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

General Information of Drug (ID: DMWYJHC)

• Drug Name: PF-4480682 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Neuropathic pain	8E43.0	Discontinued in Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DMWYJHC

Molecule-Related Drug Atlas

Drug(s) Targeting GABA(A) receptor delta (GABRD)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[3]
Gaboxadol	DMI53FU	Insomnia	7A00-7A0Z	Approved	[4]
Ganaxolone	DMXJMKF	Epileptic seizures	8A61-8A6Z	Approved	[5]
SAGE-217b	DMRFK0B	Major depressive disorder	6A70.3	Phase 2	[3]
PF-2393296	DM5R2MG	Neuropathic pain	8E43.0	Discontinued in Phase 1	[6]
Co-60549	DMGIZHX	Anxiety disorder	6B00-6B0Z	Terminated	[7]
Org-20599	DMQU8AR	Anaesthesia	9A78.6	Terminated	[8]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[6]
RU-5135	DMCASRD	Discovery agent	N.A.	Investigative	[9]

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	[10]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[11]
CGS-17867A	DMMZJY3	Alcohol dependence	6C40.2	Terminated	[12]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[10]
AMENTOFLAVONE	DMLRNV2	Discovery agent	N.A.	Investigative	[13]
Ro-15-3505	DM4NW3U	Discovery agent	N.A.	Investigative	[14]
isonipecotic acid	DMO1ZHE	Discovery agent	N.A.	Investigative	[10]
[3H]Ro154513	DMMBWKL	Discovery agent	N.A.	Investigative	[15]
[3H]CGS8216	DMLP68J	Inflammation	1A00-CA43.1	Investigative	[10]
CI-218872	DM0RH3S	Discovery agent	N.A.	Investigative	[16]

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	[2]
GABA(A) receptor delta (GABRD)	TTGXH6N	GBRD_HUMAN	Modulator	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025530)
• [2] WO patent application no. 2014,1515,17, Methods of improving microvascular integrity.
• [3] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [4] Gaboxadol--a new awakening in sleep.Curr Opin Pharmacol.2006 Feb;6(1):30-6.
• [5] Ganaxolone, a selective, high-affinity steroid modulator of the gamma-aminobutyric acid-A receptor, exacerbates seizures in animal models of absence. Ann Neurol. 1998 Oct;44(4):688-91.
• [6] 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: 416).
• [7] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012)
• [8] The anaesthetic action and modulation of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology. 1996;35(9-10):1209-22.
• [9] Complex interactions between the steroid derivative RU 5135 and the GABAA-receptor complex. Eur J Pharmacol. 1992 Oct 1;227(2):147-51.
• [10] 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).
• [11] New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. J Med Chem. 1980 Jun;23(6):702-4.
• [12] 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.
• [13] Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
• [14] The GABA(A) receptor as a target for photochromic molecules. Bioorg Med Chem. 2010 Nov 15;18(22):7731-8.
• [15] 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.
• [16] Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents f... Bioorg Med Chem. 2010 Nov 1;18(21):7548-64.