PTGDR2

Summary

PTGDR2 (prostaglandin D2 receptor 2, HGNC:4502) is a protein-coding gene on chromosome 11q12.2, encoding Prostaglandin D2 receptor 2 (Q9Y5Y4). Receptor for prostaglandin D2 (PGD2).

This gene encodes a G-protein-coupled receptor that is preferentially expressed in CD4+ effector T helper 2 (Th2) cells. This protein is a prostaglandin D2 receptor that mediates the pro-inflammatory chemotaxis of eosinophils, basophils, and Th2 lymphocytes generated during allergic inflammation. Single nucleotide polymorphisms in the 3’ UTR of this gene have been associated with asthma susceptibility.

Source: NCBI Gene 11251 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 64 total
• Druggable target: yes — 14 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_004778

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4502
Approved symbol	PTGDR2
Name	prostaglandin D2 receptor 2
Location	11q12.2
Locus type	gene with protein product
Status	Approved
Aliases	CRTH2, CD294, DP2
Ensembl gene	ENSG00000183134
Ensembl biotype	protein_coding
OMIM	604837
Entrez	11251

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000332539

RefSeq mRNA: 1 — MANE Select: NM_004778 NM_004778

CCDS: CCDS7994

Canonical transcript exons

ENST00000332539 — 2 exons

Exon	Start	End
ENSE00001304699	60855869	60855950
ENSE00001323694	60850933	60853731

Expression profiles

Bgee: expression breadth ubiquitous, 127 present calls, max score 83.14.

FANTOM5 (CAGE): breadth broad, TPM avg 2.3551 / max 232.8143, expressed in 377 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
119914	1.6656	332
119915	0.6300	194
119913	0.0595	33

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
mucosa of transverse colon	UBERON:0004991	83.14	gold quality
apex of heart	UBERON:0002098	78.27	gold quality
islet of Langerhans	UBERON:0000006	74.62	gold quality
hindlimb stylopod muscle	UBERON:0004252	73.87	gold quality
granulocyte	CL:0000094	73.53	gold quality
body of stomach	UBERON:0001161	73.39	gold quality
leukocyte	CL:0000738	73.23	gold quality
monocyte	CL:0000576	73.06	gold quality
transverse colon	UBERON:0001157	71.82	gold quality
heart left ventricle	UBERON:0002084	71.42	gold quality
rectum	UBERON:0001052	71.05	gold quality
cardiac ventricle	UBERON:0002082	70.66	gold quality
small intestine Peyer’s patch	UBERON:0003454	70.39	gold quality
stomach	UBERON:0000945	69.24	gold quality
putamen	UBERON:0001874	68.47	gold quality
small intestine	UBERON:0002108	67.91	gold quality
muscle of leg	UBERON:0001383	66.38	gold quality
tendon of biceps brachii	UBERON:0008188	65.52	gold quality
gastrocnemius	UBERON:0001388	65.46	gold quality
prefrontal cortex	UBERON:0000451	64.78	gold quality
anterior cingulate cortex	UBERON:0009835	64.49	gold quality
right frontal lobe	UBERON:0002810	64.24	gold quality
caudate nucleus	UBERON:0001873	63.60	gold quality
amygdala	UBERON:0001876	63.49	gold quality
colonic epithelium	UBERON:0000397	63.47	silver quality
nucleus accumbens	UBERON:0001882	62.10	gold quality
blood	UBERON:0000178	61.27	gold quality
intestine	UBERON:0000160	60.98	gold quality
Brodmann (1909) area 9	UBERON:0013540	60.67	gold quality
neocortex	UBERON:0001950	60.57	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.58

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): TBX21

miRNA regulators (miRDB)

66 targeting PTGDR2, 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-1193	100.00	65.93	529
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-545-3P	99.95	70.74	2783
HSA-MIR-8082	99.95	67.27	1170
HSA-MIR-515-5P	99.92	69.82	2343
HSA-MIR-519E-5P	99.92	69.62	2358
HSA-MIR-302A-3P	99.89	71.23	1777
HSA-MIR-302B-3P	99.89	71.23	1777
HSA-MIR-302C-3P	99.89	71.20	1778
HSA-MIR-302D-3P	99.89	71.25	1777
HSA-MIR-548AR-3P	99.85	71.26	3889
HSA-MIR-520E-3P	99.84	70.55	1698
HSA-MIR-373-3P	99.84	70.68	1668
HSA-MIR-6079	99.84	68.54	1170
HSA-MIR-372-3P	99.83	70.58	1691
HSA-MIR-520A-3P	99.83	70.59	1687
HSA-MIR-520B-3P	99.83	70.56	1699
HSA-MIR-520C-3P	99.83	70.56	1699
HSA-MIR-520D-3P	99.83	70.78	1676
HSA-MIR-548AZ-3P	99.82	70.56	3549
HSA-MIR-548BC	99.82	70.61	3524
HSA-MIR-548E-3P	99.82	70.59	3514
HSA-MIR-548F-3P	99.82	70.59	3540
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-548A-3P	99.76	70.58	3524
HSA-MIR-6794-5P	99.76	66.38	1048

Literature-anchored findings (GeneRIF, showing 40)

