LGALS3

Summary

LGALS3 (galectin 3, HGNC:6563) is a protein-coding gene on chromosome 14q22.3, encoding Galectin-3 (P17931). Galactose-specific lectin which binds IgE.

This gene encodes a member of the galectin family of carbohydrate binding proteins. Members of this protein family have an affinity for beta-galactosides. The encoded protein is characterized by an N-terminal proline-rich tandem repeat domain and a single C-terminal carbohydrate recognition domain. This protein can self-associate through the N-terminal domain allowing it to bind to multivalent saccharide ligands. This protein localizes to the extracellular matrix, the cytoplasm and the nucleus. This protein plays a role in numerous cellular functions including apoptosis, innate immunity, cell adhesion and T-cell regulation. The protein exhibits antimicrobial activity against bacteria and fungi. Alternate splicing results in multiple transcript variants.

Source: NCBI Gene 3958 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 59 total
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002306

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6563
Approved symbol	LGALS3
Name	galectin 3
Location	14q22.3
Locus type	gene with protein product
Status	Approved
Aliases	MAC-2, GALIG
Ensembl gene	ENSG00000131981
Ensembl biotype	protein_coding
OMIM	153619
Entrez	3958

Gene structure

Transcript identifiers

Ensembl transcripts: 31 — 27 protein_coding, 3 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000254301, ENST00000553493, ENST00000553755, ENST00000554715, ENST00000556263, ENST00000556322, ENST00000556438, ENST00000888054, ENST00000888055, ENST00000888056, ENST00000888057, ENST00000888058, ENST00000888059, ENST00000888060, ENST00000888061, ENST00000888062, ENST00000888063, ENST00000888064, ENST00000888065, ENST00000888066, ENST00000888067, ENST00000888068, ENST00000888069, ENST00000947951, ENST00000947952, ENST00000947953, ENST00000947954, ENST00000947955, ENST00000947956, ENST00000947957, ENST00000947958

RefSeq mRNA: 2 — MANE Select: NM_002306 NM_001357678, NM_002306

CCDS: CCDS41956

Canonical transcript exons

ENST00000254301 — 6 exons

Exon	Start	End
ENSE00001536493	55137370	55137391
ENSE00002501390	55145116	55145423
ENSE00002509600	55129252	55129300
ENSE00003570637	55140275	55140363
ENSE00003669363	55138045	55138368
ENSE00003691772	55142584	55142749

Expression profiles

Bgee: expression breadth ubiquitous, 299 present calls, max score 99.95.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.7198 / max 148.0984, expressed in 179 samples.

FANTOM5 promoters (14 alternative TSS)

Promoter ID	TPM avg	Samples expressed
139707	419.3164	1760
194073	1.7198	179
139704	1.5608	73
139712	0.9966	490
139715	0.6514	366
139716	0.5803	312
139714	0.5220	286
139713	0.2944	160
194074	0.1222	72
139711	0.0939	39

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
colonic mucosa	UBERON:0000317	99.95	gold quality
palpebral conjunctiva	UBERON:0001812	99.95	gold quality
bronchial epithelial cell	CL:0002328	99.94	gold quality
mucosa of sigmoid colon	UBERON:0004993	99.94	gold quality
epithelium of bronchus	UBERON:0002031	99.92	gold quality
bronchus	UBERON:0002185	99.91	gold quality
nasal cavity epithelium	UBERON:0005384	99.90	gold quality
ileal mucosa	UBERON:0000331	99.89	gold quality
decidua	UBERON:0002450	99.89	gold quality
jejunal mucosa	UBERON:0000399	99.88	gold quality
mucosa of transverse colon	UBERON:0004991	99.88	gold quality
amniotic fluid	UBERON:0000173	99.86	gold quality
visceral pleura	UBERON:0002401	99.80	gold quality
esophagus squamous epithelium	UBERON:0006920	99.80	gold quality
mammary duct	UBERON:0001765	99.77	gold quality
nasal cavity mucosa	UBERON:0001826	99.77	gold quality
trachea	UBERON:0003126	99.77	gold quality
skin of hip	UBERON:0001554	99.76	gold quality
duodenum	UBERON:0002114	99.75	gold quality
parotid gland	UBERON:0001831	99.74	gold quality
epithelium of nasopharynx	UBERON:0001951	99.74	gold quality
urethra	UBERON:0000057	99.73	gold quality
oral cavity	UBERON:0000167	99.73	gold quality
squamous epithelium	UBERON:0006914	99.73	gold quality
pharyngeal mucosa	UBERON:0000355	99.72	gold quality
epithelium of esophagus	UBERON:0001976	99.72	gold quality
synovial joint	UBERON:0002217	99.72	gold quality
parietal pleura	UBERON:0002400	99.71	gold quality
germinal epithelium of ovary	UBERON:0001304	99.70	gold quality
upper leg skin	UBERON:0004262	99.70	gold quality

Single-cell (SCXA)

Detected in 43 experiment(s), a significant marker in 37.

Experiment	Marker?	Max mean expression
E-MTAB-8410	yes	5007.45
E-GEOD-130148	yes	4033.65
E-MTAB-9435	yes	3252.20
E-MTAB-6308	yes	3209.24
E-MTAB-6653	yes	3063.42
E-HCAD-24	yes	2971.33
E-CURD-88	yes	2749.66
E-MTAB-9906	yes	2041.92
E-CURD-120	yes	1783.77
E-MTAB-8530	yes	1701.23
E-MTAB-9543	yes	1577.61
E-HCAD-8	yes	1275.04
E-MTAB-8911	yes	719.62
E-GEOD-81547	yes	719.09
E-GEOD-81383	yes	641.90

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): BCL11B, CD28, CTNNB1, ELF4, GSK3B, HIF1A, IRF1, IRF2, JUN, NFATC2, RUNX1, RUNX2, SP1, STAT1, TTF1

miRNA regulators (miRDB)

16 targeting LGALS3, 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-4789-3P	99.99	70.75	2484
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505
HSA-MIR-3681-3P	99.88	70.46	2254
HSA-MIR-4495	99.82	72.08	3080
HSA-MIR-4760-5P	99.80	69.88	1619
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-1208	99.70	68.28	1533
HSA-MIR-466	99.67	70.85	2863
HSA-MIR-8061	99.63	69.44	1411
HSA-MIR-4643	99.49	67.63	1791
HSA-MIR-4477A	98.83	69.75	2952
HSA-MIR-6873-5P	98.45	66.14	1417
HSA-MIR-1279	97.83	67.50	1898
HSA-MIR-376A-5P	97.70	65.61	863
HSA-MIR-6760-3P	96.35	68.31	1001

Literature-anchored findings (GeneRIF, showing 40)

