ACP1

gene
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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

FieldValue
HGNC IDHGNC:122
Approved symbolACP1
Nameacid phosphatase 1
Location2p25.3
Locus typegene with protein product
StatusApproved
AliasesHAAP, LMW-PTP, LMWPTP
Ensembl geneENSG00000143727
Ensembl biotypeprotein_coding
OMIM171500
Entrez52

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

ExonStartEnd
ENSE00001380378277227278283
ENSE00001907935264947265007
ENSE00003574380271866271939
ENSE00003591486275140275201
ENSE00003624955276980277085
ENSE00003641148272037272150

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 IDTPM avgSamples expressed
1853677.36001824
185359.41821780

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
spermCL:000001998.85gold quality
adrenal tissueUBERON:001830398.79gold quality
male germ cellCL:000001598.63gold quality
calcaneal tendonUBERON:000370198.26gold quality
left adrenal glandUBERON:000123498.23gold quality
right adrenal gland cortexUBERON:003582798.21gold quality
right adrenal glandUBERON:000123398.20gold quality
left adrenal gland cortexUBERON:003582598.20gold quality
adrenal cortexUBERON:000123597.97gold quality
adrenal glandUBERON:000236997.95gold quality
ventricular zoneUBERON:000305397.93gold quality
islet of LangerhansUBERON:000000697.91gold quality
body of pancreasUBERON:000115097.89gold quality
embryoUBERON:000092297.87gold quality
right testisUBERON:000453497.87gold quality
left testisUBERON:000453397.76gold quality
ganglionic eminenceUBERON:000402397.64gold quality
pancreasUBERON:000126497.56gold quality
rectumUBERON:000105297.43gold quality
palpebral conjunctivaUBERON:000181297.29gold quality
gall bladderUBERON:000211097.16gold quality
left ovaryUBERON:000211997.15gold quality
testisUBERON:000047397.08gold quality
eyeUBERON:000097097.06gold quality
body of stomachUBERON:000116197.05gold quality
metanephros cortexUBERON:001053396.89gold quality
adenohypophysisUBERON:000219696.83gold quality
right ovaryUBERON:000211896.81gold quality
monocyteCL:000057696.74gold quality
adult organismUBERON:000702396.74gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3no0.00

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):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-4455100.0065.481587
HSA-MIR-5193100.0067.261744
HSA-MIR-450099.9972.722367
HSA-MIR-433-3P99.9869.371203
HSA-MIR-807599.9767.20962
HSA-MIR-394199.8670.542735
HSA-MIR-450399.8571.451869
HSA-MIR-94499.8270.853042
HSA-MIR-7856-5P99.7569.992901
HSA-MIR-132-3P99.7370.561424
HSA-MIR-212-3P99.7370.651424
HSA-MIR-7154-5P99.6970.521900
HSA-MIR-58799.6470.862611
HSA-MIR-1212399.5271.792990
HSA-MIR-467299.5071.582893
HSA-MIR-425199.4069.193363
HSA-MIR-16-2-3P99.2970.601954
HSA-MIR-195-3P99.2970.611954
HSA-MIR-10522-5P99.2668.502087
HSA-MIR-3675-3P99.0967.70968
HSA-MIR-5001-3P98.9167.281394
HSA-MIR-4724-5P98.8767.751324
HSA-MIR-950098.6266.541845
HSA-MIR-806098.6166.931187
HSA-MIR-548AO-5P98.5569.571362
HSA-MIR-548AX98.5569.581362
HSA-MIR-124898.4767.541314
HSA-MIR-6827-5P98.4664.881256
HSA-MIR-4782-5P98.3569.331474
HSA-MIR-570698.3569.331463

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

OrganismSymbolGene ID
mus_musculusAcp1ENSMUSG00000044573
rattus_norvegicusAcp1ENSRNOG00000005260
drosophila_melanogasterCG14297FBGN0038655
drosophila_melanogasterArgpFBGN0051469

Paralogs (1): PTRHD1 (ENSG00000184924)

