PTPN7
gene geneOn this page
Also known as HEPTPLC-PTP
Summary
PTPN7 (protein tyrosine phosphatase non-receptor type 7, HGNC:9659) is a protein-coding gene on chromosome 1q32.1, encoding Tyrosine-protein phosphatase non-receptor type 7 (P35236). Protein phosphatase that acts preferentially on tyrosine-phosphorylated MAPK1.
The protein encoded by this gene is a member of the protein tyrosine phosphatase (PTP) family. PTPs are known to be signaling molecules that regulate a variety of cellular processes including cell growth, differentiation, mitotic cycle, and oncogenic transformation. This gene is preferentially expressed in a variety of hematopoietic cells, and is an early response gene in lymphokine stimulated cells. The non-catalytic N-terminus of this PTP can interact with MAP kinases and suppress the MAP kinase activities. This PTP was shown to be involved in the regulation of T cell antigen receptor (TCR) signaling, which was thought to function through dephosphorylating the molecules related to MAP kinase pathway. Multiple alternatively spliced transcript variants have been found for this gene.
Source: NCBI Gene 5778 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 81 total
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_002832
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:9659 |
| Approved symbol | PTPN7 |
| Name | protein tyrosine phosphatase non-receptor type 7 |
| Location | 1q32.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | HEPTP, LC-PTP |
| Ensembl gene | ENSG00000143851 |
| Ensembl biotype | protein_coding |
| OMIM | 176889 |
| Entrez | 5778 |
Gene structure
Transcript identifiers
Ensembl transcripts: 25 — 17 protein_coding, 4 nonsense_mediated_decay, 2 retained_intron, 2 protein_coding_CDS_not_defined
ENST00000309017, ENST00000367279, ENST00000435759, ENST00000462815, ENST00000464870, ENST00000467283, ENST00000468385, ENST00000476061, ENST00000477554, ENST00000477625, ENST00000479092, ENST00000480836, ENST00000486116, ENST00000491584, ENST00000492451, ENST00000492977, ENST00000495688, ENST00000496197, ENST00000629151, ENST00000691036, ENST00000854611, ENST00000854612, ENST00000854613, ENST00000854614, ENST00000854615
RefSeq mRNA: 5 — MANE Select: NM_002832
NM_001199797, NM_001364877, NM_001364878, NM_002832, NM_080588
CCDS: CCDS1422, CCDS1423
Canonical transcript exons
ENST00000691036 — 10 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001927044 | 202160545 | 202160602 |
| ENSE00003519003 | 202157739 | 202157823 |
| ENSE00003552765 | 202154186 | 202154323 |
| ENSE00003581167 | 202155533 | 202155609 |
| ENSE00003676719 | 202153725 | 202153835 |
| ENSE00003685300 | 202152542 | 202152699 |
| ENSE00003693260 | 202150311 | 202150424 |
| ENSE00003790609 | 202158118 | 202158301 |
| ENSE00003928474 | 202147016 | 202148699 |
| ENSE00004282191 | 202159281 | 202159454 |
Expression profiles
Bgee: expression breadth ubiquitous, 185 present calls, max score 96.39.
FANTOM5 (CAGE): breadth broad, TPM avg 14.2904 / max 863.6909, expressed in 550 samples.
FANTOM5 promoters (10 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 16705 | 12.3266 | 529 |
| 16704 | 0.9593 | 187 |
| 16708 | 0.3261 | 106 |
| 16709 | 0.3165 | 110 |
| 16702 | 0.1913 | 109 |
| 16703 | 0.1089 | 27 |
| 16707 | 0.0292 | 10 |
| 16710 | 0.0165 | 6 |
| 16711 | 0.0104 | 4 |
| 16706 | 0.0056 | 1 |
Top tissues by expression
285 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| granulocyte | CL:0000094 | 96.39 | gold quality |
| lymph node | UBERON:0000029 | 92.07 | gold quality |
| bone marrow cell | CL:0002092 | 90.77 | gold quality |
| vermiform appendix | UBERON:0001154 | 90.06 | gold quality |
| thymus | UBERON:0002370 | 88.84 | gold quality |
| blood | UBERON:0000178 | 88.26 | gold quality |
| spleen | UBERON:0002106 | 88.11 | gold quality |
| adrenal tissue | UBERON:0018303 | 86.99 | gold quality |
| bone marrow | UBERON:0002371 | 84.84 | gold quality |
| right testis | UBERON:0004534 | 84.71 | gold quality |
| caecum | UBERON:0001153 | 84.37 | gold quality |
| left testis | UBERON:0004533 | 84.10 | gold quality |
| putamen | UBERON:0001874 | 83.67 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 81.98 | gold quality |
| testis | UBERON:0000473 | 81.85 | gold quality |
| leukocyte | CL:0000738 | 81.68 | gold quality |
| caudate nucleus | UBERON:0001873 | 81.44 | gold quality |
| gall bladder | UBERON:0002110 | 80.79 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 80.72 | gold quality |
| mononuclear cell | CL:0000842 | 80.60 | gold quality |
| monocyte | CL:0000576 | 80.53 | gold quality |
| ileal mucosa | UBERON:0000331 | 80.26 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 79.83 | gold quality |
| left adrenal gland | UBERON:0001234 | 79.45 | gold quality |
| adrenal gland | UBERON:0002369 | 79.33 | gold quality |