• CRTH2 is involved in mediating some of the therapeutic and/or unwanted side effects of indomethacin, independently of cyclooxygenases and peroxisome proliferator-activated receptors. (PMID:11801628)
• Association of a new-type prostaglandin D2 receptor CRTH2 with circulating T helper 2 cells in patients with atopic dermatitis. (PMID:12230502)
• data show that 11-dehydro-thromboxane B(2) is a full agonist of the chemoattractant receptor-homologous molecule expressed on TH2 cells(CRTH2) receptor and hence might cause CRTH2 activation in cellular contexts (PMID:14668348)
• CRTH2 protein structure and expression (review) (PMID:15065763)
• Sequence variants of CRTH2 are associated with asthma and differentially influence mRNA stability. (PMID:15345705)
• restoration of CRTH2/CCR3 expression may be an indicator for optimal recovery after septic shock (PMID:15507393)
• selective effect of other PGD2 metabolites on CRTH2 (PMID:15789622)
• analysis of prostaglandin D2 receptor CRTH2 determinants of ligand binding affinity and selectivity (PMID:16030019)
• Data show that the prostaglandin PGD(2) metabolite, 9alpha,11beta-PGF(2), and its stereoisomer, PGF(2alpha), are CRTH2 chemoattractant receptor agonists. (PMID:16378605)
• PGD(2) exerts its effects partly through CRTH2. The PGD(2)/CRTH2 system mediates the chemotaxis of eosinophils, basophils, & Th2 cells involved in the induction of allergic inflammation. Human bronchial epithelial cells express CRTH2. (PMID:17541272)
• These data further emphasize the importance of CRTH2 in eosinophil function (recruitment, respiratory burst, and granulation). (PMID:17714552)
• D-type prostanoid (DP) receptors comediate with CRTH2 the mobilization of eosinophils from bone marrow and their chemotaxis, which might provide the rationale for DP antagonists in the treatment of allergic disease (PMID:17878378)
• demonstrated GATA-3 binding to a probe from the CRTh2 promoter (PMID:17910949)
• relationship between G1544C and A1651G SNPs and serum IL-13 levels in Chinese children patients with asthma (PMID:18777142)
• These results suggest that expression of DP and CRTH2 is associated with the pathophysiology of chronic rhinosinusitis, and the expression of these receptors may be regulated by h-PGDS and PGD. (PMID:18802357)
• PGH2 causes activation of the PGD2 receptors CRTH2 and DP via a dual mechanism: by interacting directly with the receptors and/or by giving rise to PGD2 after catalytic conversion by plasma proteins. (PMID:18835884)
• CRTH2 inhibition by its C terminus may represent a rather unappreciated strategy employed by a GPCR to specify the extent of G protein activation (PMID:19010788)
• CRTH2 expressions of leukocytes in allergic nasal mucosa are significantly up-regulated compared with those in nonallergic nasal mucosa suggesting that CRTH2 may play an important role in the recruitment of leukocytes into allergic nasal mucosa (PMID:19230460)
• The CRTH2 -466T>C gene polymorphism may not affect on the phenotype of chronic urticaria, but controbutes to the required dose of antihistamines in patients. (PMID:19290788)
• Genetic variation within CRTh2 modifies the development of allergic sensitization and asthma in a population of German children. (PMID:19392992)
• activation of CRTH2 only inhibits apoptosis induced by cytokine deprivation (PMID:19494281)
• The CRTH2 -466T>C polymorphism increases serum and cellular eotaxin-2 production through lowered CRTH2 expression (PMID:19796209)
• in immunologically activated nasal polyp tissue, PGD(2) produced by mast cells promotes the migration of Th2 cells through a CRTH2 dependent mechanism. (PMID:19839971)
• CRTH2 is GPR44, a G protein-coupled receptor 44. Characterization of C-terminal tail determinants involved in CRTH2 receptor trafficking identified a recycling motif. (PMID:20035740)
• Indomethacin may exert its therapeutic effect in eosinophilic pustular folliculitis (Ofuji’s disease) by reducing CRTH2 expression, as well as by inhibiting PGD2 synthesis. (PMID:20107720)
• CRTH2 was enriched significantly on interleukin (IL)-4+/IL-13+ T cells compared to interferon (IFN)-gamma+ T cells. There were more CRTH2+ T cells in the bronchoalveolar lavage (BAL) of asthmatics vs. controls. (PMID:20491797)
• DK-PGD-induced CLC/Gal-10 mRNA level can serve as a potential marker for monitoring pharmacodynamic effects of blood exposure to CRTH2 modulating agents (PMID:20858065)
• DP mediates eosinophils through the elevation of intracellular cAMP production but does not change CRTH2 expression; balance between DP and CRTH2 could influence the degree of PGD2-induced eosinophil migration (PMID:21624751)
• This study provides the first clinical evidence that CRTH2 receptors contribute to airflow limitation, symptoms and eosinophilic airway inflammation in asthma. (PMID:21762224)
• expression defines IL-25- and IL-33-responsive type 2 innate lymphoid cells (PMID:21909091)
• DP receptors amplify the biological response to CRTH2 activation and the CRTH2/DP heteromer might represent both a functional signaling unit for PGD(2) and a potential target for development of heteromer-directed therapy for allergic diseases (PMID:21930295)
• The frequencies of the TT genotype of CRTH2 -466T>C were higher than those of the CC/CT genotype in aspirin-exacerbated respiratory disease patients compared to aspirin-tolerant asthma patients (PMID:22101342)
• identify PGH(1) as an important lipid intermediate and novel CRTH2 agonist which may trigger CRTH2 activation in vivo in the absence of functional prostaglandin D synthase. (PMID:22442685)
• DGCR2, GPR44 and SerpinB10, found in beta cells, were negative in all other cell types within pancreas and exposed epitopes at the cell surface (PMID:22465717)
• we show that CRTH2+ CD4+ T cells may be involved in the enhanced Th2 cell-mediated immunity in IgG4-related lacrimal gland enlargement. (PMID:22627365)
• These data show that prostaglandin D(2) induces human osteoclast apoptosis through activation of CRTH2 and the apoptosis intrinsic pathway. (PMID:22705147)
• CRTh2 rs533116 was associated with allergic asthma in White people (PMID:22947041)
• Confocal images and FACS demonstrated a strong association and co-localization between VIP peptide and CRTH2 molecules (PMID:23168411)
• CRTH2 is not expressed on human amniocytes or myocytes and plays no role in the mechanism of 15dPGJ2-mediated inhibition of NF-kappaB (PMID:23226366)
• Low DP2 prostanoid receptor is associated with gastric cancer progression. (PMID:24922638)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
mus_musculus	Ptgdr2	ENSMUSG00000034117
rattus_norvegicus	Ptgdr2	ENSRNOG00000090389
drosophila_melanogaster	Rh7	FBGN0036260
caenorhabditis_elegans	trhr-1	WBGENE00016265

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR4 (ENSG00000132671), SSTR1 (ENSG00000139874), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Prostaglandin D2 receptor 2 — Q9Y5Y4 (reviewed: Q9Y5Y4)

Alternative names: Chemoattractant receptor-homologous molecule expressed on Th2 cells, G-protein coupled receptor 44

All UniProt accessions (1): Q9Y5Y4

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin-sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, GRK2, GPRK5/GRK5 and GRK6. Receptor activation is responsible, at least in part, in immune regulation and allergic/inflammation responses.

