Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQL5VC)

• DTT Name: Platelet-activating factor receptor (PTAFR)
• Synonyms: PTAFR; PAF-R
• Gene Name: PTAFR
• DTT Type: Successful target; [1]
• Related Disease: Ischaemic/haemorrhagic stroke [ICD-11: 8B20]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: PTAFR_HUMAN
• TTD ID: T87023
• Sequence:
  MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLT
  MADMLFLITLPLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVT
  RPIKTAQANTRKRGISLSLVIWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKG
  SVPVLIIHIFIVFSFFLVFLIILFCNLVIIRTLLMQPVQQQRNAEVKRRALWMVCTVLAV
  FIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLCLLSTNCVLDPVIYCFLTKKF
  RKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN
• Function: Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth- muscle contractile and hypotensive activity. Seems to mediate its action via a G protein that activates a phosphatidylinositol- calcium second messenger system.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Staphylococcus aureus infection (hsa05150)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  Interferon gamma signaling (R-HSA-877300)
  Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ticlopidine	DMO946V	Stroke	8B20	Approved	[1]
Rupatadine	DMBPN7T	N. A.	N. A.	Phase 4	[2]

7 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ISRAPAFANT	DMP61YB	Asthma	CA23	Phase 3	[3], [4]
60P002	DMHBN8X	Dengue	1D20-1D2Z	Phase 2	[5]
CMI-392	DM1NCUY	Psoriasis vulgaris	EA90	Phase 2	[6]
Dersalazine	DMH96JW	Inflammatory bowel disease	DD72	Phase 2	[7]
Lexipafant	DMZ2YBE	Nerve injury	ND56.4	Phase 2	[8]
YM-264	DMAZNVX	Sepsis	1G40-1G41	Phase 2	[9]
PegCNTF	DMW7VGZ	Obesity	5B81	Phase 1	[10]

33 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BN 50730	DMZK70E	Asthma	CA23	Discontinued in Phase 3	[11], [12]
FOROPAFANT	DML1DGP	Asthma	CA23	Discontinued in Phase 3	[13], [14], [4]
BN50727	DMC35T1	Inflammatory bowel disease	DD72	Discontinued in Phase 2	[15]
DE-081	DM3AVO1	Conjunctivitis	9A60	Discontinued in Phase 2	[16], [17], [18]
E-6123	DMUW6QX	Asthma	CA23	Discontinued in Phase 2	[19]
Minopafant	DMVF2R1	Sepsis	1G40-1G41	Discontinued in Phase 2	[20]
MK-287	DMCAKPG	Sepsis	1G40-1G41	Discontinued in Phase 2	[21], [4]
Ro-24-4736	DM01MRZ	Sepsis	1G40-1G41	Discontinued in Phase 2	[22]
SM-10661	DMZYGW0	Sepsis	1G40-1G41	Discontinued in Phase 2	[23], [4]
TCV-309	DM3VZ87	Sepsis	1G40-1G41	Discontinued in Phase 2	[24]
UK-74505	DMAD1S5	Sepsis	1G40-1G41	Discontinued in Phase 2	[25]
ABT-299	DM8GZAS	Sepsis	1G40-1G41	Discontinued in Phase 1	[26]
AGN-191743	DM8XODL	Allergy	4A80-4A85	Discontinued in Phase 1	[27]
DACOPAFANT	DMDUZ5W	Sepsis	1G40-1G41	Discontinued in Phase 1	[28], [4]
DF-1111301	DMZYVFH	Allergy	4A80-4A85	Discontinued in Phase 1	[29], [4]
SDZ-62-434	DMU3TQJ	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[30], [4]
Bepafant	DMVK78Q	Sepsis	1G40-1G41	Terminated	[31]
BN-50726	DMTKJDS	Nerve injury	ND56.4	Terminated	[32]
BN50739	DMU1TRQ	Cerebral infarction	8B11.5Z	Terminated	[33], [34]
CL-184005	DMJBGI1	Sepsis	1G40-1G41	Terminated	[35]
CMI-206	DMEIW7K	Inflammation	1A00-CA43.1	Terminated	[36]
CV 6209	DMQBULC	Asthma	CA23	Terminated	[37]
FR-128998	DMMOBHW	Thrombocytopenia	3B64	Terminated	[38]
KC-11404	DM3H90W	Asthma	CA23	Terminated	[39]
KC-11425	DMC295V	Asthma	CA23	Terminated	[40]
L-659989	DMLENQ7	N. A.	N. A.	Terminated	[41]
Ro-24-0238	DMJQA0D	Sepsis	1G40-1G41	Terminated	[42]
Sch-40338	DM3G5IB	Allergy	4A80-4A85	Terminated	[43]
SDZ-64-412	DM2CBTU	N. A.	N. A.	Terminated	[44]
TIAPAFANT	DM0SCDB	Sepsis	1G40-1G41	Terminated	[45], [4]
TULOPAFANT	DMASENP	Cardiac arrhythmias	BC9Z	Terminated	[46], [4]
UR-12460	DMV8GUE	Thrombosis	DB61-GB90	Terminated	[47]
WEB-2347	DMY9NG1	Allergy	4A80-4A85	Terminated	[48]