| right adrenal gland | UBERON:0001233 | 78.93 | gold quality |
| tonsil | UBERON:0002372 | 78.90 | gold quality |
| adrenal cortex | UBERON:0001235 | 78.68 | gold quality |
| rectum | UBERON:0001052 | 78.51 | gold quality |
| small intestine | UBERON:0002108 | 78.41 | gold quality |
Single-cell (SCXA)
Detected in 6 experiment(s), a significant marker in 5.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-9467 | yes | 33.09 |
| E-MTAB-10287 | yes | 29.19 |
| E-CURD-112 | yes | 9.05 |
| E-HCAD-10 | yes | 6.68 |
| E-GEOD-70580 | no | 922.59 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
81 targeting PTPN7, 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-6851-5P | 100.00 | 65.63 | 1294 |
| HSA-MIR-4510 | 100.00 | 66.60 | 2050 |
| HSA-MIR-6127 | 100.00 | 66.76 | 2188 |
| HSA-MIR-6129 | 100.00 | 66.46 | 2080 |
| HSA-MIR-6130 | 100.00 | 66.69 | 2012 |
| HSA-MIR-6133 | 100.00 | 66.48 | 2064 |
| HSA-MIR-3689D | 100.00 | 66.14 | 1181 |
| HSA-MIR-4500 | 99.99 | 72.72 | 2367 |
| HSA-MIR-6778-3P | 99.96 | 67.29 | 2693 |
| HSA-MIR-6825-5P | 99.96 | 69.81 | 3431 |
| HSA-MIR-6721-5P | 99.93 | 68.92 | 2981 |
| HSA-MIR-4492 | 99.87 | 68.25 | 3611 |
| HSA-MIR-6079 | 99.84 | 68.54 | 1170 |
| 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-6764-5P | 99.75 | 67.89 | 2304 |
| HSA-MIR-4446-5P | 99.72 | 69.19 | 2544 |
| HSA-MIR-1200 | 99.71 | 70.42 | 1838 |
| HSA-MIR-4677-5P | 99.70 | 70.09 | 1940 |
| HSA-MIR-6715B-5P | 99.64 | 69.63 | 1420 |
| HSA-MIR-298 | 99.63 | 67.56 | 1916 |
| HSA-MIR-425-5P | 99.59 | 67.67 | 900 |
| HSA-MIR-1915-3P | 99.58 | 66.79 | 1988 |
| HSA-MIR-4269 | 99.55 | 69.89 | 1373 |
| HSA-MIR-105-5P | 99.54 | 69.24 | 2060 |
| HSA-MIR-7853-5P | 99.54 | 69.30 | 2055 |
| HSA-MIR-4753-5P | 99.54 | 68.51 | 1356 |
| HSA-MIR-4441 | 99.49 | 66.56 | 3216 |
| HSA-MIR-6081 | 99.48 | 66.07 | 1446 |
Literature-anchored findings (GeneRIF, showing 4)
- structure of the protein tyrosine phosphatase catalytic domain of HePTP, residues 44-339 (PMID:16226275)
- determined high-resolution structures of all of the human family members of Mitogen-Activated Protein Kinase-specific protein tyrosine phosphatases (PMID:16441242)
- Interactions at the active site between KIM (kinase interaction motif)-phosphatases and their substrates are predominantly nonspecific, with the majority of the KIM-phosphatase residues coordinating the peptide backbone rather than residue side chains. (PMID:19053285)
- PTPN7 regulates platelet functional responses downstream of GPCR agonists, but not GPVI agonists, through inhibition of ERK activation and thromboxane generation. (PMID:31266805)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Ptpn7 | ENSMUSG00000031506 |
| rattus_norvegicus | Ptpn7 | ENSRNOG00000005807 |
Paralogs (35): PTPRN (ENSG00000054356), PTPRU (ENSG00000060656), PTPN3 (ENSG00000070159), PTPN21 (ENSG00000070778), PTPN18 (ENSG00000072135), PTPN23 (ENSG00000076201), PTPRH (ENSG00000080031), PTPRC (ENSG00000081237), PTPN4 (ENSG00000088179), PTPRS (ENSG00000105426), PTPRZ1 (ENSG00000106278), PTPN5 (ENSG00000110786), PTPN6 (ENSG00000111679), PTPRB (ENSG00000127329), PTPN12 (ENSG00000127947), PTPRE (ENSG00000132334), PTPRA (ENSG00000132670), PTPN22 (ENSG00000134242), PTPRF (ENSG00000142949), PTPRG (ENSG00000144724), PTPRJ (ENSG00000149177), PTPRO (ENSG00000151490), PTPN14 (ENSG00000152104), PTPRK (ENSG00000152894), PTPRR (ENSG00000153233), PTPRD (ENSG00000153707), PTPRN2 (ENSG00000155093), PTPN13 (ENSG00000163629), PTPN9 (ENSG00000169410), PTPRM (ENSG00000173482), PTPN2 (ENSG00000175354), PTPN11 (ENSG00000179295), PTPRT (ENSG00000196090), PTPN1 (ENSG00000196396), PTPN20 (ENSG00000204179)
Protein
Protein identifiers
Tyrosine-protein phosphatase non-receptor type 7 — P35236 (reviewed: P35236)
Alternative names: Hematopoietic protein-tyrosine phosphatase, Protein-tyrosine phosphatase LC-PTP
All UniProt accessions (12): P35236, C9IYI6, C9JAW7, C9JBA9, E7EUM0, E9PE54, F8WEY3, F8WF08, F8WF66, H7C4T8, H7C5I3, J3KR55
UniProt curated annotations — full annotation on UniProt →
Function. Protein phosphatase that acts preferentially on tyrosine-phosphorylated MAPK1. Plays a role in the regulation of T and B-lymphocyte development and signal transduction.
Subunit / interactions. Monomer. Interacts with MAPK1, MAPK3 and several other MAP kinases.
Subcellular location. Cytoplasm. Cytoskeleton.
Tissue specificity. Expressed exclusively in thymus and spleen.
Post-translational modifications. Phosphorylated on serine residues in resting T-cells. Phosphorylation increases upon exposure to stimuli that increase intracellular cAMP levels. Phosphorylation leads to dissociation of bound MAP kinases. Oxidized at active site cysteine. Treatment with pervanadate (vanadate and H(2)O(2)) or with antigen enhanced oxidation of active site cysteine.
Activity regulation. Inhibited in cells after FCER1A triggering.
