CMKLR2

Summary

CMKLR2 (chemerin chemokine-like receptor 2, HGNC:4463) is a protein-coding gene on chromosome 2q33.3, encoding Chemerin-like receptor 2 (P46091). Receptor for chemoattractant adipokine chemerin/RARRES2 suggesting a role for this receptor in the regulation of inflammation and energy homesotasis.

Enables adipokinetic hormone binding activity and adipokinetic hormone receptor activity. Predicted to be involved in glucose homeostasis and neuropeptide signaling pathway. Located in nucleoplasm and plasma membrane.

Source: NCBI Gene 2825 — RefSeq curated summary.

At a glance

• GWAS associations: 7
• Clinical variants (ClinVar): 60 total
• Druggable target: yes
• MANE Select transcript: NM_001389445

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4463
Approved symbol	CMKLR2
Name	chemerin chemokine-like receptor 2
Location	2q33.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000183671
Ensembl biotype	protein_coding
OMIM	600239
Entrez	2825

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 8 protein_coding

ENST00000407325, ENST00000411719, ENST00000437420, ENST00000439932, ENST00000442134, ENST00000451790, ENST00000458440, ENST00000621141

RefSeq mRNA: 7 — MANE Select: NM_001389445 NM_001098199, NM_001261452, NM_001261453, NM_001261454, NM_001261455, NM_001389445, NM_005279

CCDS: CCDS2368

Canonical transcript exons

ENST00000621141 — 2 exons

Exon	Start	End
ENSE00001682006	206213307	206213371
ENSE00001904753	206175316	206177275

Expression profiles

Bgee: expression breadth ubiquitous, 121 present calls, max score 79.10.

FANTOM5 (CAGE): breadth broad, TPM avg 4.2862 / max 175.9283, expressed in 709 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
33356	3.0389	619
33358	0.8995	365
33357	0.3071	166
33360	0.0266	1
33359	0.0141	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
placenta	UBERON:0001987	79.10	gold quality
stromal cell of endometrium	CL:0002255	74.82	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	73.10	gold quality
esophagus mucosa	UBERON:0002469	71.30	gold quality
skin of leg	UBERON:0001511	70.87	gold quality
right adrenal gland cortex	UBERON:0035827	69.95	gold quality
zone of skin	UBERON:0000014	69.61	gold quality
right adrenal gland	UBERON:0001233	68.89	gold quality
ventricular zone	UBERON:0003053	68.63	gold quality
left adrenal gland	UBERON:0001234	68.37	gold quality
gall bladder	UBERON:0002110	68.25	gold quality
left adrenal gland cortex	UBERON:0035825	68.23	gold quality
smooth muscle tissue	UBERON:0001135	68.16	gold quality
skin of abdomen	UBERON:0001416	67.89	gold quality
vagina	UBERON:0000996	67.88	gold quality
apex of heart	UBERON:0002098	67.83	gold quality
skeletal muscle tissue	UBERON:0001134	66.51	gold quality
adrenal gland	UBERON:0002369	66.41	gold quality
muscle tissue	UBERON:0002385	66.32	gold quality
esophagus	UBERON:0001043	65.44	gold quality
lower esophagus mucosa	UBERON:0035834	65.25	gold quality
lymph node	UBERON:0000029	64.36	gold quality
heart left ventricle	UBERON:0002084	64.06	gold quality
right coronary artery	UBERON:0001625	63.28	gold quality
heart	UBERON:0000948	62.47	gold quality
monocyte	CL:0000576	62.23	gold quality
ectocervix	UBERON:0012249	60.79	gold quality
nucleus accumbens	UBERON:0001882	60.11	gold quality
leukocyte	CL:0000738	59.73	gold quality
left coronary artery	UBERON:0001626	59.68	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.02

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): KLF15

miRNA regulators (miRDB)

