Target Information
Target General Information | Top | |||||
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Target ID |
T87023
(Former ID: TTDR01165)
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Target Name |
Platelet-activating factor receptor (PTAFR)
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Synonyms |
PTAFR; PAF-R
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Gene Name |
PTAFR
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Ischaemic/haemorrhagic stroke [ICD-11: 8B20] | |||||
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.
Click to Show/Hide
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLT
MADMLFLITLPLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVT RPIKTAQANTRKRGISLSLVIWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKG SVPVLIIHIFIVFSFFLVFLIILFCNLVIIRTLLMQPVQQQRNAEVKRRALWMVCTVLAV FIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLCLLSTNCVLDPVIYCFLTKKF RKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A00264 | |||||
HIT2.0 ID | T72IYV |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Ticlopidine | Drug Info | Approved | Stroke | [2], [3] | |
Clinical Trial Drug(s) | [+] 7 Clinical Trial Drugs | + | ||||
1 | ISRAPAFANT | Drug Info | Phase 3 | Asthma | [4], [5] | |
2 | 60P002 | Drug Info | Phase 2 | Dengue | [6] | |
3 | CMI-392 | Drug Info | Phase 2 | Psoriasis vulgaris | [7] | |
4 | Dersalazine | Drug Info | Phase 2 | Inflammatory bowel disease | [8] | |
5 | Lexipafant | Drug Info | Phase 2 | Nerve injury | [9] | |
6 | YM-264 | Drug Info | Phase 2 | Sepsis | [10] | |
7 | PegCNTF | Drug Info | Phase 1 | Obesity | [11] | |
Discontinued Drug(s) | [+] 31 Discontinued Drugs | + | ||||
1 | BN 50730 | Drug Info | Discontinued in Phase 3 | Asthma | [12] | |
2 | FOROPAFANT | Drug Info | Discontinued in Phase 3 | Asthma | [13], [14] | |
3 | BN50727 | Drug Info | Discontinued in Phase 2 | Inflammatory bowel disease | [15] | |
4 | DE-081 | Drug Info | Discontinued in Phase 2 | Conjunctivitis | [16] | |
5 | E-6123 | Drug Info | Discontinued in Phase 2 | Asthma | [17] | |
6 | Minopafant | Drug Info | Discontinued in Phase 2 | Sepsis | [18] | |
7 | MK-287 | Drug Info | Discontinued in Phase 2 | Sepsis | [19] | |
8 | Ro-24-4736 | Drug Info | Discontinued in Phase 2 | Sepsis | [20] | |
9 | SM-10661 | Drug Info | Discontinued in Phase 2 | Sepsis | [21] | |
10 | TCV-309 | Drug Info | Discontinued in Phase 2 | Sepsis | [22] | |
11 | UK-74505 | Drug Info | Discontinued in Phase 2 | Sepsis | [23] | |
12 | ABT-299 | Drug Info | Discontinued in Phase 1 | Sepsis | [24], [25] | |
13 | AGN-191743 | Drug Info | Discontinued in Phase 1 | Allergy | [26] | |
14 | DACOPAFANT | Drug Info | Discontinued in Phase 1 | Sepsis | [27] | |
15 | DF-1111301 | Drug Info | Discontinued in Phase 1 | Allergy | [28] | |
16 | SDZ-62-434 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [29] | |
17 | Bepafant | Drug Info | Terminated | Sepsis | [30], [31] | |
18 | BN-50726 | Drug Info | Terminated | Nerve injury | [32] | |
19 | BN50739 | Drug Info | Terminated | Cerebral infarction | [33], [34] | |
20 | CL-184005 | Drug Info | Terminated | Sepsis | [35] | |
21 | CMI-206 | Drug Info | Terminated | Inflammation | [36] | |
22 | CV 6209 | Drug Info | Terminated | Asthma | [37], [38] | |
23 | FR-128998 | Drug Info | Terminated | Thrombocytopenia | [39] | |
24 | KC-11404 | Drug Info | Terminated | Asthma | [40] | |
25 | KC-11425 | Drug Info | Terminated | Asthma | [41] | |
26 | Ro-24-0238 | Drug Info | Terminated | Sepsis | [42] | |
27 | Sch-40338 | Drug Info | Terminated | Allergy | [43], [44] | |
28 | TIAPAFANT | Drug Info | Terminated | Sepsis | [45], [46] | |
29 | TULOPAFANT | Drug Info | Terminated | Cardiac arrhythmias | [47] | |
30 | UR-12460 | Drug Info | Terminated | Thrombosis | [48] | |
31 | WEB-2347 | Drug Info | Terminated | Allergy | [49] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Modulator | [+] 28 Modulator drugs | + | ||||
1 | Ticlopidine | Drug Info | [1] | |||
2 | CMI-392 | Drug Info | [7] | |||
3 | Lexipafant | Drug Info | [54] | |||
4 | PegCNTF | Drug Info | [44] | |||