Similarity. Belongs to the protein-tyrosine phosphatase family. Non-receptor class subfamily.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P35236-1 | 1 | yes |
| P35236-2 | 2 | |
| P35236-3 | 3 |
RefSeq proteins (5): NP_001186726, NP_001351806, NP_001351807, NP_002823, NP_542155 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000242 | PTP_cat | Domain |
| IPR000387 | Tyr_Pase_dom | Domain |
| IPR003595 | Tyr_Pase_cat | Domain |
| IPR008356 | Tyr_Pase_KIM-con | Family |
| IPR016130 | Tyr_Pase_AS | Active_site |
| IPR029021 | Prot-tyrosine_phosphatase-like | Homologous_superfamily |
Pfam: PF00102
Enzyme classification (BRENDA):
- EC 3.1.3.48 — protein-tyrosine-phosphatase (BRENDA: 59 organisms, 501 substrates, 1326 inhibitors, 270 Km, 165 kcat entries)
Substrate kinetics (BRENDA)
70 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| 4-NITROPHENYL PHOSPHATE | 0.0008–148 | 84 |
| 6,8-DIFLUORO-4-METHYLUMBELLIFERYL PHOSPHATE | 0.0039–0.862 | 27 |
| P-NITROPHENYL PHOSPHATE | 0.0024–10 | 20 |
| DADEPYLIPQQG | 0.0003–0.1 | 12 |
| PHOSPHOTYROSINE | 0.012–30 | 11 |
| LYSOZYME | 0.0003–0.012 | 5 |
| MYELIN BASIC PROTEIN | 0.0001–0.022 | 5 |
| ACETYL-DADEPY-NH2 | 0.0228–0.219 | 4 |
| ACETYL-DADEPYL-NH2 | 1.1–97.5 | 4 |
| 4,6,8-TRIMETHYL-2-OXO-2H-CHROMEN-7-YL DIHYDROGEN | 0.02–0.156 | 3 |
| SASASPYSASA | 0.53–2.3 | 3 |
| 1-NAPHTHYL PHOSPHATE | 1.19–1.88 | 2 |
| 3,6-FLUORESCEIN DIPHOSPHATE | 15–19 | 2 |
| 4-METHYLUMBELLIFERYL PHOSPHATE | 0.953–2.41 | 2 |
| BOVINE SERUM ALBUMIN | 0.0001–0.0003 | 2 |
Catalyzed reactions (Rhea), 1 shown:
- O-phospho-L-tyrosyl-[protein] + H2O = L-tyrosyl-[protein] + phosphate (RHEA:10684)
UniProt features (54 total): helix 14, strand 13, mutagenesis site 8, modified residue 6, sequence conflict 3, binding site 3, splice variant 2, region of interest 2, chain 1, domain 1, active site 1
Structure
Experimental structures (PDB)
14 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 1ZC0 | X-RAY DIFFRACTION | 1.85 |
| 2GPH | X-RAY DIFFRACTION | 1.9 |
| 3D44 | X-RAY DIFFRACTION | 1.9 |
| 3O4S | X-RAY DIFFRACTION | 1.9 |
| 2QDC | X-RAY DIFFRACTION | 2 |
| 2GP0 | X-RAY DIFFRACTION | 2.05 |
| 2QDM | X-RAY DIFFRACTION | 2.05 |
| 8YP8 | X-RAY DIFFRACTION | 2.14 |
| 3O4U | X-RAY DIFFRACTION | 2.25 |
| 2HVL | X-RAY DIFFRACTION | 2.4 |
| 3D42 | X-RAY DIFFRACTION | 2.46 |
| 2A3K | X-RAY DIFFRACTION | 2.55 |
| 3O4T | X-RAY DIFFRACTION | 2.6 |
| 2QDP | X-RAY DIFFRACTION | 2.72 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P35236-F1 | 86.39 | 0.70 |
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): 291 (phosphocysteine intermediate)
Ligand- & substrate-binding residues (3): 257; 291–297; 335
Post-translational modifications (6): 93, 110, 143, 291, 44, 66
Mutagenesis-validated functional residues (8):
| Position | Phenotype |
|---|---|
| 44 | prevents dissociation of bound map kinase and enhances their dephosphorylation. |
| 44 | reduces binding of map kinase. |
| 66 | prevents dissociation of bound map kinase and enhances their dephosphorylation; when associated with a-93. |
| 93 | prevents dissociation of bound map kinase and enhances their dephosphorylation; when associated with a-66. |
| 125 | strongly reduced catalytic activity. |
| 257 | loss of catalytic activity. |
| 291 | loss of catalytic activity. |
| 335 | reduced catalytic activity. |
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-5675221 | Negative regulation of MAPK pathway |
| R-HSA-9008059 | Interleukin-37 signaling |
MSigDB gene sets: 169 (showing top):
WALLACE_PROSTATE_CANCER_RACE_UP, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, KEGG_MAPK_SIGNALING_PATHWAY, MODULE_45, AP4_Q6, MODULE_16, ADDYA_ERYTHROID_DIFFERENTIATION_BY_HEMIN, MODULE_118, WEI_MYCN_TARGETS_WITH_E_BOX, AML_Q6, PID_TCR_RAS_PATHWAY, MODULE_213, ZHAN_V1_LATE_DIFFERENTIATION_GENES_DN, MARZEC_IL2_SIGNALING_UP, MAF_Q6
GO Biological Process (4): MAPK cascade (GO:0000165), protein dephosphorylation (GO:0006470), signal transduction (GO:0007165), dephosphorylation (GO:0016311)
GO Molecular Function (5): protein tyrosine phosphatase activity (GO:0004725), non-membrane spanning protein tyrosine phosphatase activity (GO:0004726), phosphoprotein phosphatase activity (GO:0004721), protein binding (GO:0005515), hydrolase activity (GO:0016787)
GO Cellular Component (7): nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), cytoplasmic side of plasma membrane (GO:0009898), microtubule cytoskeleton (GO:0015630), mitotic spindle (GO:0072686), cytoskeleton (GO:0005856)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| RAF/MAP kinase cascade | 1 |
| Interleukin-1 family signaling | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| intracellular signaling cassette | 1 |
