SFRP1

Summary

SFRP1 (secreted frizzled related protein 1, HGNC:10776) is a protein-coding gene on chromosome 8p11.21, encoding Secreted frizzled-related protein 1 (Q8N474). Soluble frizzled-related proteins (sFRPS) function as modulators of Wnt signaling through direct interaction with Wnts.

This gene encodes a member of the SFRP family that contains a cysteine-rich domain homologous to the putative Wnt-binding site of Frizzled proteins. Members of this family act as soluble modulators of Wnt signaling; epigenetic silencing of SFRP genes leads to deregulated activation of the Wnt-pathway which is associated with cancer. This gene may also be involved in determining the polarity of photoreceptor cells in the retina.

Source: NCBI Gene 6422 — RefSeq curated summary.

At a glance

• GWAS associations: 7
• Clinical variants (ClinVar): 33 total
• Druggable target: yes
• MANE Select transcript: NM_003012

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10776
Approved symbol	SFRP1
Name	secreted frizzled related protein 1
Location	8p11.21
Locus type	gene with protein product
Status	Approved
Aliases	SARP2, FRP, FRP-1
Ensembl gene	ENSG00000104332
Ensembl biotype	protein_coding
OMIM	604156
Entrez	6422

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000220772, ENST00000379845, ENST00000923189

RefSeq mRNA: 1 — MANE Select: NM_003012 NM_003012

CCDS: CCDS34886

Canonical transcript exons

ENST00000220772 — 3 exons

Exon	Start	End
ENSE00000691820	41303461	41303538
ENSE00001254466	41308616	41309473
ENSE00002111007	41261962	41265489

Expression profiles

Bgee: expression breadth ubiquitous, 272 present calls, max score 99.66.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 26.7536 / max 915.7706, expressed in 1106 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
92815	25.4071	1099
92814	1.0750	418
92816	0.2370	101
92806	0.0344	9

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
ventricular zone	UBERON:0003053	99.66	gold quality
parotid gland	UBERON:0001831	99.52	gold quality
mammary duct	UBERON:0001765	99.39	gold quality
epithelium of mammary gland	UBERON:0003244	99.38	gold quality
choroid plexus epithelium	UBERON:0003911	99.34	gold quality
ganglionic eminence	UBERON:0004023	99.15	gold quality
hair follicle	UBERON:0002073	98.25	gold quality
renal medulla	UBERON:0000362	98.19	gold quality
nipple	UBERON:0002030	98.17	gold quality
embryo	UBERON:0000922	98.12	gold quality
synovial joint	UBERON:0002217	97.81	gold quality
vena cava	UBERON:0004087	97.74	gold quality
mammary gland	UBERON:0001911	97.73	gold quality
endocervix	UBERON:0000458	97.72	gold quality
thoracic mammary gland	UBERON:0005200	97.70	gold quality
ectocervix	UBERON:0012249	97.40	gold quality
pericardium	UBERON:0002407	97.37	gold quality
pigmented layer of retina	UBERON:0001782	97.16	gold quality
retina	UBERON:0000966	97.14	gold quality
upper leg skin	UBERON:0004262	96.58	gold quality
seminal vesicle	UBERON:0000998	96.35	gold quality
saliva-secreting gland	UBERON:0001044	96.00	gold quality
germinal epithelium of ovary	UBERON:0001304	95.96	gold quality
mucosa of paranasal sinus	UBERON:0005030	95.87	gold quality
gall bladder	UBERON:0002110	95.80	gold quality
adult mammalian kidney	UBERON:0000082	95.18	gold quality
minor salivary gland	UBERON:0001830	95.12	gold quality
layer of synovial tissue	UBERON:0007616	95.10	gold quality
vagina	UBERON:0000996	94.99	gold quality
skin of hip	UBERON:0001554	94.96	gold quality

Single-cell (SCXA)

Detected in 14 experiment(s), a significant marker in 13.

Experiment	Marker?	Max mean expression
E-MTAB-10485	yes	2078.33
E-MTAB-8894	yes	1757.12
E-HCAD-5	yes	1382.42
E-MTAB-9841	yes	1353.36
E-GEOD-114530	yes	1228.88
E-MTAB-10885	yes	1204.14
E-GEOD-75140	yes	973.05
E-MTAB-10287	yes	776.67
E-MTAB-9154	yes	372.09
E-GEOD-75688	yes	204.99
E-GEOD-93593	yes	14.67
E-GEOD-135922	yes	14.55
E-MTAB-10018	no	882.76
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): DNMT1, DNMT3A, EZH2, FOXC1, FOXO1, FOXO3, GLI1, GLI2, HAND2, HDAC1, HOXD13, MYC, NKX3-1, PAX6, RUNX1, TFAP2C, ZEB2

miRNA regulators (miRDB)