5 | BN 50730 | Drug Info | [56], [57] | |||
6 | BN50727 | Drug Info | [60] | |||
7 | DE-081 | Drug Info | [61], [62], [63] | |||
8 | E-6123 | Drug Info | [64] | |||
9 | TCV-309 | Drug Info | [69] | |||
10 | AGN-191743 | Drug Info | [72] | |||
11 | BN50739 | Drug Info | [78], [79] | |||
12 | CL-184005 | Drug Info | [80] | |||
13 | CMI-206 | Drug Info | [81] | |||
14 | CV 6209 | Drug Info | [82] | |||
15 | FR-128998 | Drug Info | [83] | |||
16 | KC-11404 | Drug Info | [40] | |||
17 | Sch-40338 | Drug Info | [87] | |||
18 | UR-12460 | Drug Info | [91] | |||
19 | WEB-2347 | Drug Info | [92] | |||
20 | A 137491 | Drug Info | [94] | |||
21 | BB-823 | Drug Info | [91] | |||
22 | FR-900452 | Drug Info | [96] | |||
23 | KO-286011 | Drug Info | [97] | |||
24 | SRI-63-675 | Drug Info | [104] | |||
25 | UR-10324 | Drug Info | [105] | |||
26 | UR-11353 | Drug Info | [105] | |||
27 | UR-12510 | Drug Info | [106] | |||
28 | UR-12519 | Drug Info | [107] | |||
Inhibitor | [+] 7 Inhibitor drugs | + | ||||
1 | RUPATADINE | Drug Info | [50] | |||
2 | Dersalazine | Drug Info | [8] | |||
3 | L-659989 | Drug Info | [85] | |||
4 | Ro-24-0238 | Drug Info | [86] | |||
5 | SDZ-64-412 | Drug Info | [88] | |||
6 | L-652731 | Drug Info | [85] | |||
7 | VERAGUENSIN | Drug Info | [85] | |||
Antagonist | [+] 34 Antagonist drugs | + | ||||
1 | ISRAPAFANT | Drug Info | [51], [52] | |||
2 | 60P002 | Drug Info | [53] | |||
3 | YM-264 | Drug Info | [55] | |||
4 | FOROPAFANT | Drug Info | [52], [58], [59] | |||
5 | Minopafant | Drug Info | [65] | |||
6 | MK-287 | Drug Info | [66], [52] | |||
7 | Ro-24-4736 | Drug Info | [67] | |||
8 | SM-10661 | Drug Info | [68], [52] | |||
9 | UK-74505 | Drug Info | [70] | |||
10 | ABT-299 | Drug Info | [71] | |||
11 | DACOPAFANT | Drug Info | [73], [52] | |||
12 | DF-1111301 | Drug Info | [74], [52] | |||
13 | SDZ-62-434 | Drug Info | [75], [52] | |||
14 | Bepafant | Drug Info | [76] | |||
15 | BN-50726 | Drug Info | [77] | |||
16 | KC-11425 | Drug Info | [84] | |||
17 | TIAPAFANT | Drug Info | [89], [52] | |||
18 | TULOPAFANT | Drug Info | [90], [52] | |||
19 | 10-OBn-7alpha-F-gingkolide B | Drug Info | [93] | |||
20 | 10-OBn-epi-ginkgolide C | Drug Info | [93] | |||
21 | 10-OBn-ginkgolide B | Drug Info | [93] | |||
22 | 10-OBn-ginkgolide C | Drug Info | [93] | |||
23 | 7-epi-ginkgolide C | Drug Info | [93] | |||
24 | 7alpha-Cl-ginkgolide B | Drug Info | [93] | |||
25 | 7alpha-F-ginkgolide B | Drug Info | [93] | |||
26 | 7alpha-N3-ginkgolide B | Drug Info | [93] | |||
27 | 7alpha-NH2-ginkgolide B | Drug Info | [93] | |||
28 | 7alpha-NHEt-ginkgolide B | Drug Info | [93] | |||
29 | 7alpha-NHMe-ginkgolide B | Drug Info | [93] | |||
30 | 7alpha-OAc-ginkgolide B | Drug Info | [93] | |||
31 | 7alpha-OCOCH2Ph-ginkgolide B | Drug Info | [93] | |||
32 | CV-3988 | Drug Info | [95] | |||
33 | LAU-0901 | Drug Info | [98], [99] | |||
34 | RP-52770 | Drug Info | [103] | |||
Agonist | [+] 5 Agonist drugs | + | ||||
1 | 2-O-ethyl-PAF C-16 | Drug Info | [62] | |||
2 | 2-O-methyl-PAF C-18 | Drug Info | [62] | |||
3 | enantio PAF C-16 | Drug Info | [62] | |||
4 | methylcarbamyl PAF | Drug Info | [100] | |||
5 | PAF | Drug Info | [101], [102] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | Neuroactive ligand-receptor interaction | |||||
3 | Staphylococcus aureus infection | |||||
NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
1 | IL5 Signaling Pathway | |||||
2 | Leptin Signaling Pathway | |||||
Reactome | [+] 3 Reactome Pathways | + | ||||
1 | Class A/1 (Rhodopsin-like receptors) | |||||
2 | G alpha (q) signalling events | |||||
3 | Interferon gamma signaling | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | GPCRs, Class A Rhodopsin-like | |||||
2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
3 | Small Ligand GPCRs | |||||
4 | Interferon gamma signaling | |||||
5 | GPCR ligand binding | |||||
6 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 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. (Ligand id: 7307). | |||||
REF 3 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | |||||
REF 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. (Ligand id: 1857). | |||||
REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001699) | |||||
REF 6 | ClinicalTrials.gov (NCT02569827) Celgosivir or Modipafant as Treatment for Adult Participants With Uncomplicated Dengue Fever in Singapore. U.S. National Institutes of Health. | |||||
REF 7 | Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20. | |||||
REF 8 | The intestinal anti-inflammatory effect of dersalazine sodium is related to a down-regulation in IL-17 production in experimental models of rodent colitis. Br J Pharmacol. 2012 February; 165(3): 729-740. | |||||
REF 9 | Randomized, double-blind phase II trial of Lexipafant, a platelet-activating factor antagonist, in human acute pancreatitis. Br J Surg. 1995 Oct;82(10):1414-20. | |||||
REF 10 | Current Pharmaceutical Design. Page(175). | |||||
REF 11 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001346) | |||||
REF 13 | 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: 1856). | |||||
REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002078) | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005290) | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000113) | |||||
REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001351) | |||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002131) | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001713) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001180) | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004382) | |||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002130) | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001719) | |||||
REF 24 | 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: 1849). | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005514) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003636) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000051) | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003701) | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002021) | |||||
REF 30 | 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: 6078). | |||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000108) | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001821) | |||||
REF 33 | 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: 1851). | |||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002032) | |||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001674) | |||||
REF 36 | Cmi206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor. Bioorganic & Medicinal Chemistry Letters. 03/1995; 5(6):643-648. | |||||
REF 37 | 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: 1852). | |||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001311) | |||||
REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004313) | |||||
REF 40 | Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85. | |||||
REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005461) | |||||
REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003729) | |||||
REF 43 | 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: 1854). | |||||
REF 44 | Sch 37370: a new drug combining antagonism of platelet-activating factor (PAF) with antagonism of histamine. Agents Actions Suppl. 1991;34:313-21. | |||||
REF 45 | 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: 6080). | |||||
REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001989) | |||||
REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001254) | |||||
REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005037) | |||||
REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001720) | |||||
REF 50 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | |||||
REF 51 | Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor. J Biol Chem. 2010 Feb 19;285(8):5931-40. | |||||
REF 52 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | |||||
REF 53 | Clinical pipeline report, company report or official report of 60 Degrees Pharmaceuticals. | |||||
REF 54 | Lexipafant and acute pancreatitis: a critical appraisal of the clinical trials.Eur J Surg.2002;168(4):215-9. | |||||