Protein

Protein identifiers

Low molecular weight phosphotyrosine protein phosphataseP24666 (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 IDNamesCanonical?
P24666-11, F, A, Alpha, LMPTP-A, HCPTP-Ayes
P24666-22, S, B, Beta, LMPTP-B, HCPTP-B
P24666-33, C, LMPTP-C
P24666-44

RefSeq proteins (3): NP_001035739, NP_004291, NP_009030 (=MANE)

Domains & families (InterPro)

IDNameType
IPR002115Tyr_Pase_low_mol_wt_mmlFamily
IPR017867Tyr_phospatase_low_mol_wtFamily
IPR023485Ptyr_pPaseDomain
IPR036196Ptyr_pPase_sfHomologous_superfamily
IPR050438LMW_PTPaseFamily

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.

SubstrateKm (mM)Measurements
4-NITROPHENYL PHOSPHATE0.0008–14884
6,8-DIFLUORO-4-METHYLUMBELLIFERYL PHOSPHATE0.0039–0.86227
P-NITROPHENYL PHOSPHATE0.0024–1020
DADEPYLIPQQG0.0003–0.112
PHOSPHOTYROSINE0.012–3011
LYSOZYME0.0003–0.0125
MYELIN BASIC PROTEIN0.0001–0.0225
ACETYL-DADEPY-NH20.0228–0.2194
ACETYL-DADEPYL-NH21.1–97.54
4,6,8-TRIMETHYL-2-OXO-2H-CHROMEN-7-YL DIHYDROGEN0.02–0.1563
SASASPYSASA0.53–2.33
1-NAPHTHYL PHOSPHATE1.19–1.882
3,6-FLUORESCEIN DIPHOSPHATE15–192
4-METHYLUMBELLIFERYL PHOSPHATE0.953–2.412
BOVINE SERUM ALBUMIN0.0001–0.00032

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.

PDBMethodResolution (Å)
7KH8X-RAY DIFFRACTION1.3
5JNTX-RAY DIFFRACTION1.45
5KQLX-RAY DIFFRACTION1.45
3N8IX-RAY DIFFRACTION1.5
5KQGX-RAY DIFFRACTION1.5
7UW6X-RAY DIFFRACTION1.5
1XWWX-RAY DIFFRACTION1.63
6Y2WX-RAY DIFFRACTION1.77
5JNSX-RAY DIFFRACTION1.8
5KQMX-RAY DIFFRACTION1.91
5JNRX-RAY DIFFRACTION2
6Y2VX-RAY DIFFRACTION2
5KQPX-RAY DIFFRACTION2.05
4Z9AX-RAY DIFFRACTION2.1
5PNTX-RAY DIFFRACTION2.2
4Z99X-RAY DIFFRACTION2.3
4Z9BX-RAY DIFFRACTION2.41

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P24666-F196.160.96

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):

PositionPhenotype
13inactive.
132reduced phosphorylation and activity.
133reduced 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:

CategoryTerms
cellular anatomical structure3
phosphatase activity2
plasma membrane2
anterograde trans-synaptic signaling1
dephosphorylation1
protein modification process1
phosphoprotein phosphatase activity1
protein tyrosine phosphatase activity1
protein domain specific binding1
catalytic activity, acting on a protein1
binding1
catalytic activity1
phosphoric ester hydrolase activity1
intracellular anatomical structure1
cytoplasm1
cytoplasmic side of membrane1
cell junction1
extracellular vesicle1

Protein interactions and networks

STRING

2558 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
ACP1G6PDP11413772
ACP1PTSQ03393764
ACP1A0A096LPE2A0A096LPE2717
ACP1SAA4P35542711
ACP1H6PDO95479708
ACP1EPHA2P29317672
ACP1LDHCP07864668
ACP1PTPN1P18031650
ACP1TCN2P20062647
ACP1GSRP00390635
ACP1CTNNB1P35222609
ACP1ARHGAP35Q9NRY4597
ACP1LDHAP00338588
ACP1ESDP10768583
ACP1KCNC1P48547582

IntAct

53 interactions, top by confidence:

ABTypeScore
CFTRESYT2psi-mi:“MI:0914”(association)0.710
ACP1ACTBpsi-mi:“MI:0914”(association)0.530
CFTRPLEKHG3psi-mi:“MI:0914”(association)0.480
DDX21MED19psi-mi:“MI:2364”(proximity)0.480
MACP1psi-mi:“MI:0915”(physical association)0.400
ERBB2ACP1psi-mi:“MI:0915”(physical association)0.370
ACP1SFMBT1psi-mi:“MI:0915”(physical association)0.370
KSR1FBLL1psi-mi:“MI:0914”(association)0.350
DLDNFKBIEpsi-mi:“MI:0914”(association)0.350
COPS5FBLL1psi-mi:“MI:0914”(association)0.350
PRDM11ERCC3psi-mi:“MI:0914”(association)0.350
TEX101PSMD12psi-mi:“MI:0914”(association)0.350
TNK1ACP1psi-mi:“MI:0914”(association)0.350
TESK1ACACBpsi-mi:“MI:0914”(association)0.350
RIOK1SUPT5Hpsi-mi:“MI:0914”(association)0.350
RHOATAX1BP3psi-mi:“MI:0914”(association)0.350
AGPSpsi-mi:“MI:0914”(association)0.350
MAPTSHTN1psi-mi:“MI:0914”(association)0.350
ITM2BILVBLpsi-mi:“MI:0914”(association)0.350
KLHL22TRAV18psi-mi:“MI:0914”(association)0.350
PIP4K2ASAP18psi-mi:“MI:0914”(association)0.350
US3ACOT8psi-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.

AEffectBMechanism
ACP1“down-regulates activity”PDGFRBdephosphorylation
ACP1“down-regulates activity”PTK2dephosphorylation
ACP1“up-regulates activity”PKMdephosphorylation
ACP1“up-regulates activity”SRCdephosphorylation
ACP1“down-regulates activity”AKT1dephosphorylation
ACP1“down-regulates activity”AKT2dephosphorylation
ACP1“down-regulates activity”AKT3dephosphorylation
ACP1“down-regulates activity”AKTdephosphorylation
ACP1“down-regulates activity”EPHA2dephosphorylation
FYN“up-regulates activity”ACP1phosphorylation
LCK“up-regulates activity”ACP1phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic25
Likely pathogenic2
Uncertain significance25
Likely benign4
Benign6

Top pathogenic / likely-pathogenic (27)

Variant IDHGVSClassification
1330210GRCh37/hg19 2p25.3(chr2:10501-2386917)x1Pathogenic
146223GRCh38/hg38 2p25.3(chr2:30341-3449132)x1Pathogenic
146260GRCh38/hg38 2p25.3(chr2:30341-1969402)x1Pathogenic
147583GRCh38/hg38 2p25.3(chr2:39193-1542734)x1Pathogenic
148175GRCh38/hg38 2p25.3(chr2:30341-2656139)x1Pathogenic
148269GRCh38/hg38 2p25.3-23.3(chr2:17019-26318846)x3Pathogenic
150293GRCh38/hg38 2p25.3(chr2:24400-817581)x3Pathogenic
152888GRCh38/hg38 2p25.3(chr2:17019-2305267)x1Pathogenic
153475GRCh38/hg38 2p25.3(chr2:12770-2748672)x1Pathogenic
154817GRCh38/hg38 2p25.3(chr2:131730-2713517)x1Pathogenic
160975GRCh38/hg38 2p25.3(chr2:30341-507042)x3Pathogenic
1808728GRCh37/hg19 2p25.3(chr2:12771-1947832)x1Pathogenic
2671972GRCh37/hg19 2p25.3(chr2:12770-2832894)x1Pathogenic
3242306GRCh37/hg19 2p25.3(chr2:11314-3033976)x1Pathogenic
442997GRCh37/hg19 2p25.3-q37.3(chr2:12771-242783384)x3Pathogenic
443675GRCh37/hg19 2p25.3-24.1(chr2:12770-20081474)x3Pathogenic
4526718NC_000002.12:g.100000_1793802delPathogenic
562667GRCh37/hg19 2p25.3-25.2(chr2:12770-4823625)x3Pathogenic
59131GRCh38/hg38 2p25.3-24.3(chr2:30342-14866951)x3Pathogenic
59132GRCh38/hg38 2p25.3-25.1(chr2:50661-9652907)x3Pathogenic
686001GRCh37/hg19 2p25.3(chr2:12770-2832894)x1Pathogenic
686548GRCh37/hg19 2p25.3-25.1(chr2:12770-7502796)x3Pathogenic
686549GRCh37/hg19 2p25.3-25.1(chr2:12770-7502796)x3Pathogenic
688279GRCh37/hg19 2p25.3(chr2:12770-2348876)x1Pathogenic
814206GRCh37/hg19 2p25.3(chr2:12770-3000954)x1Pathogenic
148892GRCh38/hg38 2p25.3(chr2:17019-1645317)x1Likely pathogenic
152440GRCh38/hg38 2p25.3-25.2(chr2:17019-4957745)x3Likely pathogenic

