PTAFR

Summary

PTAFR (platelet activating factor receptor, HGNC:9582) is a protein-coding gene on chromosome 1p35.3, encoding Platelet-activating factor receptor (P25105). Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth-muscle contractile and hypotensive activity.

This gene encodes a seven-transmembrane G-protein-coupled receptor for platelet-activating factor (PAF) that localizes to lipid rafts and/or caveolae in the cell membrane. PAF (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine) is a phospholipid that plays a significant role in oncogenic transformation, tumor growth, angiogenesis, metastasis, and pro-inflammatory processes. Binding of PAF to the PAF-receptor (PAFR) stimulates numerous signal transduction pathways including phospholipase C, D, A2, mitogen-activated protein kinases (MAPKs), and the phosphatidylinositol-calcium second messenger system. Following PAFR activation, cells become rapidly desensitized and this refractory state is dependent on PAFR phosphorylation, internalization, and down-regulation. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 5724 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 47 total
• Druggable target: yes — 8 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000952

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:9582
Approved symbol	PTAFR
Name	platelet activating factor receptor
Location	1p35.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000169403
Ensembl biotype	protein_coding
OMIM	173393
Entrez	5724

Gene structure

Transcript identifiers

Ensembl transcripts: 19 — 19 protein_coding

ENST00000305392, ENST00000373857, ENST00000539896, ENST00000887612, ENST00000887614, ENST00000887616, ENST00000887618, ENST00000887620, ENST00000924885, ENST00000964581, ENST00000964582, ENST00000964583, ENST00000964584, ENST00000964585, ENST00000964586, ENST00000964587, ENST00000964588, ENST00000964589, ENST00000964590

RefSeq mRNA: 4 — MANE Select: NM_000952 NM_000952, NM_001164721, NM_001164722, NM_001164723

CCDS: CCDS318

Canonical transcript exons

ENST00000373857 — 2 exons

Exon	Start	End
ENSE00001159108	28176592	28176690
ENSE00001461771	28147166	28151059

Expression profiles

Bgee: expression breadth ubiquitous, 250 present calls, max score 95.60.

FANTOM5 (CAGE): breadth broad, TPM avg 18.6910 / max 973.7425, expressed in 655 samples.

FANTOM5 promoters (20 alternative TSS)

Promoter ID	TPM avg	Samples expressed
11333	9.0192	434
11331	7.2585	374
11344	0.8845	206
11332	0.5094	177
11338	0.1547	20
11336	0.1495	27
11325	0.1455	70
11326	0.1402	61
11340	0.1364	41
11330	0.0612	32

Top tissues by expression

283 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
monocyte	CL:0000576	95.60	gold quality
blood	UBERON:0000178	95.14	gold quality
leukocyte	CL:0000738	94.98	gold quality
mononuclear cell	CL:0000842	94.91	gold quality
granulocyte	CL:0000094	93.01	gold quality
olfactory bulb	UBERON:0002264	90.14	silver quality
bone marrow	UBERON:0002371	89.76	gold quality
type B pancreatic cell	CL:0000169	89.54	gold quality
vena cava	UBERON:0004087	88.27	gold quality
nasal cavity epithelium	UBERON:0005384	87.44	silver quality
pericardium	UBERON:0002407	86.24	gold quality
caecum	UBERON:0001153	86.22	gold quality
body of tongue	UBERON:0011876	85.86	gold quality
bone marrow cell	CL:0002092	85.57	gold quality
epithelium of nasopharynx	UBERON:0001951	85.42	silver quality
nasopharynx	UBERON:0001728	85.41	gold quality
vermiform appendix	UBERON:0001154	85.27	gold quality
subthalamic nucleus	UBERON:0001906	84.86	gold quality
inferior vagus X ganglion	UBERON:0005363	84.33	gold quality
gluteal muscle	UBERON:0002000	84.28	silver quality
trabecular bone tissue	UBERON:0002483	84.07	gold quality
parotid gland	UBERON:0001831	83.92	gold quality
ileal mucosa	UBERON:0000331	83.84	silver quality
heart right ventricle	UBERON:0002080	83.33	gold quality
lateral nuclear group of thalamus	UBERON:0002736	83.28	gold quality
esophagus squamous epithelium	UBERON:0006920	83.28	silver quality
amniotic fluid	UBERON:0000173	83.15	gold quality
palpebral conjunctiva	UBERON:0001812	82.81	gold quality
upper leg skin	UBERON:0004262	82.80	silver quality
pons	UBERON:0000988	82.73	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	15.98
E-MTAB-5061	no	3.47

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): NFKB1, NFKB, NR1I2, PPARA, RELA

miRNA regulators (miRDB)

119 targeting PTAFR, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-4283	100.00	66.42	2097
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-548AW	99.99	72.57	3559
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-32-5P	99.98	75.21	1964
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-367-3P	99.98	74.83	1819
HSA-MIR-4650-5P	99.98	64.69	999
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-9985	99.98	72.11	2939
HSA-LET-7D-5P	99.96	71.76	1632
HSA-MIR-4458	99.96	71.64	1650
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-545-3P	99.95	70.74	2783
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505

Literature-anchored findings (GeneRIF, showing 40)