REF 55 | Effects of YM264, a novel PAF antagonist, on puromycin aminonucleoside-induced nephropathy in the rat. Biochem Biophys Res Commun. 1991 Apr 30;176(2):781-5. | |||||
REF 56 | Platelet-activating factor antagonist BN 50730 attenuates hypoxic-ischemic brain injury in neonatal rats. Pediatr Res. 2001 Jun;49(6):804-11. | |||||
REF 57 | Effects of BN-50730 (PAF receptor antagonist) and physostigmine (AChE inhibitor) on learning and memory in mice. Methods Find Exp Clin Pharmacol. 1997 Nov;19(9):585-8. | |||||
REF 58 | Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist. J Pharmacol Exp Ther. 1991 Oct;259(1):44-51. | |||||
REF 59 | In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation. Vet Res. 2000 Mar-Apr;31(2):267-72. | |||||
REF 60 | Platelet-activating factor preferentially stimulates the phospholipase A2/cyclooxygenase cascade in the rabbit cornea. Curr Eye Res. 1995 Sep;14(9):769-75. | |||||
REF 61 | Characterization of [3H]apafant binding to PAF receptor on rabbit platelet membranes: a comparison of a microplate filtration system and a standard... J Pharmacol Toxicol Methods. 1996 Sep;36(1):53-62. | |||||
REF 62 | A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor. J Immunol Methods. 1995 Oct 26;186(2):225-31. | |||||
REF 63 | Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20. | |||||
REF 64 | Inhibitory effects of a novel PAF antagonist E6123 on anaphylactic responses in passively and actively sensitized guinea pigs and passively sensiti... Prostaglandins. 1991 Dec;42(6):541-55. | |||||
REF 65 | Formation of spherical micelles composed of the novel platelet activating factor receptor antagonist, E5880. Pharm Dev Technol. 2005;10(1):11-6. | |||||
REF 66 | MK 287: a potent, specific, and orally active receptor antagonist of platelet-activating factor. J Lipid Mediat. 1993 Jun;7(2):115-34. | |||||
REF 67 | Pharmacology of a potent platelet-activating factor antagonist: Ro 24-4736. J Pharmacol Exp Ther. 1991 Oct;259(1):78-85. | |||||
REF 68 | Effect of the PAF-receptor antagonist SM-12502 on human platelets. Inflammation. 1996 Feb;20(1):71-85. | |||||
REF 69 | Inhibitory effect of TCV-309, a novel platelet activating factor (PAF) antagonist, on endotoxin-induced disseminated intravascular coagulation in r... Thromb Res. 1993 May 15;70(4):281-93. | |||||
REF 70 | Differential effects of the PAF receptor antagonist UK-74,505 on neutrophil and eosinophil accumulation in guinea-pig skin. Br J Pharmacol. 1994 Oct;113(2):513-21. | |||||
REF 71 | ABT-299, a novel PAF antagonist, attenuates multiple effects of endotoxemia in conscious rats. Shock. 1996 Aug;6(2):112-7. | |||||
REF 72 | US patent application no. 6,274,627, Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor. | |||||
REF 73 | RP 55778, a PAF receptor antagonist, prevents and reverses LPS-induced hemoconcentration and TNF release. J Lipid Mediat. 1989 Nov-Dec;1(6):349-60. | |||||
REF 74 | US patent application no. 2007,0196,421, Soft tissue implants and drug combination compositions, and use thereof. | |||||
REF 75 | In vitro antitumour activity of the novel imidazoisoquinoline SDZ 62-434. Br J Cancer. 1993 May;67(5):989-95. | |||||
REF 76 | Pharmacologic activity of bepafant (WEB 2170), a new and selective hetrazepinoic antagonist of platelet activating factor. J Pharmacol Exp Ther. 1990 Dec;255(3):962-8. | |||||
REF 77 | Effects of the PAF antagonists BN50726 and BN50739 on arrhythmogenesis and extent of necrosis during myocardial ischaemia/reperfusion in rabbits. Br J Pharmacol. 1992 Nov;107(3):705-9. | |||||
REF 78 | Effect of the platelet-activating factor antagonist BN 50739 and its diluents on mitochondrial respiration and membrane lipids during and following... J Neurochem. 1994 May;62(5):1929-38. | |||||
REF 79 | Pharmacologic profile of BN 50739, a new PAF antagonist in vitro and in vivo. Prostaglandins. 1990 May;39(5):469-80. | |||||
REF 80 | Studies of the effect of a platelet-activating factor antagonist, CL 184,005, in animal models of gram-negative bacterial sepsis. Antimicrob Agents Chemother. 1992 Sep;36(9):1971-7. | |||||
