Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM2EKX5)

• Drug Name: Antalarmin Drug Info
• Synonyms: Antalarmin; 157284-96-3; CHEMBL296641; 7H-Pyrrolo(2,3-d)pyrimidin-4-amine, N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)-; SCHEMBL466243; GTPL3489; AC1L433C; DTXSID50166241; CHEBI:139557; ZINC1539136; NSC715590; BDBM50074501; AKOS030559812; NSC-715590; NCGC00165732-01; NCI60_039940; LS-139513; N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[3,2-e]pyrimidin-4-amine; N-butyl-N-ethyl-7-mesityl-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Indication

Disease Entry	ICD 11	Status	REF
Depression	6A70-6A7Z	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 177990
  ChEBI ID: CHEMBL139557
  CAS Number: CAS 157284-96-3
  TTD Drug ID: DM2EKX5

Molecule-Related Drug Atlas

Drug(s) Targeting Corticotropin-releasing factor receptor 1 (CRHR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Telavancin	DM58VQX	Staphylococcus infection	1B5Y	Approved	[4]
Pexacerfont	DMBJ15R	Anxiety disorder	6B00-6B0Z	Phase 2/3	[5]
SSR125543	DMGJEB8	Anxiety disorder	6B00-6B0Z	Phase 2	[6]
ONO-2333Ms	DMOT0WR	Anxiety disorder	6B00-6B0Z	Phase 2	[7]
GSK561679	DMEVARK	Alcohol dependence	6C40.2	Phase 2	[8]
Tildacerfont	DMAB8LH	Congenital adrenal hyperplasia	5A71.01	Phase 2	[9]
GSK586529	DM5E9LX	Anxiety disorder	6B00-6B0Z	Phase 1	[8]
GW876008	DMAXRBI	Irritable bowel syndrome	DD91.0	Discontinued in Phase 2	[5]
CP-316,311	DMZ76EM	Major depressive disorder	6A70.3	Discontinued in Phase 2	[5]
CRA1000	DMWMBIV	Anxiety disorder	6B00-6B0Z	Preclinical	[4]

Drug(s) Affected By Steroidogenic acute regulatory protein, mitochondrial (STAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[10]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[11]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[12]
Lamotrigine	DM8SXYG	Bipolar disorder	6A60	Approved	[13]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[14]
Lindane	DMB8CNL	Infestations of lice and scabies	1G00.Z	Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[17]
Hydrocortisone	DMGEMB7	Acne vulgaris	ED80	Approved	[18]
Mifepristone	DMGZQEF	Cushing disease	5A70	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Corticotropin-releasing factor receptor 1 (CRHR1)	TT7EFHR	CRFR1_HUMAN	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Steroidogenic acute regulatory protein, mitochondrial (STAR)	OTFEZ5AI	STAR_HUMAN	Gene/Protein Processing	[3]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3489).
• [2] Chronic administration of the non-peptide CRH type 1 receptor antagonist antalarmin does not blunt hypothalamic-pituitary-adrenal axis responses to acute immobilization stress. Life Sci. 1999;65(4):PL53-8.
• [3] Corticotropin-releasing hormone (CRH) and urocortin act through type 1 CRH receptors to stimulate dehydroepiandrosterone sulfate production in human fetal adrenal cells. J Clin Endocrinol Metab. 2005 Sep;90(9):5393-400.
• [4] A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
• [5] Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
• [6] Pharma & Vaccines. Product Development Pipeline. April 29 2009.
• [7] Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism. Drug Alcohol Depend. 2013 Mar 1;128(3):175-86.
• [8] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [9] Clinical advances in the pharmacotherapy of congenital adrenal hyperplasia. Eur J Endocrinol. 2021 Nov 30;186(1):R1-R14.
• [10] Retinoids and retinol differentially regulate steroid biosynthesis in ovarian theca cells isolated from normal cycling women and women with polycystic ovary syndrome. J Clin Endocrinol Metab. 2005 Aug;90(8):4858-65. doi: 10.1210/jc.2005-0330. Epub 2005 May 24.
• [11] Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
• [12] Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
• [13] Antiepileptic drugs are endocrine disruptors for the human fetal testis ex vivo. Toxicol Sci. 2023 Sep 28;195(2):169-183. doi: 10.1093/toxsci/kfad076.
• [14] Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
• [15] Steroidogenic gene expression in H295R cells and the human adrenal gland: adrenotoxic effects of lindane in vitro. J Appl Toxicol. 2006 Nov-Dec;26(6):484-92.
• [16] Differential effects of antiepileptic drugs on steroidogenesis in a human in vitro cell model. Acta Neurol Scand Suppl. 2009;(189):14-21.
• [17] Chronic ethanol exposure increases goosecoid (GSC) expression in human embryonic carcinoma cell differentiation. J Appl Toxicol. 2014 Jan;34(1):66-75.
• [18] Glucocorticoid-activation system mediated glucocorticoid-insulin-like growth factor 1 (GC-IGF1) axis programming alteration of adrenal dysfunction induced by prenatal caffeine exposure. Toxicol Lett. 2019 Mar 1;302:7-17.
• [19] Mifepristone induced progesterone withdrawal reveals novel regulatory pathways in human endometrium. Mol Hum Reprod. 2007 Sep;13(9):641-54.