Subcellular location. Cell membrane.

Tissue specificity. Widespread expression. High expression in stomach, small intestine, heart and thymus. Intermediate expression in colon, spinal cord and peripheral blood and low expression in brain, skeletal muscle and spleen. Expressed also on Th2- and Tc2- type cells, eosinophils and basophils.

Post-translational modifications. Phosphorylated.

Domain organisation. The 330-DSEL-333 motif is involved in the recycling of PTGDR2 to the cell surface after agonist-induced internalization. This motif seems to be required for GRK2 and GPRK5/GRK5 to promote agonist-induced internalization. Thr-347 is a major site for PKC-induced internalization of the receptor.

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

RefSeq proteins (1): NP_004769* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000826	Formyl_rcpt-rel	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (47 total): helix 13, topological domain 8, transmembrane region 7, mutagenesis site 5, strand 4, modified residue 2, glycosylation site 2, chain 1, region of interest 1, short sequence motif 1, disulfide bond 1, sequence variant 1, turn 1

Structure

Experimental structures (PDB)

6 structures.

PDB	Method	Resolution (Å)
8XXV	ELECTRON MICROSCOPY	2.33
8XXU	ELECTRON MICROSCOPY	2.54
7M8W	X-RAY DIFFRACTION	2.61
6D27	X-RAY DIFFRACTION	2.74
6D26	X-RAY DIFFRACTION	2.8
9IYB	ELECTRON MICROSCOPY	2.82

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y5Y4-F1	81.63	0.55

Functional residue map

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

Post-translational modifications (2): 331, 345

Disulfide bonds (1): 104–182

Glycosylation sites (2): 4, 25

Mutagenesis-validated functional residues (5):

Position	Phenotype
330	45% increases internalization of ptgdr2.
331	45% increases internalization of ptgdr2.
332	45% increases internalization of ptgdr2.
333	45% increase in internalization of ptgdr2.
347	decreases in pkc-induced internalization of ptgdr2.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-391908	Prostanoid ligand receptors
R-HSA-418594	G alpha (i) signalling events

MSigDB gene sets: 152 (showing top): MODULE_97, GOBP_NEGATIVE_REGULATION_OF_REPRODUCTIVE_PROCESS, REACTOME_EICOSANOID_LIGAND_BINDING_RECEPTORS, GOBP_CELLULAR_RESPONSE_TO_LIPID, STEARMAN_LUNG_CANCER_EARLY_VS_LATE_DN, GOBP_CELLULAR_RESPONSE_TO_PROSTAGLANDIN_STIMULUS, MODULE_182, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, EVI1_05, BROWNE_HCMV_INFECTION_48HR_DN, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_TAXIS, GOBP_NEGATIVE_REGULATION_OF_MULTICELLULAR_ORGANISMAL_PROCESS, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_RESPONSE_TO_PROSTAGLANDIN

GO Biological Process (10): chemotaxis (GO:0006935), immune response (GO:0006955), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), neuropeptide signaling pathway (GO:0007218), calcium-mediated signaling (GO:0019722), positive regulation of G protein-coupled receptor signaling pathway (GO:0045745), cellular response to prostaglandin D stimulus (GO:0071799), negative regulation of male germ cell proliferation (GO:2000255), signal transduction (GO:0007165)

GO Molecular Function (7): prostaglandin J receptor activity (GO:0001785), G protein-coupled receptor activity (GO:0004930), prostaglandin D receptor activity (GO:0004956), prostaglandin F receptor activity (GO:0004958), neuropeptide binding (GO:0042923), icosanoid receptor activity (GO:0004953), protein binding (GO:0005515)

GO Cellular Component (3): plasma membrane (GO:0005886), neuron projection (GO:0043005), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Eicosanoid ligand-binding receptors	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
prostaglandin receptor activity	3
G protein-coupled receptor activity	2
response to chemical	1
taxis	1
immune system process	1
response to stimulus	1
signal transduction	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase inhibitor activity	1
intracellular signaling cassette	1
regulation of G protein-coupled receptor signaling pathway	1
positive regulation of signal transduction	1
cellular response to prostaglandin stimulus	1
response to prostaglandin D	1
cellular response to alcohol	1
cellular response to ketone	1
male germ cell proliferation	1
negative regulation of germ cell proliferation	1
negative regulation of reproductive process	1
regulation of male germ cell proliferation	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
transmembrane signaling receptor activity	1
peptide binding	1
icosanoid binding	1
binding	1
membrane	1
cell periphery	1
plasma membrane bounded cell projection	1
cellular anatomical structure	1

Protein interactions and networks

STRING

884 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PTGDR2	NCR3LG1	Q68D85	897
PTGDR2	PTGDR	Q13258	852
PTGDR2	IL7R	P16871	772
PTGDR2	IL4	P05112	749
PTGDR2	IL9	P15248	718
PTGDR2	IL5	P05113	711
PTGDR2	KLRB1	Q12918	696
PTGDR2	IL13	P35225	696
PTGDR2	TSLP	Q969D9	693
PTGDR2	PRELID1	Q9Y255	692
PTGDR2	IL33	O95760	667
PTGDR2	TBXA2R	P21731	625
PTGDR2	GATA3	P23771	623
PTGDR2	CCL17	Q92583	620
PTGDR2	NCR2	O95944	620

IntAct

0 interactions, top by confidence:

BioGRID (6): PTGDR2 (Affinity Capture-Western), PTGDR (Affinity Capture-Western), PTGDR2 (Positive Genetic), ANKRD13C (Affinity Capture-Western), RNF5 (Affinity Capture-Western), JKAMP (Affinity Capture-Western)

ESM2 similar proteins: A0A6I8PUB9, O00155, O00270, O14842, O14843, O15529, O43603, O46685, O60755, O88626, O88634, O88853, O88854, O88855, P0C5I1, P46092, P46093, P50132, Q149R9, Q15722, Q15743, Q1JQB3, Q3T181, Q3UFD7, Q3ZC80, Q4KLH9, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q86VZ1, Q8BUD0, Q8BYC4, Q8HYC3, Q8K3T4, Q8TDS5, Q8TDU9, Q920E0, Q924U0, Q96G91

Diamond homologs: A4FUQ5, B1PHQ8, B9VR26, O08565, O08790, O35210, O35786, O62747, O70129, O75388, O77590, O88416, O88536, O88537, O97571, O97664, P0C7U4, P0C7U5, P21462, P21730, P25025, P25089, P25090, P25095, P25104, P28646, P29089, P29754, P29755, P30555, P30556, P30872, P30873, P30937, P30992, P30993, P31391, P33766, P34976, P35373

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	59
Likely benign	3
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

150 predictions. Top by Δscore:

Variant	Effect	Δscore
11:60853730:CT:C	acceptor_gain	1.0000
11:60853728:GGCT:G	acceptor_gain	0.9900
11:60853731:TC:T	acceptor_loss	0.9900
11:60853732:C:CA	acceptor_loss	0.9900
11:60853732:C:CC	acceptor_gain	0.9900
11:60855863:CCTTA:C	donor_loss	0.9900
11:60855864:CTTA:C	donor_loss	0.9900
11:60855865:TTACC:T	donor_loss	0.9900
11:60855866:TACCT:T	donor_loss	0.9900
11:60855867:ACC:A	donor_loss	0.9900
11:60855868:CCTG:C	donor_loss	0.9900
11:60853727:GGGCT:G	acceptor_gain	0.9800
11:60853729:GCT:G	acceptor_gain	0.9800
11:60853730:CTC:C	acceptor_gain	0.9800
11:60853731:TCT:T	acceptor_gain	0.9800
11:60853736:A:T	acceptor_gain	0.9800
11:60853737:G:C	acceptor_gain	0.9800
11:60853737:G:GC	acceptor_gain	0.9800
11:60853735:C:CT	acceptor_gain	0.9700
11:60853732:C:G	acceptor_gain	0.9500
11:60855867:A:AC	donor_gain	0.9100
11:60855868:C:CC	donor_gain	0.9100
11:60853681:C:CT	acceptor_gain	0.8300
11:60855869:C:A	donor_loss	0.8300
11:60853734:G:C	acceptor_loss	0.7600
11:60853678:CTCCA:C	acceptor_gain	0.7300
11:60855231:G:A	donor_gain	0.7100
11:60854964:T:C	donor_gain	0.6800
11:60855008:C:CA	donor_gain	0.6800
11:60853379:A:C	acceptor_gain	0.6700

AlphaMissense

2511 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:60853432:C:A	W97C	0.999
11:60853432:C:G	W97C	0.999
11:60853178:C:G	C182S	0.998
11:60853179:A:T	C182S	0.998
11:60853412:C:G	C104S	0.998
11:60853412:C:T	C104Y	0.998
11:60853413:A:T	C104S	0.998
11:60852850:G:C	S291R	0.997
11:60852850:G:T	S291R	0.997
11:60852852:T:G	S291R	0.997
11:60853177:G:C	C182W	0.997
11:60853178:C:T	C182Y	0.997
11:60853179:A:G	C182R	0.997
11:60853345:G:C	S126R	0.997
11:60853345:G:T	S126R	0.997
11:60853347:T:G	S126R	0.997
11:60853354:G:C	S123R	0.997
11:60853354:G:T	S123R	0.997
11:60853356:T:G	S123R	0.997
11:60853411:G:C	C104W	0.997
11:60853412:C:A	C104F	0.997
11:60853434:A:G	W97R	0.997
11:60853434:A:T	W97R	0.997
11:60853178:C:A	C182F	0.996
11:60852958:G:C	F255L	0.995
11:60852958:G:T	F255L	0.995
11:60852960:A:G	F255L	0.995
11:60853214:C:G	R170P	0.995
11:60853096:G:C	S209R	0.994
11:60853096:G:T	S209R	0.994

dbSNP variants (sampled 300 via entrez): RS1000303945 (11:60857777 C>T), RS1000406199 (11:60851281 T>C), RS1000906031 (11:60856385 G>C), RS1001253340 (11:60856161 G>A), RS1001395839 (11:60853743 G>A), RS1001691225 (11:60857009 G>A), RS1002140588 (11:60857313 C>G), RS1002744901 (11:60855951 A>G), RS1003102220 (11:60855604 C>T), RS1003636099 (11:60852413 G>A,T), RS1003699634 (11:60854073 G>A), RS1003730997 (11:60852572 C>A,T), RS1003819370 (11:60855238 G>A,T), RS1004158409 (11:60854308 A>T), RS1005109835 (11:60853399 G>A)

Disease associations

OMIM: gene MIM:604837 | 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
GCST001725_10	Inflammatory bowel disease	9.000000e-13

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5071 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

14 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 179,157 (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
CHEMBL361812	RAMATROBAN	4	3,250
CHEMBL426559	LAROPIPRANT	4	541
CHEMBL6	INDOMETHACIN	4	156,366
CHEMBL2386081	SETIPIPRANT	3	226
CHEMBL3137332	FEVIPIPRANT	3	288
CHEMBL560993	TIMAPIPRANT	3	285
CHEMBL1914489	AZD1981	2	161
CHEMBL1951575	VIDUPIPRANT	2	890
CHEMBL2442750	QAV680	2	73
CHEMBL551813	BI-671800	2	95
CHEMBL589092	FENTIAZAC	2	16,627
CHEMBL2181753	AM-211	1	288
CHEMBL3286797	PF-04418948	1	38
CHEMBL561132	MK-7246	1	29