• activates the extracellular signal-regulated kinase mitogen-activated protein kinase and induces proliferation of epidermal cells (PMID:11861812)
• Neuroblastoma clone cells show an inverse relationship between invasiveness and differentiative capacity and by the expression of specific cell surface PAF receptors. (PMID:11928813)
• PAF receptor transcripts in five human cancer cell lines derived from the breast (BT20, SKBR3 and T47D cells), the pancreas (Miapaca cells) and the bladder (5,637 cells) confirm the existence of a splice variant of the PAF-R transcript 2. (PMID:12467527)
• a novel pathway whereby the epidermal PAF-R can augment chemotherapy-induced apoptotic effects through an NF-kappaB-dependent process (PMID:12601006)
• the epidermal platelet-activating factor receptor augments staphylococcal alpha-toxin signaling (PMID:12713583)
• platelet-activating factor receptor is desensitized and internalized by coumermycin-gyrase B-induced dimerization (PMID:12756251)
• The C-terminal tail of the PAFR is of critical importance for platelet-activating factor-induced Janus kinase 2 activation. (PMID:14500680)
• PAFR degradation can occur via both the proteasome and lysosomal pathways and ligand-stimulated degradation is ubiquitin-dependent (PMID:14500726)
• platelet-activating factor receptor-mediated signaling has a critical role in differentiated endothelial cell functions, including cell migration and proteolytic activation of MMP2 (PMID:14617636)
• investigated whether the increase of uPA monocyte expression and chemokine releases induced by oxidised low density lipoproteins involved proinflammatory phospholipid products having platelet-activating factor-like activity via the PAFR pathway (PMID:15149885)
• Analysis of 102 B-CLL patients revealed dramatic differences for their membrane PAF-R expression, a result that might be related to their plasma IL-4 levels. (PMID:15160913)
• the PAFR gene missense mutation has a relation to the susceptibility for multiple sclerosis . (PMID:15748960)
• UVB photo-oxidizes cellular phospholipids, creating PAF analogs that stimulate the PAF receptor to induce further PAF synthesis and apoptosis (PMID:16115894)
• PAF induced CREB and ATF-1 phosphorylation via a PAFR-mediated signal transduction mechanism that required pertussis toxin-insensitive Galphaq protein and adenylate cyclase activity and was antagonized by a cAMP-dependent PKA and p38 MAPK inhibitors. (PMID:16306050)
• presence of functional PAF-R in arterial spindle-shaped smooth muscle cells of synthetic phenotype may be important for their migration from the media into the intima and atherosclerotic plaques formation (PMID:16793019)
• The functional PAF-R are present in blast cells of patients with acute leukemia; a result that could be of physiologic importance regarding the important effect of PAF on leukocytes maturation and functions. (PMID:16837045)
• These studies suggest that SZ95 sebocytes express functional PAF-Rs and PAF-Rs are involved in regulating the expression of inflammatory mediators, including COX-2, PGE(2) and IL-8. (PMID:16984258)
• epidermal PAF-R can modulate UVB-mediated early gene expression (PMID:17928889)
• a lower expression of PAFR in HCC correlated with both poor differentiation and portal venous invasion. (PMID:18187960)
• analysis of PAFR activation and pleiotropic effects on tyrosine phospho-EGFR/Src/FAK/paxillin in ovarian cancer (PMID:18632638)
• cis-urocanic acid stimulates mediator production by a pathway that is independent of these serotonin 2A and PAF receptors in human keratinocytes (PMID:19474802)
• PAFR is localized in lipid rafts and/or caveolae, a position that is important for proper coupling to downstream signaling elements. (PMID:19620302)
• analysis of the cross-talk between protease-activated receptor 1 and platelet-activating factor receptor regulates melanoma cell adhesion molecule (MCAM/MUC18) expression and melanoma metastasis (PMID:19703903)
• conserved proline in TM6 is crucial for intracellular trafficking of PAFR. (PMID:20007715)
• Results reveal that some strains of Gram-positive bacteria exploit hypoxia-inducible factor 1 alpha-regulated platelet-activating factor receptor as a means for translocation through intestinal epithelial cells. (PMID:20032301)
• role in activation of mast cells by PAF. (PMID:20392487)
• The expression of PAF receptor (PAF-R) in early endothelial progenitor cell and the release of PAF under stimulation with factors involved in endothelial dysfunction, were investigated. (PMID:20637897)
• Platelet-activating factor plays a pivotal role in the oxLDL-induced recruitment of hBMSCs through mechanisms involving platelet-activating factor receptor dependent activation of Mitogen-Activated Protein Kinases. (PMID:21063106)
• Urban particulate matter (PM) increases adhesion of S. pneumoniae to human airway epithelial cells. PM-stimulated adhesion is mediated by oxidative stress and PAFR. (PMID:21247619)
• Pneumococcal ligands keratin 10, laminin receptor and platelet-activating factor receptor are elevated in aged lungs and contribute to the enhanced susceptibility to pneumonia. (PMID:21615674)
• An implication of platelet-activating factor receptor A224D mutation in the susceptibility to relapsing-remitting multiple sclerosis in Tunisian population. (PMID:21658861)
• PAFR may have a role in tumor response mechanisms, such as stress responses caused by chemotherapeutic agents (PMID:22570511)
• recognition of apoptotic cells by phagocytes leads to activation of PAFR pathways, resulting in a microenvironment response favorable to melanoma growth (PMID:22577252)
• Eosinophils use their platelet-activating factor receptors (PAFRs) to interact directly with Staphylococcus aureus. (PMID:22595142)
• Data suggest that expression of PAFR and SIRT1 (sirtuin 1) is down-regulated in endothelial progenitor cells of type 2 diabetic patients with poor glycaemic control compared to those with good glycaemic control. (PMID:23070058)
• Inhibition of platelet aggregation by lipoteichoic acid was blocked using a monoclonal anti-PafR antibody and Ginkgolide B,a well-defined PafR antagonist, demonstrating that the LTA inhibitory signal occurs via PafR. (PMID:23911710)
• oxLDL induces alternative macrophage activation by mechanisms involving CD36 and PAFR (PMID:24062612)
• oxLDL induces the recruitment of PAFR and CD36 into the same lipid rafts, which is important for oxLDL uptake and IL-10 production (PMID:24130805)
• Data suggest PAF/PAF receptor signaling exerts proinflammatory effect on neutrophil via down-regulation of LXRa (liver X receptor alpha) and target genes (ATP-binding cassette transporter (ABC) A1, ABC G1, sterol response element binding protein 1c). (PMID:24289152)
• patients presenting elevated PAFR expression had significantly longer survival times compared to those with low PAFR expression (log-rank test, p<0.001). (PMID:24824933)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	ptafr	ENSDARG00000042370
mus_musculus	Ptafr	ENSMUSG00000056529
rattus_norvegicus	Ptafr	ENSRNOG00000013231

