WNT3A
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Summary
WNT3A (Wnt family member 3A, HGNC:15983) is a protein-coding gene on chromosome 1q42.13, encoding Protein Wnt-3a (P56704). Ligand for members of the frizzled family of seven transmembrane receptors.
The WNT gene family consists of structurally related genes which encode secreted signaling proteins. These proteins have been implicated in oncogenesis and in several developmental processes, including regulation of cell fate and patterning during embryogenesis. This gene is a member of the WNT gene family. It encodes a protein which shows 96% amino acid identity to mouse Wnt3A protein, and 84% to human WNT3 protein, another WNT gene product. This gene is clustered with WNT14 gene, another family member, in chromosome 1q42 region.
Source: NCBI Gene 89780 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 182 total
- Phenotypes (HPO): 6
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_033131
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:15983 |
| Approved symbol | WNT3A |
| Name | Wnt family member 3A |
| Location | 1q42.13 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000154342 |
| Ensembl biotype | protein_coding |
| OMIM | 606359 |
| Entrez | 89780 |
Gene structure
Transcript identifiers
Ensembl transcripts: 2 — 2 protein_coding
ENST00000284523, ENST00000948304
RefSeq mRNA: 1 — MANE Select: NM_033131
NM_033131
CCDS: CCDS1564
Canonical transcript exons
ENST00000284523 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001015348 | 228050656 | 228050921 |
| ENSE00001015349 | 228006998 | 228007199 |
| ENSE00001015350 | 228058986 | 228061271 |
| ENSE00002426379 | 228022667 | 228022908 |
Expression profiles
Bgee: expression breadth broad, 31 present calls, max score 86.63.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1885 / max 15.3457, expressed in 98 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 8906 | 0.1885 | 98 |
Top tissues by expression
128 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| placenta | UBERON:0001987 | 86.63 | gold quality |
| right lung | UBERON:0002167 | 68.32 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 67.63 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 62.63 | gold quality |
| lung | UBERON:0002048 | 62.14 | gold quality |
| skin of leg | UBERON:0001511 | 60.02 | gold quality |
| zone of skin | UBERON:0000014 | 59.64 | gold quality |
| skin of abdomen | UBERON:0001416 | 59.15 | gold quality |
| esophagus mucosa | UBERON:0002469 | 56.62 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 55.95 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 53.59 | gold quality |
| minor salivary gland | UBERON:0001830 | 53.16 | gold quality |
| prostate gland | UBERON:0002367 | 53.02 | gold quality |
| vagina | UBERON:0000996 | 48.41 | gold quality |
| tonsil | UBERON:0002372 | 46.94 | silver quality |
| bone marrow cell | CL:0002092 | 43.82 | gold quality |
| colonic epithelium | UBERON:0000397 | 41.59 | gold quality |
| esophagus | UBERON:0001043 | 40.36 | gold quality |
| stromal cell of endometrium | CL:0002255 | 40.11 | gold quality |
| sural nerve | UBERON:0015488 | 39.63 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 39.26 | silver quality |
| fallopian tube | UBERON:0003889 | 37.40 | gold quality |
| uterine cervix | UBERON:0000002 | 36.81 | gold quality |
| bone marrow | UBERON:0002371 | 36.75 | gold quality |
| right uterine tube | UBERON:0001302 | 36.63 | silver quality |
| ventricular zone | UBERON:0003053 | 36.48 | gold quality |
| cortical plate | UBERON:0005343 | 36.47 | gold quality |
| ectocervix | UBERON:0012249 | 36.40 | gold quality |
| cortex of kidney | UBERON:0001225 | 35.59 | gold quality |
| granulocyte | CL:0000094 | 35.55 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.43 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
4 targets.
| Target | Regulation |
|---|---|
| AXIN2 | Activation |
| CACNA1G | Activation |
| LEF1 | Repression |
| TERT | Activation |
Upstream regulators (CollecTRI, top): ERG, FOXQ1, HNF1B, HNF4A, KDM5B, MSGN1, MSX2, SMAD1, STAT3, TBX6
miRNA regulators (miRDB)
72 targeting WNT3A, 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-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-9985 | 99.98 | 72.11 | 2939 |
| HSA-MIR-103A-3P | 99.98 | 69.14 | 1595 |
| HSA-MIR-107 | 99.98 | 69.14 | 1595 |
| HSA-MIR-548AA | 99.96 | 70.64 | 3753 |
| HSA-MIR-548AP-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-548T-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-128-3P | 99.95 | 71.17 | 2484 |
| HSA-MIR-216A-3P | 99.95 | 71.19 | 2505 |
| HSA-MIR-185-3P | 99.95 | 67.01 | 1743 |
| HSA-MIR-497-5P | 99.92 | 71.83 | 2674 |
| HSA-MIR-15A-5P | 99.90 | 72.80 | 2787 |
| HSA-MIR-15B-5P | 99.90 | 72.78 | 2798 |
| HSA-MIR-16-5P | 99.90 | 72.80 | 2780 |
| HSA-MIR-195-5P | 99.90 | 72.81 | 2805 |
| HSA-MIR-424-5P | 99.89 | 71.90 | 2641 |
| HSA-MIR-6838-5P | 99.89 | 71.94 | 2690 |
| HSA-MIR-3681-3P | 99.88 | 70.46 | 2254 |
| HSA-MIR-6857-5P | 99.87 | 65.32 | 985 |
| HSA-MIR-4492 | 99.87 | 68.25 | 3611 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-1321 | 99.84 | 65.30 | 1811 |
| HSA-MIR-4756-5P | 99.84 | 64.98 | 1809 |
| HSA-MIR-4739 | 99.84 | 65.25 | 1832 |
| HSA-MIR-765 | 99.84 | 68.24 | 2442 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-6763-5P | 99.76 | 64.68 | 1767 |
| HSA-MIR-6764-5P | 99.75 | 67.89 | 2304 |
| HSA-MIR-11181-3P | 99.75 | 66.38 | 2205 |
Literature-anchored findings (GeneRIF, showing 40)
- Regulation of WNT3 and WNT3A mRNAs in human cancer cell lines NT2, MCF-7, and MKN45 (PMID:11788904)
- Clustered with WNT14 on 1q42. (PMID:11836627)
- wnt3a-beta catenin signaling regulates LEF-1 gene expression (PMID:12052822)
- CKI epsilon-dependent phosphorylation of Dvl enhances the formation of a complex of Dvl-1 with Frat-1 and this complex leads to the activation of Wnt-3a-induced accumulation of beta-catenin (PMID:12556519)
- These results suggest that Wnt responsiveness is a stage-specific phenomenon in B-cell development and that the morphological changes associated with Wnt signaling may play a role in the motility and metastatic potential of myeloma cells. (PMID:12629517)
- Results suggest that disabled-2 functions as a negative regulator of canonical Wnt signaling by stabilizing the beta-catenin degradation complex. (PMID:12805222)
- Wnt3a may stimulate a cellular phosphatase to dephosphorylate and activate CKIepsilon (PMID:14722104)
- Wnt/beta-catenin pathway activation by Wnt3a raised beta-catenin in monocytes & decreased migration thru a dermal microvascular endothelial cell layer. This was associated with specific monocyte adherence to endothelial cells after Wnt3a exposure. (PMID:16565323)
- BMP-2 antagonizes Wnt-3a signaling in osteoblast progenitors by promoting an interaction between Smad1 and Dvl-1 that restricts beta-catenin activation (PMID:16621789)
