GPR27

Summary

GPR27 (G protein-coupled receptor 27, HGNC:4482) is a protein-coding gene on chromosome 3p13, encoding Probable G-protein coupled receptor 27 (Q9NS67). Orphan receptor.

GPR27 is a member of the G protein-coupled receptors (GPCRs), a large family of receptors that have a similar structure characterized by 7 transmembrane domains. Activation of GPCRs by extracellular stimuli such as neurotransmitters, hormones, or light induces an intracellular signaling cascade mediated by heterotrimeric GTP-binding proteins, or G proteins.

Source: NCBI Gene 2850 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 19 total
• Druggable target: yes
• MANE Select transcript: NM_018971

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4482
Approved symbol	GPR27
Name	G protein-coupled receptor 27
Location	3p13
Locus type	gene with protein product
Status	Approved
Aliases	SREB1
Ensembl gene	ENSG00000170837
Ensembl biotype	protein_coding
OMIM	605187
Entrez	2850

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000304411

RefSeq mRNA: 1 — MANE Select: NM_018971 NM_018971

CCDS: CCDS2915

Canonical transcript exons

ENST00000304411 — 1 exons

Exon	Start	End
ENSE00001138190	71753855	71756496

Expression profiles

Bgee: expression breadth ubiquitous, 244 present calls, max score 94.98.

FANTOM5 (CAGE): breadth broad, TPM avg 1.9817 / max 327.2458, expressed in 563 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
37296	0.8472	386
37297	0.6908	142
37295	0.4437	260

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
medial globus pallidus	UBERON:0002477	94.98	gold quality
cortical plate	UBERON:0005343	93.91	gold quality
globus pallidus	UBERON:0001875	93.60	gold quality
endothelial cell	CL:0000115	93.27	gold quality
superior vestibular nucleus	UBERON:0007227	92.80	gold quality
Brodmann (1909) area 23	UBERON:0013554	92.75	gold quality
subthalamic nucleus	UBERON:0001906	92.11	gold quality
inferior vagus X ganglion	UBERON:0005363	92.03	gold quality
nucleus accumbens	UBERON:0001882	91.79	gold quality
spinal cord	UBERON:0002240	90.34	gold quality
caudate nucleus	UBERON:0001873	90.31	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	90.28	gold quality
entorhinal cortex	UBERON:0002728	90.14	gold quality
ventral tegmental area	UBERON:0002691	89.96	gold quality
pons	UBERON:0000988	89.28	gold quality
temporal lobe	UBERON:0001871	89.25	gold quality
adult organism	UBERON:0007023	89.10	gold quality
dorsal plus ventral thalamus	UBERON:0001897	88.98	gold quality
amygdala	UBERON:0001876	88.59	gold quality
middle temporal gyrus	UBERON:0002771	88.28	gold quality
substantia nigra pars compacta	UBERON:0001965	88.08	gold quality
putamen	UBERON:0001874	88.02	gold quality
Ammon’s horn	UBERON:0001954	87.79	gold quality
medulla oblongata	UBERON:0001896	87.76	gold quality
parietal lobe	UBERON:0001872	87.62	gold quality
lateral globus pallidus	UBERON:0002476	87.53	gold quality
superior frontal gyrus	UBERON:0002661	87.52	gold quality
postcentral gyrus	UBERON:0002581	87.35	gold quality
germinal epithelium of ovary	UBERON:0001304	86.82	gold quality
telencephalon	UBERON:0001893	86.80	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.22

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 2)

• Prognostic significance and immune characteristics of GPR27 in gastric cancer. (PMID:37702614)
• GPR27 expression correlates with prognosis and tumor progression in gliomas. (PMID:38638156)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	gpr27	ENSDARG00000006607
mus_musculus	Gpr27	ENSMUSG00000072875
rattus_norvegicus	Gpr27	ENSRNOG00000010880

Paralogs (2): GPR85 (ENSG00000164604), GPR173 (ENSG00000184194)

Protein

Protein identifiers

Probable G-protein coupled receptor 27 — Q9NS67 (reviewed: Q9NS67)

Alternative names: Super conserved receptor expressed in brain 1

All UniProt accessions (2): Q9NS67, F1DAM3

UniProt curated annotations — full annotation on UniProt →

Function. Orphan receptor. Possible candidate for amine-like G-protein coupled receptor.

Subcellular location. Cell membrane.