| dephosphorylation | 1 |
| protein modification process | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| phosphate-containing compound metabolic process | 1 |
| phosphoprotein phosphatase activity | 1 |
| protein tyrosine phosphatase activity | 1 |
| phosphatase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| catalytic activity | 1 |
| nuclear lumen | 1 |
| intracellular anatomical structure | 1 |
| cytoplasm | 1 |
| plasma membrane | 1 |
| cytoplasmic side of membrane | 1 |
| cytoskeleton | 1 |
| spindle | 1 |
| intracellular membraneless organelle | 1 |
Protein interactions and networks
STRING
1266 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PTPN7 | PTS | Q03393 | 923 |
| PTPN7 | MAPK1 | P28482 | 919 |
| PTPN7 | MAPK14 | Q16539 | 700 |
| PTPN7 | DUSP3 | P51452 | 640 |
| PTPN7 | MAPK3 | P27361 | 575 |
| PTPN7 | DUSP6 | Q16828 | 558 |
| PTPN7 | MAP2K1 | Q02750 | 537 |
| PTPN7 | RPS6KA1 | Q15418 | 530 |
| PTPN7 | OSBP | P22059 | 520 |
| PTPN7 | RPS6KA3 | P51812 | 516 |
| PTPN7 | PTPN11 | Q06124 | 516 |
| PTPN7 | DUSP23 | Q9BVJ7 | 488 |
| PTPN7 | PLPP1 | O14494 | 472 |
| PTPN7 | ACP1 | P24666 | 463 |
| PTPN7 | DUSP10 | Q9Y6W6 | 461 |
IntAct
27 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| PTPN7 | MAPK1 | psi-mi:“MI:0915”(physical association) | 0.770 |
| PTPN7 | MAPK1 | psi-mi:“MI:2364”(proximity) | 0.770 |
| PTPN7 | MAPK1 | psi-mi:“MI:0203”(dephosphorylation reaction) | 0.770 |
| PTPN7 | Mapk14 | psi-mi:“MI:0915”(physical association) | 0.590 |
| Mapk14 | PTPN7 | psi-mi:“MI:0915”(physical association) | 0.590 |
| PTPN7 | CCDC57 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PTPN7 | FLJ13057 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CCDC57 | PTPN7 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FLJ13057 | PTPN7 | psi-mi:“MI:0915”(physical association) | 0.560 |
| Mapk1 | PTPN7 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| PTPN7 | AATK | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | EGFR | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | ERBB3 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | ROR2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | PTK7 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | EPHA2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | ERBB4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | IGF1R | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN7 | MAPK14 | psi-mi:“MI:2364”(proximity) | 0.270 |
| PTPN7 | CDH2 | psi-mi:“MI:0203”(dephosphorylation reaction) | 0.000 |
BioGRID (84): GMCL1 (Two-hybrid), CCDC57 (Two-hybrid), MAPK1 (Co-localization), MAPK14 (Co-localization), PTPN7 (Biochemical Activity), PTPN7 (Biochemical Activity), PTPN7 (Two-hybrid), PTPN7 (Two-hybrid), PTPN7 (Two-hybrid), DHPS (Affinity Capture-MS), MAPK1 (Affinity Capture-MS), MAPK14 (Affinity Capture-MS), MAPK3 (Affinity Capture-MS), ME1 (Affinity Capture-MS), OPA1 (Affinity Capture-MS)
ESM2 similar proteins: A2ALK8, A5D6R3, B2GV87, O08617, O35239, O55082, P0C599, P0C5A1, P18052, P18433, P23469, P25044, P26045, P28202, P28204, P28205, P28206, P28209, P28219, P29350, P29351, P35234, P35235, P35236, P41499, P43378, P49445, P49446, P54755, P54830, P81718, Q03348, Q06124, Q15256, Q4JDL3, Q4RQD3, Q5I127, Q5I139, Q5I141, Q5I142
Diamond homologs: A0A6I8TCE0, A1L1L3, A2ALK8, A4IFW2, B0V2N1, B0X4T2, B1AUH1, B2GV87, B2RU80, B3DK56, B9EKR1, E9Q0N2, E9Q612, F1NWE3, G5EC24, G5EGJ9, H2KZM6, O02695, O08617, O13016, O35239, O55082, P06800, P16620, P17706, P18031, P18052, P18433, P20417, P23467, P23468, P23469, P23470, P23471, P26045, P28191, P29074, P29350, P29351, P29352
SIGNOR signaling
22 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CD40LG | down-regulates | PTPN7 | |
| PRKACA | down-regulates | PTPN7 | phosphorylation |
| PTPN7 | down-regulates | MAPK14 | binding |
| PTPN7 | “down-regulates activity” | MAPK1 | dephosphorylation |
| PTPN7 | “down-regulates activity” | MAPK14 | dephosphorylation |
| PRKCQ | “up-regulates activity” | PTPN7 | phosphorylation |
| PTPN7 | down-regulates | MAPK1 | dephosphorylation |
| MAPK1 | “up-regulates activity” | PTPN7 | phosphorylation |
| MAPK3 | “up-regulates activity” | PTPN7 | phosphorylation |
| MAPK14 | “down-regulates activity” | PTPN7 | phosphorylation |
| Gbeta | “up-regulates activity” | PTPN7 | phosphorylation |
| ERK1/2 | “up-regulates activity” | PTPN7 | phosphorylation |
| PRKD1 | “up-regulates activity” | PTPN7 | phosphorylation |
| PRKCZ | “up-regulates activity” | PTPN7 | phosphorylation |
| PRKCD | “up-regulates activity” | PTPN7 | phosphorylation |
| PRKCH | “up-regulates activity” | PTPN7 | phosphorylation |