38 targeting CMKLR2, 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-3064-3P	100.00	70.09	1254
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-499A-5P	99.98	70.79	1323
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-4760-3P	99.93	70.50	2385
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-30A-3P	99.87	69.74	2928
HSA-MIR-30D-3P	99.87	69.92	2917
HSA-MIR-30E-3P	99.87	69.68	2942
HSA-MIR-137-3P	99.87	74.74	2401
HSA-MIR-4766-5P	99.75	69.23	2662
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-378A-5P	99.65	66.33	1311
HSA-MIR-4261	99.59	70.30	3415
HSA-MIR-4328	99.57	71.06	4094
HSA-MIR-6833-5P	99.50	68.93	1161
HSA-MIR-4643	99.49	67.63	1791
HSA-MIR-657	99.48	66.02	848
HSA-MIR-147B-5P	99.45	70.62	2432
HSA-MIR-6507-5P	99.36	70.46	2524
HSA-MIR-504-3P	99.30	67.18	1745
HSA-MIR-1273H-3P	99.29	67.55	980
HSA-MIR-6734-3P	99.15	66.27	1627

Literature-anchored findings (GeneRIF, showing 12)

• GPR1 is a senescence-associated gene in normal human oral keratinocytes. (PMID:12837283)
• Data report that a synthetic peptide derived from the NH2-terminal extracellular region of an orphan GPCR, GPR1, inhibited infection of not only an HIV-1 variant that uses GPR1 as a co-receptor, but also X4, R5, and R5X4 viruses. (PMID:15919664)
• identified homologous amino acid sequences in amino-terminal regions between CCR5 and GPR1/ sequences are important for G protein-coupled receptors to make the conformation critical for the interaction with the Env protein of HIV-1. (PMID:20334567)
• GPR1 gene is imprinted and paternally expressed in human and mouse. (PMID:20385583)
• The Gene-based analyses revealed four significant associations in the WT1, ZC3H12C, DLGAP2, and GPR1 genes at p < 0.05. in this study. (PMID:25391383)
• CMKLR1 and GPR1 were widely expressed in vascular smooth muscle. (PMID:27742615)
• GPR1 protein and gene levels were significantly decreased in gestational diabetes mellitus patient placentas. (PMID:30835511)
• The majority of presented data report down-regulation of chemerin in cancer tissue and suggest a tumor-suppressing role of chemerin in most cancer types, being mediated by recruiting innate immune defenses and by growth-inhibitory downstream signaling by chemerin receptors CMKLR1 and GPR1. (Review) (PMID:31370263)
• Chemerin Isoform-Specific Effects on Hepatocyte Migration and Immune Cell Inflammation. (PMID:33003572)
• Chemerin causes lipid metabolic imbalance and induces passive lipid accumulation in human hepatoma cell line via the receptor GPR1. (PMID:33887347)
• The Atypical Chemerin Receptor GPR1 Displays Different Modes of Interaction with beta-Arrestins in Humans and Mice with Important Consequences on Subcellular Localization and Trafficking. (PMID:35326488)
• Structure of G protein-coupled receptor GPR1 bound to full-length chemerin adipokine reveals a chemokine-like reverse binding mode. (PMID:39466725)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	cmklr2	ENSDARG00000101366
mus_musculus	Cmklr2	ENSMUSG00000046856
rattus_norvegicus	Cmklr2	ENSRNOG00000045532
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), PTGDR2 (ENSG00000183134), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Chemerin-like receptor 2 — P46091 (reviewed: P46091)

Alternative names: Chemerin chemokine-like receptor 2, Chemokine-like receptor 2, G-protein coupled receptor 1

All UniProt accessions (6): C9J456, C9JCK1, C9JFR8, C9JQB7, C9JSU0, P46091

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for chemoattractant adipokine chemerin/RARRES2 suggesting a role for this receptor in the regulation of inflammation and energy homesotasis. Signals mainly via beta-arrestin pathway. Binding of RARRES2 activates weakly G proteins, calcium mobilization and MAPK1/MAPK3 (ERK1/2) phosphorylation too. Also acts as a receptor for TAFA1, mediates its effects on neuronal stem-cell proliferation and differentiation via the activation of ROCK/ERK and ROCK/STAT3 signaling pathway. (Microbial infection) Coreceptor for HIV-1.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in hippocampus.

Similarity. Belongs to the chemokine-like receptor (CMKLR) family.