• These results demonstrate that galectin-3 phosphorylation regulates its anti-apoptotic signaling activity (PMID:11724777)
• translocates to the perinuclear membranes and inhibits cytochrome c release from the mitochondria. A role for synexin in galectin-3 translocation. (PMID:11839755)
• galectin-3 and CD26/DPPIV as preoperative diagnostic markers for thyroid nodules (PMID:12112826)
• not a universal marker of malignancy in thyroid nodular disease in children and adolescents (PMID:12213909)
• conclude that because of its location and affinity for gonococcal lipooligosaccharides (LOS) galectin-3 could play a role in gonococcal infection (PMID:12366402)
• Galectin-3 expression is significantly stronger in metastatic lymph nodes and in poorly differentiated adenocarcinoma of stomach (PMID:12375039)
• role in mediating MDA-MB-435 human breast carcinoma cell homo- and heterotypic adhesion under flow conditions (PMID:12438311)
• role of galectin-3 on cyclin D(1) gene expression (PMID:12439750)
• galectin 3 controls proliferation in thyroid cells (PMID:12615069)
• downregulation of galectin-3 is associated with epithelial skin cancer (PMID:12673672)
• Non-small-cell lung cancers examined were found to overexpress LGALS3 gene at levels three times higher than those of normal epithelial cells. (PMID:12696064)
• Changes in the expressions of galectin-3 are potentially important for myeloid cell differentiation into specific lineages. (PMID:12714580)
• Stable thyroid galectin- 3 transfectants acquired serum-independent growth, clonogenicity in soft agar, & loss of contact inhibition, indicating transformation of thyroid follicular cells by galectin-3 & possible involvement of galectin-3 in cell cycle. (PMID:12767519)
• mechanism by which galectin-3 overexpression promoted cell death and PARP cleavage as well as caspase (-8, -9, and -3) activation during TRAIL treatment (PMID:12878156)
• results demonstrate that galectin-3 mRNA may not be a suitable target for molecular-based diagnosis of thyroid carcinomas (PMID:12963125)
• an additional marker of malignant potential of thyroid nodular lesions (PMID:14558920)
• Galectin-3 has a role in activating Ras (PMID:15205467)
• nuclear galectin-3 and TTF-1 have roles in progression of non-small cell lung carcinoma (PMID:15279903)
• exerts opposite biological activities according to its cellular localization: nuclear galectin-3 plays antitumor functions and cytoplasmic galectin-3 promotes tumor progression (PMID:15326483)
• A major circulating ligand for galectin-3, which is elevated in the sera of patients with colon cancer, is a cancer-associated glycoform of haptoglobin. (PMID:15362030)
• The aim of this study was to investigate the potential of galectin-3 as a marker of malignancy in follicular patterned thyroid lesions (PMID:15386597)
• expression is required for T. cruzi adhesion to human coronary artery smooth muscle cells and exogenous galectin-3 enhances this process, leading to parasite entry. (PMID:15501810)
• Cultured galectin-3 deficient glioblastoma cells showed increased motility potential and modifications in cytoskeleton reorganization. Galectin-3 deficient cells have increased expression of proteins implicated in cell adhesion regulation. (PMID:15555581)
• GALIG encodes a mitochondrial protein promoting cytochrome c release. (PMID:15561101)
• Alterations in galectin-3 expression and distribution correlate with breast cancer progression (PMID:15579437)
• Gal-3 and sFbg are two physiological mediators present at inflammatory sites that activate different components of the MAPK pathway and could be acting in concert to modulate the functionality and life span of neutrophils. (PMID:15604089)
• Elevated expression of galectin-3 in the nuclei but not the cytoplasm may be an important biological parameter related to histological differentiation and vascular invasion in patients with ESCC. (PMID:15643504)
• Expression of Gal-3 was higher in thin primary melanoma lesions than in benign pigmented skin lesions or metastases and seemed to correlate inversely with the aggressiveness. (PMID:15645276)
• galectin-3 has a role in cancer apoptosis [review] (PMID:15843888)
• Data give credence to the suggestion that gal-3 is a key regulator in the Wnt/beta-catenin signaling pathway and highlight the functional similarities between gal-3 and beta-catenin. (PMID:15867344)
• Cytoplasmic-perinuclear gal-3 in majority of thyroid carcinomas and follicular adenomas(FA). Suggests involvement in thyroid tumorigenesis throughout antiapoptosis. In FA might anticipate evolution towards malignancy. (PMID:15887854)
• The presence of galectin-3 in clinically silent microcarcinomas may indicate that galectin-3 is not related to growth or aggressiveness of papillary thyroid microcarcinomas but rather plays some other role in thyroid tumour biology. (PMID:16045783)
• Gal-3 immunostaining is a valuable tool to support a diagnosis of PC in highly proliferating (Ki67 >6%) tumors affecting a single parathyroid gland. (PMID:16112008)
• galectin-3 expression in adenoid cystic carcinoma; galectin-3 reactivity was significantly associated with regional and distant metastasis (P=0.045 and P<0.001, respectively) (PMID:16184379)
• TFF-3 is commonly expressed in HCC and its expression correlates with tumor grade. (PMID:16244583)
• Galectin-3 up-regulation of MUC2 transcription occurs at the level of transcription through AP-1 activation in colon cancer cells (PMID:16285957)
• The C-terminal carbohydrate recognition domain of galectin-3 is responsible for binding to chondroitin sulfate proteoglycan NG2 core protein in melanoma cells. (PMID:16365873)
• Galectin-3 is downregulated in cervical cancer tissues. (PMID:16369807)
• Plasmid-encoding galectin-3 acts as a novel treatment for chronic asthma in mice producing nearly complete blockade of antigen responses with respect to eosinophil airway accumulation, airway hyperresponsiveness, and remodeling. (PMID:16424226)
• a possible mechanism by which Tumor-associated antigen 90K may contribute to colon cancer progression is by modulating tumor cell adhesion to extracellular proteins, including galectin-3 (PMID:16518858)

Cross-species orthologs

10 orthologs

Organism	Symbol	Gene ID
danio_rerio	lgals3a	ENSDARG00000077850
mus_musculus	Lgals3	ENSMUSG00000050335
rattus_norvegicus	Lgals3	ENSRNOG00000010645
caenorhabditis_elegans		WBGENE00002264
caenorhabditis_elegans		WBGENE00002266
caenorhabditis_elegans		WBGENE00002269
caenorhabditis_elegans		WBGENE00002270
caenorhabditis_elegans		WBGENE00002271
caenorhabditis_elegans		WBGENE00004165
caenorhabditis_elegans		WBGENE00018255

Paralogs (16): LGALS14 (ENSG00000006659), LGALS2 (ENSG00000100079), LGALS1 (ENSG00000100097), LGALS13 (ENSG00000105198), CLC (ENSG00000105205), LGALS8 (ENSG00000116977), LGALSL (ENSG00000119862), LGALS12 (ENSG00000133317), LGALS9 (ENSG00000168961), LGALS9B (ENSG00000170298), LGALS4 (ENSG00000171747), LGALS9C (ENSG00000171916), LGALS7B (ENSG00000178934), LGALS7 (ENSG00000205076), LGALS16 (ENSG00000249861), GRIFIN (ENSG00000275572)

Protein

Protein identifiers

Galectin-3 — P17931 (reviewed: P17931)

Alternative names: 35 kDa lectin, Carbohydrate-binding protein 35, Galactose-specific lectin 3, Galactoside-binding protein, IgE-binding protein, L-31, Laminin-binding protein, Lectin L-29, Mac-2 antigen

All UniProt accessions (4): A0A024R693, P17931, G3V3R6, G3V407

UniProt curated annotations — full annotation on UniProt →

Function. Galactose-specific lectin which binds IgE. May mediate with the alpha-3, beta-1 integrin the stimulation by CSPG4 of endothelial cells migration. Together with DMBT1, required for terminal differentiation of columnar epithelial cells during early embryogenesis. In the nucleus: acts as a pre-mRNA splicing factor. Involved in acute inflammatory responses including neutrophil activation and adhesion, chemoattraction of monocytes macrophages, opsonization of apoptotic neutrophils, and activation of mast cells. Together with TRIM16, coordinates the recognition of membrane damage with mobilization of the core autophagy regulators ATG16L1 and BECN1 in response to damaged endomembranes.

