ACP1
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Also known as HAAPLMW-PTPLMWPTP
Summary
ACP1 (acid phosphatase 1, HGNC:122) is a protein-coding gene on chromosome 2p25.3, encoding Low molecular weight phosphotyrosine protein phosphatase (P24666). Acts on tyrosine phosphorylated proteins, low-MW aryl phosphates and natural and synthetic acyl phosphates with differences in substrate specificity between isoform 1 and isoform 2.
The product of this gene belongs to the phosphotyrosine protein phosphatase family of proteins. It functions as an acid phosphatase and a protein tyrosine phosphatase by hydrolyzing protein tyrosine phosphate to protein tyrosine and orthophosphate. This enzyme also hydrolyzes orthophosphoric monoesters to alcohol and orthophosphate. This gene is genetically polymorphic, and three common alleles segregating at the corresponding locus give rise to six phenotypes. Each allele appears to encode at least two electrophoretically different isozymes, Bf and Bs, which are produced in allele-specific ratios. Multiple alternatively spliced transcript variants encoding distinct isoforms have been identified for this gene.
Source: NCBI Gene 52 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 82 total — 25 pathogenic, 2 likely-pathogenic
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_004300
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:122 |
| Approved symbol | ACP1 |
| Name | acid phosphatase 1 |
| Location | 2p25.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | HAAP, LMW-PTP, LMWPTP |
| Ensembl gene | ENSG00000143727 |
| Ensembl biotype | protein_coding |
| OMIM | 171500 |
| Entrez | 52 |
Gene structure
Transcript identifiers
Ensembl transcripts: 20 — 12 protein_coding, 4 nonsense_mediated_decay, 2 retained_intron, 2 protein_coding_CDS_not_defined
ENST00000272065, ENST00000272067, ENST00000405233, ENST00000405364, ENST00000407983, ENST00000413140, ENST00000439645, ENST00000442386, ENST00000453390, ENST00000463831, ENST00000480874, ENST00000484125, ENST00000484464, ENST00000896686, ENST00000896687, ENST00000896688, ENST00000896689, ENST00000896690, ENST00000896691, ENST00000972067
RefSeq mRNA: 3 — MANE Select: NM_004300
NM_001040649, NM_004300, NM_007099
CCDS: CCDS1639, CCDS1640, CCDS46217
Canonical transcript exons
ENST00000272065 — 6 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001380378 | 277227 | 278283 |
| ENSE00001907935 | 264947 | 265007 |
| ENSE00003574380 | 271866 | 271939 |
| ENSE00003591486 | 275140 | 275201 |
| ENSE00003624955 | 276980 | 277085 |
| ENSE00003641148 | 272037 | 272150 |
Expression profiles
Bgee: expression breadth ubiquitous, 299 present calls, max score 98.85.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 86.7782 / max 761.2588, expressed in 1825 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 18536 | 77.3600 | 1824 |
| 18535 | 9.4182 | 1780 |
Top tissues by expression
301 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| sperm | CL:0000019 | 98.85 | gold quality |
| adrenal tissue | UBERON:0018303 | 98.79 | gold quality |
| male germ cell | CL:0000015 | 98.63 | gold quality |
| calcaneal tendon | UBERON:0003701 | 98.26 | gold quality |
| left adrenal gland | UBERON:0001234 | 98.23 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 98.21 | gold quality |
| right adrenal gland | UBERON:0001233 | 98.20 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 98.20 | gold quality |
| adrenal cortex | UBERON:0001235 | 97.97 | gold quality |
| adrenal gland | UBERON:0002369 | 97.95 | gold quality |
| ventricular zone | UBERON:0003053 | 97.93 | gold quality |
| islet of Langerhans | UBERON:0000006 | 97.91 | gold quality |
| body of pancreas | UBERON:0001150 | 97.89 | gold quality |
| embryo | UBERON:0000922 | 97.87 | gold quality |
| right testis | UBERON:0004534 | 97.87 | gold quality |
| left testis | UBERON:0004533 | 97.76 | gold quality |
| ganglionic eminence | UBERON:0004023 | 97.64 | gold quality |
| pancreas | UBERON:0001264 | 97.56 | gold quality |
| rectum | UBERON:0001052 | 97.43 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 97.29 | gold quality |
| gall bladder | UBERON:0002110 | 97.16 | gold quality |
| left ovary | UBERON:0002119 | 97.15 | gold quality |
| testis | UBERON:0000473 | 97.08 | gold quality |
| eye | UBERON:0000970 | 97.06 | gold quality |
| body of stomach | UBERON:0001161 | 97.05 | gold quality |
| metanephros cortex | UBERON:0010533 | 96.89 | gold quality |
| adenohypophysis | UBERON:0002196 | 96.83 | gold quality |
| right ovary | UBERON:0002118 | 96.81 | gold quality |
| monocyte | CL:0000576 | 96.74 | gold quality |
| adult organism | UBERON:0007023 | 96.74 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
36 targeting ACP1, 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-4455 | 100.00 | 65.48 | 1587 |
| HSA-MIR-5193 | 100.00 | 67.26 | 1744 |
| HSA-MIR-4500 | 99.99 | 72.72 | 2367 |
| HSA-MIR-433-3P | 99.98 | 69.37 | 1203 |
| HSA-MIR-8075 | 99.97 | 67.20 | 962 |
| HSA-MIR-3941 | 99.86 | 70.54 | 2735 |
| HSA-MIR-4503 | 99.85 | 71.45 | 1869 |
| HSA-MIR-944 | 99.82 | 70.85 | 3042 |
| HSA-MIR-7856-5P | 99.75 | 69.99 | 2901 |
| HSA-MIR-132-3P | 99.73 | 70.56 | 1424 |
| HSA-MIR-212-3P | 99.73 | 70.65 | 1424 |
| HSA-MIR-7154-5P | 99.69 | 70.52 | 1900 |
| HSA-MIR-587 | 99.64 | 70.86 | 2611 |
| HSA-MIR-12123 | 99.52 | 71.79 | 2990 |
| HSA-MIR-4672 | 99.50 | 71.58 | 2893 |
| HSA-MIR-4251 | 99.40 | 69.19 | 3363 |
| HSA-MIR-16-2-3P | 99.29 | 70.60 | 1954 |
| HSA-MIR-195-3P | 99.29 | 70.61 | 1954 |
| HSA-MIR-10522-5P | 99.26 | 68.50 | 2087 |
| HSA-MIR-3675-3P | 99.09 | 67.70 | 968 |
| HSA-MIR-5001-3P | 98.91 | 67.28 | 1394 |
| HSA-MIR-4724-5P | 98.87 | 67.75 | 1324 |
| HSA-MIR-9500 | 98.62 | 66.54 | 1845 |
| HSA-MIR-8060 | 98.61 | 66.93 | 1187 |
| HSA-MIR-548AO-5P | 98.55 | 69.57 | 1362 |
| HSA-MIR-548AX | 98.55 | 69.58 | 1362 |
| HSA-MIR-1248 | 98.47 | 67.54 | 1314 |
| HSA-MIR-6827-5P | 98.46 | 64.88 | 1256 |
| HSA-MIR-4782-5P | 98.35 | 69.33 | 1474 |
| HSA-MIR-5706 | 98.35 | 69.33 | 1463 |
Literature-anchored findings (GeneRIF, showing 40)
- Mycobacteriophage Fruitloop gp52 protein confers heterotypic superinfection exclusion by inactivating Mycobacterium smegmatis protein Wag31. (PMID:29488662)
- ACP1 is associated with allergy (PMID:12100313)
- Association of the ACP1 genotype with metabolic parameters upon initial diagnosis of type 1 diabetes. (PMID:12640337)
- LMW-PTP has a role in immunological synapse establishment and stabilization through the negative control of FAK activity and of cell surface receptor redistribution (PMID:12815062)
- The analysis involved the data on nine polymorphic codominant loci: HP, GC, TF, PI, PGM1, GLO1, C3, ACP1, and ESD. The loci were selected by significance of differences in genotype frequencies between tuberculosis patients and healthy controls (PMID:12942785)