SpliceAI

1295 predictions. Top by Δscore:

VariantEffectΔscore
2:265006:GG:Gdonor_gain1.0000
2:265007:GG:Gdonor_gain1.0000
2:265007:GGTA:Gdonor_loss1.0000
2:265008:GT:Gdonor_loss1.0000
2:265009:T:Gdonor_loss1.0000
2:266309:T:TAdonor_gain1.0000
2:266310:A:AAdonor_gain1.0000
2:271861:TAAAG:Tacceptor_loss1.0000
2:271864:A:ACacceptor_loss1.0000
2:271865:G:GAacceptor_loss1.0000
2:271936:GAAT:Gdonor_gain1.0000
2:271937:AATG:Adonor_loss1.0000
2:271938:AT:Adonor_gain1.0000
2:271938:ATGTA:Adonor_loss1.0000
2:271939:TGTAA:Tdonor_loss1.0000
2:271940:G:GGdonor_gain1.0000
2:271941:T:Adonor_loss1.0000
2:271942:AAG:Adonor_loss1.0000
2:264977:GC:Gdonor_gain0.9900
2:264985:G:GGdonor_gain0.9900
2:265008:G:GGdonor_gain0.9900
2:271935:AGAAT:Adonor_gain0.9900
2:271936:GAATG:Gdonor_gain0.9900
2:271937:AAT:Adonor_gain0.9900
2:271943:AGT:Adonor_loss0.9900
2:272035:A:AGacceptor_gain0.9900
2:272036:G:GGacceptor_gain0.9900
2:275261:ATTT:Adonor_gain0.9900
2:276978:A:AGacceptor_gain0.9900
2:276979:G:GGacceptor_gain0.9900

AlphaMissense

1057 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
2:271870:C:AN16K0.999
2:271870:C:GN16K0.999
2:277074:G:CD130H0.999
2:277242:T:CF139L0.999
2:277244:T:AF139L0.999
2:277244:T:GF139L0.999
2:265007:G:CG15R0.998
2:272049:A:CS44R0.998
2:272051:C:AS44R0.998
2:272051:C:GS44R0.998
2:275181:T:GC91W0.998
2:275185:G:CD93H0.998
2:277075:A:CD130A0.998
2:277075:A:GD130G0.998
2:277075:A:TD130V0.998
2:277076:T:AD130E0.998
2:277076:T:GD130E0.998
2:277265:T:GC146W0.998
2:265001:T:CC13R0.997
2:271866:G:TG15V0.997
2:271869:A:TN16I0.997
2:271874:T:CC18R0.997
2:272097:G:TG60W0.997
2:272143:C:AA75D0.997
2:275164:T:CF86L0.997
2:275166:T:AF86L0.997
2:275166:T:GF86L0.997
2:275186:A:TD93V0.997
2:277038:G:TG118W0.997
2:277277:C:GC150W0.997

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).

MoleculeNamePhasePatents
CHEMBL82202PYRIDOXAL PHOSPHATE ANHYDROUS326,220
CHEMBL169URSOLIC ACID220,825

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.