Tissue specificity. Highly expressed as a 3.0 kb transcript in brain, ovary, testis, heart, prostate and peripheral Leukocytes. Lower levels in pancreas and small intestine. A 2.3 kb transcript was also found in peripheral Leukocytes. In brain regions, detected as a 3.0 kb transcript in all regions tested. Highest levels in the caudate nucleus, putamen, hippocampus and subthalamic nucleus. Lowest level in the cerebellum.

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

RefSeq proteins (1): NP_061844* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR051509	GPCR_Orphan/Phoenixin	Family

Pfam: PF00001

UniProt features (18 total): topological domain 8, transmembrane region 7, chain 1, glycosylation site 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NS67-F1	79.54	0.48

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): 95–171

Glycosylation sites (1): 3

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-418555	G alpha (s) signalling events

MSigDB gene sets: 122 (showing top): GOBP_INSULIN_SECRETION, GOBP_CELLULAR_RESPONSE_TO_CARBOHYDRATE_STIMULUS, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, MEF2_02, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELL_CELL_SIGNALING, PAX8_B, GOBP_POSITIVE_REGULATION_OF_INSULIN_SECRETION, GOBP_REGULATION_OF_PROTEIN_SECRETION, chr3p13, GOBP_REGULATION_OF_CELLULAR_LOCALIZATION, BILD_E2F3_ONCOGENIC_SIGNATURE, GOBP_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND

GO Biological Process (4): signal transduction (GO:0007165), positive regulation of insulin secretion involved in cellular response to glucose stimulus (GO:0035774), positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathway (GO:1900738), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (1): G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
positive regulation of insulin secretion	1
insulin secretion involved in cellular response to glucose stimulus	1
regulation of insulin secretion involved in cellular response to glucose stimulus	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of G protein-coupled receptor signaling pathway	1
regulation of phospholipase C-activating G protein-coupled receptor signaling pathway	1
G protein-coupled receptor activity	1
signal transduction	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

366 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GPR27	ALDH18A1	P54886	694
GPR27	EIF4E3	Q8N5X7	580
GPR27	GPR25	O00155	512
GPR27	GPR101	Q96P66	474
GPR27	GPR63	Q9BZJ6	470
GPR27	STYX	Q8WUJ0	467
GPR27	GPR82	Q96P67	452
GPR27	GPR176	Q14439	440
GPR27	GPR150	Q8NGU9	424
GPR27	GPR62	Q9BZJ7	422
GPR27	GPR162	Q16538	421
GPR27	GPR52	Q9Y2T5	411
GPR27	GPR22	Q99680	402
GPR27	PROK2	Q9HC23	400
GPR27	ZNF891	A8MT65	400

IntAct

7 interactions, top by confidence:

A	B	Type	Score
	GPR27	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	GPR27	psi-mi:“MI:0915”(physical association)	0.400
GPR27	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	GPR27	psi-mi:“MI:0915”(physical association)	0.400
CHRNA4	TMEM223	psi-mi:“MI:0914”(association)	0.350
GPR27	TMEM259	psi-mi:“MI:0914”(association)	0.350

BioGRID (5): GPR27 (Synthetic Growth Defect), ANKRD13C (Affinity Capture-MS), TTYH3 (Affinity Capture-MS), GPR27 (Affinity Capture-MS), TMEM259 (Affinity Capture-MS)

ESM2 similar proteins: A0A287A2K5, A5A4K9, A5A4L1, O08725, O43193, O54897, O77808, O88721, P30518, P30552, P30553, P30796, P30937, P31391, P32239, P32307, P32745, P34995, P35346, P35375, P41231, P46095, P46627, P48044, P48748, P49220, P49660, P51651, P56481, P79266, Q00788, Q15722, Q684M3, Q6YNI2, Q8HYC3, Q8HZN9, Q8HZP1, Q8MJV3, Q91X56, Q92847

Diamond homologs: O54897, P60893, P60894, P60895, Q5E9H8, Q5RBG7, Q6PI62, Q9I918, Q9I919, Q9JJH2, Q9JJH3, Q9NS66, Q9NS67, O00590, O08707, O54814, O57422, O62729, O70342, O93361, O97665, P18825, P21109, P22086, P25025, P30953, P32251, P47211, P48039, P48040, P49285, P51678, P51685, P55919, P56479, P87366, Q01337, Q15761, Q24563, Q28003

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	19
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

39 predictions. Top by Δscore:

Variant	Effect	Δscore
3:71754901:G:GT	donor_gain	0.4400
3:71754892:G:GT	donor_gain	0.4200
3:71754676:C:CA	acceptor_gain	0.4000
3:71754898:C:T	donor_gain	0.3900
3:71754869:G:GT	donor_gain	0.3800
3:71755076:AG:A	acceptor_gain	0.3500
3:71755077:GG:G	acceptor_gain	0.3500
3:71754939:G:A	acceptor_gain	0.2900
3:71754896:TGC:T	donor_gain	0.2800
3:71754675:AC:A	acceptor_gain	0.2700
3:71754886:G:GT	donor_gain	0.2700
3:71754943:GCCC:G	donor_gain	0.2700
3:71755076:A:AG	acceptor_gain	0.2700
3:71755077:G:GG	acceptor_gain	0.2700
3:71754891:GGCT:G	donor_gain	0.2600
3:71755072:CAACA:C	acceptor_loss	0.2600
3:71755073:AACAG:A	acceptor_gain	0.2600
3:71755074:ACAG:A	acceptor_loss	0.2600
3:71755075:CAGGG:C	acceptor_loss	0.2600
3:71755076:A:AC	acceptor_loss	0.2600
3:71755077:G:GA	acceptor_loss	0.2600
3:71754676:C:G	acceptor_gain	0.2500
3:71755078:GGAGC:G	acceptor_loss	0.2500
3:71755234:ACGTT:A	donor_gain	0.2400
3:71755077:GGGA:G	acceptor_gain	0.2300
3:71755082:C:G	acceptor_loss	0.2300
3:71755486:TATAA:T	acceptor_gain	0.2300
3:71755487:ATAAA:A	acceptor_gain	0.2300
3:71754901:GAT:G	donor_gain	0.2200
3:71754938:T:TA	acceptor_gain	0.2200

AlphaMissense

2361 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:71754143:A:C	S32R	0.998
3:71754145:C:A	S32R	0.998
3:71754145:C:G	S32R	0.998
3:71754734:T:C	F229L	0.998
3:71754736:C:A	F229L	0.998
3:71754736:C:G	F229L	0.998
3:71754730:G:C	W227C	0.997
3:71754730:G:T	W227C	0.997
3:71754941:G:A	G298R	0.997
3:71754941:G:C	G298R	0.997
3:71754157:C:A	N36K	0.996
3:71754157:C:G	N36K	0.996
3:71754938:T:A	W297R	0.996
3:71754938:T:C	W297R	0.996
3:71755022:T:A	W325R	0.996
3:71755022:T:C	W325R	0.996
3:71754152:G:C	G35R	0.995
3:71754491:T:A	W148R	0.995
3:71754491:T:C	W148R	0.995
3:71754926:T:C	F293L	0.995
3:71754928:C:A	F293L	0.995
3:71754928:C:G	F293L	0.995
3:71754945:C:A	P299H	0.995
3:71755053:C:A	P335H	0.995
3:71754153:G:A	G35D	0.994
3:71754735:T:G	F229C	0.994
3:71754775:G:C	W242C	0.994
3:71754775:G:T	W242C	0.994
3:71754945:C:G	P299R	0.994
3:71755031:T:C	F328L	0.994

dbSNP variants (sampled 300 via entrez): RS1000236470 (3:71755752 G>A), RS1002625859 (3:71753745 G>A,C), RS1002955887 (3:71752720 T>C), RS1003049084 (3:71752557 A>G), RS1003278129 (3:71755683 T>A,G), RS1003848179 (3:71753566 C>G,T), RS1004144191 (3:71753331 C>T), RS1005283512 (3:71754991 C>A,G,T), RS1005516057 (3:71752215 G>A), RS1005601724 (3:71755276 C>A,T), RS1006534368 (3:71756760 T>C), RS1007197987 (3:71756035 G>A), RS1007366229 (3:71756555 G>A), RS1008173163 (3:71752049 C>T), RS1010258549 (3:71753767 G>A,C)

Disease associations

OMIM: gene MIM:605187 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4523923 (SINGLE PROTEIN), CHEMBL5482972 (CHIMERIC PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Class A Orphans with only surrogate ligands

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

Ligand	Action	Affinity	Parameter
compound 5128535	Agonist	6.34	pEC50
PT-91	Agonist	6.15	pEC50
compound 1a [PMID: 27184081]	Inverse agonist	5.0	pEC50