- ILK activity can modulate acute Wnt3a mediated beta-catenin phosphorylation, stabilization and nuclear activation in a PI3K-independent manner. (PMID:16799642)
- Wnt-LRP5 signalling may play a role in the adaptation of bone to mechanical load in humans, and may explain some gender-related differences in bone mass (PMID:17137849)
- Over-expression of the Wnt3a gene significantly enhances the ability of fibroblast feeder cells to support the undifferentiated growth of 3 different human embryonic stem cell lines. (PMID:17211448)
- Wnt3A/5A can function as mesenchymal regulatory factors by providing instructive cues for the recruitment, maintenance, and differentiation of mesenchymal stem cells. (PMID:17458904)
- Wnt3A treatment significantly activated human hepatic stellate cells, while this was inhibited in secreted frizzled-related protein 1 (sFRP1) overexpressing cells. (PMID:17544413)
- These results suggest that Wnt signaling crosstalk and functional antagonism with the LRP5 co-receptor are key signaling regulators of mesenchymal stem cells maintenance and differentiation. (PMID:17546602)
- Blockade of Wnt3a stimulation of IP(5) generation blocks beta-catenin accumulation (PMID:17595165)
- Results identify a novel feedback mechanism by which Wnt, including Wnt3a, negatively regulates LRP6 at the mRNA level. (PMID:17698587)
- These findings demonstrate a requirement of Wnt signaling for maintenance, proliferation, and survival of NP when cultured in neurosphere conditions. (PMID:17822920)
- Wnt3a markedly reduced the forskolin-induced expression of RANKL, a target gene of PTH/cAMP/PKA. (PMID:17990294)
- Our results suggest that Wnt/beta-catenin signaling plays important roles in human fetal skin development and homeostasis, which also provide new insights on the molecular mechanisms of oncogenesis in human epidermis. (PMID:18242164)
- bone marrow sera from 21 multiple myeloma patients significantly suppressed Wnt3a-induced OPG expression and enhanced RANKL expression in osteoblasts in a DKK1-dependent manner (PMID:18305214)
- effect of Wnt3a on bone disease and growth of multiple myeloma cells in vitro and in vivo (PMID:18344425)
- study demonstrated that Wnt3a & Wnt5a can promote proliferation of HEK293 cells & inhibit serum starvation-induced apoptosis, which implies Wnt3a & Wnt5a can maintain survival of HEK293 cells under stress (PMID:18462958)
- FGF antagonizes Wnt signaling by inhibiting Wnt-induced transcription and suggest that multiple mechanisms, including downregulation of TCFs and Wnt receptors, contribute to this effect. (PMID:18505824)
- glutamine synthetase has a role in control of glutamate signalling through Wnt3A and steroid pathways in osteoblastic cells (PMID:18555765)
- both Wnt5a and Wnt3a bound Ror2, only Wnt5a induced Ror2 homo-dimerization and tyrosine phosphorylation in U2OS human osteoblastic cells. (PMID:18615587)
- Wnt3a and Wnt5a have roles in inducing BMP-4 and 6 expression in prostate cancer osteoblast differentiation (PMID:18632632)
- essential role of Wnt3a in hepatocyte differentiation from hESCs; Wnt3a facilitates clonal plating of hESCs exhibiting functional hepatic differentiation (PMID:18719101)
- the frequent loss of stromal TGF-beta type II receptor expression in prostate cancer can relieve the paracrine suppression of Wnt3a expression (PMID:18724388)
- These findings suggest that WNT3A can mediate transcriptional changes in melanoma cells in a manner reminiscent of the known role of Wnt/beta-catenin signaling in normal melanocyte development. (PMID:19144919)
- Our study reveals an unappreciated role for noncanonical Wnt signaling in hESC specification that involves development of unique mesoderm precursors via morphogenic organization within human EBs. (PMID:19265664)
- The presence of WNT3a completely prevents normal adipocyte differentaiton. (PMID:19351711)
- Wnt3a induces canonical and non-canonical Wnt signaling in HUVECs, and stimulates their proliferation and migration. (PMID:19523451)
- Data show that mutated GPC3 lacking the GPI anchoring domain (sGPC3) significantly inhibited the in vivo growth, blocked Wnt signaling and Erk1/2 and Akt phosphorylation in tumors. (PMID:19816934)
- Wnt3A treatment greatly enhanced the effect of LRP6 on T-cell factor/lymphoid enhance factor luciferase activity in human mammary epithelial cells (PMID:19881541)
- Wnt-3A may activate canonical Wnt signaling and PI3K/AKT through distinct receptors. (PMID:19887570)
- Data demonstrate that the Wnt-beta-catenin signaling pathway is functional in platelets, and that a Wnt3a ligand inhibits platelet adhesion, activation, dense granule secretion, and aggregation. (PMID:19901330)
- Wnt/beta-catenin pathway activation might upregulate DIXDC1 through a post-translational mechanism by inhibiting the ubiquitin-mediated degradation of the DIXDC1 protein. (PMID:20085589)
- analysis of the frizzled8.Wnt3a.LRP6 signaling complex reveals multiple Wnt and Dkk1 binding sites on LRP6 (PMID:20093360)
- Loss of CYLD instigates tumor growth in human cylindromatosis through a mechanism in which hyperubiquitination of polymerized Dvl drives enhancement of Wnt3/beta-catenin responses. (PMID:20227366)
Cross-species orthologs
9 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | wnt3a | ENSDARG00000058822 |
| mus_musculus | Wnt3a | ENSMUSG00000009900 |
| rattus_norvegicus | Wnt3a | ENSRNOG00000003039 |
| drosophila_melanogaster | Wnt2 | FBGN0004360 |
| drosophila_melanogaster | Wnt5 | FBGN0010194 |
| drosophila_melanogaster | Wnt10 | FBGN0031903 |
| caenorhabditis_elegans | WBGENE00000857 | |
| caenorhabditis_elegans | WBGENE00000858 | |
| caenorhabditis_elegans | lin-44 | WBGENE00003029 |
Paralogs (18): WNT16 (ENSG00000002745), WNT8A (ENSG00000061492), WNT8B (ENSG00000075290), WNT11 (ENSG00000085741), WNT2 (ENSG00000105989), WNT3 (ENSG00000108379), WNT5B (ENSG00000111186), WNT5A (ENSG00000114251), WNT6 (ENSG00000115596), WNT1 (ENSG00000125084), WNT2B (ENSG00000134245), WNT10A (ENSG00000135925), WNT9A (ENSG00000143816), WNT7A (ENSG00000154764), WNT9B (ENSG00000158955), WNT4 (ENSG00000162552), WNT10B (ENSG00000169884), WNT7B (ENSG00000188064)
Protein
Protein identifiers
Protein Wnt-3a — P56704 (reviewed: P56704)
All UniProt accessions (1): P56704
UniProt curated annotations — full annotation on UniProt →
Function. Ligand for members of the frizzled family of seven transmembrane receptors. Functions in the canonical Wnt signaling pathway that results in activation of transcription factors of the TCF/LEF family. Required for normal embryonic mesoderm development and formation of caudal somites. Required for normal morphogenesis of the developing neural tube. Mediates self-renewal of the stem cells at the bottom on intestinal crypts (in vitro).