- We show that the association of STAT5 and LMW-PTP does not exclusively involve the phosphatase active site and phosphotyrosine residue of STAT5. (PMID:14637146)
- acid phosphatase 1 contributes to the clinical manifestations of type 2 diabetes and probably also have a marginal influence on susceptibility to the disease (PMID:15281007)
- complex interaction among maternal age, sex of infant and ACP1 concerning age at diagnosis of diabetes (PMID:15586390)
- Finds ACP1*C is a recessively deleterious allele that reduces viability during early life stages and is not maintained by overdominant selection in European populations. (PMID:15974295)
- Significant correlations between LMW-PTP overexpression and the most common clinical-pathological features of cancers exist. In colon cancer and neuroblastoma increased total LMW-PTP mRNA expression correlates with unfavourable outcome. (PMID:16036221)
- Crystal structure of the second human low molecular weight PTPase isoenzyme provides the opportunity to examine the structural basis of different substrate and inhibitor/activator responses. (PMID:16253994)
- mother/newborn pairs: ACP1 (acid phosphatase 1)distribution has fewer pairs with maternal low ACP1 S isoform and infant high S isoform concentration;Recurrent spontaneous abortion couples show wife low S isoform and husband high S isoform concentration (PMID:16762482)
- GRX plays an important role in PDGF-BB-dependent cell proliferation by regulating the redox state of LMW-PTP (PMID:16893901)
- Among newborns carrying the ACP1C allele there is an increase of Sex Ratio among the offspring of smoking mothers relative to non-smoking mothers. (PMID:16973312)
- Human recombinant LMWPTP-A displayed an RN5Pase activity that was higher than its tyrosine phosphatase activity, indicating that this phosphatase may participate in protein deglycation, a new form of protein repair. (PMID:17472574)
- results suggest a cooperative effect of ADA and ACP1 genetic polymorphism on the susceptibility to repeated spontaneous abortion and to some of its clinical characteristics (PMID:17565542)
- Women homozygous for haptoglobin with low ACP1 activity are more likely to conceive in the first part of the year. Women heterozygous for haptoglobin with medium-high ACP1 activity are more likely to conceive in the last part of the year. (PMID:17678914)
- There is a significant negative correlation between the intensity of skin test reaction and the ACP1 *B/*C genotype in allergic individuals. (PMID:17703100)
- The increase of fast isozyme concentration increased the invasive capacity of cancer cells, whereas a decrease of slow isozyme concentration in cancer did not cause growth inhibition and so resulted in cancer cell proliferation. (PMID:18262048)
- These findings suggest that carriers of high activity ACP1 genotypes are more susceptible to endometriosis but less susceptible to allergic manifestations than carriers of other ACP1 genotypes. (PMID:18490013)
- Highly significant differences in birth weight-placental weight correlations were observed among acid phosphatase locus 1 phenotypes. (PMID:18768081)
- There is an increase of the *B/*B genotype (high F isoform) & a much more marked decrease of genotypes with the high S isoform in colon cancer, compared with controls. (PMID:18786445)
- High concontration of the ACP1 F isoform may negatively regulate cell proliferation and growth of leiomyomas through dephosphorylation of the PDGF receptor. (PMID:18992867)
- Present in adipocytes, this protein may have a specific role in the regulation of quantity of adipose tissue. (PMID:19217450)
- ACP1 may be involved in susceptibility to coronary artery disease (PMID:19246900)
- The present data suggest an epistatic action of ACP1 concerning the effect of Hp on the susceptibility to convulsive disorders. (PMID:19569002)
- A possible protective effect of ACP1 genotype against cardiovascular risk factors was observed in this study (PMID:19570551)
- Variation in ACP1 is associated with fasting insulin and insulin sensitivity in a sex-specific manner. There is a sex-specific effect of variation in ACP1 to alter insulin signaling. (PMID:19622628)
- A significant interaction between ACP1 and ADA1 concerning susceptibility to type 1 diabetes, was revealed. (PMID:19789510)
- In overweight women (BMI > 25), the proportion of low activity ACP1 phenotypes is much lower in type 1 diabetes than in gestational diabetes and in healthy females. (PMID:19855922)
- the correlation between blood glucose and glycated Hb in relation to AK1 and ACP1 polymorphism was studied. (PMID:20152999)
- association with coronary artery disease evident only in diabetic subjects and dependent on female gender (PMID:20581655)
- Type 1 diabetes subjects show a highly significant increase of ACP1*A/ADA1*2 gametic type compared with healthy subjects from the same population (P = 0.003). (PMID:20805743)
- the ACP1 protein is a tyrosine phosphatase that influences Wnt signaling, a pathway regulated by lithium, making ACP1 a functional candidate for involvement in the phenotype. (PMID:21423239)
- Although both variants dephosphorylate the EPHA2 receptor, the rate and specificity of dephosphorylation for specific tyrosines are different for ACP1 and human cytoplasmic protein tyrosine phosphatase-B. (PMID:21538645)
- investigated hypothesis that favism is caused by toxic Vicia faba substances, which in some ACP1 phenotypes cause increased phosphorylation and thus increased glycolysis, with strong reduction in reduced glutathione production, resulting in hemolysis (PMID:21644204)
- the ACP1*C allele influences the risk of cardiovascular disease events in patients with rheumatoid arthritis. (PMID:21767392)
- Gain of the telomeric region 2p25.3 harboring the ACP1 gene is common in CLL (25%, 44 of 178 cases). (PMID:22035742)
- Data indicate that ACP1 rs11553742*T with increased susceptibility in systemic lupus erythematosus (SLE) patients. (PMID:22064183)
- lack of association with inflammatory bowel disease in Spanish patients (PMID:22428720)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Acp1 | ENSMUSG00000044573 |
| rattus_norvegicus | Acp1 | ENSRNOG00000005260 |
| drosophila_melanogaster | CG14297 | FBGN0038655 |
| drosophila_melanogaster | Argp | FBGN0051469 |
Paralogs (1): PTRHD1 (ENSG00000184924)
Protein
Protein identifiers
Low molecular weight phosphotyrosine protein phosphatase — P24666 (reviewed: P24666)
Alternative names: Adipocyte acid phosphatase, Low molecular weight cytosolic acid phosphatase, Red cell acid phosphatase 1
All UniProt accessions (6): P24666, A0A140VK37, D3YTI2, F2Z2Q9, F2Z2R9, G5E9R5
UniProt curated annotations — full annotation on UniProt →
Function. Acts on tyrosine phosphorylated proteins, low-MW aryl phosphates and natural and synthetic acyl phosphates with differences in substrate specificity between isoform 1 and isoform 2. Does not possess phosphatase activity.