Paralogs (6): GPR87 (ENSG00000138271), P2RY12 (ENSG00000169313), GPR34 (ENSG00000171659), P2RY14 (ENSG00000174944), GPR171 (ENSG00000174946), P2RY13 (ENSG00000181631)

Protein

Protein identifiers

Platelet-activating factor receptor — P25105 (reviewed: P25105)

All UniProt accessions (1): P25105

UniProt curated annotations — full annotation on UniProt →

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.

Subunit / interactions. Interacts with ARRB1.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in the placenta, lung, left and right heart ventricles, heart atrium, leukocytes and differentiated HL-60 granulocytes.

Induction. By CSF2/GM-CSF, IL5/interleukin-5 and n-butyrate.

Similarity. Belongs to the G-protein coupled receptor 1 family.

RefSeq proteins (4): NP_000943, NP_001158193, NP_001158194, NP_001158195 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR002282	PAF_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (44 total): helix 13, topological domain 8, transmembrane region 7, sequence conflict 7, sequence variant 2, turn 2, strand 2, chain 1, glycosylation site 1, disulfide bond 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
5ZKP	X-RAY DIFFRACTION	2.81
5ZKQ	X-RAY DIFFRACTION	2.9
8XYD	ELECTRON MICROSCOPY	2.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P25105-F1	86.61	0.59

Antibody-complex structures (SAbDab): 1 — 8XYD

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Disulfide bonds (1): 90–173

Glycosylation sites (1): 169

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-416476	G alpha (q) signalling events
R-HSA-6783783	Interleukin-10 signaling
R-HSA-6798695	Neutrophil degranulation
R-HSA-877300	Interferon gamma signaling

MSigDB gene sets: 244 (showing top): GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_UP, GOBP_G_PROTEIN_COUPLED_PURINERGIC_NUCLEOTIDE_RECEPTOR_SIGNALING_PATHWAY, REACTOME_INNATE_IMMUNE_SYSTEM, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOCC_SECRETORY_GRANULE, GOBP_CELLULAR_RESPONSE_TO_BIOTIC_STIMULUS, MODULE_45, MODULE_64, GOBP_INOSITOL_PHOSPHATE_METABOLIC_PROCESS, GOBP_POLYOL_METABOLIC_PROCESS, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS

GO Biological Process (10): chemotaxis (GO:0006935), inflammatory response (GO:0006954), immune response (GO:0006955), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), inositol trisphosphate biosynthetic process (GO:0032959), signal transduction (GO:0007165), lipopolysaccharide-mediated signaling pathway (GO:0031663), response to lipopolysaccharide (GO:0032496), G protein-coupled purinergic nucleotide receptor signaling pathway (GO:0035589)

GO Molecular Function (7): lipopolysaccharide binding (GO:0001530), lipopolysaccharide immune receptor activity (GO:0001875), G protein-coupled receptor activity (GO:0004930), platelet activating factor receptor activity (GO:0004992), phospholipid binding (GO:0005543), G protein-coupled purinergic nucleotide receptor activity (GO:0045028), protein binding (GO:0005515)