134 targeting SFRP1, 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-450A-1-3P	100.00	69.33	1837
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-5193	100.00	67.26	1744
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-1184	99.99	68.19	1458
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-520G-5P	99.99	66.76	658
HSA-MIR-9985	99.98	72.11	2939
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-8075	99.97	67.20	962
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505
HSA-MIR-144-3P	99.94	73.98	2698
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-1-3P	99.93	72.35	1914
HSA-MIR-206	99.93	72.50	1893
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-539-5P	99.93	70.30	2855
HSA-MIR-6768-5P	99.92	67.36	1942
HSA-MIR-613	99.91	71.50	1710

Literature-anchored findings (GeneRIF, showing 40)

• In this study, the disulfide linkages of recombinant sFRP-1 were determined (PMID:11741940)
• These results indicate that the human secreted frizzled-related protein (hsFRP) gene probably functions as a tumor suppressor in normal cervical epithelium and down-regulation of hsFRP contributes to development of cervical cancer. (PMID:12413893)
• the constitutive up-regulation of SFRP1 could be an adaptive cell survival mechanism (PMID:14581477)
• Our data, so far, exclude SFRP1 as a molecular cause of RD (retinal dystrophies) (PMID:15235574)
• Some hyperplastic polyps from patients with hyperplastic polyposis coli syndrome show a secreted Frizzled receptor protein 1 immunophenotype that could indicate alterations of cellular growth control. (PMID:15335268)
• findings suggest that Secreted frizzled-related proteins 1 (SFRP1) modulates glucocorticoid-induced bone loss (PMID:15677765)
• orbital adipogenesis is enhanced in Grave’s ophthalmopathy and elevated levels of sFRP-1 in the orbit may be involved in stimulating this pathogenic process (PMID:15886250)
• SFRP 1 gene is frequently downregulated by promoter hypermethylation and suppresses tumor growth activity of lung cancer cells, which suggests that SFRP 1 is a candidate tumor suppressor gene for lung cancer (PMID:16007200)
• These results establish sFRP-1 as an important negative regulator of human osteoblast and osteocyte survival. (PMID:16149051)
• Data suggest that overexpression of SFRP1 by prostatic tumor stroma may account for the previously reported capacity of prostatic tumor stroma to provide a pro-proliferative paracrine signal to adjacent epithelial cells. (PMID:16288033)
• Results indicate that SFRP1 is the Hedgehog target to confine canonical WNT signaling within stem or progenitor cells. (PMID:16328026)
• Inactivating SFRP1 methylation occurred in all Barrett esophagus samples and in 96% of esophageal adenocarcinomas. (PMID:16407829)
• SFRP1 transcripts were shown to be downregulated in 90% (45/50) of the bladder tumors as compared with the normal bladder tissue. (PMID:16410684)
• These findings suggest that frequent downregulation of SFRP1 expression in breast cancer can be attributed, in large part, to aberrant promoter hypermethylation in conjunction with or without histone deacetylation. (PMID:16410723)
• Significant methylation and silencing of SFRP1 in CLL samples suggests its potential as a major contributor to leukomogenesis (PMID:16423993)
• promoter hypermethylation is the predominant mechanism of SFRP1 gene silencing in human breast cancer (PMID:16449975)
• study identifies sFRP1 inactivation at the premalignant stage of colorectal cancer development, indicating that these pathways may be useful targets for chemoprevention strategies in this common solid tumour (PMID:16523202)
• Represses Wnt signaling in breast tissue, and its downregulation contributes to the activation of Wnt signaling. (PMID:16532032)
• The SFRP1 protein gene plays an important role in the pathogenesis of bladder tumor and can be detected using cellular DNA extracted from urine samples. (PMID:16609023)
• Epigenetic SFRP1 inactivation is associated with urothelial carcinoma (PMID:16775427)
• sFRP-1, a target gene of the hedgehog pathway, is involved in cross-talk between the hedgehog pathway and the Wnt pathway (PMID:17035233)
• Promoter hypermethylation seems to be the predominant mechanism of SFRP1 gene silencing in renal cell carcinoma and may contribute to initiation and progression of this disease. (PMID:17353908)
• knocking down SFRP1 by RNA interference in beta-catenin-deficient cell lines (SK-Hep1) stimulated Wnt signaling and promoted cell growth. Data suggested that SFRP1 suppressed liver cancer cells growth through Wnt canonical signaling (PMID:17443492)
• SFRP1 inactivation is a common and early event caused mainly by hypermethylation in gastric cancer. SFRP1 expression loss may be correlated with tumor metastasis in primary gastric cancer. (PMID:17465504)
• Structure-function analysis of SFRP1 for its Wnt antagonist function is reported. (PMID:17471511)
• DKK1 and SFRP1 inhibit the transformed phenotype of breast cancer cell lines, and DKK1 inhibits tumor formation. (PMID:17485441)
• sFRP-1 is post-translationally modified by tyrosine sulfation at tyrosines 34 and 36, which is inhibited by the treatment of heparin (PMID:17500071)
• Wnt3A treatment significantly activated human hepatic stellate cells, while this was inhibited in secreted frizzled-related protein 1 (sFRP1) overexpressing cells. (PMID:17544413)
• Down-regulation of SFRP1 as a candidate tumor suppressor gene, triggered by the epigenetic and/or genetic events, could contribute to the oncogenesis of hepatic cell carcinoma. (PMID:17626620)
• The data support a role for sFRP1 as a tumor suppressor in clear cell renal cell carcinoma and perhaps loss of sFRP1 is an early, aberrant molecular event in renal cell carcinogenesis. (PMID:17699851)
• Epigenetic inactivation by methylation is the predominant mechanism of SFRP1 gene silencing in breast cancer. (PMID:18035687)
• sFRP-1 can interact with Wnt receptors Frizzled 4 and 7 on endothelial cells to transduce downstream to cellular machineries requiring Rac-1 activity in cooperation with GSK-3beta (PMID:18156211)
• increased expression of sFRP1 in trabecular meshwork (TM) appears to be responsible for elevated IOP in glaucoma and restoring Wnt signaling in the TM may be a novel disease intervention strategy for treating glaucoma. (PMID:18274669)
• Forced expression of SFRP1 in cultured prostatic epithelial cells led to sustained activation of JNK that was essential for SFRP1-induced epithelial proliferation. (PMID:18371946)
• Loss of SFRP1 is associated with oral squamous cell carcinoma (PMID:18497987)
• Hypermethylation and aberrant expression of SFRP genes are common in pancreatic cancer, which may be involved in pancreatic carcinogenesis. (PMID:18528941)
• Ectopic expression of SFRPs downregulated T-cell factor transcriptional activity in liver cancer cells, while overexpression of a beta-catenin mutant and depletion of SFRP1 using siRNA synergistically upregulated TCF/LEF transcriptional activity. (PMID:18592156)
• SFRP1 is hypermethylated in renal cell carcinoma. (PMID:18639284)
• Data shows that aberrant expression of Wnt antagonist SFRP1 in pancreatic cancer (PMID:18706212)
• All colorectal neoplasms samples showed hypermethylation in the promoter region of SFRP1 (PMID:18795670)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	sfrp1a	ENSDARG00000035521
danio_rerio	sfrp1b	ENSDARG00000057678
mus_musculus	Sfrp1	ENSMUSG00000031548
rattus_norvegicus	Sfrp1	ENSRNOG00000017783
drosophila_melanogaster	fz3	FBGN0027343
caenorhabditis_elegans		WBGENE00022242