Subunit / interactions. Forms a soluble 1:1 complex with AFM; this prevents oligomerization and is required for prolonged biological activity. The complex with AFM may represent the physiological form in body fluids. Homooligomer; disulfide-linked, leading to inactivation. Interacts with PORCN. Interacts with APCDD1 and WLS. Component of the Wnt-Fzd-LRP5-LRP6 signaling complex that contains a WNT protein, a FZD protein and LRP5 or LRP6. Interacts directly in the complex with LRP6. Interacts with glypican GPC3. Interacts with PKD1 (via extracellular domain). Interacts with FZD5.
Subcellular location. Secreted. Extracellular space. Extracellular matrix.
Tissue specificity. Moderately expressed in placenta and at low levels in adult lung, spleen, and prostate.
Post-translational modifications. Palmitoleoylation by PORCN is required for efficient binding to frizzled receptors. Palmitoleoylation is required for proper trafficking to cell surface, vacuolar acidification is critical to release palmitoleoylated WNT3A from WLS in secretory vesicles. Depalmitoleoylated by NOTUM, leading to inhibit Wnt signaling pathway, possibly by promoting disulfide bond formation and oligomerization. Proteolytic processing by TIKI1 and TIKI2 promotes oxidation and formation of large disulfide-bond oligomers, leading to inactivation of WNT3A. Disulfide bonds have critical and distinct roles in secretion and activity. Loss of each conserved cysteine in WNT3A results in high molecular weight oxidized Wnt oligomers, which are formed through inter-Wnt disulfide bonding.
Similarity. Belongs to the Wnt family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P56704-1 | 1 | yes |
| P56704-2 | 2 |
RefSeq proteins (1): NP_149122* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR005817 | Wnt | Family |
| IPR009141 | Wnt3 | Family |
| IPR018161 | Wnt_CS | Conserved_site |
| IPR043158 | Wnt_C | Homologous_superfamily |
Pfam: PF00110
UniProt features (59 total): strand 18, helix 12, disulfide bond 11, mutagenesis site 7, turn 4, glycosylation site 2, signal peptide 1, chain 1, splice variant 1, site 1, lipid moiety-binding region 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7DRT | ELECTRON MICROSCOPY | 2.2 |
| 7URD | ELECTRON MICROSCOPY | 2.92 |
| 7URE | ELECTRON MICROSCOPY | 3.19 |
| 8TZR | ELECTRON MICROSCOPY | 3.5 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P56704-F1 | 88.62 | 0.77 |
Antibody-complex structures (SAbDab): 2 — 7URD, 7URE
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1): 26–27 (cleavage; by tiki1 and tiki2)
Post-translational modifications (1): 209
Disulfide bonds (11): 205–212, 281–312, 297–307, 311–351, 327–342, 329–339, 334–335, 77–88, 128–136, 138–155, 203–217
Glycosylation sites (2): 87, 298
Mutagenesis-validated functional residues (7):
| Position | Phenotype |
|---|---|
| 87 | strongly reduced ability to stimulate wnt-responsive reporters; when associated with q-298. |
| 209 | abrogates wls binding. |
| 209 | complete loss of palmitoleoylation. |
| 209 | no effect on palmitoleoylation and secretion; the threonine can functionally replace the serine. |
| 298 | strongly reduced ability to stimulate wnt-responsive reporters; when associated with q-87. |
| 334 | no signaling activity despite the presence of significant amounts of secreted monomeric wnt3a, exhibits dominant negativ |
| 335 | no signaling activity despite the presence of significant amounts of secreted monomeric wnt3a, exhibits dominant negativ |
Function
Pathways and Gene Ontology
Reactome pathways
11 pathways
| ID | Pathway |
|---|---|
| R-HSA-201681 | TCF dependent signaling in response to WNT |
| R-HSA-3238698 | WNT ligand biogenesis and trafficking |
| R-HSA-373080 | Class B/2 (Secretin family receptors) |
| R-HSA-3772470 | Negative regulation of TCF-dependent signaling by WNT ligand antagonists |
| R-HSA-4641262 | Disassembly of the destruction complex and recruitment of AXIN to the membrane |
| R-HSA-4641263 | Regulation of FZD by ubiquitination |
| R-HSA-5340588 | Signaling by RNF43 mutants |
| R-HSA-9793380 | Formation of paraxial mesoderm |
| R-HSA-9832991 | Formation of the posterior neural plate |
| R-HSA-9834899 | Specification of the neural plate border |
| R-HSA-9856649 | Transcriptional and post-translational regulation of MITF-M expression and activity |
MSigDB gene sets: 490 (showing top):
GOBP_SPINAL_CORD_DEVELOPMENT, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_REGULATION_OF_HEPATOCYTE_PROLIFERATION, MODULE_92, GOBP_REGULATION_OF_LEUKOCYTE_PROLIFERATION, GOBP_HEPATICOBILIARY_SYSTEM_DEVELOPMENT, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOBP_NEGATIVE_REGULATION_OF_CELL_DEVELOPMENT, GOBP_REGULATION_OF_COLLATERAL_SPROUTING, GOBP_NEGATIVE_REGULATION_OF_NEURON_DIFFERENTIATION, GOBP_REGULATION_OF_SKELETAL_MUSCLE_TISSUE_DEVELOPMENT, GOBP_MUSCLE_TISSUE_DEVELOPMENT
GO Biological Process (81): osteoblast differentiation (GO:0001649), in utero embryonic development (GO:0001701), positive regulation of cytokine production (GO:0001819), heart looping (GO:0001947), positive regulation of receptor internalization (GO:0002092), transcription by RNA polymerase II (GO:0006366), axon guidance (GO:0007411), heart development (GO:0007507), intracellular protein localization (GO:0008104), COP9 signalosome assembly (GO:0010387), positive regulation of gene expression (GO:0010628), negative regulation of neuron projection development (GO:0010977), spinal cord association neuron differentiation (GO:0021527), hippocampus development (GO:0021766), cell proliferation in forebrain (GO:0021846), Wnt signaling pathway involved in forebrain neuroblast division (GO:0021874), dorsal/ventral neural tube patterning (GO:0021904), hemopoiesis (GO:0030097), neuron differentiation (GO:0030182), extracellular matrix organization (GO:0030198), mammary gland development (GO:0030879), positive regulation of B cell proliferation (GO:0030890), cell proliferation in midbrain (GO:0033278), non-canonical Wnt signaling pathway (GO:0035567), skeletal muscle cell differentiation (GO:0035914), post-anal tail morphogenesis (GO:0036342), synaptic vesicle recycling (GO:0036465), B cell proliferation (GO:0042100), inner ear morphogenesis (GO:0042472), cell fate commitment (GO:0045165), fat cell differentiation (GO:0045444), myoblast differentiation (GO:0045445), negative regulation of fat cell differentiation (GO:0045599), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944), somatic stem cell division (GO:0048103), positive regulation of mesodermal cell fate specification (GO:0048337), paraxial mesodermal cell fate commitment (GO:0048343), positive regulation of skeletal muscle tissue development (GO:0048643), positive regulation of collateral sprouting in absence of injury (GO:0048697)