LigandMeasureValuePatent
cid_694792KI60 nM
6-bromo-N-piperonyl-pyrazolo[1,5-a]pyrimidine-2-carboxamideIC50363 nM
(E)-3-(3,4-dimethoxyphenyl)-N-[(2-hydroxy-5-nitro-phenyl)thiocarbamoyl]acrylamideIC501090 nM
cid_4640068IC501470 nM
(5Z)-2-azanylidene-3-(4-fluorophenyl)-5-[(4-hydroxyphenyl)methylidene]-1,3-thiazolidin-4-oneIC501550 nM
MLS000673878IC501570 nM
4-keto-5-methyl-2-[(E)-2-(4-methyl-3-nitro-phenyl)vinyl]-3H-thieno[2,3-d]pyrimidine-6-carboxylic acidIC501620 nM
N-(3-methylphenyl)-2-[4-[(Z)-2-[5-nitro-2,4-bis(oxidanylidene)-1H-pyrimidin-6-yl]ethenyl]phenoxy]ethanamideIC501780 nM
4-{2-[(5-bromo-3-pyridinyl)carbonyl]carbonohydrazonoyl}phenyl 1,3-benzodioxole-5-carboxylateIC501820 nM
3-[ethyl(phenyl)sulfamoyl]-4-methyl-benzoic acidIC501830 nM
N’-(3-chlorobenzoyl)thieno[2,3-b]quinoline-2-carbohydrazideIC501900 nM
(2Z)-2-[[(2-hydroxyphenyl)-oxomethyl]hydrazinylidene]-1-benzopyran-3-carboxamideIC501930 nM
4-chloranyl-5-[2-[(4-chlorophenyl)methylidene]hydrazinyl]-2-phenyl-pyridazin-3-oneIC501930 nM
3-[7-[(2-chlorophenyl)methoxy]-4,8-dimethyl-2-oxochromen-3-yl]propanoic acidIC501990 nM
cid_277512IC501990 nM
MLS001197785IC502090 nM
MLS001213411IC502170 nM
4-[[3-[(5Z)-5-(1,3-benzodioxol-5-ylmethylidene)-4-oxo-2-sulfanylidene-3-thiazolidinyl]-1-oxopropyl]amino]benzoic acidIC502300 nM
MLS001224813IC502380 nM
MLS000576933IC502450 nM
SMR001798128IC502590 nM
cid_1344193IC502640 nM
2-[(6,7-dihydroxy-2-keto-chromen-4-yl)methylthio]-3-(3-methoxyphenyl)quinazolin-4-oneIC502720 nM
1-ethyl-6-fluoro-7-[4-[(3-methylbenzoyl)carbamothioyl]piperazin-1-yl]-4-oxoquinoline-3-carboxylic acidIC502740 nM
MLS000776640IC502890 nM
6-hydroxy-3-iodo-1-methyl-2-[3-[[2-oxo-2-(4-thiophen-3-ylanilino)acetyl]amino]phenyl]indole-5-carboxylic acidIC502900 nMUS-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-amineIC502900 nMUS-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof
2-(3H-benzimidazol-5-yl)-N-(3-piperidin-3-ylpropyl)quinolin-4-amineIC502900 nMUS-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof
N-(3-piperidin-3-ylpropyl)-2-(1H-pyrrol-2-yl)quinolin-4-amineIC502900 nMUS-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-amineIC502900 nMUS-11220486: Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof
cid_17252838IC502910 nM
4-({4-[5-(2-methyl-3-phenyl-2-propen-1-ylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]butanoyl}amino)benzoic acidEC502980 nM
3-[7-[(6-chloranyl-1,3-benzodioxol-5-yl)methoxy]-4,8-dimethyl-2-oxidanylidene-chromen-3-yl]propanoic acidIC502990 nM
cid_9652363IC503040 nM
MLS000714465IC503060 nM
cid_4826777IC503080 nM
2-[4-[[6-carbethoxy-3-keto-7-methyl-5-[4-(methylthio)phenyl]-5H-thiazolo[3,2-a]pyrimidin-2-ylidene]methyl]phenoxy]acetic acidIC503140 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 acidIC503200 nM
MLS000557507IC503200 nM
SMR000606819IC503210 nM
MLS000571311IC503250 nM
N-[(E)-(5-bromanylthiophen-2-yl)methylideneamino]-3-nitro-benzamideIC503400 nM
MLS000558757IC503420 nM
SMR000567889IC503490 nM
MLS001167540IC503800 nM
2-amino-3-(1,3-benzoxazol-2-yl)-1-butyl-6-methyl-4-nitro-7-pyrrolo[2,3-d]pyridazinoneIC503870 nM
N-[(E)-[4-(2-anilino-2-oxoethoxy)phenyl]methylideneamino]-2-hydroxybenzamideIC503880 nM
N-[(E)-(3-nitrobenzylidene)amino]benzo[e]benzofuran-2-carboxamideIC503910 nM
SMR000036870IC504060 nM
N-(4-{[3-(3-nitrophenyl)acryloyl]amino}phenyl)-2-thiophenecarboxamideIC504110 nM