Paralogs (15): FZD3 (ENSG00000104290), SFRP4 (ENSG00000106483), FZD10 (ENSG00000111432), SFRP5 (ENSG00000120057), SMO (ENSG00000128602), SFRP2 (ENSG00000145423), FZD7 (ENSG00000155760), FZD1 (ENSG00000157240), FRZB (ENSG00000162998), FZD5 (ENSG00000163251), FZD6 (ENSG00000164930), FZD4 (ENSG00000174804), FZD8 (ENSG00000177283), FZD2 (ENSG00000180340), FZD9 (ENSG00000188763)

Protein

Protein identifiers

Secreted frizzled-related protein 1 — Q8N474 (reviewed: Q8N474)

Alternative names: Secreted apoptosis-related protein 2

All UniProt accessions (2): Q8N474, Q6ZSL4

UniProt curated annotations — full annotation on UniProt →

Function. Soluble frizzled-related proteins (sFRPS) function as modulators of Wnt signaling through direct interaction with Wnts. They have a role in regulating cell growth and differentiation in specific cell types. SFRP1 decreases intracellular beta-catenin levels. Has antiproliferative effects on vascular cells, in vitro and in vivo, and can induce, in vivo, an angiogenic response. In vascular cell cycle, delays the G1 phase and entry into the S phase. In kidney development, inhibits tubule formation and bud growth in metanephroi. Inhibits WNT1/WNT4-mediated TCF-dependent transcription.

Subunit / interactions. Interacts with WNT1, WNT2 and FRZD6. Interacts with WNT4, WNT8 and MYOC.

Subcellular location. Secreted.

Tissue specificity. Widely expressed. Absent from lung, liver and peripheral blood leukocytes. Highest levels in heart and fetal kidney. Also expressed in testis, ovary, fetal brain and lung, leiomyomal cells, myometrial cells and vascular smooth muscle cells. Expressed in foreskin fibroblasts and in keratinocytes.

Domain organisation. The FZ domain is involved in binding with Wnt ligands.

Induction. Down-regulated in colorectal and breast tumors. Up-regulated in uterine leiomyomas under high estrogenic conditions. Expression, in leiomyomal cells, also increased both under hypoxic and serum deprivation conditions.