Subunit / interactions. Interacts with EPHA2; dephosphorylates EPHA2. Interacts with EPHB1. Interacts with the SH3 domain of SPTAN1. There is no interaction observed for isoforms 2 or 3.
Subcellular location. Cytoplasm.
Tissue specificity. Expressed in T-lymphocytes.
Post-translational modifications. Phosphorylated by LCK. Phosphorylation at Tyr-132 increases its phosphatase activity. Not phosphorylated.
Activity regulation. Inhibited by sulfhydryl reagents.
Polymorphism. ACP1 is genetically polymorphic. Three common alleles are known in Caucasians: ACP1A, ACP1B and ACP1C. They give rise to six different phenotypes. Each allele appears to encode two electrophoretically different isozymes, F and S, which are produced in allele-specific ratios. The sequence shown is that of allele ACP1B and allele ACP1*C.
Similarity. Belongs to the low molecular weight phosphotyrosine protein phosphatase family.
Isoforms (4)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P24666-1 | 1, F, A, Alpha, LMPTP-A, HCPTP-A | yes |
| P24666-2 | 2, S, B, Beta, LMPTP-B, HCPTP-B | |
| P24666-3 | 3, C, LMPTP-C | |
| P24666-4 | 4 |
RefSeq proteins (3): NP_001035739, NP_004291, NP_009030 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR002115 | Tyr_Pase_low_mol_wt_mml | Family |
| IPR017867 | Tyr_phospatase_low_mol_wt | Family |
| IPR023485 | Ptyr_pPase | Domain |
| IPR036196 | Ptyr_pPase_sf | Homologous_superfamily |
| IPR050438 | LMW_PTPase | Family |
Pfam: PF01451
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), 2 shown:
- O-phospho-L-tyrosyl-[protein] + H2O = L-tyrosyl-[protein] + phosphate (RHEA:10684)
- a phosphate monoester + H2O = an alcohol + phosphate (RHEA:15017)
UniProt features (34 total): helix 7, splice variant 4, sequence conflict 4, strand 4, sequence variant 3, mutagenesis site 3, active site 3, modified residue 3, initiator methionine 1, chain 1, turn 1
Structure
Experimental structures (PDB)
17 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7KH8 | X-RAY DIFFRACTION | 1.3 |
| 5JNT | X-RAY DIFFRACTION | 1.45 |
| 5KQL | X-RAY DIFFRACTION | 1.45 |
| 3N8I | X-RAY DIFFRACTION | 1.5 |
| 5KQG | X-RAY DIFFRACTION | 1.5 |
| 7UW6 | X-RAY DIFFRACTION | 1.5 |
| 1XWW | X-RAY DIFFRACTION | 1.63 |
| 6Y2W | X-RAY DIFFRACTION | 1.77 |
| 5JNS | X-RAY DIFFRACTION | 1.8 |
| 5KQM | X-RAY DIFFRACTION | 1.91 |
| 5JNR | X-RAY DIFFRACTION | 2 |
| 6Y2V | X-RAY DIFFRACTION | 2 |
| 5KQP | X-RAY DIFFRACTION | 2.05 |
| 4Z9A | X-RAY DIFFRACTION | 2.1 |
| 5PNT | X-RAY DIFFRACTION | 2.2 |
| 4Z99 | X-RAY DIFFRACTION | 2.3 |
| 4Z9B | X-RAY DIFFRACTION | 2.41 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P24666-F1 | 96.16 | 0.96 |
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 (3): 13 (nucleophile); 19; 130 (proton donor)
Post-translational modifications (3): 2, 132, 133
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 13 | inactive. |
| 132 | reduced phosphorylation and activity. |
| 133 | reduced phosphorylation. no effect on activity. |
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 164 (showing top):
RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, AAGCAAT_MIR137, chr2p25, TGCGCANK_UNKNOWN, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, KAAB_FAILED_HEART_ATRIUM_DN, MORF_SNRP70, MORF_UBE2I, MORF_HDAC1, MORF_UBE2N, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, SHAFFER_IRF4_TARGETS_IN_ACTIVATED_B_LYMPHOCYTE, IVANOVA_HEMATOPOIESIS_MATURE_CELL, GOBP_CELL_CELL_SIGNALING, OUELLET_OVARIAN_CANCER_INVASIVE_VS_LMP_UP
GO Biological Process (2): chemical synaptic transmission (GO:0007268), protein dephosphorylation (GO:0006470)
GO Molecular Function (8): acid phosphatase activity (GO:0003993), protein tyrosine phosphatase activity (GO:0004725), non-membrane spanning protein tyrosine phosphatase activity (GO:0004726), SH3 domain binding (GO:0017124), phosphoprotein phosphatase activity (GO:0004721), protein binding (GO:0005515), hydrolase activity (GO:0016787), phosphatase activity (GO:0016791)
GO Cellular Component (7): cytoplasm (GO:0005737), cytosol (GO:0005829), cytoplasmic side of plasma membrane (GO:0009898), sarcolemma (GO:0042383), synapse (GO:0045202), extracellular exosome (GO:0070062), membrane (GO:0016020)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| phosphatase activity | 2 |
| plasma membrane | 2 |
| anterograde trans-synaptic signaling | 1 |
| dephosphorylation | 1 |
| protein modification process | 1 |
| phosphoprotein phosphatase activity | 1 |
| protein tyrosine phosphatase activity | 1 |
| protein domain specific binding | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| catalytic activity | 1 |
| phosphoric ester hydrolase activity | 1 |
| intracellular anatomical structure | 1 |
| cytoplasm | 1 |
| cytoplasmic side of membrane | 1 |
| cell junction | 1 |
| extracellular vesicle | 1 |
Protein interactions and networks
STRING
2558 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| ACP1 | G6PD | P11413 | 772 |
| ACP1 | PTS | Q03393 | 764 |
| ACP1 | A0A096LPE2 | A0A096LPE2 | 717 |
| ACP1 | SAA4 | P35542 | 711 |
| ACP1 | H6PD | O95479 | 708 |
