	nM	CHEMBL_ACT_3642219
PGR	8.07	AC50	8.6	nM	CHEMBL_ACT_25204207
AR	7.98	AC50	10.5	nM	CHEMBL_ACT_25203274
P15207	7.36	Ki	44	nM	CHEMBL_ACT_7648111
P15207	7.17	IC50	67	nM	CHEMBL_ACT_7648110
NR3C1	7.02	Ki	95	nM	CHEMBL_ACT_7645954
NR3C1	6.68	IC50	209	nM	CHEMBL_ACT_7645953
ESR1	5.92	AC50	1196	nM	CHEMBL_ACT_25138774
O42713	5.58	IC50	2610	nM	CHEMBL_ACT_2014941
SMN1	5.55	Potency	2818	nM	CHEMBL_ACT_3891907
MEN1	5.4	Potency	3981	nM	CHEMBL_ACT_4570053

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 0.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).