GO Cellular Component (4): plasma membrane (GO:0005886), membrane (GO:0016020), secretory granule membrane (GO:0030667), tertiary granule membrane (GO:0070821)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
GPCR ligand binding	1
GPCR downstream signalling	1
Signaling by Interleukins	1
Innate Immune System	1
Interferon Signaling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor activity	3
G protein-coupled receptor signaling pathway	2
lipid binding	2
response to chemical	1
taxis	1
defense response	1
immune system process	1
response to stimulus	1
signal transduction	1
phospholipase C activator activity	1
inositol trisphosphate metabolic process	1
inositol phosphate biosynthetic process	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
cell surface receptor signaling pathway	1
cellular response to lipopolysaccharide	1
response to molecule of bacterial origin	1
response to lipid	1
response to oxygen-containing compound	1
purinergic nucleotide receptor signaling pathway	1
carbohydrate derivative binding	1
lipopolysaccharide binding	1
lipopolysaccharide-mediated signaling pathway	1
pattern recognition receptor activity	1
transmembrane signaling receptor activity	1
purinergic nucleotide receptor activity	1
G protein-coupled purinergic nucleotide receptor signaling pathway	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1
secretory granule	1
cytoplasmic vesicle membrane	1
bounding membrane of organelle	1
secretory granule membrane	1
tertiary granule	1

Protein interactions and networks

STRING

1620 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PTAFR	GPR135	Q8IZ08	861
PTAFR	TYK2	P29597	723
PTAFR	CAV1	Q03135	652
PTAFR	TLR4	O00206	627
PTAFR	ARRB1	P49407	615
PTAFR	ICAM1	P05362	602
PTAFR	ITGB2	P05107	544
PTAFR	GNAQ	P50148	537
PTAFR	PLA2G7	Q13093	535
PTAFR	CD36	P16671	525
PTAFR	SCARB1	Q8WTV0	523
PTAFR	SCARB2	Q14108	523
PTAFR	STAT2	P52630	521
PTAFR	CCDC117	Q8IWD4	493
PTAFR	ITGAM	P11215	481

IntAct

25 interactions, top by confidence:

A	B	Type	Score
PRNP	PTAFR	psi-mi:“MI:2364”(proximity)	0.450
MBP	PTAFR	psi-mi:“MI:2364”(proximity)	0.450
MBP	PTAFR	psi-mi:“MI:0915”(physical association)	0.450
PRNP	PTAFR	psi-mi:“MI:0915”(physical association)	0.450
PTK2	PTAFR	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	PTAFR	psi-mi:“MI:0915”(physical association)	0.400
PTAFR	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	PTAFR	psi-mi:“MI:0915”(physical association)	0.400
GRIN1	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
IFITM3	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
MFSD3	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
PLLP	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
RHBDD2	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
SERINC5	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
TMX2	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
TMEM120A	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
PPM1J	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
PTAFR	CALM1	psi-mi:“MI:0915”(physical association)	0.370
GTPBP3	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
GORAB	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
SPATA24	PTAFR	psi-mi:“MI:0915”(physical association)	0.370
PTAFR	SCAMP2	psi-mi:“MI:0914”(association)	0.350

BioGRID (53): ARRB1 (Affinity Capture-Western), PTAFR (Affinity Capture-MS), MBP (FRET), PRNP (FRET), MBP (Two-hybrid), PRNP (Two-hybrid), GRIN1 (Two-hybrid), IFITM3 (Two-hybrid), MFSD3 (Two-hybrid), PLLP (Two-hybrid), RHBDD2 (Two-hybrid), SERINC5 (Two-hybrid), TMX2 (Two-hybrid), TMEM120A (Two-hybrid), PPM1J (Two-hybrid)

ESM2 similar proteins: A0A4W3GG95, A7YY44, B0F9W3, B0UXR0, B2GV46, B3G515, B5X337, E7FEL0, O00398, O46685, O70526, P21556, P25023, P25105, P25116, P26824, P30411, P30558, P32299, P43657, P46002, P46093, P49019, P50132, P56488, Q00991, Q15743, Q1JQB3, Q28642, Q3UFD7, Q4G072, Q4KLH9, Q61038, Q62035, Q80Z39, Q8BFQ3, Q8BFU7, Q8BLG2, Q8BMC0, Q8BUD0

Diamond homologs: A0A4W3GG95, A0A6I8PUB9, A6QLE7, A6QNL7, B5X337, D4A7K7, E7FEL0, E9QJ73, O00254, O02666, O02824, O46685, O55197, O73810, O77408, O77621, O89039, O93361, P11613, P18130, P20288, P21556, P25105, P25106, P28566, P32246, P32249, P32250, P34996, P35346, P35348, P35351, P35366, P35374, P35383, P35411, P41231, P43140, P43657, P46002

SIGNOR signaling

10 interactions.

A	Effect	B	Mechanism
“ginkgolide B”	down-regulates	PTAFR	“chemical inhibition”
PTAFR	“up-regulates activity”	GNAS	binding
PTAFR	“up-regulates activity”	GNAL	binding
PTAFR	“up-regulates activity”	GNAI1	binding
PTAFR	“up-regulates activity”	GNAI3	binding
PTAFR	“up-regulates activity”	GNAO1	binding
PTAFR	“up-regulates activity”	GNAZ	binding
PTAFR	“up-regulates activity”	GNAQ	binding
PTAFR	“up-regulates activity”	GNA14	binding
2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine	“up-regulates activity”	PTAFR	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

47 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	42
Likely benign	2
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

449 predictions. Top by Δscore:

Variant	Effect	Δscore
1:28151060:C:CC	acceptor_gain	0.9900
1:28176586:CCTTA:C	donor_loss	0.9800
1:28176587:CTTA:C	donor_loss	0.9800
1:28176588:TTA:T	donor_loss	0.9800
1:28176589:TA:T	donor_loss	0.9800
1:28176590:A:AT	donor_loss	0.9800
1:28176591:CCTG:C	donor_loss	0.9800
1:28151059:CCTG:C	acceptor_loss	0.9700
1:28151061:T:C	acceptor_loss	0.9700
1:28176776:T:TA	donor_gain	0.9300
1:28172882:T:C	acceptor_gain	0.9200
1:28172882:T:TC	acceptor_gain	0.9200
1:28176765:C:CT	donor_gain	0.9200
1:28151057:TGC:T	acceptor_gain	0.9100
1:28151069:C:CT	acceptor_gain	0.9100
1:28151062:G:C	acceptor_loss	0.9000
1:28151073:C:CT	acceptor_loss	0.9000
1:28151074:A:T	acceptor_loss	0.8900
1:28151069:C:T	acceptor_gain	0.8800
1:28151056:GTGC:G	acceptor_gain	0.8600
1:28151058:GC:G	acceptor_gain	0.8400
1:28151059:CC:C	acceptor_gain	0.8400
1:28151072:A:T	acceptor_loss	0.8300
1:28155547:TCAG:T	donor_gain	0.8300
1:28175263:T:TA	donor_gain	0.8200
1:28151058:GCCT:G	acceptor_gain	0.7900
1:28172323:TGTTA:T	donor_gain	0.7900
1:28151055:GGTGC:G	acceptor_gain	0.7800
1:28151070:A:T	acceptor_loss	0.7800
1:28176590:A:AC	donor_gain	0.7800

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000027735 (1:28187815 A>T), RS1000056383 (1:28163939 G>A), RS1000088372 (1:28181392 G>C), RS1000108889 (1:28175158 C>T), RS1000170168 (1:28192145 C>T), RS1000218904 (1:28150417 A>T), RS1000237728 (1:28155268 T>C), RS1000250237 (1:28157336 G>A), RS1000311451 (1:28155000 C>T), RS1000324400 (1:28168300 C>T), RS1000389702 (1:28176341 G>A), RS1000390469 (1:28162721 G>C), RS1000444996 (1:28175962 G>A,T), RS1000518013 (1:28179741 A>G,T), RS1000529039 (1:28189091 G>A)

Disease associations

OMIM: gene MIM:173393 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST006988_75	Blond vs. brown/black hair color	4.000000e-08

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0003924	hair color

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL250 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

8 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 70,872 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL104	CLOTRIMAZOLE	4	56,325
CHEMBL32479	BROTIZOLAM	4	7,289
CHEMBL91397	RUPATADINE	4	2,155
CHEMBL2105667	ORVEPITANT	2	257
CHEMBL280164	APAFANT	2	772
CHEMBL322832	LEXIPAFANT	2	850
CHEMBL34431	CILOSTAMIDE	2	3,222
CHEMBL349811	TULOPAFANT	2	2

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Platelet-activating factor receptor

Most potent curated ligand interactions (40 total), top 25:

Ligand	Action	Affinity	Parameter
foropafant	Antagonist	10.3	pKi
ABT-299	Antagonist	9.5	pKi
ABT-491	Antagonist	9.2	pKi
israpafant	Antagonist	9.0	pIC50
[3H]PAF	Full agonist	8.9	pKd
[3H]52770 RP	Antagonist	8.4	pKd
CV-6209	Antagonist	8.3	pIC50
RP-52770	Antagonist	8.2	pKi
[3H]apafant	Antagonist	8.0	pKd
PAF	Full agonist	7.9	pKi
L659989	Antagonist	7.8	pKi
2-O-ethyl-PAF C-16	Full agonist	7.7	pIC50
apafant	Antagonist	7.5	pKi
SDZ 64-412	Antagonist	7.2	pIC50
10-OBn-7α-F-gingkolide B	Antagonist	7.0	pKi
7α-Cl-ginkgolide B	Antagonist	7.0	pKi
10-OBn-ginkgolide B	Antagonist	6.9	pKi
BN 50739	Antagonist	6.9	pKi
CV-3988	Antagonist	6.8	pIC50
bepafant	Antagonist	6.49	pIC50
7α-N3-ginkgolide B	Antagonist	6.3	pKi
10-OBn-epi-ginkgolide C	Antagonist	6.2	pKi
7α-NHMe-ginkgolide B	Antagonist	6.2	pKi
SCH 37370	Antagonist	6.2	pIC50
SCH 40338	Antagonist	6.2	pIC50

Binding affinities (BindingDB)

13 measured of 16 human assays (20 total across all organisms); most potent 13 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Halcion	KI	0.68 nM
(R)-2-{[Acetyl-(2-methoxy-3-octadecylcarbamoyloxy-propoxycarbonyl)-amino]-methyl}-1-ethyl-pyridinium; chloride	KI	1.4 nM
1H,3H-Pyrrolo[1,2-c]thiazole-7-carboxamide,N-(3-benzoylphenyl)-3-(3-pyridinyl)-	KI	11.7 nM
CAS_129364	KI	16.9 nM
2-Bromo-4-(2-chloro-phenyl)-9-methyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulene	KI	17.4 nM
3-[4-(2-Chloro-phenyl)-9-methyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-2-yl]-1-morpholin-4-yl-propan-1-one(WEB2086)	KI	23.2 nM
NSC_108044	KI	129 nM
(L 652731)2,5-Bis-(3,4,5-trimethoxy-phenyl)-tetrahydro-furan	KI	215 nM
5-Allyl-2-(3,4-dimethoxy-phenyl)-3a-methoxy-3-methyl-3,3a-dihydro-2H-benzofuran-6-one	KI	225 nM
CV-3988	KI	575 nM
BN 52021	KI	643 nM
SR 147778	KI	1000 nM
RP 59228	KI	1360 nM