| ACP1 | EPHA2 | P29317 | 672 |
| ACP1 | LDHC | P07864 | 668 |
| ACP1 | PTPN1 | P18031 | 650 |
| ACP1 | TCN2 | P20062 | 647 |
| ACP1 | GSR | P00390 | 635 |
| ACP1 | CTNNB1 | P35222 | 609 |
| ACP1 | ARHGAP35 | Q9NRY4 | 597 |
| ACP1 | LDHA | P00338 | 588 |
| ACP1 | ESD | P10768 | 583 |
| ACP1 | KCNC1 | P48547 | 582 |
IntAct
53 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CFTR | ESYT2 | psi-mi:“MI:0914”(association) | 0.710 |
| ACP1 | ACTB | psi-mi:“MI:0914”(association) | 0.530 |
| CFTR | PLEKHG3 | psi-mi:“MI:0914”(association) | 0.480 |
| DDX21 | MED19 | psi-mi:“MI:2364”(proximity) | 0.480 |
| M | ACP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ERBB2 | ACP1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| ACP1 | SFMBT1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| KSR1 | FBLL1 | psi-mi:“MI:0914”(association) | 0.350 |
| DLD | NFKBIE | psi-mi:“MI:0914”(association) | 0.350 |
| COPS5 | FBLL1 | psi-mi:“MI:0914”(association) | 0.350 |
| PRDM11 | ERCC3 | psi-mi:“MI:0914”(association) | 0.350 |
| TEX101 | PSMD12 | psi-mi:“MI:0914”(association) | 0.350 |
| TNK1 | ACP1 | psi-mi:“MI:0914”(association) | 0.350 |
| TESK1 | ACACB | psi-mi:“MI:0914”(association) | 0.350 |
| RIOK1 | SUPT5H | psi-mi:“MI:0914”(association) | 0.350 |
| RHOA | TAX1BP3 | psi-mi:“MI:0914”(association) | 0.350 |
| AGPS | psi-mi:“MI:0914”(association) | 0.350 | |
| MAPT | SHTN1 | psi-mi:“MI:0914”(association) | 0.350 |
| ITM2B | ILVBL | psi-mi:“MI:0914”(association) | 0.350 |
| KLHL22 | TRAV18 | psi-mi:“MI:0914”(association) | 0.350 |
| PIP4K2A | SAP18 | psi-mi:“MI:0914”(association) | 0.350 |
| US3 | ACOT8 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (141): SFMBT1 (Two-hybrid), ABRACL (Co-fractionation), ACP1 (Co-fractionation), ACP1 (Co-fractionation), ACP1 (Co-fractionation), ACP1 (Co-fractionation), PCBP1 (Co-fractionation), PITPNA (Co-fractionation), PPIL3 (Co-fractionation), TALDO1 (Co-fractionation), ACP1 (Affinity Capture-MS), ZBTB43 (Affinity Capture-MS), ACP1 (Affinity Capture-MS), DNAJC13 (Affinity Capture-MS), GADD45GIP1 (Affinity Capture-MS)
ESM2 similar proteins: A0A0U1WZ18, A0A1S4A695, A2VE01, A3QK15, O15305, O35621, O46560, P06766, P11064, P24666, P41498, P78330, P81693, P82197, Q0II59, Q148G4, Q1W374, Q1W375, Q1W376, Q1W377, Q259G4, Q2KHU0, Q3SZJ9, Q3T186, Q4R7R3, Q5E982, Q5I0K3, Q5PQL4, Q5RB83, Q5REM7, Q5VST6, Q5ZIV1, Q5ZJ01, Q5ZJL4, Q5ZKG5, Q60HD6, Q6DCC5, Q6DEY3, Q6P1N9, Q6P8M1
Diamond homologs: A0A0H3K9F2, B7INE4, O35016, O52787, P0C5D2, P11064, P24666, P39155, P40347, P41498, P41893, P53433, P58596, P65717, P81693, P82890, P82891, P9WIA0, P9WIA1, Q02191, Q2FFL4, Q2FX12, Q2YU46, Q45408, Q49YS6, Q49Z62, Q4L7J1, Q55535, Q55GW2, Q5HEP3, Q5HN53, Q5REM7, Q5ZKG5, Q6G853, Q6GFH6, Q7A0I2, Q7A4S1, Q8CNQ1, Q99T00, Q9D358
SIGNOR signaling
17 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| ACP1 | “down-regulates activity” | PDGFRB | dephosphorylation |
| ACP1 | “down-regulates activity” | PTK2 | dephosphorylation |
| ACP1 | “up-regulates activity” | PKM | dephosphorylation |
| ACP1 | “up-regulates activity” | SRC | dephosphorylation |
| ACP1 | “down-regulates activity” | AKT1 | dephosphorylation |
| ACP1 | “down-regulates activity” | AKT2 | dephosphorylation |
| ACP1 | “down-regulates activity” | AKT3 | dephosphorylation |
| ACP1 | “down-regulates activity” | AKT | dephosphorylation |
| ACP1 | “down-regulates activity” | EPHA2 | dephosphorylation |
| FYN | “up-regulates activity” | ACP1 | phosphorylation |
| LCK | “up-regulates activity” | ACP1 | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
82 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 25 |
| Likely pathogenic | 2 |
| Uncertain significance | 25 |
| Likely benign | 4 |
| Benign | 6 |
Top pathogenic / likely-pathogenic (27)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1330210 | GRCh37/hg19 2p25.3(chr2:10501-2386917)x1 | Pathogenic |
| 146223 | GRCh38/hg38 2p25.3(chr2:30341-3449132)x1 | Pathogenic |
| 146260 | GRCh38/hg38 2p25.3(chr2:30341-1969402)x1 | Pathogenic |
| 147583 | GRCh38/hg38 2p25.3(chr2:39193-1542734)x1 | Pathogenic |
| 148175 | GRCh38/hg38 2p25.3(chr2:30341-2656139)x1 | Pathogenic |
| 148269 | GRCh38/hg38 2p25.3-23.3(chr2:17019-26318846)x3 | Pathogenic |
| 150293 | GRCh38/hg38 2p25.3(chr2:24400-817581)x3 | Pathogenic |
| 152888 | GRCh38/hg38 2p25.3(chr2:17019-2305267)x1 | Pathogenic |
| 153475 | GRCh38/hg38 2p25.3(chr2:12770-2748672)x1 | Pathogenic |
| 154817 | GRCh38/hg38 2p25.3(chr2:131730-2713517)x1 | Pathogenic |
| 160975 | GRCh38/hg38 2p25.3(chr2:30341-507042)x3 | Pathogenic |
| 1808728 | GRCh37/hg19 2p25.3(chr2:12771-1947832)x1 | Pathogenic |
| 2671972 | GRCh37/hg19 2p25.3(chr2:12770-2832894)x1 | Pathogenic |
| 3242306 | GRCh37/hg19 2p25.3(chr2:11314-3033976)x1 | Pathogenic |
| 442997 | GRCh37/hg19 2p25.3-q37.3(chr2:12771-242783384)x3 | Pathogenic |
| 443675 | GRCh37/hg19 2p25.3-24.1(chr2:12770-20081474)x3 | Pathogenic |
| 4526718 | NC_000002.12:g.100000_1793802del | Pathogenic |
| 562667 | GRCh37/hg19 2p25.3-25.2(chr2:12770-4823625)x3 | Pathogenic |