Subunit / interactions. Probably forms homo- or heterodimers. Interacts with DMBT1. Interacts with CD6 and ALCAM. Forms a complex with the ITGA3, ITGB1 and CSPG4. Interacts with LGALS3BP, LYPD3, ZFTRAF1 and UACA. Interacts with TRIM16; this interaction mediates autophagy of damage endomembranes. Interacts with cargo receptor TMED10; the interaction mediates the translocation from the cytoplasm into the ERGIC (endoplasmic reticulum-Golgi intermediate compartment) and thereby secretion.

Subcellular location. Cytoplasm. Nucleus. Secreted.

Tissue specificity. A major expression is found in the colonic epithelium. It is also abundant in the activated macrophages. Expressed in fetal membranes.

RefSeq proteins (2): NP_001344607, NP_002297* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001079	Galectin_CRD	Domain
IPR013320	ConA-like_dom_sf	Homologous_superfamily
IPR044156	Galectin-like	Family

Pfam: PF00337

UniProt features (42 total): strand 12, repeat 8, modified residue 4, sequence variant 3, sequence conflict 3, region of interest 2, compositionally biased region 2, helix 2, initiator methionine 1, chain 1, domain 1, short sequence motif 1, binding site 1, disulfide bond 1

Structure

Experimental structures (PDB)

152 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
3ZSJ	X-RAY DIFFRACTION	0.86
3ZSK	X-RAY DIFFRACTION	0.9
6RZH	X-RAY DIFFRACTION	0.95
6I74	X-RAY DIFFRACTION	0.96
4BM8	X-RAY DIFFRACTION	0.96
6QLR	X-RAY DIFFRACTION	0.97
7XFA	X-RAY DIFFRACTION	0.98
9I4O	X-RAY DIFFRACTION	0.99
6QLN	X-RAY DIFFRACTION	1
6FK2	X-RAY DIFFRACTION	1.01
6RZG	X-RAY DIFFRACTION	1.01
6RZF	X-RAY DIFFRACTION	1.02
6RZL	X-RAY DIFFRACTION	1.04
6RZK	X-RAY DIFFRACTION	1.05
6QLS	X-RAY DIFFRACTION	1.05
7RH3	X-RAY DIFFRACTION	1.05
7ZQX	X-RAY DIFFRACTION	1.05
9UG4	X-RAY DIFFRACTION	1.05
9S62	X-RAY DIFFRACTION	1.06
9I4N	X-RAY DIFFRACTION	1.07
6QLQ	X-RAY DIFFRACTION	1.08
3ZSL	X-RAY DIFFRACTION	1.08
4BLI	X-RAY DIFFRACTION	1.08
7DF5	X-RAY DIFFRACTION	1.08
8PFF	X-RAY DIFFRACTION	1.08
8YMD	X-RAY DIFFRACTION	1.08
6QLP	X-RAY DIFFRACTION	1.08
6G0V	X-RAY DIFFRACTION	1.09
28VW	X-RAY DIFFRACTION	1.09
8PF9	X-RAY DIFFRACTION	1.09

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P17931-F1	76.49	0.59

Antibody-complex structures (SAbDab): 1 — 6ZVF

Functional residue map

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

Ligand- & substrate-binding residues (1): 181–187

Post-translational modifications (4): 2, 6, 12, 188

Disulfide bonds (1): 173

Function

Pathways and Gene Ontology

Reactome pathways

11 pathways

ID	Pathway
R-HSA-6798695	Neutrophil degranulation
R-HSA-879415	Advanced glycosylation endproduct receptor signaling
R-HSA-8939246	RUNX1 regulates transcription of genes involved in differentiation of myeloid cells
R-HSA-8941333	RUNX2 regulates genes involved in differentiation of myeloid cells
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System
R-HSA-212436	Generic Transcription Pathway
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-8878166	Transcriptional regulation by RUNX2
R-HSA-8878171	Transcriptional regulation by RUNX1

MSigDB gene sets: 717 (showing top): GSE18804_SPLEEN_MACROPHAGE_VS_BRAIN_TUMORAL_MACROPHAGE_UP, GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, GOBP_REGULATION_OF_T_CELL_RECEPTOR_SIGNALING_PATHWAY, FERRANDO_TAL1_NEIGHBORS, GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_REGULATION_OF_ANTIGEN_RECEPTOR_MEDIATED_SIGNALING_PATHWAY, GOBP_REGULATION_OF_LEUKOCYTE_PROLIFERATION, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_DENDRITIC_CELL_DIFFERENTIATION, REACTOME_INNATE_IMMUNE_SYSTEM, BENPORATH_ES_WITH_H3K27ME3, GOBP_ANTIMICROBIAL_HUMORAL_RESPONSE, SHIPP_DLBCL_VS_FOLLICULAR_LYMPHOMA_UP

GO Biological Process (26): monocyte chemotaxis (GO:0002548), mRNA processing (GO:0006397), RNA splicing (GO:0008380), neutrophil chemotaxis (GO:0030593), epithelial cell differentiation (GO:0030855), positive regulation of protein-containing complex assembly (GO:0031334), regulation of T cell proliferation (GO:0042129), innate immune response (GO:0045087), negative regulation of endocytosis (GO:0045806), eosinophil chemotaxis (GO:0048245), macrophage chemotaxis (GO:0048246), negative regulation of T cell receptor signaling pathway (GO:0050860), positive chemotaxis (GO:0050918), negative regulation of NK T cell activation (GO:0051134), regulation of T cell apoptotic process (GO:0070232), mononuclear cell migration (GO:0071674), positive regulation of mononuclear cell migration (GO:0071677), positive regulation of calcium ion import (GO:0090280), regulation of extrinsic apoptotic signaling pathway via death domain receptors (GO:1902041), positive regulation of protein localization to plasma membrane (GO:1903078), negative regulation of immunological synapse formation (GO:2000521), negative regulation of T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cell (GO:2001189), negative regulation of extrinsic apoptotic signaling pathway (GO:2001237), immune system process (GO:0002376), cell differentiation (GO:0030154), NK T cell activation (GO:0051132)

GO Molecular Function (12): RNA binding (GO:0003723), protein phosphatase inhibitor activity (GO:0004864), IgE binding (GO:0019863), protein phosphatase binding (GO:0019903), carbohydrate binding (GO:0030246), chemoattractant activity (GO:0042056), laminin binding (GO:0043236), disaccharide binding (GO:0048030), molecular condensate scaffold activity (GO:0140693), receptor ligand inhibitor activity (GO:0141069), protein binding (GO:0005515), signaling receptor inhibitor activity (GO:0030547)

GO Cellular Component (16): immunological synapse (GO:0001772), extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), nucleus (GO:0005634), nucleoplasm (GO:0005654), spliceosomal complex (GO:0005681), cytoplasm (GO:0005737), mitochondrial inner membrane (GO:0005743), cytosol (GO:0005829), plasma membrane (GO:0005886), cell surface (GO:0009986), membrane (GO:0016020), secretory granule membrane (GO:0030667), extracellular matrix (GO:0031012), extracellular exosome (GO:0070062), ficolin-1-rich granule membrane (GO:0101003)

Reactome top-level categories

Rollup of top-7 pathways:

Category	Pathways
Innate Immune System	2
Generic Transcription Pathway	2
Transcriptional regulation by RUNX1	1
Transcriptional regulation by RUNX2	1
Immune System	1
RNA Polymerase II Transcription	1
Gene expression (Transcription)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	7
leukocyte chemotaxis	2
mononuclear cell migration	2
RNA processing	2
granulocyte chemotaxis	2
binding	2
receptor ligand activity	2
molecular function inhibitor activity	2
myeloid leukocyte migration	1
mRNA metabolic process	1
neutrophil migration	1
cell differentiation	1
epithelium development	1
regulation of protein-containing complex assembly	1
positive regulation of cellular component biogenesis	1
positive regulation of cellular component organization	1
protein-containing complex assembly	1
T cell proliferation	1
regulation of lymphocyte proliferation	1
regulation of T cell activation	1
immune response	1
defense response to symbiont	1
endocytosis	1
regulation of endocytosis	1
negative regulation of transport	1
negative regulation of cellular component organization	1
eosinophil migration	1
macrophage migration	1
T cell receptor signaling pathway	1
regulation of T cell receptor signaling pathway	1
negative regulation of antigen receptor-mediated signaling pathway	1
chemotaxis	1
negative regulation of alpha-beta T cell activation	1
NK T cell activation	1
regulation of NK T cell activation	1
regulation of lymphocyte apoptotic process	1
T cell apoptotic process	1
leukocyte migration	1
positive regulation of leukocyte migration	1
regulation of mononuclear cell migration	1

Protein interactions and networks

STRING

3802 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LGALS3	LGALS3BP	Q08380	998
LGALS3	MUC1	P13931	995
LGALS3	TRIM16	O95361	992
LGALS3	CLEC7A	Q9BXN2	992
LGALS3	LAG3	P18627	990
LGALS3	FCGR2B	P31994	988
LGALS3	PTPRC	P08575	983
LGALS3	FN1	P02751	982
LGALS3	ELN	P15502	979
LGALS3	GP6	Q9HCN6	974
LGALS3	KRAS	P01116	953
LGALS3	MUC16	Q8WXI7	947
LGALS3	TLR2	O60603	945
LGALS3	TLR4	O00206	933
LGALS3	ANXA7	P20073	929

IntAct

260 interactions, top by confidence:

A	B	Type	Score
PRR13	LGALS3	psi-mi:“MI:0915”(physical association)	0.670
LGALS3	PRR13	psi-mi:“MI:0915”(physical association)	0.670
ENG	LGALS3	psi-mi:“MI:0407”(direct interaction)	0.630
ENG	LGALS3	psi-mi:“MI:0915”(physical association)	0.630
ENG	LGALS3	psi-mi:“MI:0403”(colocalization)	0.630
LPAR2	LGALS3	psi-mi:“MI:0914”(association)	0.620
NCR3	LGALS3	psi-mi:“MI:0915”(physical association)	0.600
NCR3	LGALS3	psi-mi:“MI:0407”(direct interaction)	0.600
LGALS3	SS18L1	psi-mi:“MI:0915”(physical association)	0.560
LGALS3	GOLGA2	psi-mi:“MI:0915”(physical association)	0.560
LGALS3	PPIG	psi-mi:“MI:0915”(physical association)	0.560
GOLGA2	LGALS3	psi-mi:“MI:0915”(physical association)	0.560
SS18L1	LGALS3	psi-mi:“MI:0915”(physical association)	0.560
TMEM182	LGALS3	psi-mi:“MI:0915”(physical association)	0.560
CRX	LGALS3	psi-mi:“MI:0915”(physical association)	0.560
LGALS3	INCA1	psi-mi:“MI:0915”(physical association)	0.560
LGALS3	KIF16B	psi-mi:“MI:0915”(physical association)	0.560
TMEM182	LGALS3	psi-mi:“MI:0914”(association)	0.560
LGALS3	LGALS3	psi-mi:“MI:0915”(physical association)	0.550

BioGRID (577): LGALS3 (Two-hybrid), LGALS3 (Two-hybrid), PPIG (Two-hybrid), SS18L1 (Two-hybrid), PRR13 (Two-hybrid), LGALS3 (Affinity Capture-MS), LGALS3 (Affinity Capture-MS), COLEC12 (Affinity Capture-MS), LAMB1 (Affinity Capture-MS), ABCC4 (Affinity Capture-MS), KIAA0319L (Affinity Capture-MS), ATP2B4 (Affinity Capture-MS), SLC9A6 (Affinity Capture-MS), LAMA4 (Affinity Capture-MS), RRAGC (Affinity Capture-MS)

ESM2 similar proteins: A1CL82, A1CQZ0, A1CXK7, A1D3V4, A1D611, A2QI25, A2QU58, A2RB75, A3LSY7, A4QTY2, A5D9W7, A5DZS4, A6R7B8, A6SDT7, A6SEH9, A6ZP43, A7EJY3, A7F075, B0XPP3, B0Y081, O74477, P08699, P0CM58, P0CM59, P16110, P17931, P20072, P27214, P30601, P33477, P47953, P50995, P97384, Q08601, Q0CQL9, Q0CTN3, Q1E0A3, Q2UCB7, Q2UN81, Q4PEQ5

Diamond homologs: A4D1Z8, A8MUM7, O00182, O00214, O08573, O44126, O54891, O54974, O88644, P07583, P08520, P08699, P16110, P17931, P23668, P38486, P38552, P47845, P47929, P47953, P47967, P56217, P56470, P97400, P97590, P97840, Q09605, Q09610, Q1ECW6, Q29058, Q29373, Q3B8N2, Q3MHZ8, Q3T0D6, Q3ZCW2, Q5R5K6, Q5ZHQ2, Q62665, Q68FJ4, Q6DDR8

SIGNOR signaling

13 interactions.

A	Effect	B	Mechanism
CSNK1A1	up-regulates	LGALS3	phosphorylation
ABL2	up-regulates	LGALS3	phosphorylation
ABL1	unknown	LGALS3	phosphorylation
GSK3B	“up-regulates quantity by expression”	LGALS3	“transcriptional regulation”
LGALS3	down-regulates	Apoptosis
LGALS3	“up-regulates quantity by stabilization”	MCL1
LGALS3	“up-regulates quantity by stabilization”	BCL2L1
LGALS3	“up-regulates quantity by stabilization”	BAD
LGALS3	“up-regulates activity”	“Av/b3 integrin”	binding
CSNK1A1	unknown	LGALS3	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 158 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.

GO biological processes:

GO term	Partners	Fold	FDR
establishment of localization in cell	7	9.6×	9e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	34
Likely benign	4
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

881 predictions. Top by Δscore:

Variant	Effect	Δscore
14:55129298:GCG:G	donor_gain	1.0000
14:55137392:G:GG	donor_gain	1.0000
14:55138043:A:AG	acceptor_gain	1.0000
14:55138044:G:GA	acceptor_gain	1.0000
14:55138044:GCTCC:G	acceptor_gain	1.0000
14:55140269:TCCCA:T	acceptor_loss	1.0000
14:55140270:CCCAG:C	acceptor_loss	1.0000
14:55140271:CCA:C	acceptor_loss	1.0000
14:55140272:CAG:C	acceptor_loss	1.0000
14:55140273:A:AG	acceptor_gain	1.0000
14:55140273:A:C	acceptor_loss	1.0000
14:55140274:G:GG	acceptor_gain	1.0000
14:55140274:GATT:G	acceptor_gain	1.0000
14:55140360:ACAGG:A	donor_loss	1.0000
14:55140361:CAGGT:C	donor_loss	1.0000
14:55140362:AGGTA:A	donor_loss	1.0000
14:55140364:GTAAG:G	donor_loss	1.0000
14:55140365:T:A	donor_loss	1.0000
14:55129296:GAGCG:G	donor_gain	0.9900
14:55129301:G:GG	donor_gain	0.9900
14:55137392:GTAAG:G	donor_loss	0.9900
14:55137393:T:A	donor_loss	0.9900
14:55138039:TTCCA:T	acceptor_loss	0.9900
14:55138040:TCCA:T	acceptor_loss	0.9900
14:55138041:CCA:C	acceptor_loss	0.9900
14:55138042:CAGC:C	acceptor_loss	0.9900
14:55138043:AGC:A	acceptor_loss	0.9900
14:55138044:GC:G	acceptor_gain	0.9900
14:55138044:GCT:G	acceptor_gain	0.9900
14:55138044:GCTC:G	acceptor_gain	0.9900