RefSeq proteins (7): NP_001091669, NP_001248381, NP_001248382, NP_001248383, NP_001248384, NP_001376374, NP_005270 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000826	Formyl_rcpt-rel	Family
IPR002275	CML2	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (39 total): helix 10, topological domain 8, transmembrane region 7, strand 5, turn 3, sequence conflict 2, chain 1, glycosylation site 1, disulfide bond 1, sequence variant 1

Structure

Experimental structures (PDB)

9 structures.

PDB	Method	Resolution (Å)
8JJP	ELECTRON MICROSCOPY	2.9
9UYN	ELECTRON MICROSCOPY	2.9
9UYI	ELECTRON MICROSCOPY	3.2
8XGM	ELECTRON MICROSCOPY	3.29
9UYH	ELECTRON MICROSCOPY	3.3
9UYJ	ELECTRON MICROSCOPY	3.3
9UYL	ELECTRON MICROSCOPY	3.3
9UYM	ELECTRON MICROSCOPY	3.5
9L3Y	ELECTRON MICROSCOPY	3.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P46091-F1	83.29	0.52

Antibody-complex structures (SAbDab): 8 — 8JJP, 8XGM, 9UYH, 9UYI, 9UYJ, 9UYL, 9UYM, 9UYN

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): 110–187

Glycosylation sites (1): 14

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 120 (showing top): GOBP_INFLAMMATORY_RESPONSE, ACEVEDO_LIVER_CANCER_WITH_H3K27ME3_UP, CAGCTG_AP4_Q5, MORF_RAD51L3, FREAC3_01, MORF_CTSB, BLALOCK_ALZHEIMERS_DISEASE_UP, MORF_IL4, MORF_PRKCA, GOBP_REGULATION_OF_RESPONSE_TO_STRESS, GOBP_CARBOHYDRATE_HOMEOSTASIS, GOBP_REGULATION_OF_RESPONSE_TO_EXTERNAL_STIMULUS, GOCC_NEURON_PROJECTION, GOBP_REGULATION_OF_INFLAMMATORY_RESPONSE, GOBP_REGULATION_OF_DEFENSE_RESPONSE

GO Biological Process (6): G protein-coupled receptor signaling pathway (GO:0007186), neuropeptide signaling pathway (GO:0007218), glucose homeostasis (GO:0042593), cell communication (GO:0007154), signal transduction (GO:0007165), signaling (GO:0023052)

GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), neuropeptide binding (GO:0042923), adipokinetic hormone receptor activity (GO:0097003), adipokinetic hormone binding (GO:0097004), protein binding (GO:0005515)

GO Cellular Component (4): nucleoplasm (GO:0005654), plasma membrane (GO:0005886), neuron projection (GO:0043005), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	2
cellular process	2
cellular anatomical structure	2
G protein-coupled receptor activity	1
signal transduction	1
carbohydrate homeostasis	1
cell communication	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
regulation of biological process	1
transmembrane signaling receptor activity	1
peptide binding	1
protein-hormone receptor activity	1
adiponectin binding	1
adipokinetic hormone binding	1
peptide hormone binding	1
binding	1
nuclear lumen	1
membrane	1
cell periphery	1
plasma membrane bounded cell projection	1

Protein interactions and networks

STRING

702 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CMKLR2	RARRES2	Q99969	996
CMKLR2	GPHA2	Q96T91	987
CMKLR2	GPR22	Q99680	816
CMKLR2	NAMPT	P43490	779
CMKLR2	ZDBF2	Q9HCK1	712
CMKLR2	NUMA1	Q14980	677
CMKLR2	TAFA1	Q7Z5A9	658
CMKLR2	GPR37	O15354	584
CMKLR2	GNAO1	P09471	582
CMKLR2	GPHB5	Q86YW7	582
CMKLR2	ARRB1	P49407	580
CMKLR2	ADIPOQ	Q15848	568
CMKLR2	GRP	P07491	556
CMKLR2	ADIPOR1	Q96A54	546
CMKLR2	CAPN10	Q9HC96	546

IntAct

7 interactions, top by confidence:

A	B	Type	Score
	CMKLR2	psi-mi:“MI:0915”(physical association)	0.520
CMKLR2		psi-mi:“MI:0915”(physical association)	0.520
CMKLR2	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	CMKLR2	psi-mi:“MI:0915”(physical association)	0.400
CMKLR2	RAMP3	psi-mi:“MI:0915”(physical association)	0.400