ChEMBL bioactivities

60 potent at pChembl≥5 of 61 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.90	EC50	125.9	nM	CHEMBL5438097
6.85	EC50	141.2	nM	CHEMBL4869253
6.71	EC50	195	nM	CHEMBL5422942
6.69	EC50	204.2	nM	CHEMBL5409423
6.64	EC50	229.1	nM	CHEMBL4861825
6.61	EC50	245.5	nM	CHEMBL5428000
6.58	EC50	263	nM	CHEMBL5407924
6.56	EC50	275.4	nM	CHEMBL5438642
6.44	EC50	363.1	nM	CHEMBL4878026
6.44	EC50	363.1	nM	CHEMBL5440210
6.43	EC50	371.5	nM	CHEMBL5418323
6.42	EC50	380.2	nM	CHEMBL5439395
6.38	EC50	416.9	nM	CHEMBL4852965
6.38	EC50	416.9	nM	CHEMBL5425829
6.35	EC50	446.7	nM	CHEMBL5397942
6.34	EC50	457.1	nM	CHEMBL4852965
6.32	EC50	478.6	nM	CHEMBL4850346
6.26	EC50	549.5	nM	CHEMBL5405394
6.25	EC50	562.3	nM	CHEMBL5400267
6.24	EC50	575.4	nM	CHEMBL4869721
6.23	EC50	588.8	nM	CHEMBL5411849
6.20	EC50	631	nM	CHEMBL5433874
6.18	EC50	660.7	nM	CHEMBL4869637
6.11	EC50	776.2	nM	CHEMBL5433355
6.09	EC50	812.8	nM	CHEMBL5414526
6.07	EC50	851.1	nM	CHEMBL4857582
6.04	EC50	912	nM	CHEMBL4873007
6.04	EC50	912	nM	CHEMBL4852965
6.02	EC50	955	nM	CHEMBL5424423
6.01	EC50	977.2	nM	CHEMBL5409423
6.01	EC50	977.2	nM	CHEMBL5417483
5.99	EC50	1023	nM	CHEMBL4865504
5.99	EC50	1023	nM	CHEMBL4854273
5.91	EC50	1230	nM	CHEMBL4866235
5.91	EC50	1230	nM	CHEMBL5403541
5.90	EC50	1259	nM	CHEMBL4850296
5.90	EC50	1259	nM	CHEMBL5438150
5.89	EC50	1300	nM	CHEMBL4869637
5.70	EC50	1995	nM	CHEMBL5438150
5.67	EC50	2138	nM	CHEMBL5433355
5.67	EC50	2138	nM	CHEMBL5432356
5.64	EC50	2291	nM	CHEMBL4868057
5.59	EC50	2570	nM	CHEMBL4852817
5.52	EC50	3020	nM	CHEMBL1322660
5.52	EC50	3020	nM	CHEMBL5395036
5.49	EC50	3236	nM	CHEMBL5403541
5.41	EC50	3890	nM	CHEMBL5397942
5.41	EC50	3890	nM	CHEMBL5399326
5.40	EC50	3981	nM	CHEMBL4868300
5.29	EC50	5129	nM	CHEMBL4860248

