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

General Information of DTT (ID: TT9JZCK)

• DTT Name: Sphingosine-1-phosphate receptor 1 (S1PR1) DTT Info
• Gene Name: S1PR1

Molecule-Related Drug & Molecule List

5 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Etrasimod	DMT0A3Y	Ulcerative colitis	DD71	Approved	[1]
Fingolimod	DM5JVAN	Multiple sclerosis	8A40	Approved	[2]
Ozanimod	DMT6AM2	Multiple sclerosis	8A40	Approved	[3]
Ponesimod	DMEAOYJ	Multiple sclerosis	8A40	Approved	[4]
Siponimod	DM2R86O	Multiple sclerosis	8A40	Approved	[5]

12 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CBP-307	DM3TH6Y	Ulcerative colitis	DD71	Phase 2	[6]
KRP-203	DMOW9X2	Cutaneous lupus erythematosus	EB5Z	Phase 2	[7]
MT-1303	DMSE9TH	Crohn disease	DD70	Phase 2	[8]
ONO-4641	DMLUM3Y	Rheumatoid arthritis	FA20	Phase 2	[7]
VTX-002	DMZ8Z5A	Ulcerative colitis	DD71	Phase 2	[9]
ASP-4058	DM1RD0T	Multiple sclerosis	8A40	Phase 1	[10]
BMS-986104	DMZ4WMT	Rheumatoid arthritis	FA20	Phase 1	[1]
CS-0777	DMG0SPO	Multiple sclerosis	8A40	Phase 1	[11]
GSK-2018682	DMRU4YV	Immune System disease	4A01-4B41	Phase 1	[7]
SAR247799	DMUAJZD	Cardiovascular disease	BA00-BE2Z	Phase 1	[12]
Sonepcizumab	DMB3YZJ	Macular degeneration	9B78.3	Phase 1	[7]
Sphingosine-1-phosphate	DMJCQKA	Acne vulgaris	ED80	Phase 1	[13]

2 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-4629991	DMNLAU7	Rheumatoid arthritis	FA20	Discontinued in Phase 1	[14]
XL-541	DM965P4	Solid tumour/cancer	2A00-2F9Z	Terminated	[15]