AlphaMissense

1605 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:55142667:T:A	V172D	1.000
14:55142693:T:A	W181R	1.000
14:55142693:T:C	W181R	1.000
14:55142695:G:C	W181C	1.000
14:55142695:G:T	W181C	1.000
14:55140333:T:A	I134N	0.999
14:55140339:G:A	G136D	0.999
14:55142598:T:C	F149S	0.999
14:55142622:T:C	F157S	0.999
14:55142624:C:G	H158D	0.999
14:55142628:T:C	F159S	0.999
14:55142636:C:A	R162S	0.999
14:55142637:G:C	R162P	0.999
14:55142640:T:C	F163S	0.999
14:55142674:T:A	N174K	0.999
14:55142674:T:G	N174K	0.999
14:55142694:G:C	W181S	0.999
14:55142727:T:C	F192S	0.999
14:55142745:T:C	F198S	0.999
14:55145144:T:C	F209S	0.999
14:55145150:T:A	V211D	0.999
14:55145152:G:C	A212P	0.999
14:55140324:T:C	L131P	0.998
14:55140338:G:C	G136R	0.998
14:55142632:C:A	N160K	0.998
14:55142632:C:G	N160K	0.998
14:55142636:C:G	R162G	0.998
14:55142673:A:T	N174I	0.998
14:55142694:G:T	W181L	0.998
14:55142704:A:C	E184D	0.998

dbSNP variants (sampled 300 via entrez): RS1000022826 (14:55143048 G>A,T), RS1001146222 (14:55144500 T>A,C), RS1001196032 (14:55131229 G>A), RS1001304312 (14:55134010 C>T), RS1001429120 (14:55127584 G>A), RS1001494226 (14:55129218 A>T), RS1001513978 (14:55144726 A>G,T), RS1001552573 (14:55133590 G>T), RS1001565189 (14:55139887 G>T), RS1001776584 (14:55131764 A>G), RS1001989503 (14:55130801 C>A,G,T), RS1002073653 (14:55144324 C>G), RS1002143780 (14:55132150 G>C), RS1002506960 (14:55130216 G>A,C), RS1002539789 (14:55137323 A>G)

Disease associations

OMIM: gene MIM:153619 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST001711_2	Protein biomarker	2.000000e-188
GCST004635_27	Testicular germ cell tumor	3.000000e-08
GCST006585_2373	Blood protein levels	3.000000e-45
GCST009731_52	Blood protein levels in cardiovascular risk	7.000000e-94
GCST010676_4	Leukoderma in response to rhododendrol	9.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004747	protein measurement
EFO:0008137	galectin-3 measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4531 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,011 (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
CHEMBL5314358	LACTOSE, ANHYDROUS	3
CHEMBL4297442	OLITIGALTIN	2	559
CHEMBL5182222	SELVIGALTIN	2	20
CHEMBL562318	MARDEPODECT	2	432

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs11125	Toxicity	3	Antibiotics	Hypersensitivity

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs11125	LGALS3	3	4.00	1	Antibiotics
rs4644	LGALS3		0.00	0
rs4652	LGALS3		0.00	0

Binding affinities (BindingDB)

824 measured of 829 human assays (829 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-(methoxy-d3)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	7 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-bromo-5-cyanophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	8 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-bromo-5-cyanophenyl)-4-(4-(3-fluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	8 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)—N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)-2-oxoethoxy)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	9 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-4-(4-(2,3-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-(2-morpholino-2-oxoethoxy)tetrahydro-2H-pyran-2-carboxamide	IC50	9 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-4-(4-(3,4-difluoro-5-methoxyphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	9 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
2-(((2R,3R,4S,5R,6R)-2-((3,5-dichlorophenyl)((1S,2S)-2-hydroxycyclohexyl)carbamoyl)-5-hydroxy-6-(hydroxymethyl)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3-yl)oxy)acetic acid	IC50	9 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(5-chloro-2-methylphenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	10 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(4-chloro-3-fluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	10 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4R,5R,6R)-4-(4-(2,3-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-2-(hydroxymethyl)-6-((3-(1-methylcyclopropyl)isoxazol-5-yl)methyl)tetrahydro-2H-pyran-3,5-diol	IC50	10 nM	US-12319672: Alpha-D-galactopyranoside derivatives
N-(tert-butyl)-4-(4-(((2R,3R,4S,5R,6R)-5-hydroxy-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-yl)methyl)-1H-1,2,3-triazol-1-yl)piperidine-1-carboxamide	IC50	10 nM	US-12319672: Alpha-D-galactopyranoside derivatives
(2R,3R,4S,5R,6R)-N-(3-bromo-5-fluorophenyl)-4-(4-(3,5-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	11 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
2-(((2R,3R,4S,5R,6R)-2-((3-chloro-5-cyanophenyl)((1S,2S)-2-hydroxycyclohexyl)carbamoyl)-4-(4-(2,3-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)oxy)aceticacid	IC50	11 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-4-(4-(3-fluoro-4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	11 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-4-(4-(3,4-dichlorophenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	11 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-N-(pyridin-2-yl)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	11 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)—N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-(2-morpholino-2-oxoethoxy)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	12 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)—N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-(2-(4-hydroxypiperidin-1-yl)-2-oxoethoxy)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	12 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-4-(4-(3,5-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	12 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-4-(4-(2,3-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	12 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-2-(hydroxymethyl)-5-methoxy-6-((1-(1-(methylsulfonyl)piperidin-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3-ol	IC50	12 nM	US-12319672: Alpha-D-galactopyranoside derivatives
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	13 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3,5-dibromophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	13 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-5-hydroxy-3-(2-(3-hydroxyazetidin-1-yl)-2-oxoethoxy)-N-((1S,2S)-2-hydroxycyclohexyl-hydroxymethl)-4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	13 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(3-chloro-4,5-difluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3-chloro-5-cyanophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	13 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(4-bromo-2,3-difluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3-chloro-5-cyanophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	13 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(4-bromo-2,3-difluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	13 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-2-(hydroxymethyl)-5-methoxy-6-((1-(1-(propylsulfonyl)piperidin-4-yl)-1H-1,2,3-triazol-4-yl)methyl)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3-ol	IC50	13 nM	US-12319672: Alpha-D-galactopyranoside derivatives
1-(benzylimino)-4-(4-(((2R,3R,4S,5R,6R)-5-hydroxy-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-yl)methyl)-1H-1,2,3-triazol-1-yl)hexahydro-1l6-thiopyran 1-oxide	IC50	13 nM	US-12319672: Alpha-D-galactopyranoside derivatives
(2R,3R,4S,5R,6R)-N-(3-bromo-5-chlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	14 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(5-chloro-2-fluorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	14 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(4-chloro-3,5-difluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	14 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-4-(4-(3,4-dichloro-5-fluorophenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	14 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-4-(4-(3,5-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	15 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(4-bromo-2,3-difluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3-cyano-5-fluorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	15 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
benzyl 4-(4-(((2R,3R,4S,5R,6R)-4-(4-(3,5-difluorophenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-yl)methyl)-1H-1,2,3-triazol-1-yl)piperidine-1-carboxylate	IC50	15 nM	US-12319672: Alpha-D-galactopyranoside derivatives
(2R,3R,4S,5R,6R)-N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide [1,3-di-deoxy-2-O-methyl-3-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-(N-(3,5-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl))-beta-D-galacto-pyranose-1-carboxamide]	IC50	16 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-(trifluoromethyl)phenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	16 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)—N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)-2-oxoethoxy)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	16 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-cyano-5-methoxyphenyl)-4-(4-(3,5-difluorophenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	17 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(5-bromo-2-methylphenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	17 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-4-(4-(3,4-dichlorophenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	17 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-chloro-5-cyanophenyl)-4-(4-(3-fluoro-5-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	17 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
ethyl 4-(5-(((2R,3R,4S,5R,6R)-4-(4-(2,3-difluoro-4-methylphenyl)-1H-1,2,3-triazol-1-yl)-5-hydroxy-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-yl)methyl)isoxazol-3-yl)-4-methylpiperidine-1-carboxylate	IC50	17 nM	US-12319672: Alpha-D-galactopyranoside derivatives
tert-butyl ((S)-1-(((1R,4S)-4-(5-(((2R,3R,4S,5R,6R)-5-hydroxy-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-yl)methyl)isoxazol-3-yl)cyclohexyl)amino)-3-methyl-1-oxobutan-2-yl)carbamate	IC50	17 nM	US-12319672: Alpha-D-galactopyranoside derivatives
benzyl 4-(4-(((2R,3R,4S,5R,6R)-5-hydroxy-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-yl)methyl)-1H-1,2,3-triazol-1-yl)piperidine-1-carboxylate	IC50	17 nM	US-12319672: Alpha-D-galactopyranoside derivatives
(2R,3R,4S,5R,6R)-N-(3-bromo-4-fluorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	18 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-N-(3-cyano-5-fluorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxy-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-2-carboxamide	IC50	18 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(3-bromo-5-fluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3-chloro-5-cyanophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	18 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl
(2R,3R,4S,5R,6R)-4-(4-(4-bromo-3-fluorophenyl)-1H-1,2,3-triazol-1-yl)-N-(3,5-dichlorophenyl)-5-hydroxy-N-((1S,2S)-2-hydroxycyclohexyl)-6-(hydroxymethyl)-3-methoxytetrahydro-2H-pyran-2-carboxamide	IC50	18 nM	US-12291519: 2-hydroxycycloalkane-1-carbamoyl