ChEMBL bioactivities

448 potent at pChembl≥5 of 476 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.82	IC50	0.015	nM	CHEMBL157078
9.82	Ki	0.15	nM	CHEMBL1235246
9.70	IC50	0.2	nM	CHEMBL277701
9.55	IC50	0.28	nM	CHEMBL1235246
9.52	IC50	0.3	nM	CHEMBL20195
9.42	Ki	0.38	nM	LEXIPAFANT
9.40	IC50	0.4	nM	CHEMBL5439289
9.40	IC50	0.4	nM	CHEMBL5408810
9.30	IC50	0.5	nM	CHEMBL5433867
9.30	IC50	0.5	nM	CHEMBL5411872
9.24	Ki	0.57	nM	CHEMBL369225
9.22	IC50	0.6	nM	CHEMBL19640
9.22	IC50	0.6	nM	CHEMBL5439944
9.22	IC50	0.6	nM	CHEMBL5422270
9.15	IC50	0.7	nM	CHEMBL19747
9.15	IC50	0.7	nM	CHEMBL20019
9.15	IC50	0.7	nM	CHEMBL5425646
9.05	IC50	0.9	nM	CHEMBL5399089
9.05	IC50	0.9	nM	CHEMBL5431916
9.01	Ki	0.98	nM	CHEMBL317090
9.00	IC50	1	nM	CHEMBL99294
9.00	IC50	1	nM	CHEMBL281779
9.00	IC50	1	nM	CHEMBL283162
9.00	IC50	1	nM	CHEMBL282883
9.00	Ki	1	nM	CHEMBL293773
9.00	IC50	1	nM	CHEMBL293773
8.96	IC50	1.1	nM	CHEMBL5411707
8.89	IC50	1.3	nM	CHEMBL5413888
8.89	IC50	1.3	nM	CHEMBL5400532
8.73	Ki	1.85	nM	CHEMBL118105
8.70	IC50	2	nM	CHEMBL29067
8.70	IC50	2	nM	CHEMBL279665
8.70	IC50	2	nM	CHEMBL296149
8.70	IC50	2	nM	CHEMBL2113725
8.70	IC50	2	nM	CHEMBL57676
8.64	IC50	2.3	nM	CHEMBL104967
8.64	IC50	2.3	nM	CHEMBL156461
8.60	Ki	2.5	nM	CHEMBL117413
8.54	Ki	2.9	nM	CHEMBL118105
8.54	Ki	2.86	nM	CHEMBL334115
8.52	IC50	3	nM	CHEMBL99924
8.52	IC50	3	nM	CHEMBL104290
8.52	IC50	3	nM	CHEMBL429066
8.52	IC50	3	nM	CHEMBL20163
8.52	IC50	3	nM	CHEMBL34548
8.52	Ki	3	nM	CHEMBL407427
8.49	Ki	3.2	nM	CHEMBL299944
8.43	Ki	3.72	nM	CHEMBL116072
8.43	Ki	3.7	nM	CHEMBL334115
8.40	IC50	4	nM	CHEMBL20418