REF 81 | DOI: 10.1016/0960-894X(95)00088-B | |||||
REF 82 | CV-6209, a highly potent antagonist of platelet activating factor in vitro and in vivo. J Pharmacol Exp Ther. 1987 Jul;242(1):263-8. | |||||
REF 83 | Effect of FR128998, a novel PAF receptor antagonist, on endotoxin-induced disseminated intravascular coagulation. Eur J Pharmacol. 1994 Jun 13;258(3):239-46. | |||||
REF 84 | WO patent application no. 2002,01223,5, 1,4-dihydropyridines as bradykinin antagonists. | |||||
REF 85 | Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,... J Med Chem. 1992 Sep 18;35(19):3474-82. | |||||
REF 86 | Pentadienyl carboxamide derivatives as antagonists of platelet-activating factor. J Med Chem. 1989 Aug;32(8):1820-35. | |||||
REF 87 | Conformational considerations in the design of dual antagonists of platelet-activating factor (PAF) and histamine. Bioorg Med Chem. 1999 Jul;7(7):1413-23. | |||||
REF 88 | Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists. J Med Chem. 1993 Oct 15;36(21):3098-102. | |||||
REF 89 | PCA-4248, a PAF receptor antagonist, inhibits PAF-induced phosphoinositide turnover. Eur J Pharmacol. 1995 Aug 15;290(3):183-8. | |||||
REF 90 | Tulopafant, a PAF receptor antagonist, increases capillary patency and prolongs survival in discordant cardiac xenotransplants. J Lipid Mediat. 1993 May;7(1):79-84. | |||||
REF 91 | Platelet-activating factor: the effector of protein-rich plasma extravasation and nitric oxide synthase induction in rat immune complex peritonitis. Br J Pharmacol. 1995 Feb;114(4):895-901. | |||||
REF 92 | WEB 2347: pharmacology of a new very potent and long acting hetrazepinoic PAF-antagonist and its action in repeatedly sensitized guinea-pigs. J Lipid Mediat. 1991 Jul-Aug;4(1):39-44. | |||||
REF 93 | Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists. J Med Chem. 2003 Feb 13;46(4):601-8. | |||||
REF 94 | The role of platelet-activating factor (PAF) and the efficacy of ABT-491, a highly potent and selective PAF antagonist, in experimental allergic rhinitis. J Pharmacol Exp Ther. 1998 Jan;284(1):83-8. | |||||
REF 95 | Inhibition by CV-3988 of the binding of [3H]-platelet activating factor (PAF) to the platelet. Biochem Pharmacol. 1985 May 1;34(9):1491-5. | |||||
REF 96 | FR-900452, a specific antagonist of platelet activating factor (PAF) produced by Streptomyces phaeofaciens. I. Taxonomy, fermentation, isolation, a... J Antibiot (Tokyo). 1986 Feb;39(2):198-204. | |||||
REF 97 | Platelet-activating factor (PAF) inhibitory profile of KO-286011 on blood platelets in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 1990 Dec;342(6):713-8. | |||||
REF 98 | Superior Neuroprotective Efficacy of LAU-0901, a Novel Platelet-Activating Factor Antagonist, in Experimental Stroke. Transl Stroke Res. 2012 Mar;3(1):154-63. | |||||
REF 99 | LAU-0901, a novel platelet-activating factor antagonist, is highly neuroprotective in cerebral ischemia. Exp Neurol. 2008 Dec;214(2):253-8. | |||||
REF 100 | 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: 334). | |||||
REF 101 | Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis. J Biol Chem. 1996 Sep20;271(38):23298-303. | |||||
REF 102 | Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation. J Biol Chem. 2001 Nov 16;276(46):43025-30. | |||||
REF 103 | [3H]52770 RP, a platelet-activating factor receptor antagonist, and tritiated platelet-activating factor label a common specific binding site in human polymorphonuclear leukocytes. J Pharmacol Exp Ther. 1988 Feb;244(2):709-15. | |||||
REF 104 | The effect of SRI 63-675, a competitive platelet-activating factor receptor-antagonist, in the generalized Shwartzman reaction. J Lipid Mediat Cell Signal. 1994 Sep;10(3):229-42. | |||||
REF 105 | Effects of PAF-antagonists in mouse ear oedema induced by several inflammatory agents. Br J Pharmacol. 1991 Dec;104(4):990-4. | |||||
REF 106 | US patent application no. 6,673,908, Tumor necrosis factor receptor 2. | |||||
REF 107 | Evidence for the autocrine induction of capacitation of mammalian spermatozoa.J Biol Chem.2001 Jul 20;276(29):26962-8. |
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