Miscellaneous. May have therapeutic use in cardiac surgery.

Similarity. Belongs to the secreted frizzled-related protein (sFRP) family.

RefSeq proteins (1): NP_003003* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001134	Netrin_domain	Domain
IPR008993	TIMP-like_OB-fold	Homologous_superfamily
IPR015526	Frizzled/SFRP	Family
IPR018933	Netrin_module_non-TIMP	Domain
IPR020067	Frizzled_dom	Domain
IPR036790	Frizzled_dom_sf	Homologous_superfamily
IPR041760	SFRP1_CRD	Domain

Pfam: PF01392, PF01759

UniProt features (17 total): disulfide bond 8, mutagenesis site 2, sequence conflict 2, domain 2, signal peptide 1, chain 1, glycosylation site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8N474-F1	80.60	0.51

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 (8): 186–256, 189–258, 203–306, 58–121, 68–114, 105–140, 129–166, 133–157

Glycosylation sites (1): 173

Mutagenesis-validated functional residues (2):

Position	Phenotype
173	reduced molecular weight.
263	no effect on molecular weight.

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-201681	TCF dependent signaling in response to WNT
R-HSA-3772470	Negative regulation of TCF-dependent signaling by WNT ligand antagonists
R-HSA-162582	Signal Transduction
R-HSA-195721	Signaling by WNT

MSigDB gene sets: 628 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_UP, GOBP_MYELOID_CELL_DIFFERENTIATION, GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_UP, GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_UP, GOBP_NEGATIVE_REGULATION_OF_EPITHELIAL_CELL_PROLIFERATION, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_HEMATOPOIETIC_PROGENITOR_CELL_DIFFERENTIATION, MODULE_52, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_RESPONSE_TO_IONIZING_RADIATION, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOBP_NEGATIVE_REGULATION_OF_CELL_DEVELOPMENT

GO Biological Process (87): osteoblast differentiation (GO:0001649), ureteric bud development (GO:0001657), neural tube closure (GO:0001843), positive regulation of cell-matrix adhesion (GO:0001954), hematopoietic progenitor cell differentiation (GO:0002244), positive regulation of cell population proliferation (GO:0008284), negative regulation of cell population proliferation (GO:0008285), male gonad development (GO:0008584), female gonad development (GO:0008585), cellular response to starvation (GO:0009267), response to xenobiotic stimulus (GO:0009410), dorsal/ventral axis specification (GO:0009950), regulation of cell cycle process (GO:0010564), negative regulation of gene expression (GO:0010629), negative regulation of epithelial to mesenchymal transition (GO:0010719), regulation of neuron projection development (GO:0010975), neural crest cell fate commitment (GO:0014034), Wnt signaling pathway (GO:0016055), positive regulation of Wnt signaling pathway (GO:0030177), negative regulation of Wnt signaling pathway (GO:0030178), negative regulation of ossification (GO:0030279), positive regulation of cell growth (GO:0030307), negative regulation of cell growth (GO:0030308), osteoclast differentiation (GO:0030316), negative regulation of cell migration (GO:0030336), BMP signaling pathway (GO:0030509), negative regulation of BMP signaling pathway (GO:0030514), negative regulation of osteoblast proliferation (GO:0033689), somatic stem cell population maintenance (GO:0035019), non-canonical Wnt signaling pathway (GO:0035567), positive regulation of apoptotic process (GO:0043065), negative regulation of apoptotic process (GO:0043066), negative regulation of B cell differentiation (GO:0045578), positive regulation of fat cell differentiation (GO:0045600), negative regulation of osteoblast differentiation (GO:0045668), negative regulation of osteoclast differentiation (GO:0045671), regulation of angiogenesis (GO:0045765), positive regulation of smoothened signaling pathway (GO:0045880), negative regulation of DNA-templated transcription (GO:0045892), positive regulation of DNA-templated transcription (GO:0045893)

GO Molecular Function (6): cysteine-type endopeptidase activity (GO:0004197), frizzled binding (GO:0005109), heparin binding (GO:0008201), Wnt-protein binding (GO:0017147), identical protein binding (GO:0042802), protein binding (GO:0005515)

GO Cellular Component (7): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), cytosol (GO:0005829), plasma membrane (GO:0005886), cell surface (GO:0009986), extracellular matrix (GO:0031012), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Signaling by WNT	1
TCF dependent signaling in response to WNT	1
Signal Transduction	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
cell differentiation	2
cell population proliferation	2
regulation of cell population proliferation	2
gonad development	2
Wnt signaling pathway	2
regulation of Wnt signaling pathway	2
protein binding	2
ossification	1
mesonephric tubule development	1
primary neural tube formation	1
tube closure	1
regulation of cell-matrix adhesion	1
cell-matrix adhesion	1
positive regulation of cell-substrate adhesion	1
hemopoiesis	1
positive regulation of cellular process	1
negative regulation of cellular process	1
development of primary male sexual characteristics	1
development of primary female sexual characteristics	1
cellular response to nutrient levels	1
cellular response to stress	1
response to starvation	1
response to chemical	1
axis specification	1
dorsal/ventral pattern formation	1
cell cycle process	1
regulation of cell cycle	1
gene expression	1
regulation of gene expression	1
negative regulation of macromolecule biosynthetic process	1
epithelial to mesenchymal transition	1
regulation of epithelial to mesenchymal transition	1
negative regulation of cell differentiation	1
negative regulation of multicellular organismal process	1
neuron projection development	1
regulation of plasma membrane bounded cell projection organization	1
neural crest formation	1
neural crest cell differentiation	1
stem cell fate commitment	1