32 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(3-Tetradecylamino-cyclohexyl)-phosphonic acid	DM6P35D	Discovery agent	N.A.	Investigative	[16]
(3-Tetradecylamino-cyclopentyl)-phosphonic acid	DMFMBPT	Discovery agent	N.A.	Investigative	[16]
(S)-FTY720P	DM5WETL	N. A.	N. A.	Investigative	[17]
1-(4-nonylbenzyl)azetidine-3-carboxylic acid	DMQKMCG	Discovery agent	N.A.	Investigative	[18]
1-(4-nonylbenzyl)pyrrolidin-3-ylphosphonic acid	DM8U2HP	Discovery agent	N.A.	Investigative	[18]
1-(4-nonylbenzyl)pyrrolidine-3-carboxylic acid	DMAR39L	Discovery agent	N.A.	Investigative	[18]
3-(N-alkylamino) propylphosphonic acid derivative	DMJDG9C	Discovery agent	N.A.	Investigative	[16]
3-(tetradecylamino)propylphosphonic acid	DMNA6LF	Discovery agent	N.A.	Investigative	[18]
3-amino-5-(4-octylphenyl)pentanoic acid	DMONHFR	Discovery agent	N.A.	Investigative	[19]
4-amino-6-(4-octylphenyl)hexanoic acid	DMZRM0Q	Discovery agent	N.A.	Investigative	[19]
AFD(R)	DME9Y8Q	Discovery agent	N.A.	Investigative	[20]
AMG-247	DMU6WR9	Inflammation	1A00-CA43.1	Investigative	[21]
AUY954	DMVGIO5	Discovery agent	N.A.	Investigative	[22]
BMS-520	DMAY9TM	Immune System disease	4A01-4B41	Investigative	[21]
CYM5181	DMGTZ9Q	Discovery agent	N.A.	Investigative	[23]
CYM5442	DMURD2E	Discovery agent	N.A.	Investigative	[23]
FTY720-phosphate	DMDZBQH	Discovery agent	N.A.	Investigative	[20]
GNF-PF-78	DM7SPRJ	Discovery agent	N.A.	Investigative	[24]
GNF-PF-826	DM37ORC	Discovery agent	N.A.	Investigative	[24]
GSK-1842799C	DM2KT17	Cardiovascular disease	BA00-BE2Z	Investigative	[21]
KRP 203-phosphate	DMLIK7X	Discovery agent	N.A.	Investigative	[25]
KRP-107	DM5KFBP	Autoimmune diabetes	5A10	Investigative	[21]
LPA	DMI5XR1	Discovery agent	N.A.	Investigative	[26]
NIBR-0213	DMH6MVJ	Discovery agent	N.A.	Investigative	[27]
NIBR-785	DMU0BMQ	Multiple sclerosis	8A40	Investigative	[21]
NOX-S91	DMVS6DW	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
SEW2871	DMJBW7X	Discovery agent	N.A.	Investigative	[28]
VPC03090-P	DMIXUM3	Discovery agent	N.A.	Investigative	[29]
VPC23019	DMVQFY4	Discovery agent	N.A.	Investigative	[30]
VPC44116	DMQ4OTJ	Discovery agent	N.A.	Investigative	[31]
W146	DMDYTSW	Discovery agent	N.A.	Investigative	[32]
[3-(4-Nonyl-benzylamino)-propyl]-phosphonic acid	DMGD487	Discovery agent	N.A.	Investigative	[16]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] Clinical pipeline report, company report or official report of Connect Biopharma
• [7] Targeting the sphingosine-1-phosphate axis in cancer, inflammation and beyond. Nat Rev Drug Discov. 2013 Sep;12(9):688-702.
• [8] Sphingosine 1-Phosphate Receptor Modulators in Multiple Sclerosis. CNS Drugs. 2015 Jul;29(7):565-75.
• [9] Clinical pipeline report, company report or official report of Ventyx Biosciences
• [10] ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile. PLoS One. 2014 Oct 27;9(10):e110819.
• [11] Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist. ACS Med Chem Lett. 2011 Mar 2;2(5):368-72.
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2520-4.
• [14] US patent application no. 2010,0158,905, Combination therapy of arthritis with tranilast.
• [15] Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists. J Med Chem. 2012 Feb 9;55(3):1368-81.
• [16] Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) rec... Bioorg Med Chem Lett. 2004 Oct 4;14(19):4861-6.
• [17] Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors. Nat Chem Biol. 2009 Jun;5(6):428-34.
• [18] A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 re... J Med Chem. 2004 Dec 30;47(27):6662-5.
• [19] S1P receptor mediated activity of FTY720 phosphate mimics. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1485-7.
• [20] The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem. 2002 Jun 14;277(24):21453-7.
• [21] 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: 275).
• [22] A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol. 2006 Nov;13(11):1227-34.
• [23] Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions. Mol Pharmacol. 2008 Nov;74(5):1308-18.
• [24] In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
• [25] A novel sphingosine 1-phosphate receptor agonist, 2-amino-2-propanediol hydrochloride (KRP-203), regulates chronic colitis in interleukin-10 gene-d... J Pharmacol Exp Ther. 2008 Jan;324(1):276-83.
• [26] Lysophosphatidic acid stimulates the G-protein-coupled receptor EDG-1 as a low affinity agonist. J Biol Chem. 1998 Aug 21;273(34):22105-12.
• [27] A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis. Chem Biol. 2012 Sep 21;19(9):1142-51.
• [28] Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem. 2004 Apr 2;279(14):13839-48.
• [29] Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. J Pharmacol Exp Ther. 2011 Sep;338(3):879-89.
• [30] Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem. 2005 Mar 18;280(11):9833-41.
• [31] Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists. Bioorg Med Chem. 2007 Jan 15;15(2):663-77.
• [32] Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol. 2006 Aug;2(8):434-41.