GO Molecular Function (9): transcription coactivator activity (GO:0003713), signaling receptor binding (GO:0005102), frizzled binding (GO:0005109), cytokine activity (GO:0005125), protein domain specific binding (GO:0019904), co-receptor binding (GO:0039706), identical protein binding (GO:0042802), receptor ligand activity (GO:0048018), protein binding (GO:0005515)
GO Cellular Component (13): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), endoplasmic reticulum lumen (GO:0005788), Golgi lumen (GO:0005796), plasma membrane (GO:0005886), cell surface (GO:0009986), endocytic vesicle membrane (GO:0030666), early endosome membrane (GO:0031901), extracellular exosome (GO:0070062), presynapse (GO:0098793), glutamatergic synapse (GO:0098978), Wnt-Frizzled-LRP5/6 complex (GO:1990851), synapse (GO:0045202)
Reactome top-level categories
Rollup of top-6 pathways:
| Category | Pathways |
|---|---|
| TCF dependent signaling in response to WNT | 3 |
| Gastrulation | 3 |
| Signaling by WNT | 2 |
| GPCR ligand binding | 1 |
| Signaling by WNT in cancer | 1 |
| MITF-M-regulated melanocyte development | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein binding | 4 |
| cellular anatomical structure | 3 |
| cell differentiation | 2 |
| intracellular organelle lumen | 2 |
| synapse | 2 |
| ossification | 1 |
| chordate embryonic development | 1 |
| cytokine production | 1 |
| regulation of cytokine production | 1 |
| positive regulation of gene expression | 1 |
| positive regulation of multicellular organismal process | 1 |
| embryonic heart tube morphogenesis | 1 |
| determination of heart left/right asymmetry | 1 |
| regulation of receptor internalization | 1 |
| receptor internalization | 1 |
| positive regulation of receptor-mediated endocytosis | 1 |
| DNA-templated transcription | 1 |
| axonogenesis | 1 |
| neuron projection guidance | 1 |
| animal organ development | 1 |
| circulatory system development | 1 |
| macromolecule localization | 1 |
| protein-containing complex assembly | 1 |
| gene expression | 1 |
| regulation of gene expression | 1 |
| positive regulation of macromolecule biosynthetic process | 1 |
| regulation of neuron projection development | 1 |
| neuron projection development | 1 |
| negative regulation of cell projection organization | 1 |
| cell differentiation in spinal cord | 1 |
| dorsal spinal cord development | 1 |
| central nervous system neuron differentiation | 1 |
| pallium development | 1 |
| limbic system development | 1 |
| anatomical structure development | 1 |
| forebrain development | 1 |
| neural precursor cell proliferation | 1 |
| Wnt signaling pathway | 1 |
| forebrain neuroblast division | 1 |
| dorsal/ventral pattern formation | 1 |
Protein interactions and networks
STRING
2818 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| WNT3A | LRP6 | O75581 | 998 |
| WNT3A | LRP5 | O75197 | 998 |
| WNT3A | FZD1 | Q9UP38 | 994 |
| WNT3A | FZD2 | Q14332 | 981 |
| WNT3A | FZD8 | Q9H461 | 954 |
| WNT3A | CTNNB1 | P35222 | 949 |
| WNT3A | APCDD1 | Q8J025 | 949 |
| WNT3A | DVL1 | O14640 | 928 |
| WNT3A | AXIN1 | O15169 | 927 |
| WNT3A | RYK | P34925 | 925 |
| WNT3A | DKK1 | O94907 | 908 |
| WNT3A | WIF1 | Q9Y5W5 | 903 |
| WNT3A | RSPO1 | Q2MKA7 | 901 |
| WNT3A | AXIN2 | Q9Y2T1 | 887 |
| WNT3A | FZD4 | Q9ULV1 | 882 |
IntAct
28 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| WNT3A | WLS | psi-mi:“MI:0915”(physical association) | 0.780 |
| LRP6 | WNT3A | psi-mi:“MI:0407”(direct interaction) | 0.770 |
| WNT3A | LRP6 | psi-mi:“MI:0915”(physical association) | 0.770 |
| WNT3 | WNT3A | psi-mi:“MI:0914”(association) | 0.640 |
| FZD7 | LRP6 | psi-mi:“MI:0914”(association) | 0.620 |
| FZD5 | tcdB | psi-mi:“MI:0915”(physical association) | 0.610 |
| WNT3A | CANX | psi-mi:“MI:0914”(association) | 0.530 |
| APCDD1 | WNT3A | psi-mi:“MI:0915”(physical association) | 0.520 |
| TRABD2B | WNT3A | psi-mi:“MI:0194”(cleavage reaction) | 0.520 |
| FZD7 | TRABD2B | psi-mi:“MI:0914”(association) | 0.520 |
| TRABD2B | FZD7 | psi-mi:“MI:0914”(association) | 0.520 |
| WNT3A | FZD8 | psi-mi:“MI:0915”(physical association) | 0.500 |
| FZD8 | WNT3A | psi-mi:“MI:0914”(association) | 0.500 |
| NOTUM | WNT3A | psi-mi:“MI:0197”(deacetylation reaction) | 0.440 |
| FZD2 | WNT3A | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| WNT3A | AFM | psi-mi:“MI:0915”(physical association) | 0.400 |
| WNT3A | Fzd8 | psi-mi:“MI:0915”(physical association) | 0.400 |
| WNT3A | MANBA | psi-mi:“MI:0914”(association) | 0.350 |
| WNT3A | LRP5 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC22A1 | FNDC10 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (57): CANX (Affinity Capture-MS), HSPA5 (Affinity Capture-MS), WNT3 (Affinity Capture-MS), PPP2R1B (Affinity Capture-MS), PPP2R5D (Affinity Capture-MS), PPP2R5A (Affinity Capture-MS), PPP2R5B (Affinity Capture-MS), PPP2R5E (Affinity Capture-MS), FEM1B (Affinity Capture-MS), PPP2R2D (Affinity Capture-MS), TRAF2 (Affinity Capture-MS), WNT3 (Affinity Capture-MS), PPP2R5A (Affinity Capture-MS), PPP2R5B (Affinity Capture-MS), PPP2R5E (Affinity Capture-MS)
ESM2 similar proteins: A2AIR5, A5D8T8, A6QLN9, O18739, O35217, O35393, O54951, O75077, O75078, O75900, P27467, P28686, P42642, P49641, P56704, Q00961, Q01098, Q08DW9, Q14957, Q1LZB9, Q2TBM7, Q4V7F2, Q5EA46, Q5R890, Q642A6, Q6P988, Q6PCB0, Q6UXF7, Q7TNS7, Q8NCF0, Q8R2Z5, Q8TCU5, Q91XD7, Q96CW9, Q96FT7, Q96HD1, Q96N03, Q9BZ11, Q9ESM2, Q9ESM3