ChEMBL bioactivities

985 potent at pChembl≥5 of 1087 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	Kd	1	nM	CHEMBL5512479
9.00	Kd	1	nM	CHEMBL6011223
9.00	Kd	1	nM	CHEMBL5820894
9.00	Kd	1	nM	CHEMBL5926251
9.00	Kd	1	nM	CHEMBL5853208
8.96	Kd	1.1	nM	CHEMBL4102995
8.80	Kd	1.6	nM	CHEMBL4066068
8.77	Kd	1.7	nM	CHEMBL4104417
8.70	Kd	2	nM	CHEMBL6042998
8.70	Kd	2	nM	CHEMBL5925349
8.70	Kd	2	nM	CHEMBL6048926
8.70	Kd	2	nM	CHEMBL5786235
8.70	Kd	2	nM	CHEMBL5971766
8.70	Kd	2	nM	CHEMBL5862405
8.70	Kd	2	nM	OLITIGALTIN
8.66	Kd	2.2	nM	OLITIGALTIN
8.64	Kd	2.3	nM	CHEMBL4091143
8.64	Kd	2.3	nM	CHEMBL4104417
8.64	Kd	2.3	nM	OLITIGALTIN
8.57	Kd	2.7	nM	CHEMBL4065371
8.54	Kd	2.9	nM	CHEMBL4102995
8.52	Kd	3	nM	CHEMBL5181494
8.52	Kd	3	nM	CHEMBL5971640
8.52	Kd	3	nM	CHEMBL5919610
8.49	Kd	3.2	nM	CHEMBL4066068
8.40	Kd	4	nM	CHEMBL4065371
8.40	Kd	4	nM	CHEMBL4064035
8.30	IC50	5	nM	CHEMBL5081052
8.30	Kd	5	nM	CHEMBL5798312
8.22	Kd	6	nM	CHEMBL6007059
8.16	IC50	6.9	nM	CHEMBL5181786
8.16	IC50	6.9	nM	CHEMBL5589832
8.15	IC50	7	nM	CHEMBL5593643
8.15	Kd	7	nM	CHEMBL5799558
8.15	Kd	7	nM	CHEMBL5746404
8.15	IC50	7	nM	CHEMBL5181786
8.15	Kd	7	nM	CHEMBL6022588
8.15	Kd	7	nM	CHEMBL5782642
8.14	IC50	7.2	nM	CHEMBL5410487
8.10	Kd	8	nM	CHEMBL5955206
8.10	Kd	8	nM	CHEMBL5832884
8.06	Kd	8.7	nM	CHEMBL4071878
8.06	Kd	8.7	nM	CHEMBL4091143
8.06	IC50	8.8	nM	CHEMBL5435736
8.06	IC50	8.7	nM	CHEMBL5902543
8.05	IC50	9	nM	CHEMBL5592031
8.04	IC50	9.2	nM	CHEMBL5591506
8.01	IC50	9.7	nM	CHEMBL5204834
8.00	IC50	10	nM	OLITIGALTIN
8.00	IC50	10	nM	CHEMBL5591451