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Prostanoid receptors

Most potent curated ligand interactions (29 total), top 25:

Ligand	Action	Affinity	Parameter
L-888,607	Full agonist	9.1	pKi
fevipiprant	Antagonist	8.99	pKd
TM30089	Antagonist	8.92	pIC50
15(R)-15-methyl-PGD2	Full agonist	8.9	pKi
PGD2	Full agonist	8.6	pKi
vidupiprant	Antagonist	8.52	pIC50
15-deoxy-Δ12,14-PGJ2	Full agonist	8.5	pKi
13,14-dihydro-15-keto-PGD2	Full agonist	8.5	pKi
AZD1981	Antagonist	8.37	pIC50
AM-461	Antagonist	8.28	pIC50
setipiprant	Antagonist	8.22	pIC50
Δ12-PGJ2	Full agonist	8.2	pKi
PGJ2	Full agonist	8.2	pKi
[3H]PGD2	Full agonist	8.2	pKd
compound 51 [Crosignani et al., 2011]	Antagonist	8.16	pKi
[3H]ramatroban	Antagonist	8.1	pKd
timapiprant	Antagonist	7.89	pKi
QAV680	Antagonist	7.82	pKd
indomethacin	Full agonist	7.7	pKi
ARRY-502	Antagonist	7.59	pEC50
15(S)-15-methyl-PGD2	Full agonist	7.5	pKi
ramatroban	Antagonist	7.4	pKi
PGD3	Full agonist	7.4	pKi
L-888,291	Full agonist	7.32	pKi
15-deoxy-Δ12,14-PGD2	Full agonist	7.3	pKi

Binding affinities (BindingDB)

1685 measured of 1865 human assays (1865 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[1-[[4-[(5-methoxy-3-methyl-1H-indole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(6-fluoro-1-propylindole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-ethyl-6-fluoroindole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-ethyl-6-fluoroindole-2-carbonyl)amino]-2-fluorophenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[2-fluoro-4-[(6-fluoro-1-propylindole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[2-fluoro-4-[(5-methoxy-3-methyl-1-benzofuran-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-butyl-5-fluoroindole-2-carbonyl)amino]-2-fluorophenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-(naphthalene-2-carbonylamino)phenyl]methyl]-5-propan-2-yl-3-propylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[5-cyclopropyl-3-ethyl-1-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.1 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(3,4-dichlorophenyl)methoxycarbonylamino]phenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-(naphthalen-2-ylmethoxycarbonylamino)phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.1 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[1-[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]ethyl]pyrazol-4-yl]acetic acid	KI	0.1 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[4-[4-[[3,5-bis(trifluoromethyl)phenyl]sulfonylamino]phenyl]-6-fluoro-3-methylnaphthalen-2-yl]acetic acid	IC50	0.1 nM	US-9000044: Substituted naphthylacetic acids
2-[1-[[4-(1H-benzo[f]benzimidazol-2-yl)phenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-9206164: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-(6-tert-butyl-1H-benzimidazol-2-yl)-2-fluorophenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.1 nM	US-9206164: Pyrazole compounds as CRTH2 antagonists
2-[3-cyclopropyl-5-ethyl-1-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.1 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-benzylindole-2-carbonyl)amino]-2-fluorophenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-(1H-indole-2-carbonylamino)phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(6-fluoro-1H-indole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(5-fluoro-1H-indole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(5-chloro-1-benzofuran-2-carbonyl)amino]phenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-[(1-ethylindole-2-carbonyl)amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-[(6-fluoro-1H-indole-2-carbonyl)amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-ethylindole-2-carbonyl)amino]-2-fluorophenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-ethyl-5-fluoroindole-2-carbonyl)amino]-2-fluorophenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(6-chloro-1-benzofuran-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(1-butylindole-2-carbonyl)amino]-2-fluorophenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[2-fluoro-4-[(5-fluoro-1-propylindole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[2-fluoro-4-[(1-propylindole-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(4-tert-butylbenzoyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-(naphthalene-2-carbonylamino)phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(3,4-dichlorobenzoyl)amino]phenyl]methyl]-5-propan-2-yl-3-propylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[5-propan-2-yl-3-propyl-1-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[3-ethyl-5-methyl-1-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[4-chloro-2-[(4R)-5-[(3-fluorophenyl)methoxycarbonyl]-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-4-yl]phenoxy]acetic acid	IC50	0.2 nM	US-9169270: 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
2-[1-[[4-(5,6-dichloro-1H-benzimidazol-2-yl)phenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-9206164: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.2 nM	US-9206164: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-(6-tert-butyl-1H-benzimidazol-2-yl)phenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.2 nM	US-9206164: Pyrazole compounds as CRTH2 antagonists
2-[3-ethoxy-4-[5-fluoro-2-[2-(7-fluoro-3,4-dihydro-2H-chromen-4-yl)acetyl]-3,4-dihydro-1H-isoquinolin-8-yl]phenyl]acetic acid	IC50	0.2 nM	US-9255090: Heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
2-[3-[5-fluoro-2-[2-[2-(trifluoromethyl)phenyl]cyclopropanecarbonyl]-3,4-dihydro-1H-isoquinolin-8-yl]-4-methoxyphenyl]acetic acid	IC50	0.22 nM	US-9255090: Heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
2-[1-[[4-[(3,4-dichlorobenzoyl)amino]phenyl]methyl]-3,5-diethylpyrazol-4-yl]acetic acid	KI	0.25 nM	US-8791272: Pyrazole compounds as CRTH2 antagonists
2-[4-(cyclopropylmethoxy)-3-(5-fluoro-2-phenylmethoxycarbonyl-3,4-dihydro-1H-isoquinolin-8-yl)phenyl]acetic acid	IC50	0.28 nM	US-9255090: Heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
2-[3-(5-fluoro-2-phenylmethoxycarbonyl-3,4-dihydro-1H-isoquinolin-8-yl)-4-propoxyphenyl]acetic acid	IC50	0.28 nM	US-9255090: Heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
2-[1-[[4-[(5-chloro-1-benzofuran-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.3 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-(1-benzothiophene-2-carbonylamino)phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.3 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-(1H-indole-2-carbonylamino)phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.3 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-[(1-methylindole-2-carbonyl)amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.3 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[3,5-diethyl-1-[[4-[(5-fluoro-1H-indole-2-carbonyl)amino]phenyl]methyl]pyrazol-4-yl]acetic acid	KI	0.3 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists
2-[1-[[4-[(3-ethyl-7-fluoro-1-benzofuran-2-carbonyl)amino]phenyl]methyl]-3,5-dimethylpyrazol-4-yl]acetic acid	KI	0.3 nM	US-8759386: Pyrazole compounds as CRTH2 antagonists