Diamond homologs: A0M8S1, A0M8T2, A1X153, A4D7S0, B2GUT4, O00755, O13267, O15978, O42122, O70283, P04426, P04628, P09544, P09615, P10108, P17553, P21551, P21552, P22724, P22725, P22726, P22727, P24257, P24383, P27467, P28047, P28465, P31285, P31286, P33945, P34888, P34889, P41221, P43446, P47793, P49337, P49338, P49339, P49340, P49893
SIGNOR signaling
26 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| WNT3A | up-regulates | RYK | binding |
| WNT3A | “up-regulates activity” | LRP5 | binding |
| WNT3A | “up-regulates activity” | LRP6 | binding |
| WNT3A | “up-regulates activity” | FZD1 | binding |
| WNT3A | “up-regulates activity” | FZD3 | binding |
| WNT3A | “up-regulates activity” | DVL1 | |
| WNT3A | up-regulates | ALPL | |
| DKK1 | down-regulates | WNT3A | |
| SOST | down-regulates | WNT3A | |
| WNT3A | up-regulates | FZD2 | binding |
| GPC4 | up-regulates | WNT3A | binding |
| WNT3A | up-regulates | FZD8 | binding |
| SOSTDC1 | “down-regulates activity” | WNT3A | |
| WNT3A | “up-regulates activity” | Frizzled | binding |
| PORCN | “up-regulates activity” | WNT3A | palmitoylation |
| WLS | “up-regulates activity” | WNT3A | relocalization |
| WNT3A | “up-regulates quantity by stabilization” | FBN1 | |
| ERG | “up-regulates quantity by expression” | WNT3A | “transcriptional regulation” |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 18 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Class B/2 (Secretin family receptors) | 5 | 79.3× | 9e-08 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| canonical Wnt signaling pathway | 7 | 71.5× | 5e-10 |
| Wnt signaling pathway | 6 | 39.9× | 4e-07 |
| neuron differentiation | 5 | 33.4× | 1e-05 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
182 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 113 |
| Likely benign | 60 |
| Benign | 7 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1023 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:228022906:AAGG:A | donor_loss | 1.0000 |
| 1:228022907:AGG:A | donor_loss | 1.0000 |
| 1:228022908:GGTA:G | donor_loss | 1.0000 |
| 1:228022909:GTAT:G | donor_loss | 1.0000 |
| 1:228022910:T:G | donor_loss | 1.0000 |
| 1:228050919:CAGG:C | donor_loss | 1.0000 |
| 1:228050921:GGTA:G | donor_loss | 1.0000 |
| 1:228050922:G:C | donor_loss | 1.0000 |
| 1:228050923:T:A | donor_loss | 1.0000 |
| 1:228007197:GTG:G | donor_gain | 0.9900 |
| 1:228007200:GT:G | donor_loss | 0.9900 |
| 1:228007202:G:GT | donor_loss | 0.9900 |
| 1:228007204:G:GG | donor_gain | 0.9900 |
| 1:228022661:CTGCA:C | acceptor_loss | 0.9900 |
| 1:228022662:TGCA:T | acceptor_loss | 0.9900 |
| 1:228022663:GCAG:G | acceptor_loss | 0.9900 |
| 1:228022664:CAGG:C | acceptor_loss | 0.9900 |
| 1:228022665:A:AG | acceptor_gain | 0.9900 |
| 1:228022666:G:GG | acceptor_gain | 0.9900 |
| 1:228050651:TACA:T | acceptor_loss | 0.9900 |
| 1:228050654:A:AG | acceptor_gain | 0.9900 |
| 1:228050655:G:GA | acceptor_gain | 0.9900 |
| 1:228050655:GCT:G | acceptor_gain | 0.9900 |
| 1:228007195:TGGTG:T | donor_gain | 0.9800 |
| 1:228007196:GGTGG:G | donor_gain | 0.9800 |
| 1:228007200:G:GG | donor_gain | 0.9800 |
| 1:228007203:A:AG | donor_gain | 0.9800 |
| 1:228016775:TGG:T | donor_gain | 0.9800 |
| 1:228022666:GGTC:G | acceptor_gain | 0.9800 |
| 1:228050651:TACAG:T | acceptor_gain | 0.9800 |
AlphaMissense
2306 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 1:228022762:G:A | C56Y | 1.000 |
| 1:228022824:T:A | C77S | 1.000 |
| 1:228022825:G:C | C77S | 1.000 |
| 1:228022826:C:G | C77W | 1.000 |
| 1:228022851:T:A | W86R | 1.000 |
| 1:228022851:T:C | W86R | 1.000 |
| 1:228022853:G:C | W86C | 1.000 |
| 1:228022853:G:T | W86C | 1.000 |
| 1:228022858:G:A | C88Y | 1.000 |
| 1:228022859:C:G | C88W | 1.000 |
| 1:228050682:G:C | A114P | 1.000 |
| 1:228050798:G:C | W152C | 1.000 |
| 1:228050798:G:T | W152C | 1.000 |
| 1:228050848:T:G | F169C | 1.000 |
| 1:228050903:C:A | N187K | 1.000 |
| 1:228050903:C:G | N187K | 1.000 |
| 1:228050913:G:T | G191W | 1.000 |
| 1:228059245:T:G | F280C | 1.000 |
| 1:228059247:T:A | C281S | 1.000 |
| 1:228059248:G:A | C281Y | 1.000 |
| 1:228059248:G:C | C281S | 1.000 |
| 1:228059295:T:A | C297S | 1.000 |
| 1:228059296:G:C | C297S | 1.000 |
| 1:228022719:T:A | C42S | 0.999 |
| 1:228022720:G:C | C42S | 0.999 |
| 1:228022761:T:A | C56S | 0.999 |
| 1:228022761:T:C | C56R | 0.999 |
| 1:228022762:G:C | C56S | 0.999 |
| 1:228022763:C:G | C56W | 0.999 |
| 1:228022800:G:C | G69R | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000026843 (1:228013599 A>T), RS1000066759 (1:228008914 A>G), RS1000182727 (1:228030844 T>C), RS1000276301 (1:228019133 A>T), RS1000366662 (1:228059833 T>A,C,G), RS1000380136 (1:228024885 G>A), RS1000400741 (1:228029983 C>A), RS1000436733 (1:228053273 A>G), RS1000449178 (1:228018869 G>A), RS1000454573 (1:228037021 C>T), RS1000537972 (1:228008072 G>A), RS1000655760 (1:228008130 A>G), RS1000664638 (1:228058937 G>A,C), RS1000699529 (1:228058401 G>A), RS1000716586 (1:228023424 G>A)
Disease associations
OMIM: gene MIM:606359 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
6 total (6 of 6 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000939 | Osteoporosis |
| HP:0001288 | Gait disturbance |
| HP:0002653 | Bone pain |
| HP:0002757 | Recurrent fractures |
| HP:0002808 | Kyphosis |
| HP:0002953 | Vertebral compression fracture |
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004280_9 | Diastolic blood pressure | 2.000000e-16 |
| GCST007930_8 | Medication use (agents acting on the renin-angiotensin system) | 3.000000e-10 |
| GCST008362_97 | Birth weight | 2.000000e-09 |
| GCST008839_18 | Height | 3.000000e-18 |
| GCST90092003_2 | Alcohol-related hepatocellular carcinoma | 1.000000e-08 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006336 | diastolic blood pressure |
| EFO:0009931 | Agents acting on the renin-angiotensin system use measurement |
| EFO:0004344 | birth weight |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL1255137 (SINGLE PROTEIN), CHEMBL6066542 (PROTEIN COMPLEX)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,238 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL3188386 | WNT-974 | 2 | 1,238 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
