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

General Information of Drug (ID: DMRHDGN)

• Drug Name: TP003 Drug Info
• Synonyms: TP-003; TP 003

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 10001434
  CAS Number: CAS 628690-75-5
  TTD Drug ID: DMRHDGN

Molecule-Related Drug Atlas

Drug(s) Targeting GABA(A) receptor alpha-5 (GABRA5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flumazenil	DMPCG2L	Benzodiazepine overdose	PC91	Approved	[4]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[6]
Basmisanil	DMQ8J0U	Alzheimer disease	8A20	Phase 2	[7]
RG-7816	DMD16JK	Autism spectrum disorder	6A02	Phase 1	[8]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[4]
AMENTOFLAVONE	DMLRNV2	Discovery agent	N.A.	Investigative	[9]
Ro-15-3505	DM4NW3U	Discovery agent	N.A.	Investigative	[10]
isonipecotic acid	DMO1ZHE	Discovery agent	N.A.	Investigative	[4]
[3H]Ro154513	DMMBWKL	Discovery agent	N.A.	Investigative	[11]
[3H]CGS8216	DMLP68J	Inflammation	1A00-CA43.1	Investigative	[4]

Drug(s) Targeting GABA(A) receptor gamma-3 (GABRG3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zolpidem	DMWOSKJ	Insomnia	7A00-7A0Z	Approved	[5]
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[7]
Clobazam - Lundbeck	DMW1OQ0	Anxiety disorder	6B00-6B0Z	Approved	[12]
Flumazenil	DMPCG2L	Benzodiazepine overdose	PC91	Approved	[5]
Stiripentol	DMMSDOY	Dravet syndrome	8A61.11	Approved	[13]
Thiamylal	DMHDF7B	Anaesthesia	9A78.6	Approved	[12]
Ganaxolone	DMXJMKF	Epileptic seizures	8A61-8A6Z	Approved	[7]
Mebutamate	DM0KYI4	Anxiety disorder	6B00-6B0Z	Approved	[12]
Metharbital	DM5A38V	Epilepsy	8A60-8A68	Approved	[12]
Etomidate	DMZI3WO	Anaesthesia	9A78.6	Approved	[12]

Drug(s) Targeting GABA(A) receptor alpha-2 (GABRA2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flumazenil	DMPCG2L	Benzodiazepine overdose	PC91	Approved	[2]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[6]
PF-4480682	DMWYJHC	Neuropathic pain	8E43.0	Discontinued in Phase 2	[14]
CGS-17867A	DMMZJY3	Alcohol dependence	6C40.2	Terminated	[15]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[2]
AMENTOFLAVONE	DMLRNV2	Discovery agent	N.A.	Investigative	[9]
Ro-15-3505	DM4NW3U	Discovery agent	N.A.	Investigative	[10]
isonipecotic acid	DMO1ZHE	Discovery agent	N.A.	Investigative	[2]
[3H]Ro154513	DMMBWKL	Discovery agent	N.A.	Investigative	[11]
[3H]CGS8216	DMLP68J	Inflammation	1A00-CA43.1	Investigative	[2]

Drug(s) Targeting GABA(A) receptor alpha-3 (GABRA3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flumazenil	DMPCG2L	Benzodiazepine overdose	PC91	Approved	[3]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[6]
Adipiplon	DM821BS	Sleep-wake disorder	7A00-7B2Z	Phase 2	[16]
NS-2710	DMMUR6V	Anxiety disorder	6B00-6B0Z	Phase 2	[17]
AZD6280	DMFAZLU	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[18]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[3]
AMENTOFLAVONE	DMLRNV2	Discovery agent	N.A.	Investigative	[9]
Ro-15-3505	DM4NW3U	Discovery agent	N.A.	Investigative	[10]
isonipecotic acid	DMO1ZHE	Discovery agent	N.A.	Investigative	[3]
[3H]Ro154513	DMMBWKL	Discovery agent	N.A.	Investigative	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
GABA(A) receptor alpha-2 (GABRA2)	TTBMV1G	GBRA2_HUMAN	Modulator (allosteric modulator)	[2]
GABA(A) receptor alpha-3 (GABRA3)	TT37EDJ	GBRA3_HUMAN	Modulator (allosteric modulator)	[3]
GABA(A) receptor alpha-5 (GABRA5)	TTNZPQ1	GBRA5_HUMAN	Modulator (allosteric modulator)	[4]
GABA(A) receptor gamma-3 (GABRG3)	TTEX6LM	GBRG3_HUMAN	Modulator (allosteric modulator)	[5]

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: 4326).
• [2] 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. (Target id: 405).
• [3] 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. (Target id: 406).
• [4] 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. (Target id: 408).
• [5] 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. (Target id: 415).
• [6] New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. J Med Chem. 1980 Jun;23(6):702-4.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [9] Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
• [10] The GABA(A) receptor as a target for photochromic molecules. Bioorg Med Chem. 2010 Nov 15;18(22):7731-8.
• [11] Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABA... J Med Chem. 1996 Apr 26;39(9):1928-34.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [13] Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
• [14] WO patent application no. 2014,1515,17, Methods of improving microvascular integrity.
• [15] 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.
• [16] Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem. Eur J Pharmacol. 2011 Oct 1;668(1-2):190-3.
• [17] GABAA receptor subtype-selective modulators. I. alpha2/alpha3-selective agonists as non-sedating anxiolytics. Curr Top Med Chem. 2011;11(9):1176-202.
• [18] AZD6280, a novel partial -aminobutyric acid A receptor modulator, demonstrates a pharmacodynamically selective effect profile in healthy male volunteers.J Clin Psychopharmacol.2015 Feb;35(1):22-33.