PubChem BioAssay actives

236 with measured affinity, of 750 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,3R,4S,5R,6R)-4-[4-(3,5-difluorophenyl)triazol-1-yl]-2-[[(2S,3R,4S,5R,6R)-4-[4-(3,5-difluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]disulfanyl]-6-(hydroxymethyl)oxane-3,5-diol	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0010	uM
(2S,3R,4S,5R,6R)-2-[[(2S,3R,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-2-yl]disulfanyl]-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-3,5-diol	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0010	uM
(2S,3R,4S,5R,6R)-4-[4-(3,4-difluorophenyl)triazol-1-yl]-2-[[(2S,3R,4S,5R,6R)-4-[4-(3,4-difluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]disulfanyl]-6-(hydroxymethyl)oxane-3,5-diol	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0010	uM
4-[1-[(2S,3R,4S,5R,6R)-2-[(2S,3R,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-2-yl]sulfanyl-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]triazol-4-yl]-3H-1,3-thiazol-2-one	2064806: Binding affinity to human galectin-3 assessed as dissociation constant by competitive fluorescence polarization assay	kd	0.0010	uM
(2S,3R,4S,5R,6R)-4-[4-(3-fluorophenyl)triazol-1-yl]-2-[(2S,3R,4S,5R,6R)-4-[4-(3-fluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]sulfanyl-6-(hydroxymethyl)oxane-3,5-diol	1984906: Binding affinity at recombinant human Galectin-3 assessed as dissociation constant by fluorescence anisotropy assay	kd	0.0022	uM
(2S,3R,4S,5R,6R)-4-[4-(3-fluorophenyl)triazol-1-yl]-2-[[(2S,3R,4S,5R,6R)-4-[4-(3-fluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]disulfanyl]-6-(hydroxymethyl)oxane-3,5-diol	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0023	uM
(2S,3R,4S,5R,6R)-4-[4-(4-fluorophenyl)triazol-1-yl]-2-[[(2S,3R,4S,5R,6R)-4-[4-(4-fluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]disulfanyl]-6-(hydroxymethyl)oxane-3,5-diol	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0027	uM
(2S,3R,4S,5R,6R)-4-[4-(3-fluorophenyl)triazol-1-yl]-2-[(2S,3R,4S,5R,6R)-4-[4-(3-fluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]sulfanyl-6-methyloxane-3,5-diol	1857068: Binding affinity to human galectin-3 assessed as dissociation constant by competitive fluorescence polarization assay	kd	0.0030	uM
3-[[(2S,3R,4S,5S,6R)-2-[[(2S,3R,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-2-yl]disulfanyl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxymethyl]-5,6-difluorochromen-2-one	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0040	uM
(2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(3R,4R,5S)-4-hydroxy-5-[4-(1,3-thiazol-2-yl)triazol-1-yl]oxan-3-yl]sulfanyl-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0050	uM
(2S,3R,4R,5R,6R)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-2-[2-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	1870977: Inhibition of His-tagged recombinant human Gal-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by time resolved fluorescence based assay	ic50	0.0069	uM
3-[(2S,3R,4R,5R,6R)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-4-[5-chloro-2-(trifluoromethyl)phenyl]-1H-1,2,4-triazole-5-thione	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0069	uM
3-[(2S,3R,4R,5R,6R)-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-4-[5-chloro-2-(trifluoromethoxy)phenyl]-1H-1,2,4-triazole-5-thione	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0070	uM
(2S,3R,4R,5R,6R)-2-[2-(1,3-benzothiazol-6-yl)-5-methyl-1,2,4-triazol-3-yl]-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-6-(hydroxymethyl)oxane-3,5-diol	1984893: Inhibition of human Galectin-3	ic50	0.0072	uM
N-[[1-[(2S,3R,4S,5R,6R)-2-[[(2S,3R,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-2-yl]disulfanyl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]triazol-4-yl]methyl]-3’,6’-dihydroxy-3-oxospiro[2-benzofuran-1,9’-xanthene]-5-carboxamide	1472920: Binding affinity to human galectin-3 expressed in Escherichia coli BL21(DE3) in presence of BSA by direct fluorescence polarization titration assay	kd	0.0087	uM
(2S,3R,4R,5R,6R)-2-[2-(1,3-benzothiazol-6-yl)-5-methyl-1,2,4-triazol-3-yl]-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-6-(hydroxymethyl)oxane-3,5-diol	1984893: Inhibition of human Galectin-3	ic50	0.0088	uM
(2R,3R,4S,5R,6S)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-6-[4-[5-chloro-2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0090	uM
5-[(2S,3R,4R,5R,6R)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-4-[5-chloro-2-(trifluoromethyl)phenyl]-2-methyl-1,2,4-triazole-3-thione	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0092	uM
(2S,3R,4R,5R,6R)-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-2-[2-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	1870977: Inhibition of His-tagged recombinant human Gal-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by time resolved fluorescence based assay	ic50	0.0097	uM
(2S,3R,4R,5R,6R)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-2-[4-[5-chloro-2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0100	uM
(2S,3R,4R,5R,6R)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-2-[4-[5-chloro-2-(trifluoromethoxy)phenyl]-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0110	uM
(2R,3R,4S,5R,6S)-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-6-[4-[5-chloro-2-(trifluoromethoxy)phenyl]-1,2,4-triazol-3-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0110	uM
(2R,3R,4S,5R,6S)-6-[2-(1,3-benzothiazol-6-yl)-5-methyl-1,2,4-triazol-3-yl]-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	1984893: Inhibition of human Galectin-3	ic50	0.0110	uM
(2S,3R,4R,5R,6R)-4-[4-(4-chloro-3,5-difluorophenyl)triazol-1-yl]-2-[4-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0120	uM
(2R,3R,4S,5R,6S)-6-[(3R,4R,5S)-4-hydroxy-5-[4-(2-methoxypyrimidin-5-yl)triazol-1-yl]oxan-3-yl]sulfanyl-2-(hydroxymethyl)-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0120	uM
(2R,3R,4S,5R,6S)-6-[2-(1,3-benzothiazol-6-yl)-5-methyl-1,2,4-triazol-3-yl]-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	1984893: Inhibition of human Galectin-3	ic50	0.0130	uM
(2S,3R,4R,5R,6R)-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-2-[4-[5-chloro-2-(trifluoromethoxy)phenyl]-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0130	uM
N-[(2R,5S)-5-[(2S,5S)-3,5-dihydroxy-6-(hydroxymethyl)-4-(naphthalen-2-ylmethoxy)oxan-2-yl]oxy-2-[2-[6-(2,5-dioxopyrrol-1-yl)hexanoylamino]ethoxy]-4-hydroxy-6-(hydroxymethyl)oxan-3-yl]-3-methoxybenzamide	1802696: Fluorescence Polarization Assay from Article 10.1002/cbic.201600673: “Lactosamine-Based Derivatives as Tools to Delineate the Biological Functions of Galectins: Application to Skin Tissue Repair.”	kd	0.0140	uM
(2R,3R,4S,5R,6R)-N-(1,3-benzothiazol-6-yl)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-5-hydroxy-6-(hydroxymethyl)-3-methoxy-N-methyloxane-2-carboxamide	1984893: Inhibition of human Galectin-3	ic50	0.0140	uM
(2R,3R,4S,5R,6R)-N-(1,3-benzothiazol-6-yl)-4-[4-(3,4-dichloro-2-fluorophenyl)triazol-1-yl]-5-hydroxy-6-(hydroxymethyl)-3-methoxy-N-methyloxane-2-carboxamide	1685176: Inhibition of recombinant human His6-tagged Galectin-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by HTRF assay	ic50	0.0140	uM
N-butyl-1-[(2S,3R,4S,5R,6R)-2-[[(2S,3R,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-2-yl]disulfanyl]-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]triazole-4-carboxamide	1472914: Displacement of 3,3’-dideoxy-3-[4-(fluorescein-5-yl-carbonylaminomethyl)-1H-1,2,3-triazol-1-yl]-3’-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1,1’-sulfanediyl-di-beta D-galactopyranoside from human galectin 3 C-terminal domain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	kd	0.0150	uM