ChEMBL bioactivities

455 potent at pChembl≥5 of 578 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.92Ki1.2nMCHEMBL5218807
8.40IC504nMCHEMBL5218807
8.22IC506nMCHEMBL4875137
8.10IC508nMCHEMBL5219822
7.70IC5020nMCHEMBL4856707
7.40Kd39.49nMCHEMBL5653589
7.40ED5039.49nMCHEMBL5653589
7.31IC5049nMCHEMBL5218783
7.25IC5056nMCHEMBL5220687
7.08IC5083nMCHEMBL4857535
7.06IC5087nMCHEMBL4855952
6.98IC50104nMCHEMBL4874911
6.97IC50106nMCHEMBL4848127
6.93IC50117nMCHEMBL4873827
6.92IC50119nMCHEMBL4859307
6.92IC50121nMCHEMBL5220615
6.83IC50147nMCHEMBL4858034
6.77IC50171nMCHEMBL4861843
6.70IC50200nMCHEMBL5220051
6.66IC50220nMCHEMBL1765349
6.62IC50239nMCHEMBL4847980
6.62IC50239nMCHEMBL4870698
6.61IC50245nMCHEMBL4868378
6.57Ki270nMCHEMBL515146
6.54IC50288nMCHEMBL4857590
6.52IC50300nMCHEMBL5218478
6.52IC50300nMCHEMBL5219403
6.51IC50306nMCHEMBL4852414
6.47IC50340nMCHEMBL2396718
6.47Ki340nMCHEMBL515146
6.42IC50380nMCHEMBL4846731
6.40IC50400nMCHEMBL5218609
6.40IC50400nMCHEMBL5219065
6.30IC50500nMCHEMBL1765349
6.30IC50500nMCHEMBL5865295
6.30IC50500nMCHEMBL6023401
6.30IC50500nMCHEMBL6010131
6.30IC50500nMCHEMBL5812199
6.30IC50500nMCHEMBL5954976
6.30IC50500nMCHEMBL5811959
6.30IC50500nMCHEMBL5821488
6.30IC50500nMCHEMBL5902805
6.30IC50500nMCHEMBL5964614
6.30IC50500nMCHEMBL5925675
6.30IC50500nMCHEMBL5783597
6.30IC50500nMCHEMBL5993213
6.30IC50500nMCHEMBL5772777
6.30IC50500nMCHEMBL5900713
6.30IC50500nMCHEMBL5946013
6.30IC50500nMCHEMBL5863654

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.