ChEMBL bioactivities

4397 potent at pChembl≥5 of 4431 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.92	IC50	0.012	nM	CHEMBL1088284
10.70	IC50	0.02	nM	CHEMBL2181748
10.14	IC50	0.072	nM	CHEMBL1081033
10.10	IC50	0.079	nM	CHEMBL1087029
10.07	IC50	0.085	nM	CHEMBL1087622
10.01	IC50	0.098	nM	CHEMBL1080695
10.00	Ki	0.1	nM	CHEMBL3639847
10.00	Ki	0.1	nM	CHEMBL3690164
10.00	Ki	0.1	nM	CHEMBL3690165
10.00	Ki	0.1	nM	CHEMBL3690177
10.00	Ki	0.1	nM	CHEMBL3690178
10.00	Ki	0.1	nM	CHEMBL3690185
10.00	Ki	0.1	nM	CHEMBL3690191
10.00	Ki	0.1	nM	CHEMBL3685926
10.00	Ki	0.1	nM	CHEMBL2181751
10.00	Ki	0.1	nM	CHEMBL3685933
10.00	Ki	0.1	nM	CHEMBL3685949
10.00	Ki	0.1	nM	CHEMBL3685952
10.00	Ki	0.1	nM	CHEMBL3686053
10.00	IC50	0.1	nM	CHEMBL3667662
10.00	Ki	0.1	nM	CHEMBL3947507
10.00	Ki	0.1	nM	CHEMBL3977228
10.00	IC50	0.1	nM	CHEMBL1778632
9.70	Ki	0.2	nM	CHEMBL2181803
9.70	Ki	0.2	nM	CHEMBL3685833
9.70	Ki	0.2	nM	CHEMBL3685840
9.70	Ki	0.2	nM	CHEMBL3685841
9.70	Ki	0.2	nM	CHEMBL3685842
9.70	Ki	0.2	nM	CHEMBL3690155
9.70	Ki	0.2	nM	CHEMBL3690158
9.70	Ki	0.2	nM	CHEMBL3690161
9.70	Ki	0.2	nM	CHEMBL3690167
9.70	Ki	0.2	nM	CHEMBL3690168
9.70	Ki	0.2	nM	CHEMBL3690172
9.70	Ki	0.2	nM	CHEMBL3690189
9.70	Ki	0.2	nM	CHEMBL3690190
9.70	Ki	0.2	nM	CHEMBL3690192
9.70	Ki	0.2	nM	CHEMBL3685864
9.70	Ki	0.2	nM	CHEMBL3685885
9.70	Ki	0.2	nM	CHEMBL3685891
9.70	Ki	0.2	nM	CHEMBL3685924
9.70	Ki	0.2	nM	CHEMBL3685925
9.70	Ki	0.2	nM	CHEMBL3685936
9.70	IC50	0.2	nM	CHEMBL3936579
9.70	Ki	0.2	nM	CHEMBL3961172
9.70	Ki	0.2	nM	CHEMBL3974100
9.70	Ki	0.2	nM	CHEMBL3903436
9.70	IC50	0.2	nM	CHEMBL3904070
9.70	IC50	0.2	nM	CHEMBL1086856
9.70	IC50	0.2	nM	CHEMBL1778637