| 59131 | GRCh38/hg38 2p25.3-24.3(chr2:30342-14866951)x3 | Pathogenic |
| 59132 | GRCh38/hg38 2p25.3-25.1(chr2:50661-9652907)x3 | Pathogenic |
| 686001 | GRCh37/hg19 2p25.3(chr2:12770-2832894)x1 | Pathogenic |
| 686548 | GRCh37/hg19 2p25.3-25.1(chr2:12770-7502796)x3 | Pathogenic |
| 686549 | GRCh37/hg19 2p25.3-25.1(chr2:12770-7502796)x3 | Pathogenic |
| 688279 | GRCh37/hg19 2p25.3(chr2:12770-2348876)x1 | Pathogenic |
| 814206 | GRCh37/hg19 2p25.3(chr2:12770-3000954)x1 | Pathogenic |
| 148892 | GRCh38/hg38 2p25.3(chr2:17019-1645317)x1 | Likely pathogenic |
| 152440 | GRCh38/hg38 2p25.3-25.2(chr2:17019-4957745)x3 | Likely pathogenic |
SpliceAI
1295 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:265006:GG:G | donor_gain | 1.0000 |
| 2:265007:GG:G | donor_gain | 1.0000 |
| 2:265007:GGTA:G | donor_loss | 1.0000 |
| 2:265008:GT:G | donor_loss | 1.0000 |
| 2:265009:T:G | donor_loss | 1.0000 |
| 2:266309:T:TA | donor_gain | 1.0000 |
| 2:266310:A:AA | donor_gain | 1.0000 |
| 2:271861:TAAAG:T | acceptor_loss | 1.0000 |
| 2:271864:A:AC | acceptor_loss | 1.0000 |
| 2:271865:G:GA | acceptor_loss | 1.0000 |
| 2:271936:GAAT:G | donor_gain | 1.0000 |
| 2:271937:AATG:A | donor_loss | 1.0000 |
| 2:271938:AT:A | donor_gain | 1.0000 |
| 2:271938:ATGTA:A | donor_loss | 1.0000 |
| 2:271939:TGTAA:T | donor_loss | 1.0000 |
| 2:271940:G:GG | donor_gain | 1.0000 |
| 2:271941:T:A | donor_loss | 1.0000 |
| 2:271942:AAG:A | donor_loss | 1.0000 |
| 2:264977:GC:G | donor_gain | 0.9900 |
| 2:264985:G:GG | donor_gain | 0.9900 |
| 2:265008:G:GG | donor_gain | 0.9900 |
| 2:271935:AGAAT:A | donor_gain | 0.9900 |
| 2:271936:GAATG:G | donor_gain | 0.9900 |
| 2:271937:AAT:A | donor_gain | 0.9900 |
| 2:271943:AGT:A | donor_loss | 0.9900 |
| 2:272035:A:AG | acceptor_gain | 0.9900 |
| 2:272036:G:GG | acceptor_gain | 0.9900 |
| 2:275261:ATTT:A | donor_gain | 0.9900 |
| 2:276978:A:AG | acceptor_gain | 0.9900 |
| 2:276979:G:GG | acceptor_gain | 0.9900 |
AlphaMissense
1057 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:271870:C:A | N16K | 0.999 |
| 2:271870:C:G | N16K | 0.999 |
| 2:277074:G:C | D130H | 0.999 |
| 2:277242:T:C | F139L | 0.999 |
| 2:277244:T:A | F139L | 0.999 |
| 2:277244:T:G | F139L | 0.999 |
| 2:265007:G:C | G15R | 0.998 |
| 2:272049:A:C | S44R | 0.998 |
| 2:272051:C:A | S44R | 0.998 |
| 2:272051:C:G | S44R | 0.998 |
| 2:275181:T:G | C91W | 0.998 |
| 2:275185:G:C | D93H | 0.998 |
| 2:277075:A:C | D130A | 0.998 |
| 2:277075:A:G | D130G | 0.998 |
| 2:277075:A:T | D130V | 0.998 |
| 2:277076:T:A | D130E | 0.998 |
| 2:277076:T:G | D130E | 0.998 |
| 2:277265:T:G | C146W | 0.998 |
| 2:265001:T:C | C13R | 0.997 |
| 2:271866:G:T | G15V | 0.997 |
| 2:271869:A:T | N16I | 0.997 |
| 2:271874:T:C | C18R | 0.997 |
| 2:272097:G:T | G60W | 0.997 |
| 2:272143:C:A | A75D | 0.997 |
| 2:275164:T:C | F86L | 0.997 |
| 2:275166:T:A | F86L | 0.997 |
| 2:275166:T:G | F86L | 0.997 |
| 2:275186:A:T | D93V | 0.997 |
| 2:277038:G:T | G118W | 0.997 |
| 2:277277:C:G | C150W | 0.997 |
dbSNP variants (sampled 300 via entrez): RS1000129166 (2:266901 T>A,C), RS1000313362 (2:272555 G>A), RS1000332887 (2:278735 G>A,C), RS1000464476 (2:270596 T>G), RS1000602361 (2:273794 T>C), RS1000620127 (2:277372 G>A), RS1000912933 (2:274270 C>T), RS1000997769 (2:263425 G>C), RS1001110613 (2:267309 C>G,T), RS1001288348 (2:270614 A>G), RS1001346205 (2:271535 C>T), RS1001400000 (2:271359 C>T), RS1001509690 (2:278205 T>G), RS1001588921 (2:265495 A>G), RS1001719873 (2:271037 T>A)
Disease associations
OMIM: gene MIM:171500 | disease phenotypes: MIM:616521
GenCC curated gene-disease
Mondo (1): intellectual disability, autosomal dominant 39 (MONDO:0014678)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4903 (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: 47,045 (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 |
|---|---|---|---|
| CHEMBL82202 | PYRIDOXAL PHOSPHATE ANHYDROUS | 3 | 26,220 |
| CHEMBL169 | URSOLIC ACID | 2 | 20,825 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
258 measured of 319 human assays (344 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| cid_694792 | KI | 60 nM | |
| 6-bromo-N-piperonyl-pyrazolo[1,5-a]pyrimidine-2-carboxamide | IC50 | 363 nM | |
| (E)-3-(3,4-dimethoxyphenyl)-N-[(2-hydroxy-5-nitro-phenyl)thiocarbamoyl]acrylamide | IC50 | 1090 nM | |
| cid_4640068 | IC50 | 1470 nM | |
| (5Z)-2-azanylidene-3-(4-fluorophenyl)-5-[(4-hydroxyphenyl)methylidene]-1,3-thiazolidin-4-one | IC50 | 1550 nM | |
| MLS000673878 | IC50 | 1570 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 | |
| N-(3-methylphenyl)-2-[4-[(Z)-2-[5-nitro-2,4-bis(oxidanylidene)-1H-pyrimidin-6-yl]ethenyl]phenoxy]ethanamide | IC50 | 1780 nM | |
| 4-{2-[(5-bromo-3-pyridinyl)carbonyl]carbonohydrazonoyl}phenyl 1,3-benzodioxole-5-carboxylate | IC50 | 1820 nM | |
| 3-[ethyl(phenyl)sulfamoyl]-4-methyl-benzoic acid | IC50 | 1830 nM | |
| N’-(3-chlorobenzoyl)thieno[2,3-b]quinoline-2-carbohydrazide | IC50 | 1900 nM | |
| (2Z)-2-[[(2-hydroxyphenyl)-oxomethyl]hydrazinylidene]-1-benzopyran-3-carboxamide | IC50 | 1930 nM | |