CompoundAssayTypeValueUnit
(3,5-dibromo-4-methylphenyl)carbamoylsulfamic acid1917679: Competitive inhibition of LMW-PTP (unknown origin) assessed as inhibition constant by Lineweaver-Burk plot analysiski0.0012uM
3-[(3,5-dichloro-4-pyridinyl)methyl]-8-(2-methylphenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.0060uM
azane;(3-bromo-4-morpholin-4-ylphenyl)carbamoylsulfamic acid1917631: 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 analysisic500.0080uM
3-[(2,6-dichlorophenyl)methyl]-8-(2-methylphenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.0200uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide2147788: Binding affinity to human ACP1 incubated for 45 mins by Kinobead based pull down assaykd0.0395uM
azane;1,3-thiazol-2-ylcarbamoylsulfamic acid1917631: 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 analysisic500.0490uM
azane;1,3-benzothiazol-2-ylcarbamoylsulfamic acid1917631: 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 analysisic500.0560uM
3-[(3,5-dichloro-4-pyridinyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.0830uM
3-[(2,6-dichlorophenyl)methyl]-8-(3-methylphenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.0870uM
3-[(2,6-dichlorophenyl)methyl]-8-phenyl-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.1040uM
3-[(2,6-dichlorophenyl)methyl]-8-(2-methoxyphenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.1060uM
3-[(2,6-dichlorophenyl)methyl]-8-(4-fluorophenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.1170uM
3-[(2,6-dichlorophenyl)methyl]-8-(4-methylphenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.1190uM
azane;phenylcarbamoylsulfamic acid1917631: 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 analysisic500.1210uM
3-[(2,6-dichlorophenyl)methyl]-8-(2-fluorophenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.1470uM
8-(2-chlorophenyl)-3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.1710uM
2-[(6-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic500.2000uM
4-[[(5Z)-5-[[3-[(4-carboxyphenyl)methoxy]phenyl]methylidene]-4-oxo-2-phenylimino-1,3-thiazolidin-3-yl]methyl]benzoic acid696430: Inhibition of human LMW-PTPase isoform 2ic500.2200uM
3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.2390uM
3-[(2,6-dichlorophenyl)methyl]-8-(3-fluorophenyl)-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.2390uM
2-[3-[(2,6-dichlorophenyl)methyl]-6-imino-7H-purin-8-yl]benzonitrile1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.2450uM
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(4-phenylphenyl)methyl]chromen-4-one414657: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 by competitive inhibition assayki0.2700uM
8-(4-chlorophenyl)-3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.2880uM
2-oxo-2-[[6-(pyrrolidine-1-carbonyl)-1,3-benzothiazol-2-yl]amino]ethanesulfonic acid1917631: 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 analysisic500.3000uM
2-[(6-methylsulfonyl-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic500.3000uM
3-[(2,6-dichlorophenyl)methyl]-8-methyl-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.3060uM
3-[2-(3-chlorophenyl)ethynyl]-6-hydroxy-2-[4-[2-oxo-2-(propylamino)ethoxy]phenyl]-1-benzofuran-5-carboxylic acid755757: Inhibition of recombinant LMWPTP (unknown origin) using pNPP as substrate by spectrophotometric analysisic500.3400uM
8-(3-chlorophenyl)-3-[(2,6-dichlorophenyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic500.3800uM
2-[(6-methyl-4-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic500.4000uM
2-[(5-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic500.4000uM
2-oxo-2-[[6-(trifluoromethyl)-1,3-benzothiazol-2-yl]amino]ethanesulfonic acid1917631: 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 analysisic500.6000uM
2-hydroxy-4-[4-[[2-(4-hydroxyphenyl)-4-oxochromen-3-yl]methyl]phenyl]benzoic acid414644: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1ic500.7000uM
3-[[2-methoxy-4-[(E)-[1-[(4-methylphenyl)methyl]-2,5-dioxoimidazolidin-4-ylidene]methyl]phenoxy]methyl]benzoic acid2004707: 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 analysiski0.9000uM
4-[[(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid300020: Inhibition of human low molecular weight Protein-tyrosine phosphatase IF1ic500.9000uM
2-[(6-nitro-1,3-benzothiazol-2-yl)amino]-2-oxo-1-phenylethanesulfonic acid1713620: 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 analysiski1.0000uM