| PRKCE | “up-regulates activity” | PTPN7 | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 15 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 |
|---|---|---|---|
| positive regulation of MAPK cascade | 5 | 33.6× | 2e-05 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
81 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 62 |
| Likely benign | 4 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2071 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:202148696:CCCT:C | acceptor_gain | 1.0000 |
| 1:202148697:CCT:C | acceptor_gain | 1.0000 |
| 1:202148697:CCTC:C | acceptor_gain | 1.0000 |
| 1:202148698:CT:C | acceptor_gain | 1.0000 |
| 1:202148698:CTC:C | acceptor_gain | 1.0000 |
| 1:202148699:TCTGC:T | acceptor_gain | 1.0000 |
| 1:202152537:CGCA:C | donor_loss | 1.0000 |
| 1:202152538:GCA:G | donor_loss | 1.0000 |
| 1:202152539:CA:C | donor_loss | 1.0000 |
| 1:202152540:ACCT:A | donor_loss | 1.0000 |
| 1:202152696:GGTA:G | acceptor_gain | 1.0000 |
| 1:202152697:GTA:G | acceptor_gain | 1.0000 |
| 1:202152698:TA:T | acceptor_gain | 1.0000 |
| 1:202152698:TAC:T | acceptor_loss | 1.0000 |
| 1:202152700:C:CC | acceptor_gain | 1.0000 |
| 1:202152701:T:A | acceptor_loss | 1.0000 |
| 1:202152705:T:TC | acceptor_gain | 1.0000 |
| 1:202153721:GTA:G | donor_loss | 1.0000 |
| 1:202153722:TA:T | donor_loss | 1.0000 |
| 1:202153723:ACCT:A | donor_loss | 1.0000 |
| 1:202153831:CATTT:C | acceptor_gain | 1.0000 |
| 1:202153832:ATTT:A | acceptor_gain | 1.0000 |
| 1:202153833:TTT:T | acceptor_gain | 1.0000 |
| 1:202153834:TT:T | acceptor_gain | 1.0000 |
| 1:202153834:TTCTA:T | acceptor_loss | 1.0000 |
| 1:202153835:TCTA:T | acceptor_loss | 1.0000 |
| 1:202153836:C:A | acceptor_loss | 1.0000 |
| 1:202153837:T:G | acceptor_loss | 1.0000 |
| 1:202154184:ACCT:A | donor_gain | 1.0000 |
| 1:202154185:CCTC:C | donor_gain | 1.0000 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000434821 (1:202162125 T>C), RS1000493902 (1:202158468 C>T), RS1000543952 (1:202153788 G>A), RS1000602285 (1:202152834 A>C), RS1001040410 (1:202163276 G>A), RS1001085084 (1:202147957 G>A,T), RS1001105306 (1:202147545 G>A), RS1001229189 (1:202150258 G>A), RS1001264429 (1:202148944 C>T), RS1001317357 (1:202160303 A>G,T), RS1001324290 (1:202156116 A>C), RS1001868389 (1:202159121 G>C), RS1002284043 (1:202157338 C>T), RS1002388356 (1:202151970 G>A), RS1002562499 (1:202163398 A>G)
Disease associations
OMIM: gene MIM:176889 | 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 |
|---|---|---|
| GCST001930_15 | Breast cancer | 1.000000e-08 |
| GCST90002380_117 | Basophil percentage of white cells | 5.000000e-10 |
| GCST90002380_118 | Basophil percentage of white cells | 6.000000e-10 |
| GCST90002397_789 | Mean spheric corpuscular volume | 3.000000e-12 |
| GCST90002400_534 | Plateletcrit | 9.000000e-19 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007992 | basophil percentage of leukocytes |
| EFO:0007985 | platelet crit |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2219 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 327,449 (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 |
|---|---|---|---|
| CHEMBL1440 | TETRACYCLINE | 4 | 324,384 |
| CHEMBL1632 | CEPHALOTHIN SODIUM | 4 | 3,065 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
316 measured of 520 human assays (581 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| MLS000116276 | EC50 | 0.00207 nM |
| 2-[[7-(2-furanylmethyl)-5,6-diphenyl-4-pyrrolo[2,3-d]pyrimidinyl]amino]ethanol | EC50 | 0.00424 nM |
| SMR000071260 | EC50 | 15.5 nM |
| 3-[2-(hydroximinomethyl)pyrrol-1-yl]benzoic acid | IC50 | 23 nM |
| 4-chloranyl-N-(3,4-dihydro-2H-thiochromen-4-yl)-3-sulfamoyl-benzamide | IC50 | 121 nM |
| 7-hexacosenoic acid | IC50 | 220 nM |
| 4-amino-3-(4-methylphenyl)-5-[(4-methyl-1-piperazinyl)carbonyl]-1,3-thiazole-2(3H)-thione | IC50 | 250 nM |
| 1-(2,6-dichlorophenyl)-3-(2-phenylethyl)thiourea | IC50 | 342 nM |
| 4-[[2-bromanyl-4-[(E)-2-cyano-2-(3-fluorophenyl)ethenyl]phenoxy]methyl]benzoic acid | IC50 | 400 nM |
| 2-[2-chloranyl-6-ethoxy-4-[(E)-[2-(naphthalen-2-ylamino)-4-oxidanylidene-1,3-thiazol-5-ylidene]methyl]phenoxy]ethanoic acid | IC50 | 440 nM |
| MLS-0054638.0001 | IC50 | 478 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-(2-methoxyethyl)urea | IC50 | 492 nM |
| MLS000050448 | IC50 | 716 nM |
| MLS-0109562.0001 | IC50 | 727 nM |
| cid_6161440 | IC50 | 730 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-(2-phenylethyl)urea | IC50 | 814 nM |
| Cephalothin | IC50 | 920 nM |
| 2-[4-[(E)-[[4-[2-(4-chloroanilino)-1,3-thiazol-4-yl]benzoyl]hydrazinylidene]methyl]phenoxy]acetic acid | IC50 | 924 nM |