ESM2 similar proteins: A4FUQ5, B9VR26, O08790, O35786, O70129, O75388, O88416, O88536, O88537, O97664, P0C7U4, P21462, P21730, P25089, P25090, P30992, P30993, P33766, P35343, P35407, P46090, P46091, P79175, P79176, P79177, P79178, P79188, P79189, P79190, P79191, P79234, P79235, P79236, P79237, P79240, P79241, P79242, P79243, P97468, P97520

Diamond homologs: A0T2N3, F1MV99, O00155, O00590, O08707, O08858, O09027, O35210, O77590, O88410, O89039, O97666, P0C5I1, P0C7U4, P11613, P21109, P25024, P25025, P25095, P25104, P25106, P29089, P29754, P29755, P30555, P30556, P30680, P30874, P30875, P30935, P30936, P30937, P30938, P31391, P32303, P32745, P33396, P33535, P34976, P34993

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	55
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

548 predictions. Top by Δscore:

Variant	Effect	Δscore
2:206177290:T:C	acceptor_gain	1.0000
2:206213429:T:C	acceptor_gain	1.0000
2:206217804:CTCA:C	donor_loss	1.0000
2:206217805:TCA:T	donor_loss	1.0000
2:206217806:CA:C	donor_loss	1.0000
2:206217808:CCT:C	donor_gain	1.0000
2:206217808:CCTCT:C	donor_gain	1.0000
2:206177271:GAAAT:G	acceptor_gain	0.9900
2:206177273:AATC:A	acceptor_loss	0.9900
2:206177275:TC:T	acceptor_loss	0.9900
2:206177276:C:CA	acceptor_loss	0.9900
2:206177276:C:CC	acceptor_gain	0.9900
2:206177290:T:TC	acceptor_gain	0.9900
2:206196720:C:CT	donor_gain	0.9900
2:206196721:T:TT	donor_gain	0.9900
2:206213429:T:TC	acceptor_gain	0.9900
2:206213440:G:GC	acceptor_gain	0.9900
2:206217807:A:AC	donor_gain	0.9900
2:206217808:C:CC	donor_gain	0.9900
2:206177274:AT:A	acceptor_gain	0.9800
2:206177285:C:CT	acceptor_gain	0.9800
2:206177289:T:TC	acceptor_gain	0.9800
2:206213422:CTGG:C	acceptor_gain	0.9800
2:206213440:G:C	acceptor_gain	0.9800
2:206217807:AC:A	donor_gain	0.9800
2:206217808:CC:C	donor_gain	0.9800
2:206177273:AAT:A	acceptor_gain	0.9700
2:206177286:A:T	acceptor_gain	0.9700
2:206177289:T:C	acceptor_gain	0.9700
2:206213366:C:CT	acceptor_gain	0.9700

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000055000 (2:206195728 G>A,T), RS1000071596 (2:206175385 C>G), RS1000101925 (2:206176802 C>T), RS1000205230 (2:206214406 C>T), RS1000237242 (2:206177079 C>A,T), RS1000330452 (2:206214620 T>A,G), RS1000351343 (2:206183262 C>T), RS1000420527 (2:206208801 G>A,T), RS1000473880 (2:206207566 G>A), RS1000534016 (2:206178614 G>A,T), RS1000548888 (2:206215363 C>T), RS1000663374 (2:206215715 G>C,T), RS1000826908 (2:206202864 T>C), RS1000848481 (2:206190893 A>C), RS1000887949 (2:206209253 G>A)

Disease associations

OMIM: gene MIM:600239 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

7 associations (top):

Study	Trait	p-value
GCST001567_11	Bipolar disorder and schizophrenia	9.000000e-06
GCST005951_45	Body mass index	1.000000e-09
GCST010346_41	TPE interval (resting)	2.000000e-08
GCST010989_208	Body size at age 10	3.000000e-44
GCST90000025_866	Appendicular lean mass	9.000000e-15
GCST90002397_459	Mean spheric corpuscular volume	1.000000e-09
GCST90002409_19	Childhood body mass index	3.000000e-08

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index
EFO:0004644	TPE interval measurement
EFO:0009819	comparative body size at age 10, self-reported
EFO:0004980	appendicular lean mass