Protein interactions and networks

STRING

2474 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SFRP1	TNFSF11	O14788	925
SFRP1	WIF1	Q9Y5W5	920
SFRP1	WNT1	P04628	915
SFRP1	WNT7B	P56706	875
SFRP1	DKK1	O94907	874
SFRP1	CTNNB1	P35222	871
SFRP1	WNT5A	P41221	869
SFRP1	LRP5	O75197	848
SFRP1	DKK2	Q9UBU2	829
SFRP1	LRP6	O75581	826
SFRP1	FZD2	Q14332	825
SFRP1	WNT8B	Q93098	801
SFRP1	WNT3A	P56704	790
SFRP1	DVL1	O14640	772
SFRP1	DKK4	Q9UBT3	772

IntAct

16 interactions, top by confidence:

A	B	Type	Score
SFRP1	TMEM86B	psi-mi:“MI:0915”(physical association)	0.560
WNT2	SFRP1	psi-mi:“MI:0915”(physical association)	0.400
SFRP1	SFRP1	psi-mi:“MI:0915”(physical association)	0.400
FZD6	SFRP1	psi-mi:“MI:0915”(physical association)	0.400
SFRP1	FZD6	psi-mi:“MI:0915”(physical association)	0.400
SFRP1	NHSL3	psi-mi:“MI:0915”(physical association)	0.370
EBNA1	IGF2BP3	psi-mi:“MI:0914”(association)	0.350
E7	COPE	psi-mi:“MI:0914”(association)	0.350
APP	ESYT2	psi-mi:“MI:0914”(association)	0.350
MAPT	SHTN1	psi-mi:“MI:0914”(association)	0.350
SFRP1	TMEM86B	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (26): SFRP1 (Two-hybrid), SFRP1 (Reconstituted Complex), SFRP1 (Affinity Capture-Western), SFRP1 (Affinity Capture-Western), SFRP1 (Affinity Capture-Western), TMEM86B (Two-hybrid), SFRP1 (Affinity Capture-Western), SFRP1 (Affinity Capture-Western), SFRP1 (Affinity Capture-Western), FZD6 (Affinity Capture-Western), SFRP1 (Proximity Label-MS), WNT4 (Reconstituted Complex), SFRP1 (Affinity Capture-MS), SFRP1 (Affinity Capture-MS), DNMT1 (Co-localization)

ESM2 similar proteins: A2AFS3, B1AXV0, D0PRN2, D3ZE85, D4ABL6, E9PV86, M0R7X9, M0RAS4, O19116, O42224, O54951, O60243, O70141, P0DI97, P58400, Q00961, Q01098, Q13507, Q13635, Q14957, Q28142, Q3ZBS2, Q4R766, Q5E9M6, Q5RF67, Q61200, Q63366, Q63373, Q6DN14, Q6NW40, Q76LW2, Q7TNR6, Q7Z5A7, Q8C4U3, Q8N2K0, Q8N474, Q8NBT3, Q8WXS5, Q90693, Q91WE9

Diamond homologs: A0A0K3AWM6, B3DIG4, G5ECQ2, O00144, O19116, O42579, O57328, O57329, O60353, O70421, O75084, O93274, P18537, P58421, P97299, P97401, Q08463, Q08464, Q13467, Q14332, Q24760, Q498S8, Q5BL72, Q5RCN4, Q5RF67, Q5T4F7, Q61086, Q61088, Q61089, Q61090, Q61091, Q6FHJ7, Q7YRN1, Q80YN4, Q863H1, Q8AVJ9, Q8BKG4, Q8C4U3, Q8CHL0, Q8K4C8

SIGNOR signaling

6 interactions.