PubChem BioAssay actives

60 with measured affinity, of 220 total; 46 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
4-bromo-2,5-dimethyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.1259	uM
4-chloro-2,5-difluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.1412	uM
4-chloro-N-[4-(phenylsulfamoyl)phenyl]-2-(trifluoromethoxy)benzamide	2024705: Agonist activity at CLuc-tagged human GPR27-V2 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.1950	uM
4-chloro-2-methoxy-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.2042	uM
4-cyano-2-fluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.2291	uM
2-bromo-N-[4-(phenylsulfamoyl)phenyl]-4-(trifluoromethyl)benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.2455	uM
4,5-dichloro-2-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.2630	uM
4-chloro-2,5-dimethyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.2754	uM
2-fluoro-N-[4-(phenylsulfamoyl)phenyl]-4-(trifluoromethyl)benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.3631	uM
2,5-dichloro-4-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.3631	uM
2,4-dichloro-5-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.3715	uM
2,4-dichloro-5-fluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.3802	uM
4-bromo-2,5-difluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.4169	uM
2,4-dichloro-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024688: Agonist activity at CLuc-tagged human GPR27-V2 expressed in HEK293 cells incubated overnight by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.4169	uM
2,4-difluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.4467	uM
4-bromo-2-fluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.4786	uM
N-[4-(phenylsulfamoyl)phenyl]-2,4-bis(trifluoromethyl)benzamide	2024705: Agonist activity at CLuc-tagged human GPR27-V2 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.5495	uM
4-bromo-5-fluoro-2-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.5623	uM
2,4-dichloro-N-[4-[(3-chlorophenyl)sulfamoyl]phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.5754	uM
2,4,5-trichloro-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.5888	uM
2,3,4-trichloro-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.6310	uM
2,4-dichloro-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]benzamide	2024688: Agonist activity at CLuc-tagged human GPR27-V2 expressed in HEK293 cells incubated overnight by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.6607	uM
2,4-dimethyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.7762	uM
4-chloro-5-fluoro-2-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.8128	uM
4-bromo-2-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.8511	uM
4-chloro-2-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	0.9120	uM
3-chloro-N-[4-(phenylsulfamoyl)phenyl]naphthalene-2-carboxamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.9550	uM
2-chloro-4-cyano-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	0.9772	uM
4-bromo-2-methoxy-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	1.0233	uM
2-bromo-4-chloro-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	1.0233	uM
2,4-dichloro-N-[4-[(2-methylphenyl)sulfamoyl]phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	1.2303	uM
2,4-dibromo-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	1.2303	uM
2,4-dichloro-N-[4-[(2-chlorophenyl)sulfamoyl]phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	1.2589	uM
2-methoxy-N-[4-(phenylsulfamoyl)phenyl]-4-(trifluoromethyl)benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	1.2589	uM
4-bromo-2-fluoro-5-methyl-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	2.1380	uM
6-chloro-2-fluoro-N-[4-(phenylsulfamoyl)phenyl]pyridine-3-carboxamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	2.2909	uM
2,4-dichloro-N-[4-[methyl(phenyl)sulfamoyl]phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	2.5704	uM
2,4-dichloro-N-[4-(pyridin-2-ylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	3.0200	uM
2-bromo-4-methoxy-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024708: Agonist activity at CLuc-tagged human GPR27 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	3.0200	uM
2-chloro-N-[4-(phenylsulfamoyl)phenyl]-4-(trifluoromethyl)benzamide	2024705: Agonist activity at CLuc-tagged human GPR27-V2 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	3.8904	uM
4-chloro-2-fluoro-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	3.9811	uM
2-fluoro-4-iodo-N-[4-(phenylsulfamoyl)phenyl]benzamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	5.1286	uM
3,5-dichloro-N-[4-(phenylsulfamoyl)phenyl]pyridine-2-carboxamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	5.7544	uM
2-oxo-N-[4-(phenylsulfamoyl)phenyl]chromene-3-carboxamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	7.7625	uM
2-chloro-4-methoxy-N-[4-(phenylsulfamoyl)phenyl]benzamide	2024705: Agonist activity at CLuc-tagged human GPR27-V2 expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay	ec50	8.1283	uM
N-[4-(phenylsulfamoyl)phenyl]naphthalene-2-carboxamide	1771449: Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase complementation assay	ec50	8.5114	uM

CTD chemical–gene interactions

27 total (human), top 27 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression	5
trichostatin A	affects cotreatment, decreases expression	2
mercuric bromide	affects cotreatment, decreases expression	2
Panobinostat	affects cotreatment, decreases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
triphenyl phosphate	affects expression	1
bisphenol A	decreases expression	1
sodium arsenite	decreases expression	1
cobaltous chloride	increases expression	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
belinostat	decreases expression	1
abrine	decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
jinfukang	affects cotreatment, decreases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Sunitinib	decreases expression	1
Vorinostat	decreases expression	1
Atrazine	increases expression	1
Benzo(a)pyrene	increases methylation	1
Cadmium	decreases expression	1
Cisplatin	affects cotreatment, decreases expression	1
Doxorubicin	decreases expression	1
Estradiol	increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Sarin	increases expression	1
Thiram	decreases expression	1

ChEMBL screening assays

18 unique, capped per target: 10 binding, 8 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4830744	Functional	Agonist activity at human GPR27 expressed in HEK293 cells co-expressing FnLArrb2.GPR27V2LFc assessed as induction of beta-arrestin recruitment incubated for 10 mins measured followed by addition of D-luciferin by firefly-luciferase compleme	Structure-activity relationships of agonists for the orphan G protein-coupled receptor GPR27. — Eur J Med Chem
CHEMBL4883443	Binding	PRESTO-Tango GPCRome screening (GPR27)	Data for DCP probe UCSF924

Cellosaurus cell lines

1 cell lines: 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_KX54	PathHunter CHO-K1 GPR27 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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