516 measured of 536 human assays (536 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2-fluoro-5-methyl-4-(2-methylpyridin-4-yl)phenyl)acetamide | IC50 | 0.04 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[5-(3-fluorophenyl)-2-pyridinyl]-2-[6-(2-methyl-4-pyridinyl)-3-pyridinyl]acetamide | IC50 | 0.06 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-(2-methyl-4-pyridinyl)phenyl]-N-(5-pyridin-3-yl-2-pyridinyl)acetamide | IC50 | 0.07 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[6-(2-methyl-4-pyridinyl)-3-pyridinyl]-N-(6-phenylpyridazin-3-yl)acetamide | IC50 | 0.08 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[3-methyl-4-(2-methyl-4-pyridinyl)phenyl]-N-(5-pyridin-2-yl-2-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-pyridazin-4-yl-3-(trifluoromethyl)phenyl]-N-(5-pyridin-2-yl-2-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(pyrazin-2-yl)pyridin-2-yl)-2-(4-(pyridazin-4-yl)-3-(trifluoromethyl)phenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[5-(3-fluorophenyl)-2-pyridinyl]-2-(4-pyridazin-4-ylphenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-(2-methyl-4-pyridinyl)-3-(trifluoromethyl)phenyl]-N-(5-pyridin-2-yl-2-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| Methyl 4-(6-(2-(4-(2-methylpyridin-4-yl)phenyl)acetamido)pyridin-3-yl)piperazine-1-carboxylate | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-(3-methyl-4-pyridazin-4-ylphenyl)-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| methyl 4-[6-[[2-[5-methyl-6-(2-methyl-4-pyridinyl)-3-pyridinyl]acetyl]amino]-3-pyridinyl]piperazine-1-carboxylate | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| methyl 4-[6-[[2-[3-methyl-4-(2-methyl-4-pyridinyl)phenyl]acetyl]amino]-3-pyridinyl]piperazine-1-carboxylate | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-fluoro-4-(2-methylpyridin-4-yl)phenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[5-(4-acetylpiperazin-1-yl)-2-pyridinyl]-2-[3-chloro-4-(2-methyl-4-pyridinyl)phenyl]acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(4-(2-methylpyridin-4-yl)-3-(trifluoromethyl)phenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[3-cyano-4-(2-methyl-4-pyridinyl)phenyl]-N-(6-phenyl-3-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(4-(2-fluoropyridin-4-yl)phenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[3-cyano-4-(2-methyl-4-pyridinyl)phenyl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[3-cyano-4-(2-methyl-4-pyridinyl)phenyl]-N-(6-pyrazin-2-yl-3-pyridinyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-(3-cyano-4-(2-methylpyridin-4-yl)phenyl)-N-(5-(pyridazin-3-yl)pyridin-2-yl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-methoxy-4-(2-methylpyridin-4-yl)phenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-chloro-2’-methyl-2,4’-bipyridin-5-yl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[5-[(3S)-4-acetyl-3-methylpiperazin-1-yl]-2-pyridinyl]-2-[3-cyano-4-(2-methyl-4-pyridinyl)phenyl]acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| propan-2-yl 4-[6-[[2-[5-methyl-6-(2-methyl-4-pyridinyl)-3-pyridinyl]acetyl]amino]-3-pyridinyl]piperazine-1-carboxylate | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2’-methyl-3-(trifluoromethyl)-2,4’-bipyridin-5-yl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2’-fluoro-3-methyl-2,4’-bipyridin-5-yl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-(2’,3-difluoro-2,4’-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-cyano-4-(2-fluoropyridin-4-yl)phenyl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-(3-fluoro-4-(2-fluoropyridin-4-yl)phenyl)-N-(5-(pyridazin-3-yl)pyridin-2-yl)acetamide | IC50 | 0.1 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[6-(3-fluorophenyl)-3-pyridinyl]-2-[4-pyridazin-4-yl-3-(trifluoromethyl)phenyl]acetamide | IC50 | 0.11 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-cyano-4-(2-methylpyridin-4-yl)phenyl)acetamide | IC50 | 0.11 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-(3-methyl-4-pyridazin-4-ylphenyl)-N-(5-pyridin-2-yl-2-pyridinyl)acetamide | IC50 | 0.12 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-(2-methyl-4-pyridinyl)-3-(trifluoromethyl)phenyl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide | IC50 | 0.13 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[5-(3-fluorophenyl)-2-pyridinyl]-2-[5-methyl-6-(2-methyl-4-pyridinyl)-3-pyridinyl]acetamide | IC50 | 0.13 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-(2-methyl-4-pyridinyl)phenyl]-N-(6-phenylpyridazin-3-yl)acetamide | IC50 | 0.14 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-(2-methyl-4-pyridinyl)phenyl]-N-(5-pyridazin-3-yl-2-pyridinyl)acetamide | IC50 | 0.15 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[5-(3-fluorophenyl)-2-pyridinyl]-2-[4-(2-methyl-4-pyridinyl)-3-(trifluoromethyl)phenyl]acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-[6-(3-fluorophenyl)-3-pyridinyl]-2-[6-(2-methyl-4-pyridinyl)-3-pyridinyl]acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-pyridazin-3-yl-2-pyridinyl)-2-[4-pyridazin-4-yl-3-(trifluoromethyl)phenyl]acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(2,3’-bipyridin-6’-yl)-2-(2’,3-dimethyl-2,4’-bipyridin-5-yl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| tert-butyl 4-(6-(2-(4-(2-methylpyridin-4-yl)phenyl)acetamido)pyridin-3-yl)piperazine-1-carboxylate | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-methyl-4-(2-methylpyridin-4-yl)phenyl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| ethyl 4-[6-[[2-[3-methyl-2-(2-methyl-4-pyridinyl)-2H-pyran-5-yl]acetyl]amino]-3-pyridinyl]piperazine-1-carboxylate | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(4-(2-chloropyridin-4-yl)phenyl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-cyano-2’-methyl-2,4’-bipyridin-5-yl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(3-fluoro-2’-methyl-2,4’-bipyridin-5-yl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(4-(2-methylpyrimidin-4-yl)-3-(trifluoromethyl)phenyl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-(2’-fluoro-3-methyl-2,4’-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