A	Effect	B	Mechanism
SFRP1	down-regulates	WNT4	binding
MYC	“down-regulates quantity by repression”	SFRP1	“transcriptional regulation”
SFRP1	down-regulates	Wnt	binding
hsa-miR-582-3p	“down-regulates quantity by repression”	SFRP1	“post transcriptional regulation”
SFRP1	down-regulates	WNT1	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	27
Likely benign	1
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

788 predictions. Top by Δscore:

Variant	Effect	Δscore
8:41265485:CAGTG:C	acceptor_gain	1.0000
8:41265488:TG:T	acceptor_gain	1.0000
8:41265496:A:AC	acceptor_gain	1.0000
8:41265496:A:C	acceptor_gain	1.0000
8:41308610:CCTTA:C	donor_loss	1.0000
8:41308611:CTTA:C	donor_loss	1.0000
8:41308612:TTACC:T	donor_loss	1.0000
8:41308613:TACCT:T	donor_loss	1.0000
8:41308614:ACCTT:A	donor_loss	1.0000
8:41308615:C:CG	donor_loss	1.0000
8:41265486:AGTG:A	acceptor_gain	0.9900
8:41265489:GC:G	acceptor_loss	0.9900
8:41265490:C:CA	acceptor_loss	0.9900
8:41265490:C:CC	acceptor_gain	0.9900
8:41265491:T:G	acceptor_loss	0.9900
8:41265506:C:CT	acceptor_gain	0.9900
8:41303460:CCAAA:C	donor_gain	0.9900
8:41308614:A:AC	donor_gain	0.9900
8:41308615:C:CC	donor_gain	0.9900
8:41265487:GTG:G	acceptor_gain	0.9800
8:41265507:A:T	acceptor_gain	0.9800
8:41275117:A:AC	donor_gain	0.9600
8:41303459:A:AC	donor_gain	0.9600
8:41303460:C:CC	donor_gain	0.9600
8:41303537:GCCTG:G	acceptor_loss	0.9600
8:41303539:C:CA	acceptor_loss	0.9600
8:41303539:C:CC	acceptor_gain	0.9600
8:41303540:T:A	acceptor_loss	0.9600
8:41308614:AC:A	donor_gain	0.9500
8:41308615:CC:C	donor_gain	0.9500

AlphaMissense

2095 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:41265339:C:T	C258Y	1.000
8:41265340:A:G	C258R	1.000
8:41303475:C:G	C203S	1.000
8:41303476:A:T	C203S	1.000
8:41303517:C:T	C189Y	1.000
8:41303527:A:G	C186R	1.000
8:41308662:G:C	C166W	1.000
8:41308663:C:T	C166Y	1.000
8:41308664:A:G	C166R	1.000
8:41308690:C:G	C157S	1.000
8:41308690:C:T	C157Y	1.000
8:41308691:A:G	C157R	1.000
8:41308691:A:T	C157S	1.000
8:41308707:C:A	W151C	1.000
8:41308707:C:G	W151C	1.000
8:41308709:A:G	W151R	1.000
8:41308709:A:T	W151R	1.000
8:41308740:G:C	C140W	1.000
8:41308741:C:A	C140F	1.000
8:41308741:C:G	C140S	1.000
8:41308741:C:T	C140Y	1.000
8:41308742:A:G	C140R	1.000
8:41308742:A:T	C140S	1.000
8:41308750:C:G	R137P	1.000
8:41308761:G:C	C133W	1.000
8:41308762:C:A	C133F	1.000
8:41308762:C:G	C133S	1.000
8:41308762:C:T	C133Y	1.000
8:41308763:A:G	C133R	1.000
8:41308763:A:T	C133S	1.000

dbSNP variants (sampled 300 via entrez): RS1000015705 (8:41271879 A>G), RS1000077658 (8:41281917 A>G), RS1000132818 (8:41304110 G>A,C), RS1000167215 (8:41303031 C>A,G), RS1000179079 (8:41265598 T>G), RS1000277666 (8:41287002 G>A), RS1000455770 (8:41298308 T>C), RS1000505265 (8:41261615 A>G), RS1000593953 (8:41267058 G>A,C), RS1000602993 (8:41305133 A>C), RS1000612128 (8:41277258 A>T), RS1000672119 (8:41265790 G>A), RS1000728968 (8:41297685 G>A,T), RS1000762252 (8:41299683 A>T), RS1000786950 (8:41302798 C>G,T)

Disease associations

OMIM: gene MIM:604156 | 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
GCST005025_26	Anti-saccade response	5.000000e-06
GCST006585_2691	Blood protein levels	2.000000e-06
GCST007160_19	Refractive astigmatism	8.000000e-06
GCST010796_890	Electrocardiogram morphology (amplitude at temporal datapoints)	1.000000e-09
GCST010796_891	Electrocardiogram morphology (amplitude at temporal datapoints)	2.000000e-09
GCST011358_6	Academic attainment (English)	8.000000e-06
GCST90000025_355	Appendicular lean mass	1.000000e-09

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0006874	antisaccade response measurement
EFO:0004327	electrocardiography
EFO:0011015	educational attainment
EFO:0004980	appendicular lean mass

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5517 (SINGLE PROTEIN)