| 3-[(5E)-5-[[4-[(4-chlorophenyl)methoxy]-3-methoxyphenyl]methylidene]-4-oxo-2-sulfanylidene-3-thiazolidinyl]benzoic acid | IC50 | 953 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-butylurea | IC50 | 966 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-phenylurea | IC50 | 968 nM |
| 2-[4-[(Z)-[2-(4-fluoroanilino)-4-keto-2-thiazolin-5-ylidene]methyl]phenoxy]acetic acid methyl ester | IC50 | 1050 nM |
| 2-[3-[2-hydroxyethyl(dimethyl)azaniumyl]propanoylamino]-2-methyl-propane-1-sulfonate | EC50 | 1160 nM |
| 2-[2-chloranyl-6-methoxy-4-[(Z)-[3-[2-[(4-methylphenyl)amino]-2-oxidanylidene-ethyl]-2,4-bis(oxidanylidene)-1,3-thiazolidin-5-ylidene]methyl]phenoxy]ethanoic acid | IC50 | 1180 nM |
| 2-[2,6-bis(chloranyl)-4-[(Z)-[3-[2-[(4-methylphenyl)amino]-2-oxidanylidene-ethyl]-2,4-bis(oxidanylidene)-1,3-thiazolidin-5-ylidene]methyl]phenoxy]ethanoic acid | IC50 | 1200 nM |
| (7Z)-3-bromanyl-7-(furan-2-ylmethylidene)-[1,3]thiazolo[4,5]imidazo[1,2-b]pyridin-8-one | IC50 | 1230 nM |
| 3-(2-{(E)-[1-(4-chlorophenyl)-2,5-dioxoimidazolidin-4-ylidene]methyl}-1H-pyrrol-1-yl)benzoic acid | IC50 | 1230 nM |
| 3-[(5E)-5-[1-(2-chlorobenzyl)-2-keto-indolin-3-ylidene]-4-keto-2-thioxo-thiazolidin-3-yl]propionic acid | IC50 | 1230 nM |
| 2-[5-[(Z)-(3-bromanyl-8-oxidanylidene-[1,3]thiazolo[4,5]imidazo[1,2-b]pyridin-7-ylidene)methyl]furan-2-yl]benzoic acid | IC50 | 1250 nM |
| 3-(3-chloranyl-4-methoxy-phenyl)-1-(3-methylbutyl)-1-(1-propan-2-ylpiperidin-4-yl)thiourea | IC50 | 1260 nM |
| 4-[3-[(5Z)-4-keto-2-thioxo-5-veratrylidene-thiazolidin-3-yl]propanoylamino]benzoic acid | IC50 | 1270 nM |
| 2-[4-[[[4-[2-(4-chloroanilino)-1,3-thiazol-4-yl]benzoyl]hydrazinylidene]methyl]phenoxy]acetic acid | IC50 | 1300 nM |
| 3-[[2,3-bis(2-furyl)quinoxalin-6-yl]carbamoylamino]propionic acid ethyl ester | IC50 | 1420 nM |
| 1-ethyl-6-methyl-3-[(E)-2-phenylethenyl]pyrimido[5,4-e][1,2,4]triazine-5,7-dione | EC50 | 1440 nM |
| cid_9595040 | IC50 | 1490 nM |
| 2-hydroxy-4-({4-[5-(2-methyl-3-phenyl-2-propen-1-ylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]butanoyl}amino)benzoic acid | IC50 | 1560 nM |
| MLS-0202048.0001 | IC50 | 1600 nM |
| 1,3,6-Trimethyl-1H-pyrimido[5,4-e][1,2,4]triazine-5,7-dione | EC50 | 1610 nM |
| 4-keto-5-methyl-2-[(E)-2-(4-methyl-3-nitro-phenyl)vinyl]-3H-thieno[2,3-d]pyrimidine-6-carboxylic acid | IC50 | 1620 nM |
| 9-octacosynoic acid | IC50 | 1760 nM |
| 1,6-dimethyl-3-propyl-pyrimido[5,4-e][1,2,4]triazine-5,7-dione | EC50 | 1770 nM |
| MLS-0336006.0001 | IC50 | 1830 nM |
| 4-[[5-(4-bromophenyl)-2-furoyl]thiocarbamoylamino]benzoic acid | IC50 | 1880 nM |
| 5,6-dihydro-4H-cyclopenta[b]thiophene-2-carboxylic acid [2-[(1,1-diketothiolan-3-yl)-isobutyl-amino]-2-keto-ethyl] ester | IC50 | 1910 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-(1-naphthalenyl)urea | IC50 | 2040 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-(4-chlorophenyl)urea | IC50 | 2140 nM |
| 2-(5,6-dihydro-4H-cyclopent[d]isoxazole-3-carbonylamino)benzoic acid methyl ester | IC50 | 2180 nM |
| N-[5-(1,3-benzothiazol-2-yl)-2-methylphenyl]-2-chloro-5-(4H-1,2,4-triazol-4-yl)benzamide | IC50 | 2210 nM |
| 1-[2,3-bis(2-furanyl)-6-quinoxalinyl]-3-methylurea | IC50 | 2300 nM |
| MLS000527911 | IC50 | 2310 nM |
ChEMBL bioactivities
315 potent at pChembl≥5 of 441 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.84 | IC50 | 14.4 | nM | CHEMBL1605172 |
| 7.60 | IC50 | 25 | nM | CHEMBL1322542 |
| 7.46 | IC50 | 34.5 | nM | CHEMBL1408579 |
| 7.23 | IC50 | 58.6 | nM | CHEMBL1304193 |
| 7.18 | IC50 | 66 | nM | CHEMBL1460470 |
| 7.07 | IC50 | 84.6 | nM | CHEMBL1608642 |
| 7.00 | IC50 | 100 | nM | CEFAMANDOLE SODIUM |
| 6.98 | IC50 | 105 | nM | CHEMBL1445488 |
| 6.97 | IC50 | 108 | nM | CHEMBL1505246 |
| 6.90 | IC50 | 125 | nM | CHEMBL454668 |
| 6.90 | IC50 | 127 | nM | CHEMBL1603381 |
| 6.89 | IC50 | 130 | nM | CHEMBL4750435 |
| 6.89 | IC50 | 129 | nM | CHEMBL1407203 |
| 6.80 | IC50 | 159 | nM | CHEMBL1371869 |
| 6.75 | IC50 | 180 | nM | CHEMBL1448629 |
| 6.71 | IC50 | 196 | nM | CHEMBL1447397 |
| 6.71 | IC50 | 193 | nM | CHEMBL1701224 |
| 6.70 | IC50 | 200 | nM | CHEMBL492894 |
| 6.70 | IC50 | 200 | nM | CHEMBL1527520 |
| 6.70 | IC50 | 198 | nM | CHEMBL1501132 |
| 6.68 | IC50 | 209 | nM | CHEMBL1536896 |
| 6.64 | IC50 | 227 | nM | CHEMBL1393151 |
| 6.60 | IC50 | 250 | nM | CHEMBL454668 |
| 6.59 | IC50 | 256 | nM | CHEMBL1407368 |
| 6.55 | IC50 | 280 | nM | CHEMBL1334633 |
| 6.55 | IC50 | 284 | nM | CHEMBL1449836 |
| 6.55 | IC50 | 280 | nM | CHEMBL1526088 |
| 6.52 | IC50 | 304 | nM | CHEMBL1414679 |
| 6.51 | IC50 | 312 | nM | CHEMBL1438889 |
| 6.50 | IC50 | 314 | nM | CHEMBL1393151 |
| 6.48 | IC50 | 329 | nM | CHEMBL1371777 |
| 6.48 | IC50 | 331 | nM | CHEMBL1327648 |
| 6.46 | IC50 | 343 | nM | CHEMBL1390354 |