| 2-[4-(2-fluoro-4-pyridinyl)phenyl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide | IC50 | 0.2 nM | US-10251893: N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators |
ChEMBL bioactivities
850 potent at pChembl≥5 of 927 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.40 | IC50 | 0.04 | nM | CHEMBL5823795 |
| 10.22 | IC50 | 0.06 | nM | CHEMBL6039603 |
| 10.15 | IC50 | 0.07 | nM | CHEMBL5921303 |
| 10.10 | IC50 | 0.08 | nM | CHEMBL6033847 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5945646 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5937289 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL6018741 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5914153 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL6001502 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL6029730 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5989592 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL4532746 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5898705 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5889799 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5785948 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5955254 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5759987 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5815787 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5846874 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL6042520 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5840741 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5968250 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5761075 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL6056464 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL6001723 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5760694 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL4546441 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5801448 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5839562 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL5810452 |
| 9.96 | IC50 | 0.11 | nM | CHEMBL6019535 |
| 9.96 | IC50 | 0.11 | nM | CHEMBL5822915 |
| 9.92 | IC50 | 0.12 | nM | CHEMBL6055708 |
| 9.89 | IC50 | 0.13 | nM | CHEMBL5995349 |
| 9.89 | IC50 | 0.13 | nM | CHEMBL6052903 |
| 9.85 | IC50 | 0.14 | nM | CHEMBL5874786 |
| 9.82 | IC50 | 0.15 | nM | CHEMBL5798889 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5904878 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5947565 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5910225 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4591963 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5885074 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5960615 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5843321 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5928809 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5787107 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5956303 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL5818081 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL4566038 |
| 9.70 | IC50 | 0.2 | nM | CHEMBL6029645 |
PubChem BioAssay actives
49 with measured affinity, of 92 total; 49 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 |
|---|---|---|---|---|
| 1-(2-ethylphenyl)-3,5-dimethyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0013 | uM |
| 3,5-dimethyl-1-(2-methylphenyl)-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0015 | uM |
| 1-(2-bromophenyl)-5-methyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0023 | uM |
| N-(cyclopropylmethyl)-2-[4-(4-methoxybenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0035 | uM |
| 2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0036 | uM |
| 5-methyl-1-(2-methylphenyl)-N-quinolin-2-yltriazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0041 | uM |
| 8-[3-chloro-5-[4-(1-methylpyrazol-4-yl)phenyl]-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one | 1198342: Inhibition of ligand-induced WNT3A signaling in human PA-1 cells harboring TCF preincubated for 6 hrs before ligand addition measured after 24 hrs by luciferase reporter assay | ic50 | 0.0070 | uM |
| N-(cyclopropylmethyl)-2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0170 | uM |
| 2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-(2-methylpropyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0170 | uM |
| 1-(2-bromophenyl)-3,5-dimethyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0210 | uM |
| 2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-propylacetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0340 | uM |
| 2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0400 | uM |
| 3,5-dimethyl-1-(2-propan-2-ylphenyl)-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0480 | uM |
| 1-(2-bromo-6-fluorophenyl)-3,5-dimethyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0500 | uM |
| 2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(pyridin-2-ylmethyl)acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0520 | uM |
| N-benzyl-2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0650 | uM |
| N-ethyl-2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0700 | uM |
| 2-[4-(trifluoromethyl)phenyl]-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.0780 | uM |
| 1-(2-fluorophenyl)-3,5-dimethyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0870 | uM |
| 1-(2,5-dimethylphenyl)-3,5-dimethyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.0960 | uM |
| 3,5-dimethyl-1-phenyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.1350 | uM |
| 2-[4-(4-fluorobenzoyl)piperidin-1-yl]-N-methyl-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]acetamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.1930 | uM |
| 3-(2-fluorophenyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.3040 | uM |
| 1-(2-chlorophenyl)-3,5-dimethyl-N-quinolin-2-ylpyrazole-4-carboxamide | 1862157: Inhibition of recombinant human Wnt3a in HEK293 cells assessed as Wnt signalling by measuring reduction in relative luminescence units incubated for 24 hrs by luciferase reporter assay | ic50 | 0.3050 | uM |