32 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
10-OBn-7alpha-F-gingkolide B	DMM9GEA	Discovery agent	N.A.	Investigative	[49]
10-OBn-epi-ginkgolide C	DMAM5WJ	Discovery agent	N.A.	Investigative	[49]
10-OBn-ginkgolide B	DMS0I5V	Discovery agent	N.A.	Investigative	[49]
10-OBn-ginkgolide C	DMOXKLH	Discovery agent	N.A.	Investigative	[49]
2-O-ethyl-PAF C-16	DMZK0JV	Discovery agent	N.A.	Investigative	[17]
2-O-methyl-PAF C-18	DME7K64	Discovery agent	N.A.	Investigative	[17]
7-epi-ginkgolide C	DMRAZDW	Discovery agent	N.A.	Investigative	[49]
7alpha-Cl-ginkgolide B	DMD6UC9	Discovery agent	N.A.	Investigative	[49]
7alpha-F-ginkgolide B	DMRQ24A	Discovery agent	N.A.	Investigative	[49]
7alpha-N3-ginkgolide B	DMGNWBV	Discovery agent	N.A.	Investigative	[49]
7alpha-NH2-ginkgolide B	DMZUYX1	Discovery agent	N.A.	Investigative	[49]
7alpha-NHEt-ginkgolide B	DMWAB7F	Discovery agent	N.A.	Investigative	[49]
7alpha-NHMe-ginkgolide B	DMSPLYF	Discovery agent	N.A.	Investigative	[49]
7alpha-OAc-ginkgolide B	DMN1U56	Discovery agent	N.A.	Investigative	[49]
7alpha-OCOCH2Ph-ginkgolide B	DMGAPCD	Discovery agent	N.A.	Investigative	[49]
A 137491	DM1H3FJ	Discovery agent	N.A.	Investigative	[50]
BB-823	DMZPL63	Discovery agent	N.A.	Investigative	[47]
CV-3988	DMM7RAD	Discovery agent	N.A.	Investigative	[51]
enantio PAF C-16	DMASQWV	Discovery agent	N.A.	Investigative	[17]
FR-900452	DMMGWXQ	Discovery agent	N.A.	Investigative	[52]
KO-286011	DMVGNZJ	Discovery agent	N.A.	Investigative	[53]
L-652731	DM360VU	Discovery agent	N.A.	Investigative	[41]
LAU-0901	DMMDZ4B	Brain ischaemia	8B1Z	Investigative	[54], [55]
methylcarbamyl PAF	DMV865Q	Discovery agent	N.A.	Investigative	[56]
PAF	DMRZAQW	Discovery agent	N.A.	Investigative	[57], [58]
RP-52770	DM5IXOS	Discovery agent	N.A.	Investigative	[59]
SRI-63-675	DM8GDZS	Discovery agent	N.A.	Investigative	[60]
UR-10324	DMPF1VU	Discovery agent	N.A.	Investigative	[61]
UR-11353	DM8G9NY	Discovery agent	N.A.	Investigative	[61]
UR-12510	DM2HVUW	Allergy	4A80-4A85	Investigative	[62]
UR-12519	DMVZQ47	Discovery agent	N.A.	Investigative	[63]
VERAGUENSIN	DMJRVBS	Discovery agent	N.A.	Investigative	[41]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Psoriasis	EA90	Skin	5.94E-02	0.08	0.17
Asthma	CA23	Nasal and bronchial airway	3.75E-05	0.25	0.35
Thrombocytopenia	3B64	Whole blood	4.42E-01	0.49	1.01
Sepsis with septic shock	1G41	Whole blood	2.87E-10	0.6	0.77
Sjogren's syndrome	4A43.2	Salivary gland tissue	3.53E-02	0.33	2.12

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