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

ChEMBL bioactivities

119 potent at pChembl≥5 of 119 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.70	IC50	20	nM	CHEMBL455476
7.70	IC50	20	nM	CHEMBL503825
7.70	IC50	20	nM	CHEMBL452196
7.70	IC50	20	nM	CHEMBL600850
7.70	IC50	20	nM	CHEMBL592214
7.52	IC50	30	nM	CHEMBL495534
7.52	IC50	30	nM	CHEMBL527086
7.52	IC50	30	nM	CHEMBL501433
7.52	IC50	30	nM	CHEMBL451431
7.52	IC50	30	nM	CHEMBL591301
7.40	IC50	40	nM	CHEMBL500903
7.40	IC50	40	nM	CHEMBL447079
7.40	IC50	40	nM	CHEMBL505036
7.40	IC50	40	nM	CHEMBL503281
7.40	IC50	40	nM	CHEMBL606033
7.40	IC50	40	nM	CHEMBL592670
7.30	IC50	50	nM	CHEMBL507695
7.30	IC50	50	nM	CHEMBL591473
7.30	IC50	50	nM	CHEMBL600050
7.22	IC50	60	nM	CHEMBL449276
7.22	IC50	60	nM	CHEMBL589066
7.22	IC50	60	nM	CHEMBL591482
7.22	IC50	60	nM	CHEMBL603165
7.22	EC50	60	nM	CHEMBL449276
7.16	IC50	70	nM	CHEMBL510748
7.16	IC50	70	nM	CHEMBL454478
7.16	IC50	70	nM	CHEMBL589088
7.16	IC50	70	nM	CHEMBL600049
7.16	EC50	70	nM	CHEMBL606033
7.10	IC50	80	nM	CHEMBL589067
7.10	EC50	80	nM	CHEMBL600050
7.05	IC50	90	nM	CHEMBL525899
7.05	IC50	90	nM	CHEMBL501332
7.05	IC50	90	nM	CHEMBL592455
7.00	IC50	100	nM	CHEMBL523726
7.00	IC50	100	nM	CHEMBL589559
7.00	IC50	100	nM	CHEMBL591035
6.96	IC50	110	nM	CHEMBL495526
6.96	IC50	110	nM	CHEMBL495535
6.96	IC50	110	nM	CHEMBL462363
6.96	IC50	110	nM	CHEMBL605196
6.96	EC50	110	nM	CHEMBL592214
6.92	IC50	120	nM	CHEMBL372397
6.92	IC50	120	nM	CHEMBL496581
6.92	IC50	120	nM	CHEMBL591017
6.92	EC50	120	nM	CHEMBL589067
6.92	IC50	120	nM	CHEMBL591064
6.89	IC50	130	nM	CHEMBL504979
6.89	IC50	130	nM	CHEMBL590478
6.89	IC50	130	nM	CHEMBL589363