PubChem BioAssay actives

2683 with measured affinity, of 3472 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
2-[2-[bis(4-fluorophenyl)methyl]-4-(3-fluorophenyl)pyrimidin-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	<0.0001	uM
2-[4-[(3-bromo-5-methylsulfonyl-2-pyridinyl)oxy]-6-fluoro-3-methylnaphthalen-2-yl]acetic acid	705370: Inhibition of CRTH2	ic50	<0.0001	uM
2-[4-(4-fluorophenyl)-2-(N-phenylanilino)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0001	uM
2-[4-(3-fluorophenyl)-2-(N-phenylanilino)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0001	uM
2-[4-(4-chlorophenyl)-2-(N-phenylanilino)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0001	uM
2-[2-(1,1-diphenylethyl)-4-(4-fluorophenyl)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0001	uM
2-[2-[2-chloro-4-[methyl(methylsulfonyl)amino]phenyl]-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0001	uM
2-[2-(4-fluoro-N-(4-fluorophenyl)anilino)-4-(4-fluorophenyl)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0002	uM
2-[5-chloro-1’-[(3-methyl-5-phenyl-1,2-oxazol-4-yl)methyl]-2,2’-dioxospiro[indole-3,4’-pyrrolidine]-1-yl]acetic acid	330825: Antagonist activity at human CRTH2 receptor assessed as inhibition of DK-PGD2-induced eosinophil chemotaxis	ic50	0.0002	uM
2-[[2-[bis(4-fluorophenyl)methyl]-4-(3-fluorophenyl)-1,3-thiazol-5-yl]oxy]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0002	uM
2-[2-(2-chloro-4-methylsulfonylphenyl)-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0002	uM
2-[2-(5-cyano-2-fluorophenyl)-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0002	uM
2-[2-(5-cyano-2-methylphenyl)-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0002	uM
2-[6-fluoro-3-(2-fluoro-4-methylsulfonylphenyl)sulfanyl-2-methylindolizin-1-yl]acetic acid	705352: Displacement of [3H]PGD2 from CRTH2 expressed in HEK293 cells after 3 hrs by liquid scintillation counting	ki	0.0002	uM
5-[2-(4-fluorophenyl)-6-[[(1R)-1-(4-fluorophenyl)ethyl]carbamoyl]-1-oxoisoquinolin-3-yl]pentanoic acid	1367776: Antagonist activity at CRTh2 (unknown origin) assessed as inhibition of CD11b activation	ki	0.0002	uM
2-[4-(3-fluorophenyl)-2-(4-methoxy-N-(4-methoxyphenyl)anilino)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0003	uM
2-[2-[[(3S)-4-[2-(4-fluorophenyl)acetyl]-3-methylpiperazin-1-yl]methyl]-4-(trifluoromethyl)phenoxy]acetic acid	586985: Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay	ic50	0.0003	uM
2-[2-(2-chloro-4-ethylsulfonylphenyl)-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0003	uM
2-[2-methyl-1-[[4-methylsulfonyl-2-(trifluoromethyl)phenyl]methyl]pyrrolo[2,3-b]pyridin-3-yl]acetic acid	1433030: Antagonist activity at DP2 receptor in human isolated eosinophils assessed as inhibition of DK-PGD2-induced shape change preincubated for 5 mins followed by DK-PGD2 addition measured after 5 mins by flow cytometry	ic50	0.0004	uM
2-[2-[2-methyl-4-[methyl(methylsulfonyl)amino]phenyl]-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0004	uM
2-[2-(3-cyanophenyl)-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0004	uM
5-[2-(4-fluorophenyl)-1-oxo-6-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]isoquinolin-3-yl]pentanoic acid	1367776: Antagonist activity at CRTh2 (unknown origin) assessed as inhibition of CD11b activation	ki	0.0004	uM
2-[(3R)-3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]acetic acid	239567: Inhibition of [3H]PGD-2 binding to human chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2)	ki	0.0005	uM
2-[2-(N-(4-cyanophenyl)anilino)-4-(4-fluorophenyl)-1,3-thiazol-5-yl]acetic acid	465035: Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay	ic50	0.0005	uM
2-[2-[bis(4-fluorophenyl)methyl]-4-(2-fluoro-4-pyridinyl)-1,3-thiazol-5-yl]acetic acid	458064: Displacement of[3H]PGD2 from human CRTH2 receptor expressed in HEK385-7 cells	ic50	0.0005	uM
2-[4-chloro-2-[[(3S)-4-[2-(4-chlorophenyl)acetyl]-3-methylpiperazin-1-yl]methyl]phenoxy]acetic acid	586985: Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay	ic50	0.0005	uM
2-[3-cyclopropyl-5-ethyl-1-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrazol-4-yl]acetic acid	705370: Inhibition of CRTH2	ki	0.0005	uM
2-[3-(4-chlorophenyl)sulfanyl-2-methyl-4-pyrazin-2-ylindol-1-yl]acetic acid	630011: Displacement of [3H]PGD2 from human CRTH2 receptor	ic50	0.0006	uM
2-[3-[(4-fluorophenyl)sulfonyl-methylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]acetic acid	705370: Inhibition of CRTH2	ki	0.0006	uM
2-[2-[[(3S)-4-benzylsulfonyl-3-methylpiperazin-1-yl]methyl]-4-chlorophenyl]acetic acid	586985: Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay	ic50	0.0006	uM
2-[3-[2-[benzyl-(4-fluorophenyl)sulfonylamino]ethyl]indol-1-yl]acetic acid	309663: Displacement of [3H]PGD2 from human CRTH2 receptor	ki	0.0006	uM
2-[(3R)-3-[(4-fluorophenyl)sulfonyl-methylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]acetic acid	239567: Inhibition of [3H]PGD-2 binding to human chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2)	ki	0.0006	uM
(2R)-2-[2-(3-cyanophenyl)-4-(trifluoromethyl)phenoxy]propanoic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0006	uM
2-[4-chloro-2-(2-chloro-4-methylsulfonylphenyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0006	uM
(2R)-2-[2-(2-chloro-4-ethylsulfonylphenyl)-4-(trifluoromethyl)phenoxy]propanoic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0006	uM
2-[1-[[4-ethylsulfonyl-2-(trifluoromethyl)phenyl]methyl]-2-methylpyrrolo[2,3-b]pyridin-3-yl]acetic acid	1433030: Antagonist activity at DP2 receptor in human isolated eosinophils assessed as inhibition of DK-PGD2-induced shape change preincubated for 5 mins followed by DK-PGD2 addition measured after 5 mins by flow cytometry	ic50	0.0008	uM
2-[2-[[(3S)-4-(benzenesulfonyl)-3-methylpiperazin-1-yl]methyl]-4-chlorophenoxy]acetic acid	586985: Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay	ic50	0.0008	uM