PubChem BioAssay actives

340 with measured affinity, of 701 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
[(2R)-2-acetyloxy-3-hexadecoxypropyl] 2-(trimethylazaniumyl)ethyl phosphate	751655: Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs	ki	0.0001	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-3,4-dihydroquinolin-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0002	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-3-methylbenzimidazol-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0003	uM
(13S)-9-(2-chlorophenyl)-3-methyl-N-[(2S)-1,2,3,4-tetrahydronaphthalen-2-yl]spiro[16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene-7,1’-cyclopropane]-13-carboxamide	2015452: Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0004	uM
(9S,13R)-9-(2-chlorophenyl)-3-methyl-N-[[4-(trifluoromethyl)phenyl]methyl]-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,11(15)-tetraene-13-carboxamide	1968797: Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0004	uM
ethyl (2S)-4-methyl-2-[methyl-[4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]phenyl]sulfonylamino]pentanoate	161085: The compound was evaluated for its binding affinity against PAF receptor in human platelet	ki	0.0004	uM
(9R,13S)-9-(2-chlorophenyl)-N-(3-ethyl-1-bicyclo[1.1.1]pentanyl)-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,11(15)-tetraene-13-carboxamide	1968797: Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0005	uM
(13S)-9-(2-chlorophenyl)-N-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-3-methylspiro[16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene-7,1’-cyclopropane]-13-carboxamide	2015452: Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0005	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-3-methylquinazoline-2,4-dione	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0006	uM
4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide	161085: The compound was evaluated for its binding affinity against PAF receptor in human platelet	ki	0.0006	uM
(13S)-9-(2-chlorophenyl)-N-(5-fluoro-2,3-dihydro-1H-inden-1-yl)-3-methylspiro[16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene-7,1’-cyclopropane]-13-carboxamide	2015452: Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0006	uM
(13S)-9-(2-chlorophenyl)-N-(6-fluoro-2,3-dihydro-1H-inden-1-yl)-3-methylspiro[16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene-7,1’-cyclopropane]-13-carboxamide	2015452: Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0006	uM
4-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-1,4-benzoxazin-3-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0007	uM
2a-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-1,3,4,5-tetrahydrobenzo[cd]indol-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0007	uM
(9R,13S)-9-(2-chlorophenyl)-3-methyl-N,N-dipropyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,11(15)-tetraene-13-carboxamide	1968797: Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0007	uM
(13S)-9-(2-chlorophenyl)-N-(4,4-dimethylcyclohexyl)-N,3-dimethylspiro[16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene-7,1’-cyclopropane]-13-carboxamide	2015452: Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0009	uM
(13S)-9-(2-chlorophenyl)-3-methyl-N,N-dipropylspiro[16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene-7,1’-cyclopropane]-13-carboxamide	2015452: Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0009	uM
(E)-3-(1-butyl-4-methoxynaphthalen-2-yl)-N-[(2S)-5-pyridin-3-ylpentan-2-yl]prop-2-enamide	157734: Inhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog blood	ic50	0.0010	uM
7-(2-chlorophenyl)-4-(3-indazol-1-ylprop-1-ynyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0010	uM
2-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]isoquinolin-1-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0010	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-3-phenylbenzimidazol-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0010	uM
[3-[(3R)-7-[1-(dimethylcarbamoyl)-6-(4-fluorophenyl)indole-3-carbonyl]-1,3-dihydropyrrolo[1,2-c][1,3]thiazol-3-yl]pyridin-1-ium-1-yl]methyl acetate chloride	161085: The compound was evaluated for its binding affinity against PAF receptor in human platelet	ki	0.0010	uM
(9R,13R)-N-benzyl-9-(2-chlorophenyl)-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,11(15)-tetraene-13-carboxamide	1968797: Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0011	uM
(9S,13R)-9-(2-chlorophenyl)-N-(4,4-difluorocyclohexyl)-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,11(15)-tetraene-13-carboxamide	1968797: Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0013	uM
(9S,13R)-9-(2-chlorophenyl)-N-[1-(5-chloro-2-pyridinyl)cyclopropyl]-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,11(15)-tetraene-13-carboxamide	1968797: Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay	ic50	0.0013	uM
1-[3-(3-hydroxypropoxy)-2-propoxy-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]sulfonylpropan-2-one	157729: Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation	ki	0.0019	uM
1-butyl-1-hydroxy-3-[3-methoxy-2-[2-(2,3,5,6-tetrafluorophenyl)sulfanylethoxy]-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]urea	161084: Displacement of [3H]PAF from PAF receptor of human platelet membranes	ic50	0.0020	uM
(2E)-5,5-bis(3-methoxyphenyl)-N-(4-pyridin-3-ylbutyl)penta-2,4-dienamide	157737: Inhibition of platelet activating factor receptor binding activity in dog platelets using [3H]PAF as radioligand	ic50	0.0020	uM
(2E,4E)-5-(4-methoxyphenyl)-5-phenyl-N-[(2R)-5-pyridin-3-ylpentan-2-yl]penta-2,4-dienamide	157737: Inhibition of platelet activating factor receptor binding activity in dog platelets using [3H]PAF as radioligand	ic50	0.0020	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]quinolin-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0020	uM
1-[3-(3-morpholin-4-ylpropoxy)-2-propoxy-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]sulfonylpropan-2-one	157729: Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation	ki	0.0025	uM
(4S)-5-[3-methoxy-2-propoxy-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]sulfonyl-4-methylpentan-1-ol	157729: Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation	ki	0.0029	uM
1-[3-(3-imidazol-1-ylpropoxy)-2-propoxy-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]sulfonylpropan-2-one	157729: Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation	ki	0.0030	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-3H-indol-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0030	uM
7-(2-chlorophenyl)-13-methyl-4-(3-phenoxyprop-1-ynyl)-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0030	uM
(E)-3-(1-butyl-4,7-dimethoxynaphthalen-2-yl)-N-[(2S)-5-pyridin-3-ylpentan-2-yl]prop-2-enamide	157734: Inhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog blood	ic50	0.0030	uM
2-[3-methoxy-2-propoxy-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]sulfonylethanol	157726: In vitro effect on inhibition of the binding of [3H]C18-Platelet activating factor to human PMN membranes preparation	ki	0.0032	uM
(4R)-5-[3-methoxy-2-propoxy-5-[(2S,5S)-5-(3,4,5-trimethoxyphenyl)oxolan-2-yl]phenyl]sulfonyl-4-methylpentan-1-ol	157729: Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation	ki	0.0037	uM
(2E,4Z)-5-(4-methoxyphenyl)-5-phenyl-N-[(2R)-5-pyridin-3-ylpentan-2-yl]penta-2,4-dienamide	157738: Inhibition of [3H]PAF binding to dog platelets.	ic50	0.0040	uM
4-(3,4-dimethoxyphenyl)-3-ethyl-N-[(2R)-5-pyridin-3-ylpentan-2-yl]benzamide	157736: Inhibition of platelet activating factor receptor binding activity in dog platelets using [3H]PAF as radioligand.	ic50	0.0040	uM
3-butyl-4-(3,4-dimethoxyphenyl)-N-[(2R)-5-pyridin-3-ylpentan-2-yl]benzamide	157736: Inhibition of platelet activating factor receptor binding activity in dog platelets using [3H]PAF as radioligand.	ic50	0.0040	uM
2-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-3H-benzo[de]isoquinolin-1-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0040	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-4H-3,1-benzoxazin-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0040	uM
4-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]-7-fluoro-1,4-benzoxazin-3-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0040	uM
7-(2-chlorophenyl)-13-methyl-4-(3-pyridin-3-yloxyprop-1-ynyl)-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0040	uM
(2E,4E)-5-(4-methoxyphenyl)-N-[(2R)-5-pyridin-3-ylpentan-2-yl]trideca-2,4-dienamide	157738: Inhibition of [3H]PAF binding to dog platelets.	ic50	0.0050	uM
3,4-diphenyl-N-(4-pyridin-3-ylbutyl)benzamide	157736: Inhibition of platelet activating factor receptor binding activity in dog platelets using [3H]PAF as radioligand.	ic50	0.0050	uM
4-(3,4-dimethoxyphenyl)-3-ethynyl-N-[(2R)-5-pyridin-3-ylpentan-2-yl]benzamide	157736: Inhibition of platelet activating factor receptor binding activity in dog platelets using [3H]PAF as radioligand.	ic50	0.0050	uM
4-[3-[6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-8-yl]prop-2-ynyl]-1,4-benzoxazin-3-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0050	uM
1-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]benzo[cd]indol-2-one	59351: PAF-antagonist activity determined in dog platelets by PAF-binding assay	ic50	0.0050	uM