| 6.43 | IC50 | 373 | nM | CHEMBL1732016 |
| 6.41 | IC50 | 391 | nM | CHEMBL1414679 |
| 6.41 | IC50 | 394 | nM | CHEMBL1704862 |
| 6.40 | IC50 | 400 | nM | CHEMBL1539325 |
| 6.39 | IC50 | 410 | nM | CHEMBL1324051 |
| 6.39 | IC50 | 410 | nM | CHEMBL1376870 |
| 6.38 | IC50 | 420 | nM | CHEMBL1978364 |
| 6.38 | IC50 | 420 | nM | CHEMBL259355 |
| 6.38 | IC50 | 419 | nM | CHEMBL1424189 |
| 6.35 | IC50 | 447 | nM | CHEMBL1408579 |
| 6.35 | IC50 | 450 | nM | CHEMBL1715328 |
| 6.34 | IC50 | 455 | nM | CHEMBL1605172 |
| 6.34 | IC50 | 452 | nM | CHEMBL1702580 |
| 6.33 | IC50 | 472 | nM | CHEMBL1725599 |
| 6.33 | IC50 | 466 | nM | CHEMBL1732016 |
| 6.33 | IC50 | 465 | nM | CHEMBL1488869 |
| 6.32 | IC50 | 483 | nM | CHEMBL501993 |
PubChem BioAssay actives
32 with measured affinity, of 171 total; 30 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 |
|---|---|---|---|---|
| 2-[4,5-bis(1,3,2-dithiarsolan-2-yl)-3-hydroxy-6-oxoxanthen-9-yl]benzoic acid | 1495216: Inhibition of allosterically sensitized mutant form of His6-tagged human HePTP catalytic domain using pNPP as substrate incubated for 90 mins by quenched phosphatase activity assay | ic50 | 0.1250 | uM |
| 4-[1-(4-methoxyphenyl)-3-(2-oxochromen-7-yl)pyrrolo[2,3-b]pyridin-5-yl]benzoic acid | 1706923: Inhibition of PTPN7 (unknown origin) pre-incubated for 20 mins followed by fluorescence substrate addition and measured after 120 mins by DiFMUP assay | ic50 | 0.1300 | uM |
| 3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid | 2037695: Inhibition of HEPTP (unknown origin) using pNPP as substrate by high-throughput screening assay | ic50 | 0.2000 | uM |
| 2-[(5Z)-5-[[3-[4-[(4-chlorophenyl)methoxy]phenyl]-1-phenylpyrazol-4-yl]methylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]ethanesulfonic acid | 443925: Inhibition of recombinant HePTP | ic50 | 0.6200 | uM |
| 2-[4-[(Z)-[5-(4-chlorophenyl)-7-methyl-3-oxo-6-propan-2-yloxycarbonyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]acetic acid | 569652: Competitive inhibition of recombinant HePTP expressed in Escherichia coli by Michaelis-Menten kinetic analysis | ki | 0.6900 | uM |
| 2-[(5Z)-5-[[3-[4-[(2-fluorophenyl)methoxy]phenyl]-1-phenylpyrazol-4-yl]methylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]ethanesulfonic acid | 443925: Inhibition of recombinant HePTP | ic50 | 0.8700 | uM |
| 6-hydroxy-3-iodo-1-methyl-2-[3-[[2-oxo-2-(4-thiophen-3-ylanilino)acetyl]amino]phenyl]indole-5-carboxylic acid | 1182542: Inhibition of HePTP (unknown origin) | ic50 | 1.0300 | uM |
| 2-[(5Z)-5-[[3-[4-[(2-chlorophenyl)methoxy]phenyl]-1-phenylpyrazol-4-yl]methylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]ethanesulfonic acid | 443925: Inhibition of recombinant HePTP | ic50 | 1.2000 | uM |
| 2-[4-[(Z)-[5-(4-chlorophenyl)-6-ethoxycarbonyl-7-methyl-3-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]acetic acid | 569641: Inhibition of recombinant HePTP expressed in Escherichia coli | ic50 | 1.3000 | uM |
| 2-[(5Z)-4-oxo-5-[[1-phenyl-3-(4-phenylmethoxyphenyl)pyrazol-4-yl]methylidene]-2-sulfanylidene-1,3-thiazolidin-3-yl]ethanesulfonic acid | 443925: Inhibition of recombinant HePTP | ic50 | 1.5000 | uM |
| 2-[4-[(Z)-[6-ethoxycarbonyl-7-methyl-5-(4-methylsulfanylphenyl)-3-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]acetic acid | 569641: Inhibition of recombinant HePTP expressed in Escherichia coli | ic50 | 1.8000 | uM |
| 6-hydroxy-2-phenyl-3-[2-[4-(trifluoromethoxy)phenyl]ethynyl]-1-benzofuran-5-carboxylic acid | 725030: Inhibition of HEPTP (unknown origin) expressed in Escherichia coli using pNPP substrate after 5 mins by spectrophotometric analysis | ic50 | 1.9000 | uM |
| 6-hydroxy-2-phenyl-3-[2-[3-(trifluoromethyl)phenyl]ethynyl]-1-benzofuran-5-carboxylic acid | 725030: Inhibition of HEPTP (unknown origin) expressed in Escherichia coli using pNPP substrate after 5 mins by spectrophotometric analysis | ic50 | 2.1000 | uM |
| 2-[(5Z)-4-oxo-5-[[1-phenyl-3-(4-piperidin-1-ylsulfonylphenyl)pyrazol-4-yl]methylidene]-2-sulfanylidene-1,3-thiazolidin-3-yl]ethanesulfonic acid | 443925: Inhibition of recombinant HePTP | ic50 | 2.4000 | uM |
| 3-[2-(3-chlorophenyl)ethynyl]-6-hydroxy-2-[4-[2-oxo-2-(propylamino)ethoxy]phenyl]-1-benzofuran-5-carboxylic acid | 755776: Inhibition of recombinant HEPTP (unknown origin) using pNPP as substrate by spectrophotometric analysis | ic50 | 3.0000 | uM |
| 3-[2-(3,5-difluorophenyl)ethynyl]-6-hydroxy-2-phenyl-1-benzofuran-5-carboxylic acid | 725030: Inhibition of HEPTP (unknown origin) expressed in Escherichia coli using pNPP substrate after 5 mins by spectrophotometric analysis | ic50 | 3.3000 | uM |