| 4-chloranyl-5-[2-[(4-chlorophenyl)methylidene]hydrazinyl]-2-phenyl-pyridazin-3-one | IC50 | 1930 nM | |
| 3-[7-[(2-chlorophenyl)methoxy]-4,8-dimethyl-2-oxochromen-3-yl]propanoic acid | IC50 | 1990 nM | |
| cid_277512 | IC50 | 1990 nM | |
| MLS001197785 | IC50 | 2090 nM | |
| MLS001213411 | IC50 | 2170 nM | |
| 4-[[3-[(5Z)-5-(1,3-benzodioxol-5-ylmethylidene)-4-oxo-2-sulfanylidene-3-thiazolidinyl]-1-oxopropyl]amino]benzoic acid | IC50 | 2300 nM | |
| MLS001224813 | IC50 | 2380 nM | |
| MLS000576933 | IC50 | 2450 nM | |
| SMR001798128 | IC50 | 2590 nM | |
| cid_1344193 | IC50 | 2640 nM | |
| 2-[(6,7-dihydroxy-2-keto-chromen-4-yl)methylthio]-3-(3-methoxyphenyl)quinazolin-4-one | IC50 | 2720 nM | |
| 1-ethyl-6-fluoro-7-[4-[(3-methylbenzoyl)carbamothioyl]piperazin-1-yl]-4-oxoquinoline-3-carboxylic acid | IC50 | 2740 nM | |
| MLS000776640 | IC50 | 2890 nM | |
| 6-hydroxy-3-iodo-1-methyl-2-[3-[[2-oxo-2-(4-thiophen-3-ylanilino)acetyl]amino]phenyl]indole-5-carboxylic acid | IC50 | 2900 nM | US-9522881: Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) |
| 2-(1H-indol-5-yl)-N-(3-piperidin-3-ylpropyl)quinolin-4-amine | IC50 | 2900 nM | US-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof |
| 2-(3H-benzimidazol-5-yl)-N-(3-piperidin-3-ylpropyl)quinolin-4-amine | IC50 | 2900 nM | US-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof |
| N-(3-piperidin-3-ylpropyl)-2-(1H-pyrrol-2-yl)quinolin-4-amine | IC50 | 2900 nM | US-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof |
| N-(3-piperidin-3-ylpropyl)-2-[4-(tetrazolidin-5-yl)phenyl]quinolin-4-amine | IC50 | 2900 nM | US-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof |
| cid_17252838 | IC50 | 2910 nM | |
| 4-({4-[5-(2-methyl-3-phenyl-2-propen-1-ylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]butanoyl}amino)benzoic acid | EC50 | 2980 nM | |
| 3-[7-[(6-chloranyl-1,3-benzodioxol-5-yl)methoxy]-4,8-dimethyl-2-oxidanylidene-chromen-3-yl]propanoic acid | IC50 | 2990 nM | |
| cid_9652363 | IC50 | 3040 nM | |
| MLS000714465 | IC50 | 3060 nM | |
| cid_4826777 | IC50 | 3080 nM | |
| 2-[4-[[6-carbethoxy-3-keto-7-methyl-5-[4-(methylthio)phenyl]-5H-thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]acetic acid | IC50 | 3140 nM | |
| 2-[4-[[5-(4-chlorophenyl)-6-ethoxycarbonyl-7-methyl-3-oxidanylidene-5H-[1,3]thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]ethanoic acid | IC50 | 3200 nM | |
| MLS000557507 | IC50 | 3200 nM | |
| SMR000606819 | IC50 | 3210 nM | |
| MLS000571311 | IC50 | 3250 nM | |
| N-[(E)-(5-bromanylthiophen-2-yl)methylideneamino]-3-nitro-benzamide | IC50 | 3400 nM | |
| MLS000558757 | IC50 | 3420 nM | |
| SMR000567889 | IC50 | 3490 nM | |
| MLS001167540 | IC50 | 3800 nM | |
| 2-amino-3-(1,3-benzoxazol-2-yl)-1-butyl-6-methyl-4-nitro-7-pyrrolo[2,3-d]pyridazinone | IC50 | 3870 nM | |
| N-[(E)-[4-(2-anilino-2-oxoethoxy)phenyl]methylideneamino]-2-hydroxybenzamide | IC50 | 3880 nM | |
| N-[(E)-(3-nitrobenzylidene)amino]benzo[e]benzofuran-2-carboxamide | IC50 | 3910 nM | |
| SMR000036870 | IC50 | 4060 nM | |
| N-(4-{[3-(3-nitrophenyl)acryloyl]amino}phenyl)-2-thiophenecarboxamide | IC50 | 4110 nM |
ChEMBL bioactivities
455 potent at pChembl≥5 of 578 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.92 | Ki | 1.2 | nM | CHEMBL5218807 |
| 8.40 | IC50 | 4 | nM | CHEMBL5218807 |
| 8.22 | IC50 | 6 | nM | CHEMBL4875137 |
| 8.10 | IC50 | 8 | nM | CHEMBL5219822 |
| 7.70 | IC50 | 20 | nM | CHEMBL4856707 |
| 7.40 | Kd | 39.49 | nM | CHEMBL5653589 |
| 7.40 | ED50 | 39.49 | nM | CHEMBL5653589 |
| 7.31 | IC50 | 49 | nM | CHEMBL5218783 |
| 7.25 | IC50 | 56 | nM | CHEMBL5220687 |
| 7.08 | IC50 | 83 | nM | CHEMBL4857535 |
| 7.06 | IC50 | 87 | nM | CHEMBL4855952 |
| 6.98 | IC50 | 104 | nM | CHEMBL4874911 |
| 6.97 | IC50 | 106 | nM | CHEMBL4848127 |
| 6.93 | IC50 | 117 | nM | CHEMBL4873827 |
| 6.92 | IC50 | 119 | nM | CHEMBL4859307 |
| 6.92 | IC50 | 121 | nM | CHEMBL5220615 |
| 6.83 | IC50 | 147 | nM | CHEMBL4858034 |
| 6.77 | IC50 | 171 | nM | CHEMBL4861843 |
| 6.70 | IC50 | 200 | nM | CHEMBL5220051 |
| 6.66 | IC50 | 220 | nM | CHEMBL1765349 |
| 6.62 | IC50 | 239 | nM | CHEMBL4847980 |
| 6.62 | IC50 | 239 | nM | CHEMBL4870698 |
| 6.61 | IC50 | 245 | nM | CHEMBL4868378 |
| 6.57 | Ki | 270 | nM | CHEMBL515146 |
| 6.54 | IC50 | 288 | nM | CHEMBL4857590 |
| 6.52 | IC50 | 300 | nM | CHEMBL5218478 |
| 6.52 | IC50 | 300 | nM | CHEMBL5219403 |
| 6.51 | IC50 | 306 | nM | CHEMBL4852414 |
| 6.47 | IC50 | 340 | nM | CHEMBL2396718 |
| 6.47 | Ki | 340 | nM | CHEMBL515146 |
| 6.42 | IC50 | 380 | nM | CHEMBL4846731 |
| 6.40 | IC50 | 400 | nM | CHEMBL5218609 |
| 6.40 | IC50 | 400 | nM | CHEMBL5219065 |
| 6.30 | IC50 | 500 | nM | CHEMBL1765349 |
| 6.30 | IC50 | 500 | nM | CHEMBL5865295 |
| 6.30 | IC50 | 500 | nM | CHEMBL6023401 |
| 6.30 | IC50 | 500 | nM | CHEMBL6010131 |
| 6.30 | IC50 | 500 | nM | CHEMBL5812199 |
| 6.30 | IC50 | 500 | nM | CHEMBL5954976 |
| 6.30 | IC50 | 500 | nM | CHEMBL5811959 |
| 6.30 | IC50 | 500 | nM | CHEMBL5821488 |
| 6.30 | IC50 | 500 | nM | CHEMBL5902805 |
| 6.30 | IC50 | 500 | nM | CHEMBL5964614 |
| 6.30 | IC50 | 500 | nM | CHEMBL5925675 |