CTD chemical–gene interactions

67 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression, decreases methylation, increases expression	4
Tobacco Smoke Pollution	increases expression, increases methylation	3
Aflatoxin B1	increases expression, increases methylation	3
sodium arsenite	decreases expression, increases expression	2
WEB 2086	affects binding, decreases activity, decreases response to substance	2
BN 50739	decreases reaction, affects binding, decreases activity	2
MK 287	affects binding, decreases activity, decreases reaction	2
CMI 392	affects binding, decreases activity, decreases reaction	2
Vehicle Emissions	affects cotreatment, increases expression, decreases expression, increases abundance	2
Estradiol	affects expression, affects cotreatment, decreases expression	2
Nicotine	decreases expression, increases expression	2
Platelet Activating Factor	decreases reaction, increases expression, affects binding	2
Silicon Dioxide	increases expression	2
aristolochic acid I	increases expression	1
2-anisidine	affects expression	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases expression, increases abundance	1
bisphenol A	affects expression	1
tris(2-butoxyethyl) phosphate	affects expression	1
perfluorooctanoic acid	increases expression	1
potassium chromate(VI)	affects cotreatment, increases expression	1
zinc sulfide	affects cotreatment, increases expression	1
methacrylaldehyde	affects cotreatment, increases expression, increases abundance	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, increases expression	1
lipoxin A4	affects binding, decreases activity, decreases response to substance	1
epigallocatechin gallate	affects cotreatment, increases expression	1
avobenzone	increases expression	1
zileuton	affects binding, decreases activity, decreases reaction	1
BN 50730	affects binding, decreases activity, decreases reaction	1
CGP 52608	increases reaction, affects binding	1

ChEMBL screening assays

118 unique, capped per target: 100 binding, 18 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1291020	Binding	Displacement of [3H]-PAF from platelet activating factor receptor at 1 to 3 uM	Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols. — Bioorg Med Chem
CHEMBL3117956	Functional	Antagonist activity at PAF receptor (unknown origin) expressed in indo-1 loaded neutrophils assessed as inhibition of PAF-induced calcium mobilization at 10 uM by spectrofluorometric analysis	Inhibition of 5-oxo-6,8,11,14-eicosatetraenoic acid-induced activation of neutrophils and eosinophils by novel indole OXE receptor antagonists. — J Med Chem

Cellosaurus cell lines

12 cell lines: 4 cancer cell line, 4 spontaneously immortalized cell line, 3 embryonic stem cell, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_A5R4	SEES3-1V human PTAFR, clone1	Embryonic stem cell	Male
CVCL_A5R5	SEES3-1V human PTAFR, clone2	Embryonic stem cell	Male
CVCL_A5R6	SEES3-1V human PTAFR, clone3	Embryonic stem cell	Male
CVCL_D7YU	Ubigene A-549 PTAFR KO	Cancer cell line	Male
CVCL_D8U5	Ubigene HCT 116 PTAFR KO	Cancer cell line	Male
CVCL_H496	CHO-K1/PTAFR	Spontaneously immortalized cell line	Female
CVCL_KA74	HEK293/PAFR/NFAT/beta-lactamase	Transformed cell line	Female
CVCL_KV66	cAMP Hunter CHO-K1 PTAFR Gi	Spontaneously immortalized cell line	Female
CVCL_KY86	PathHunter CHO-K1 PTAFR beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LB17	PathHunter U2OS PTAFR Activated GPCR Internalization	Cancer cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.