2-[[(2aS,8R,8aR)-3-(3-fluorobenzoyl)-2,2a,8,8a-tetrahydro-1H-cyclobuta[b]quinolin-8-yl]-cyclopropylcarbamoyl]oxyacetic acid	1385034: Antagonist activity at human CRTh2 expressed in HEK cells assessed as inhibition of DK-PGD2-mediated attenuation of forskolin-induced intracellular cAMP accumulation preincubated for 10 mins followed by forskolin stimulation measured after 10 to 60 mins by ELISA based chemiluminescence assay	ic50	0.0008	uM
2-[(3S)-4-(4-chlorophenyl)sulfanyl-7-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]indol-3-yl]acetic acid	254359: Binding affinity towards human CRTH2 receptor expressed in CHO cells	ki	0.0008	uM
4-(N-[(2S,4R)-1-benzoyl-2-methyl-3,4-dihydro-2H-quinolin-4-yl]anilino)-4-oxobutanoic acid	705368: Inhibition of CRTH2 in human whole blood	ic50	0.0008	uM
2-[3-[[1-[(2,3-difluorophenyl)methyl]-6-oxo-3-pyridinyl]methyl]-5-fluoro-2-methylindol-1-yl]acetic acid	1128041: Antagonist activity at human recombinant CRTh2 expressed in CHO-K1 cells by cAMP TR FRET assay	ic50	0.0008	uM
2-[3-[[1-[(2,4-difluorophenyl)methyl]-6-oxopyridazin-3-yl]methyl]-5-fluoro-2-methylindol-1-yl]acetic acid	716477: Binding affinity to human CRTH2 receptor	ic50	0.0008	uM
2-[2-[4-[methyl(methylsulfonyl)amino]phenyl]-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0008	uM
2-[5-fluoro-2-methyl-3-[[6-oxo-1-[(2,4,5-trifluorophenyl)methyl]pyridazin-3-yl]methyl]indol-1-yl]acetic acid	716703: Displacement of [3H]PGD2 from recombinant human CRTH2 receptor expressed in CHO-K1 cells after 30 min by FRET method	ic50	0.0008	uM
2-[2-(4-ethylsulfonyl-2-methylphenyl)-4-(trifluoromethyl)phenoxy]acetic acid	598939: Displacement of [3H]-PGD2 from CRTh2 receptor by scintillation proximity assay	ic50	0.0009	uM
N-[3-fluoro-5-(2H-tetrazol-5-yl)phenyl]-N-[(4-methylsulfonylphenyl)methyl]-2-phenylacetamide	664803: Displacement of [3HPGD2 from human CRTH2 receptor expressed in CHO cell membrane after 90 mins by scintillation proximity assay	ki	0.0009	uM
2-[[(2aS,8R,8aR)-3-[4-(trifluoromethoxy)benzoyl]-2,2a,8,8a-tetrahydro-1H-cyclobuta[b]quinolin-8-yl]-cyclopropylcarbamoyl]oxyacetic acid	1385034: Antagonist activity at human CRTh2 expressed in HEK cells assessed as inhibition of DK-PGD2-mediated attenuation of forskolin-induced intracellular cAMP accumulation preincubated for 10 mins followed by forskolin stimulation measured after 10 to 60 mins by ELISA based chemiluminescence assay	ic50	0.0009	uM
2-[3-(4-chlorophenyl)sulfanyl-2-methyl-4-phenylindol-1-yl]acetic acid	630011: Displacement of [3H]PGD2 from human CRTH2 receptor	ic50	0.0010	uM
2-[4-[4-(butylcarbamoyl)-2-[(2,4-dichlorophenyl)sulfonylamino]phenoxy]-3-methoxyphenyl]acetic acid	444130: Inhibition of PGD2-induced CRTH2 receptor internalization of CD16 negative granulocytes in human whole blood by flow cytometry	ki	0.0010	uM
2-[4-chloro-2-[[(3S)-4-[2-(4-fluorophenyl)acetyl]-3-methylpiperazin-1-yl]methyl]phenoxy]acetic acid	586985: Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay	ic50	0.0010	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Prostaglandin D2	affects binding, decreases reaction, increases activity	4
Tetrachlorodibenzodioxin	increases expression	3
ramatroban	affects activity, affects binding, decreases activity, decreases reaction, increases activity	2
Air Pollutants	affects expression, increases abundance, decreases expression	2
Indomethacin	affects binding, increases activity, decreases reaction	2
triphenyl phosphate	affects expression	1
quercitrin	increases expression	1
tris(2-butoxyethyl) phosphate	affects expression	1
13,14-dihydro-15-ketoprostaglandin D2	affects binding, increases activity, decreases reaction	1
CGP 52608	affects binding, increases reaction	1
15-deoxy-delta(12,14)-prostaglandin J2	affects binding, increases activity, decreases reaction	1
15R-methyl prostaglandin D2	affects binding, increases activity, decreases reaction	1
(4-chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic acid	affects binding	1
(4-chloro-2-((2-fluoro-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic acid	affects binding	1
theaflavin-3,3’-digallate	affects expression	1
Arsenic Trioxide	increases expression	1
Leflunomide	increases expression	1
Arsenic	affects expression	1
Aspirin	affects response to substance	1
Benzo(a)pyrene	increases methylation	1
Calcium	affects abundance, affects localization	1
Cisplatin	increases expression	1
Drugs, Chinese Herbal	increases expression	1
Naphthoquinones	increases expression	1
Ozone	affects expression, increases abundance	1
Silicon Dioxide	decreases expression	1
Tobacco Smoke Pollution	decreases methylation	1
Urethane	decreases expression	1
8-Bromo Cyclic Adenosine Monophosphate	decreases expression	1
Particulate Matter	decreases expression, increases abundance	1

ChEMBL screening assays

284 unique, capped per target: 156 binding, 128 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1047087	Binding	Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting	Discovery and optimization of CRTH2 and DP dual antagonists. — Bioorg Med Chem Lett
CHEMBL1047089	Functional	Antagonist activity at human CRTH2 expressed in CEM cells assessed as inhibition of PGD2-stimulated cell migration after 3 hrs by transwell migration assay	Discovery and optimization of CRTH2 and DP dual antagonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

7 cell lines: 4 spontaneously immortalized cell line, 2 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0TK	ACTOne PTGDR2	Transformed cell line	Female
CVCL_H425	CHO-K1/DP2/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KU99	cAMP Hunter CHO-K1 CRTH2 Gi	Spontaneously immortalized cell line	Female
CVCL_KW76	PathHunter CHO-K1 CRTH2 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA10	PathHunter U2OS CRTH2 beta-arrestin	Cancer cell line	Female
CVCL_LC58	ValiScreen human CRTH2	Spontaneously immortalized cell line	Female
CVCL_ZL14	Tango GPR44 (CRTH2)-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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