| 6.30 | IC50 | 500 | nM | CHEMBL5783597 |
| 6.30 | IC50 | 500 | nM | CHEMBL5993213 |
| 6.30 | IC50 | 500 | nM | CHEMBL5772777 |
| 6.30 | IC50 | 500 | nM | CHEMBL5900713 |
| 6.30 | IC50 | 500 | nM | CHEMBL5946013 |
| 6.30 | IC50 | 500 | nM | CHEMBL5863654 |
PubChem BioAssay actives
135 with measured affinity, of 413 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 |
|---|---|---|---|---|
| (3,5-dibromo-4-methylphenyl)carbamoylsulfamic acid | 1917679: Competitive inhibition of LMW-PTP (unknown origin) assessed as inhibition constant by Lineweaver-Burk plot analysis | ki | 0.0012 | uM |
| 3-[(3,5-dichloro-4-pyridinyl)methyl]-8-(2-methylphenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.0060 | uM |
| azane;(3-bromo-4-morpholin-4-ylphenyl)carbamoylsulfamic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.0080 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(2-methylphenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.0200 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2147788: Binding affinity to human ACP1 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0395 | uM |
| azane;1,3-thiazol-2-ylcarbamoylsulfamic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.0490 | uM |
| azane;1,3-benzothiazol-2-ylcarbamoylsulfamic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.0560 | uM |
| 3-[(3,5-dichloro-4-pyridinyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.0830 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(3-methylphenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.0870 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-phenyl-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.1040 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(2-methoxyphenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.1060 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(4-fluorophenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.1170 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(4-methylphenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.1190 | uM |
| azane;phenylcarbamoylsulfamic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.1210 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(2-fluorophenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.1470 | uM |
| 8-(2-chlorophenyl)-3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.1710 | uM |
| 2-[(6-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.2000 | uM |
| 4-[[(5Z)-5-[[3-[(4-carboxyphenyl)methoxy]phenyl]methylidene]-4-oxo-2-phenylimino-1,3-thiazolidin-3-yl]methyl]benzoic acid | 696430: Inhibition of human LMW-PTPase isoform 2 | ic50 | 0.2200 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.2390 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-(3-fluorophenyl)-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.2390 | uM |
| 2-[3-[(2,6-dichlorophenyl)methyl]-6-imino-7H-purin-8-yl]benzonitrile | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.2450 | uM |
| 6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(4-phenylphenyl)methyl]chromen-4-one | 414657: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 by competitive inhibition assay | ki | 0.2700 | uM |
| 8-(4-chlorophenyl)-3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.2880 | uM |
| 2-oxo-2-[[6-(pyrrolidine-1-carbonyl)-1,3-benzothiazol-2-yl]amino]ethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.3000 | uM |
| 2-[(6-methylsulfonyl-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.3000 | uM |
| 3-[(2,6-dichlorophenyl)methyl]-8-methyl-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.3060 | uM |
| 3-[2-(3-chlorophenyl)ethynyl]-6-hydroxy-2-[4-[2-oxo-2-(propylamino)ethoxy]phenyl]-1-benzofuran-5-carboxylic acid | 755757: Inhibition of recombinant LMWPTP (unknown origin) using pNPP as substrate by spectrophotometric analysis | ic50 | 0.3400 | uM |
| 8-(3-chlorophenyl)-3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 0.3800 | uM |
| 2-[(6-methyl-4-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.4000 | uM |
| 2-[(5-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.4000 | uM |
| 2-oxo-2-[[6-(trifluoromethyl)-1,3-benzothiazol-2-yl]amino]ethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 0.6000 | uM |
| 2-hydroxy-4-[4-[[2-(4-hydroxyphenyl)-4-oxochromen-3-yl]methyl]phenyl]benzoic acid | 414644: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 | ic50 | 0.7000 | uM |
| 3-[[2-methoxy-4-[(E)-[1-[(4-methylphenyl)methyl]-2,5-dioxoimidazolidin-4-ylidene]methyl]phenoxy]methyl]benzoic acid | 2004707: Competitive inhibition of recombinant human ACP1 using pNPP as substrate assessed as inhibition constant preincubated with compound for 10 mins followed by substrate addition and measured by Lineweaver-Burk plot analysis | ki | 0.9000 | uM |
| 4-[[(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | 300020: Inhibition of human low molecular weight Protein-tyrosine phosphatase IF1 | ic50 | 0.9000 | uM |