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523229 (SINGLE PROTEIN)

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs17223074	CMKLR2		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Chemerin receptors

Most potent curated ligand interactions (3 total), top 3:

Ligand	Action	Affinity	Parameter
chemerin C-terminal peptide	Agonist	9.0	pEC50
chemerin	Full agonist	8.28	pKd
OSTN (81-102)	Agonist	6.18	pEC50

ChEMBL bioactivities

17 potent at pChembl≥5 of 17 total, top 17 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.31	Ki	4.9	nM	CHEMBL5081975
8.15	EC50	7	nM	CHEMBL6188778
8.10	EC50	7.943	nM	CHEMBL6188778
7.90	EC50	12.59	nM	CHEMBL6188778
7.89	EC50	13	nM	CHEMBL6188778
7.80	EC50	15.85	nM	CHEMBL5315640
7.55	Ki	28	nM	CHEMBL5081975
7.45	Ki	35.4	nM	CHEMBL5081975
7.40	EC50	39.81	nM	CHEMBL6188778
7.37	EC50	43	nM	CHEMBL6188778
7.34	EC50	46.1	nM	CHEMBL4470851
7.25	EC50	55.6	nM	CHEMBL4517021
7.21	EC50	60.9	nM	CHEMBL4447799
7.03	EC50	92.8	nM	CHEMBL4568879
6.00	EC50	1000	nM	CHEMBL5315640
5.88	Ki	1323	nM	CHEMBL6193503
5.83	Ki	1479	nM	CHEMBL6188778

PubChem BioAssay actives

3 with measured affinity, of 10 total; 2 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)-3-phenyl-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]propanoic acid	2066346: Agonist activity at eYFP-tagged human GPR1 expressed in TAMRA-labeled chemerin-9 stimulated HEK293 cells assessed as GPR1 internalization by fluorescence based analysis	ec50	0.0158	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoic acid	2066355: Displacement of TAMRA-labeled C9 from Nluc/eYFP-tagged GPR1 (unknown origin) transfected in HEK293 cells assessed as inhibition constant incubated for 1 hrs by BRET analysis	ki	0.0354	uM

CTD chemical–gene interactions

23 total (human), top 23 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects expression, increases expression	2
Acetaminophen	decreases expression, increases expression	2
diallyl trisulfide	increases expression	1
avobenzone	decreases expression	1
perfluorooctane sulfonic acid	increases expression	1
CGP 52608	affects binding, increases reaction	1
perfluoro-n-nonanoic acid	increases expression	1
2,2’,4,4’,5-brominated diphenyl ether	increases expression	1
Decitabine	affects expression	1
Sunitinib	increases expression	1
Arsenic	affects methylation	1
Benzo(a)pyrene	increases expression	1
Cannabidiol	increases expression	1
Cisplatin	affects expression	1
Copper	affects binding, increases expression	1
Disulfiram	affects binding, increases expression	1
Lucanthone	decreases expression	1
Sodium Dodecyl Sulfate	decreases expression	1
Triclosan	decreases expression	1
Vanadates	increases expression	1
Cyclosporine	increases expression	1
Aflatoxin B1	increases methylation	1
Asbestos, Crocidolite	decreases expression	1

ChEMBL screening assays

24 unique, capped per target: 13 functional, 11 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4418427	Binding	Agonist activity at recombinant human GPR1 expressed in CHOK1 PathHunter cells assessed as beta-arrestin 2 recruitment incubated for 90 mins by luminescence assay	Method for identifying modulators of GPCR GPR1 function
CHEMBL5505162	Functional	Agonist activity at human GPR1 expressed in HTLA cells assessed as beta-arrestin recruitment at 10 uM incubated for 24 hrs by PRESTO-Tango assay	Development of a Potent and Selective G2A (GPR132) Agonist. — J Med Chem

Cellosaurus cell lines

5 cell lines: 4 cancer cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_1R24	NP-2/GPR1	Cancer cell line	Male
CVCL_1R30	NP-2/CD4/GPR1	Cancer cell line	Male
CVCL_KX18	PathHunter CHO-K1 GPR1 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA39	PathHunter U2OS GPR1 Total GPCR Internalization	Cancer cell line	Female
CVCL_ZL12	Tango GPR1-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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