(2S,3R,4R,5R,6R)-4-[4-(4-chloro-3-fluorophenyl)triazol-1-yl]-2-[2-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	1870977: Inhibition of His-tagged recombinant human Gal-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by time resolved fluorescence based assay	ic50	0.0150	uM
methyl 6-[1-[(3S,4R,5R)-4-hydroxy-5-[(2S,3R,4S,5R,6R)-5-hydroxy-6-(hydroxymethyl)-3-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-2-yl]sulfanyloxan-3-yl]triazol-4-yl]pyridine-2-carboxylate	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0170	uM
(2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(3R,4R,5S)-4-hydroxy-5-(4-pyrazin-2-yltriazol-1-yl)oxan-3-yl]sulfanyl-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0180	uM
(2S,3R,4R,5R,6R)-2-[2-(1,3-benzothiazol-6-yl)-5-methyl-1,2,4-triazol-3-yl]-4-[4-(4-chloro-3,5-difluorophenyl)triazol-1-yl]-6-(hydroxymethyl)oxane-3,5-diol	1984893: Inhibition of human Galectin-3	ic50	0.0180	uM
(2R,3R,4S,5R,6R)-N-(1,3-benzothiazol-6-yl)-4-[4-(2,4-dichloro-3-fluorophenyl)triazol-1-yl]-5-hydroxy-6-(hydroxymethyl)-3-methoxy-N-methyloxane-2-carboxamide	1685176: Inhibition of recombinant human His6-tagged Galectin-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by HTRF assay	ic50	0.0180	uM
(2R,3R,4S,5R,6S)-4-[4-(4-bromo-2,3-difluorophenyl)triazol-1-yl]-6-[4-[5-chloro-2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-2-(hydroxymethyl)-5-(2,2,3,3-tetrafluoropropoxy)oxan-3-ol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0180	uM
(2S,3R,4R,5R,6R)-4-[4-(4-chloro-3,5-difluorophenyl)triazol-1-yl]-2-[2-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	1870977: Inhibition of His-tagged recombinant human Gal-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by time resolved fluorescence based assay	ic50	0.0190	uM
(2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(3R,4R,5S)-4-hydroxy-5-(4-pyridin-2-yltriazol-1-yl)oxan-3-yl]sulfanyl-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0190	uM
(2R,3R,4S,5R,6S)-6-[(3R,4R,5S)-5-[4-(5-fluoropyrimidin-2-yl)triazol-1-yl]-4-hydroxyoxan-3-yl]sulfanyl-2-(hydroxymethyl)-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0190	uM
(2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(3R,4R,5S)-4-hydroxy-5-(4-pyrimidin-5-yltriazol-1-yl)oxan-3-yl]sulfanyl-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0190	uM
(2R,3R,4S,5R,6S)-6-[2-(1,3-benzothiazol-6-yl)-5-methyl-1,2,4-triazol-3-yl]-4-[4-(4-chloro-3,5-difluorophenyl)triazol-1-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	1984893: Inhibition of human Galectin-3	ic50	0.0200	uM
(2S,3R,4R,5R,6R)-4-[4-(4-chloro-3-fluorophenyl)triazol-1-yl]-2-[4-[5-chloro-2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0200	uM
(2R,3R,4S,5R,6S)-6-[(3R,4R,5S)-5-[4-(4-aminopyrimidin-2-yl)triazol-1-yl]-4-hydroxyoxan-3-yl]sulfanyl-2-(hydroxymethyl)-5-methoxy-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxan-3-ol	1814263: Inhibition of biotin-asialofetuin binding to human Gal3 measured after 90 mins by HTRF competition assay	ic50	0.0200	uM
(2S,3R,4R,5R,6R)-4-[4-(3-chloro-4,5-difluorophenyl)triazol-1-yl]-2-[2-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)oxane-3,5-diol	1870977: Inhibition of His-tagged recombinant human Gal-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by time resolved fluorescence based assay	ic50	0.0210	uM
(2R,3R,4S,5R,6R)-N-(1,3-benzothiazol-6-yl)-4-[4-(4-chloro-2,3-difluorophenyl)triazol-1-yl]-5-hydroxy-6-(hydroxymethyl)-3-methoxy-N-methyloxane-2-carboxamide	1685176: Inhibition of recombinant human His6-tagged Galectin-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by HTRF assay	ic50	0.0210	uM
(2S,3R,4R,5R,6R)-2-[2-[5-chloro-2-(trifluoromethyl)phenyl]-5-methyl-1,2,4-triazol-3-yl]-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-3,5-diol	1870977: Inhibition of His-tagged recombinant human Gal-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by time resolved fluorescence based assay	ic50	0.0220	uM
(2R,3R,4S,5R,6S)-4-[4-(4-bromo-3-fluorophenyl)triazol-1-yl]-6-[4-[5-chloro-2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0220	uM
(2R,3R,4S,5R,6R)-N-(1,3-benzothiazol-6-yl)-5-hydroxy-6-(hydroxymethyl)-3-methoxy-N-methyl-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-2-carboxamide	1685176: Inhibition of recombinant human His6-tagged Galectin-3 preincubated for 30 mins followed by B-ASF addition measured after 1 hr by HTRF assay	ic50	0.0220	uM
(2R,3R,4S,5R,6S)-4-[4-(4-chloro-3,5-difluorophenyl)triazol-1-yl]-6-[4-[5-chloro-2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-2-(hydroxymethyl)-5-methoxyoxan-3-ol	2113957: Inhibition of his-tagged N-terminal recombinant human Gal-3 preincubated for 30 mins followed by Biotin-ASF addition and measured after 1 hr by HTRF assay	ic50	0.0220	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, increases expression, increases methylation	7
Valproic Acid	affects cotreatment, increases expression, affects expression	7
bisphenol A	decreases expression, increases expression, affects expression	4
Tetrachlorodibenzodioxin	increases expression	4
methylmercuric chloride	decreases expression, increases expression	3
trichostatin A	increases expression, affects cotreatment	3
Cisplatin	decreases reaction, increases expression, increases degradation, decreases response to substance	3
Cyclosporine	increases expression, decreases reaction	3
S-(1,2-dichlorovinyl)cysteine	decreases expression	2
mercuric bromide	increases expression, affects cotreatment	2
entinostat	increases expression, affects cotreatment	2
bisphenol S	decreases expression, increases expression	2
Vorinostat	affects cotreatment, increases expression	2
Leflunomide	increases expression	2
Panobinostat	affects cotreatment, increases expression	2
Dactinomycin	affects cotreatment, increases expression, decreases reaction	2
Diethylhexyl Phthalate	increases expression, decreases reaction, decreases expression	2
Doxorubicin	increases expression, decreases response to substance	2
Estradiol	affects cotreatment, decreases expression	2
Fluorouracil	affects response to substance, decreases response to substance	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Silicon Dioxide	affects reaction, decreases expression, increases abundance, increases expression, increases phosphorylation	2
Tretinoin	decreases expression, increases expression	2
aristolochic acid I	increases expression	1
GSK-J4	increases expression	1
dicrotophos	decreases expression	1
triphenyl phosphate	affects expression	1
pirinixic acid	affects binding, decreases expression, increases activity	1
benzo(b)fluoranthene	increases expression	1
1,12-benzoperylene	increases expression	1

ChEMBL screening assays

127 unique, capped per target: 127 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1005623	Binding	Binding affinity to galectin 3	Synthesis of stable and selective inhibitors of human galectins-1 and -3. — Bioorg Med Chem

Cellosaurus cell lines

11 cell lines: 10 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_5948	11-9-1-4	Cancer cell line	Female
CVCL_B8JP	Abcam HCT 116 LGALS3 KO	Cancer cell line	Male
CVCL_B9LY	Abcam A-549 LGALS3 KO	Cancer cell line	Male
CVCL_D2G5	Abcam MCF-7 LGALS3 KO	Cancer cell line	Female
CVCL_D4BX	HEK293T TetOff-SNCA-A53T mRuby3-Galectin-3 mClover3-Galectin-3	Transformed cell line	Female
CVCL_D7TI	Ubigene A-549 LGALS3 KO	Cancer cell line	Male
CVCL_E0WF	Ubigene JIMT-1 LGALS3 KO	Cancer cell line	Female
CVCL_F0QJ	U2OS-RFP-GAL3	Cancer cell line	Female
CVCL_SV48	HAP1 LGALS3 (-) 1	Cancer cell line	Male
CVCL_WG97	11-YX-1	Cancer cell line	Female

Clinical trials (associated diseases)

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