| 2-[(6-nitro-1,3-benzothiazol-2-yl)amino]-2-oxo-1-phenylethanesulfonic acid | 1713620: Competitive inhibition of His-tagged LMW-PTP isoform A (unknown origin) expressed in Escherichia coli BL21 cells using para-nitrophenyl phosphate as substrate by Lineweaver-Burk plot analysis | ki | 1.0000 | uM |
| 3-[(2,4-dichlorophenyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 1.0200 | uM |
| 2-[(5-bromo-6-morpholin-4-yl-3-pyridinyl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 1.2000 | uM |
| 2-hydroxy-4-[4-[[7-hydroxy-2-(4-hydroxyphenyl)-4-oxochromen-3-yl]methyl]phenyl]benzoic acid | 414644: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 | ic50 | 1.3000 | uM |
| 2-(3-bromo-4-morpholin-4-ylanilino)-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 1.5000 | uM |
| azane;2-(1,8-naphthyridin-3-ylamino)-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 1.5000 | uM |
| 2-oxo-2-[(5-phenyl-1,3-thiazol-2-yl)amino]ethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 1.5000 | uM |
| 2-[(7-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 1.5000 | uM |
| 2-(1,3-benzothiazol-2-ylamino)-2-oxo-1-phenylethanesulfonic acid | 1713621: Competitive inhibition of LMW-PTP isoform B (unknown origin) using para-nitrophenyl phosphate as substrate by Lineweaver-Burk plot analysis | ki | 1.7000 | uM |
| 2-[(6-methyl-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 1.7000 | uM |
| 3-[(2-chlorophenyl)methyl]-7H-purin-6-imine | 1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assay | ic50 | 1.9300 | uM |
| 2-(3,5-dibromo-4-methylanilino)-2-oxoethanesulfonic acid | 1917631: Inhibition of His-tagged human LMW-PTP expressed in Escherichia coli BL21 using pNPP as substrate incubated for 10 mins by microplate reader based spectrophotometric analysis | ic50 | 2.2000 | uM |
| 3-[[4-(3,4-dihydroxyphenyl)phenyl]methyl]-7-hydroxy-2-(4-hydroxyphenyl)chromen-4-one | 414654: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 by mixed type inhibition assay | ki | 2.2300 | uM |
| 6-hydroxy-3-iodo-1-methyl-2-[3-[[2-oxo-2-(4-thiophen-3-ylanilino)acetyl]amino]phenyl]indole-5-carboxylic acid | 1182547: Inhibition of LMWPTP (unknown origin) | ic50 | 2.3400 | uM |
| 4-[[(5Z)-2,4-dioxo-5-[(4-phenylmethoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | 300020: Inhibition of human low molecular weight Protein-tyrosine phosphatase IF1 | ic50 | 2.5000 | uM |
| 7-hydroxy-2-(4-hydroxyphenyl)-3-[(4-phenylphenyl)methyl]chromen-4-one | 414654: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 by mixed type inhibition assay | ki | 2.5000 | uM |
CTD chemical–gene interactions
58 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | increases expression, increases methylation, decreases expression | 4 |
| perfluorooctanoic acid | decreases expression, increases expression | 2 |
| chloropicrin | decreases expression | 2 |
| Nickel | increases expression | 2 |
| Tretinoin | decreases expression | 2 |
| Valproic Acid | affects expression, decreases methylation | 2 |
| aristolochic acid I | increases expression | 1 |
| FR900359 | increases phosphorylation | 1 |
| dicrotophos | decreases expression | 1 |
| alpha phellandrene | decreases expression | 1 |
| nitrophenylphosphate | increases hydrolysis, decreases reaction | 1 |
| sodium arsenate | decreases expression | 1 |
| pyrogallol 1,3-dimethyl ether | affects cotreatment, affects localization, decreases expression | 1 |
| decabromobiphenyl ether | increases expression | 1 |
| arsenite | affects binding, increases reaction | 1 |
| sodium arsenite | decreases expression | 1 |
| butyraldehyde | decreases expression | 1 |
| tetrabromobisphenol A | increases expression | 1 |
| ochratoxin A | increases expression | 1 |
| pentanal | decreases expression | 1 |
| perfluorooctane sulfonic acid | increases expression | 1 |
| 4-chloro-N-((4-(1,1-dimethylethyl)phenyl)methyl)-3-ethyl-1-methyl-1H-pyrazole-5-carboxamide | decreases expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| perfluorohexanesulfonic acid | decreases expression | 1 |
| nutlin 3 | affects cotreatment, increases secretion | 1 |
| quinocetone | decreases expression | 1 |
| 2,2’,4,4’-tetrabromodiphenyl ether | increases expression | 1 |
| (4-amino-1,4-dihydro-3-(2-pyridyl)-5-thioxo-1,2,4-triazole)copper(II) | increases expression | 1 |
| pentabrominated diphenyl ether 100 | increases expression | 1 |
| hexabrominated diphenyl ether 153 | increases expression | 1 |
ChEMBL screening assays
84 unique, capped per target: 80 binding, 4 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1011832 | Binding | Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 | Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors. — Bioorg Med Chem |
| CHEMBL2114761 | Functional | PubChem BioAssay. Dose response confirmation of small molecule inhibitors of Low Molecular Weight Protein Tyrosine Phosphatase, LMPTP, in an orthogonal absorbance-based assay. (Class of assay: confirmatory) | PubChem BioAssay data set |
Cellosaurus cell lines
1 cell lines: 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1AN | Abcam HEK293 ACP1 KO | Transformed cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): intellectual disability, autosomal dominant 39