| 3-(4-fluorophenyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.4830 | uM |
| 3-(3-hydroxyphenyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.8120 | uM |
| N-[(4-oxo-3H-quinazolin-2-yl)methyl]-3-phenyl-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 0.9370 | uM |
| 2-[4-(2-hydroxypropan-2-yl)phenyl]-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.0300 | uM |
| 4-chloro-5-cyano-N-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-2-methoxybenzamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.1000 | uM |
| 2-[4-(trifluoromethoxy)phenyl]-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.2200 | uM |
| 3-(4-hydroxyphenyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.3500 | uM |
| 2-[4-(trifluoromethyl)phenyl]-5,6,7,8-tetrahydro-3H-quinazolin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.4100 | uM |
| 2-[4-(trifluoromethyl)phenyl]-3H-quinazolin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.6700 | uM |
| 2-[4-(trifluoromethyl)phenyl]-3,6,7,8-tetrahydrothiopyrano[3,2-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.7200 | uM |
| N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-3-phenyl-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 1.9200 | uM |
| 2-[4-(trifluoromethyl)phenyl]-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 2.6500 | uM |
| methyl 4-(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)benzoate | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 3.0000 | uM |
| 3-(2-hydroxyphenyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 3.7700 | uM |
| 2-(4-bromophenyl)-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 4.1400 | uM |
| 2-[4-(dimethylamino)phenyl]-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 4.2100 | uM |
| 2-(4-chlorophenyl)-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 4.4300 | uM |
| 2-(4-methylphenyl)-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 4.6300 | uM |
| 2-[4-(trifluoromethyl)phenyl]-4a,5,7,7a-tetrahydro-3H-thieno[3,4-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 5.0400 | uM |
| 2-(4-methoxyphenyl)-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 5.0500 | uM |
| 2-(4-methylsulfonylphenyl)-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 6.2900 | uM |
| 3-(3-fluorophenyl)-N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 6.6100 | uM |
| 2-thiophen-3-yl-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-4-one | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 8.0900 | uM |
| N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-3-pyridin-4-yl-N-(thiophen-2-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 8.2500 | uM |
| N-[(4-oxo-3,5,7,8-tetrahydropyrano[4,3-d]pyrimidin-2-yl)methyl]-3-phenyl-N-(thiophen-3-ylmethyl)propanamide | 768543: Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin | ic50 | 8.5400 | uM |
CTD chemical–gene interactions
45 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Niclosamide | affects localization, decreases reaction, increases stability, decreases expression | 3 |
| Chir 99021 | affects cotreatment, decreases expression, increases expression, increases reaction, affects binding | 2 |
| XAV939 | decreases expression, increases expression, decreases reaction, affects binding, affects cotreatment | 2 |
| Cadmium | decreases expression, decreases reaction, increases abundance | 2 |
| Silicon Dioxide | decreases expression | 2 |
| abemaciclib | decreases expression | 1 |
| ETC-159 | decreases expression | 1 |
| aminomethylphosphonic acid (AMPA) | decreases expression | 1 |
| thymoquinone | decreases expression | 1 |
| baicalein | decreases expression, decreases reaction | 1 |
| bisphenol A | affects expression | 1 |
| ethyl-p-hydroxybenzoate | increases expression | 1 |
| 11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid | affects methylation, increases abundance | 1 |
| cypermethrin | increases expression | 1 |
| cyfluthrin | increases expression | 1 |
| N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide | decreases reaction, increases expression | 1 |
| taraxasterol | increases expression, decreases reaction | 1 |
| deguelin | decreases expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | increases expression, increases reaction, affects cotreatment | 1 |
| bavachin | increases expression, decreases reaction | 1 |
| belinostat | increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| FV-429 compound | affects cotreatment, decreases reaction, increases expression | 1 |
| 5-furan-2yl-isoxazole-3-carboxylic acid (3-imidazol-1yl-propyl)-amide | affects expression, affects reaction | 1 |
| LGK974 | decreases expression | 1 |
| Telmisartan | decreases expression, decreases reaction | 1 |
| Microplastics | increases abundance, increases expression | 1 |
| Matrines | decreases expression | 1 |
| Glyphosate | increases expression | 1 |
| Ethanol | affects cotreatment, increases activity | 1 |
ChEMBL screening assays
31 unique, capped per target: 31 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1267283 | Binding | Inhibition of palmitoylation of Wnt3A expressed in mouse L cell by detergent solubility fractionation assessed as [3H]palmitate incorporation at 2.5 uM by autoradiography method | Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. — Nat Chem Biol |
Cellosaurus cell lines
8 cell lines: 3 embryonic stem cell, 3 cancer cell line, 1 transformed cell line, 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_A7V7 | SEES3-1V human WNT3A, clone1 | Embryonic stem cell | Male |
| CVCL_A7V8 | SEES3-1V human WNT3A, clone2 | Embryonic stem cell | Male |
| CVCL_A7V9 | SEES3-1V human WNT3A, clone3 | Embryonic stem cell | Male |
| CVCL_B8RU | Abcam HCT 116 WNT3A KO | Cancer cell line | Male |
| CVCL_B9U8 | Abcam A-549 WNT3A KO | Cancer cell line | Male |
| CVCL_D8Y9 | Ubigene HCT 116 WNT3A KO | Cancer cell line | Male |
| CVCL_D9VT | Ubigene HEK293 WNT3A KO | Transformed cell line | Female |
| CVCL_E6SE | Genomeditech CHO-K1 H_WNT3A | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): hepatocellular carcinoma