3-[(2,4-dichlorophenyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic501.0200uM
2-[(5-bromo-6-morpholin-4-yl-3-pyridinyl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic501.2000uM
2-hydroxy-4-[4-[[7-hydroxy-2-(4-hydroxyphenyl)-4-oxochromen-3-yl]methyl]phenyl]benzoic acid414644: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1ic501.3000uM
2-(3-bromo-4-morpholin-4-ylanilino)-2-oxoethanesulfonic acid1917631: 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 analysisic501.5000uM
azane;2-(1,8-naphthyridin-3-ylamino)-2-oxoethanesulfonic acid1917631: 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 analysisic501.5000uM
2-oxo-2-[(5-phenyl-1,3-thiazol-2-yl)amino]ethanesulfonic acid1917631: 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 analysisic501.5000uM
2-[(7-nitro-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic501.5000uM
2-(1,3-benzothiazol-2-ylamino)-2-oxo-1-phenylethanesulfonic acid1713621: Competitive inhibition of LMW-PTP isoform B (unknown origin) using para-nitrophenyl phosphate as substrate by Lineweaver-Burk plot analysiski1.7000uM
2-[(6-methyl-1,3-benzothiazol-2-yl)amino]-2-oxoethanesulfonic acid1917631: 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 analysisic501.7000uM
3-[(2-chlorophenyl)methyl]-7H-purin-6-imine1778348: Inhibition of recombinant human LMPTP-A using OMFP or pNPP as substrate by fluorescence assayic501.9300uM
2-(3,5-dibromo-4-methylanilino)-2-oxoethanesulfonic acid1917631: 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 analysisic502.2000uM
3-[[4-(3,4-dihydroxyphenyl)phenyl]methyl]-7-hydroxy-2-(4-hydroxyphenyl)chromen-4-one414654: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 by mixed type inhibition assayki2.2300uM
6-hydroxy-3-iodo-1-methyl-2-[3-[[2-oxo-2-(4-thiophen-3-ylanilino)acetyl]amino]phenyl]indole-5-carboxylic acid1182547: Inhibition of LMWPTP (unknown origin)ic502.3400uM
4-[[(5Z)-2,4-dioxo-5-[(4-phenylmethoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid300020: Inhibition of human low molecular weight Protein-tyrosine phosphatase IF1ic502.5000uM
7-hydroxy-2-(4-hydroxyphenyl)-3-[(4-phenylphenyl)methyl]chromen-4-one414654: Inhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1 by mixed type inhibition assayki2.5000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
bisphenol Aincreases expression, increases methylation, decreases expression4
perfluorooctanoic aciddecreases expression, increases expression2
chloropicrindecreases expression2
Nickelincreases expression2
Tretinoindecreases expression2
Valproic Acidaffects expression, decreases methylation2
aristolochic acid Iincreases expression1
FR900359increases phosphorylation1
dicrotophosdecreases expression1
alpha phellandrenedecreases expression1
nitrophenylphosphateincreases hydrolysis, decreases reaction1
sodium arsenatedecreases expression1
pyrogallol 1,3-dimethyl etheraffects cotreatment, affects localization, decreases expression1
decabromobiphenyl etherincreases expression1
arseniteaffects binding, increases reaction1
sodium arsenitedecreases expression1
butyraldehydedecreases expression1
tetrabromobisphenol Aincreases expression1
ochratoxin Aincreases expression1
pentanaldecreases expression1
perfluorooctane sulfonic acidincreases expression1
4-chloro-N-((4-(1,1-dimethylethyl)phenyl)methyl)-3-ethyl-1-methyl-1H-pyrazole-5-carboxamidedecreases expression1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, increases expression1
perfluorohexanesulfonic aciddecreases expression1
nutlin 3affects cotreatment, increases secretion1
quinocetonedecreases expression1
2,2’,4,4’-tetrabromodiphenyl etherincreases expression1
(4-amino-1,4-dihydro-3-(2-pyridyl)-5-thioxo-1,2,4-triazole)copper(II)increases expression1
pentabrominated diphenyl ether 100increases expression1
hexabrominated diphenyl ether 153increases expression1

ChEMBL screening assays

84 unique, capped per target: 80 binding, 4 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1011832BindingInhibition of human cloned LMW-PTP isoform 1 expressed in Escherichia coli TB1Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors. — Bioorg Med Chem
CHEMBL2114761FunctionalPubChem 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):

CellosaurusNameCategorySex
CVCL_B1ANAbcam HEK293 ACP1 KOTransformed cell lineFemale

Clinical trials (associated diseases)

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