PubChem BioAssay actives

119 with measured affinity, of 243 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
(2S)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]-N-tert-butylpyrrolidine-1-carboxamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0200	uM
(2S)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]-N-phenylpyrrolidine-1-carboxamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0200	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(3,3-dimethylbutanoyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0200	uM
3-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidin-1-yl]sulfonylbenzoic acid	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0200	uM
4-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidin-1-yl]sulfonylbenzoic acid	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0200	uM
5-(benzenesulfonyl)-N-[1-(2-imidazol-1-ylacetyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0300	uM
(2S)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]-N-ethylpyrrolidine-1-carboxamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0300	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(3,3-dimethylbutyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0300	uM
(2S)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]-N,N-dimethylpyrrolidine-1-carboxamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0300	uM
5-(benzenesulfonyl)-N-[1-[3-(2H-tetrazol-5-yl)phenyl]sulfonylpiperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0300	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(2,2-dimethylpropanoyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0400	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(morpholine-4-carbonyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0400	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(cyclohexylmethyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0400	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(2-methylpropanoyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0400	uM
5-(benzenesulfonyl)-N-[1-[6-(dimethylamino)pyridine-3-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0400	uM
5-(benzenesulfonyl)-N-[1-[(3S)-pyrrolidine-3-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0400	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(cyclohexanecarbonyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0500	uM
5-(benzenesulfonyl)-2-(trifluoromethyl)-N-[1-[6-(trifluoromethyl)pyridine-3-carbonyl]piperidin-4-yl]benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0500	uM
tert-butyl (3R)-3-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]pyrrolidine-1-carboxylate	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0500	uM
tert-butyl (2S)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]pyrrolidine-1-carboxylate	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0600	uM
5-(benzenesulfonyl)-N-[1-(pyridine-2-carbonyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0600	uM
5-(benzenesulfonyl)-N-[1-[(3R)-pyrrolidine-3-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0600	uM
2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidin-1-yl]acetamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0600	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-benzoylpyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0700	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-(pyridine-4-carbonyl)pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0700	uM
tert-butyl (3S)-3-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]pyrrolidine-1-carboxylate	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0700	uM
5-(benzenesulfonyl)-N-(1-benzoylpiperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0700	uM
5-(benzenesulfonyl)-N-[1-(pyridine-3-carbonyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0800	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-[2-(dimethylamino)acetyl]pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0900	uM
5-(benzenesulfonyl)-N-[1-[(2S)-5-oxopyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.0900	uM
5-(benzenesulfonyl)-N-[1-(3-cyanophenyl)sulfonylpiperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.0900	uM
5-(benzenesulfonyl)-N-[1-(2-morpholin-4-ylacetyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1000	uM
5-(benzenesulfonyl)-N-[1-(2-piperidin-4-ylacetyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1000	uM
3-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidin-1-yl]benzoic acid	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1000	uM
5-(benzenesulfonyl)-N-[1-(6-chloropyridine-3-carbonyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1100	uM
5-(benzenesulfonyl)-N-[1-[(2S)-pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1100	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-[4-(dimethylamino)benzoyl]pyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1100	uM
5-(benzenesulfonyl)-N-[1-(2-pyrrolidin-1-ylacetyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1100	uM
5-(benzenesulfonyl)-N-[1-[(2S)-1-methylpyrrolidine-2-carbonyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1200	uM
tert-butyl (2R)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]pyrrolidine-1-carboxylate	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1200	uM
5-(benzenesulfonyl)-N-[1-(piperidine-4-carbonyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1200	uM
4-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidin-1-yl]benzoic acid	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1200	uM
tert-butyl (2S)-2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidine-1-carbonyl]-5-oxopyrrolidine-1-carboxylate	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1300	uM
5-(benzenesulfonyl)-N-[1-(6-morpholin-4-ylpyridine-3-carbonyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1300	uM
5-(benzenesulfonyl)-N-[1-(benzenesulfonyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1300	uM
5-(benzenesulfonyl)-N-[1-(2-piperazin-1-ylacetyl)piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1400	uM
N-[1-[(2S)-1-acetylpyrrolidine-2-carbonyl]piperidin-4-yl]-5-(benzenesulfonyl)-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.1600	uM
5-(benzenesulfonyl)-N-[1-[4-(dimethylamino)benzoyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	456235: Inhibition of human recombinant SFRP1 expressed in human U2OS cells assessed as increase in Wnt signaling after 16 to 18 hrs by luciferase reporter gene assay	ec50	0.1900	uM
2-[4-[[5-(benzenesulfonyl)-2-(trifluoromethyl)phenyl]sulfonylamino]piperidin-1-yl]acetic acid	456233: Displacement of fluorescence probe compound from human SFRP1 after 30 mins by fluorescence polarization assay	ic50	0.1900	uM
5-(benzenesulfonyl)-N-[1-[2-(methylamino)acetyl]piperidin-4-yl]-2-(trifluoromethyl)benzenesulfonamide	412784: Binding affinity to human purified SARP2 by fluorescent polarization assay	ic50	0.2000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, affects expression, decreases methylation	7
Decitabine	decreases methylation, affects expression, affects methylation, affects cotreatment, increases expression	6
trichostatin A	increases expression, decreases expression, affects cotreatment	4
sodium arsenite	decreases expression, increases expression	3
Air Pollutants	decreases expression, increases abundance, increases expression	3
Silicon Dioxide	decreases expression, increases expression	3
bisphenol A	decreases expression, increases methylation	2
mercuric bromide	decreases expression, affects cotreatment	2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression, decreases expression	2
Arsenic Trioxide	decreases methylation, increases expression	2
Vorinostat	affects cotreatment, decreases expression	2
Panobinostat	affects cotreatment, decreases expression	2
Folic Acid	increases expression, increases methylation, decreases methylation, affects cotreatment	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Polyamines	affects expression, affects methylation, increases expression	2
Tretinoin	increases expression, decreases expression	2
8-Bromo Cyclic Adenosine Monophosphate	increases expression	2
Cadmium Chloride	decreases expression, increases expression	2
p-Chloromercuribenzoic Acid	affects cotreatment, decreases expression	2
sporidesmin	affects reaction, decreases expression	1
methylmercuric chloride	decreases expression	1
cobaltiprotoporphyrin	affects expression, decreases reaction	1
glycidyl methacrylate	decreases expression	1
sodium arsenate	decreases expression, increases abundance	1
mono-(2-ethylhexyl)phthalate	increases abundance, increases methylation	1
boron nitride	decreases expression	1
cobaltous chloride	decreases expression	1
zinc chromate	increases abundance, increases expression	1
manganese chloride	increases abundance, increases expression	1
aflatoxin B2	increases methylation	1

ChEMBL screening assays

18 unique, capped per target: 18 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1011781	Binding	Binding affinity to human purified SARP2 by fluorescent polarization assay	Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides. — J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B2Q1	Abcam A-549 SFRP1 KO	Cancer cell line	Male
CVCL_D1UE	Abcam U-87MG SFRP1 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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