| 3-[1-[4-[(4-chloronaphthalen-1-yl)amino]-4-oxobutyl]triazol-4-yl]-6-hydroxy-2-(4-methylphenyl)-1-benzofuran-5-carboxylic acid | 566825: Inhibition of HePTP | ic50 | 3.6900 | uM |
| 6-hydroxy-2-(4-methoxyphenyl)-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]triazol-4-yl]-1-benzofuran-5-carboxylic acid | 566825: Inhibition of HePTP | ic50 | 3.7000 | uM |
| 2-[4-[(Z)-[5-(2-chlorophenyl)-6-ethoxycarbonyl-7-methyl-3-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]-2-methoxy-6-methylphenoxy]acetic acid | 569641: Inhibition of recombinant HePTP expressed in Escherichia coli | ic50 | 3.7000 | uM |
| 6-hydroxy-2-(4-methylphenyl)-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]triazol-4-yl]-1-benzofuran-5-carboxylic acid | 566825: Inhibition of HePTP | ic50 | 4.0700 | uM |
| 2-[4-[(Z)-[6-ethoxycarbonyl-5-(3-methoxyphenyl)-7-methyl-3-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]acetic acid | 569641: Inhibition of recombinant HePTP expressed in Escherichia coli | ic50 | 4.6000 | uM |
| 6-hydroxy-3-[1-[4-[(6-methoxy-1,3-benzothiazol-2-yl)amino]-4-oxobutyl]triazol-4-yl]-2-(3-methylphenyl)-1-benzofuran-5-carboxylic acid | 566825: Inhibition of HePTP | ic50 | 6.3600 | uM |
| (2S)-2-[4-[4-(2-benzyl-1-benzofuran-3-yl)phenyl]phenoxy]-3-phenylpropanoic acid | 1942820: Inhibition of HEPTP (unknown origin) | ic50 | 7.1000 | uM |
| 16221757 | 286242: Inhibition of HePTP | ic50 | 7.5000 | uM |
| 3-chloro-N-(5-methyl-1,3-benzothiazol-2-yl)-1-benzothiophene-2-carboxamide | 695227: Inhibition of HePTP expressed in Escherichia coli BL21 using pNPP substrate | ic50 | 8.0000 | uM |
| 2-(3-cyano-7,8-dimethylquinolin-2-yl)sulfanyl-N-cyclohexylacetamide | 695227: Inhibition of HePTP expressed in Escherichia coli BL21 using pNPP substrate | ic50 | 8.0000 | uM |
| 4-[1-(cyclohexylamino)-1-oxohexan-2-yl]oxy-2-hydroxy-5-[2-[2-(trifluoromethoxy)phenyl]ethynyl]benzoic acid | 1206789: Inhibition of HePTP (unknown origin) using pNPP as substrate at pH 7 at 25 degC by spectrophotometric analysis | ic50 | 8.7000 | uM |
| 2-[(5,6-dimethyl-4-oxo-3H-thieno[2,3-d]pyrimidin-2-yl)sulfanyl]-N-(6-ethoxy-1,3-benzothiazol-2-yl)acetamide | 695227: Inhibition of HePTP expressed in Escherichia coli BL21 using pNPP substrate | ic50 | 9.0000 | uM |
| (5Z)-3-(3-chlorophenyl)-5-[(4-hydroxy-3-methoxy-5-nitrophenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 1799621: PTP Assay from Article 10.1002/cbic.200600287: “Cellular inhibition of protein tyrosine phosphatase 1B by uncharged thioxothiazolidinone derivatives.” | ic50 | 9.3000 | uM |
| 2-(3-cyano-5,8-dimethylquinolin-2-yl)sulfanyl-N-(2-ethyl-6-methylphenyl)acetamide | 695227: Inhibition of HePTP expressed in Escherichia coli BL21 using pNPP substrate | ic50 | 10.0000 | uM |
CTD chemical–gene interactions
22 total (human), top 22 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| (+)-JQ1 compound | decreases expression | 2 |
| alpha phellandrene | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| sodium arsenite | increases expression | 1 |
| benzo(e)pyrene | decreases methylation | 1 |
| triphenyltin | decreases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| Grape Seed Proanthocyanidins | affects cotreatment, decreases expression | 1 |
| Acetaminophen | increases expression | 1 |
| Benzene | increases expression | 1 |
| Catechin | affects cotreatment, decreases expression | 1 |
| Curcumin | increases expression | 1 |
| Diuron | decreases expression | 1 |
| Lead | increases expression | 1 |
| Methapyrilene | decreases methylation | 1 |
| Nickel | increases expression | 1 |
| Oxygen | decreases expression | 1 |
| Rotenone | increases expression | 1 |
| Tretinoin | increases expression | 1 |
| Valproic Acid | increases methylation | 1 |
| Paclitaxel | increases expression | 1 |
| Antirheumatic Agents | decreases expression | 1 |
ChEMBL screening assays
72 unique, capped per target: 63 binding, 8 functional, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1047963 | Binding | Inhibition of recombinant HePTP | Multidentate small-molecule inhibitors of vaccinia H1-related (VHR) phosphatase decrease proliferation of cervix cancer cells. — J Med Chem |
| CHEMBL1613806 | Functional | PUBCHEM_BIOASSAY: In Vitro HePTP Dose Response Colorimetric Assay for SAR Study. (Class of assay: confirmatory) [Related pubchem assays: 521 ] | PubChem BioAssay data set |
| CHEMBL4626299 | ADMET | Inhibition of HePTP (unknown origin) expressed in Escherichia coli BL21 using p-nitrophenyl phosphate as substrate measured after 30 mins by UV-vis spectrophotometric method | Highly Potent and Selective N-Aryl Oxamic Acid-Based Inhibitors for Mycobacterium tuberculosis Protein Tyrosine Phosphatase B. — J Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.