PLEK

gene
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Also known as P47PLEK1

Summary

PLEK (pleckstrin, HGNC:9070) is a protein-coding gene on chromosome 2p14, encoding Pleckstrin (P08567). Major protein kinase C substrate of platelets.

Enables phosphatidylinositol-3,4-bisphosphate binding activity; protein homodimerization activity; and protein kinase C binding activity. Involved in several processes, including G protein-coupled receptor signaling pathway; regulation of actin filament organization; and regulation of phosphate metabolic process. Located in cytoplasm and ruffle membrane.

Source: NCBI Gene 5341 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): autosomal dominant nonsyndromic hearing loss 58 (Limited, GenCC)
  • GWAS associations: 20
  • Clinical variants (ClinVar): 50 total
  • Druggable target: yes
  • MANE Select transcript: NM_002664

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9070
Approved symbolPLEK
Namepleckstrin
Location2p14
Locus typegene with protein product
StatusApproved
AliasesP47, PLEK1
Ensembl geneENSG00000115956
Ensembl biotypeprotein_coding
OMIM173570
Entrez5341

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 1 protein_coding, 1 retained_intron

ENST00000234313, ENST00000474788

RefSeq mRNA: 1 — MANE Select: NM_002664 NM_002664

CCDS: CCDS1887

Canonical transcript exons

ENST00000234313 — 9 exons

ExonStartEnd
ENSE000007587946838072368380904
ENSE000007587966838254268382633
ENSE000007587986838650268386686
ENSE000007588006838838768388491
ENSE000009630536838032868380483
ENSE000011637946839568068397453
ENSE000019117886836528268365393
ENSE000035478036839410768394176
ENSE000035778876839316268393245

Expression profiles

Bgee: expression breadth ubiquitous, 234 present calls, max score 99.08.

FANTOM5 (CAGE): breadth broad, TPM avg 119.7135 / max 9473.8797, expressed in 530 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter IDTPM avgSamples expressed
20673114.3031512
206724.3541335
206860.323280
206850.275873
206870.156258
206890.122451
206710.099754
206900.078938

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
monocyteCL:000057699.08gold quality
mononuclear cellCL:000084299.01gold quality
leukocyteCL:000073899.00gold quality
granulocyteCL:000009498.83gold quality
bloodUBERON:000017898.02gold quality
bone marrowUBERON:000237197.66gold quality
bone marrow cellCL:000209297.16gold quality
lymph nodeUBERON:000002996.34gold quality
vermiform appendixUBERON:000115496.19gold quality
spleenUBERON:000210695.76gold quality
periodontal ligamentUBERON:000826695.43gold quality
bone elementUBERON:000147495.31gold quality
trabecular bone tissueUBERON:000248394.56gold quality
caecumUBERON:000115392.44gold quality
olfactory bulbUBERON:000226491.98gold quality
type B pancreatic cellCL:000016991.03gold quality
gall bladderUBERON:000211089.83gold quality
tongue squamous epitheliumUBERON:000691989.48gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047389.25gold quality
upper lobe of left lungUBERON:000895288.82gold quality
upper lobe of lungUBERON:000894887.77gold quality
rectumUBERON:000105287.75gold quality
superficial temporal arteryUBERON:000161486.95gold quality
tonsilUBERON:000237285.93gold quality
right lungUBERON:000216785.66gold quality
smooth muscle tissueUBERON:000113585.50gold quality
omental fat padUBERON:001041485.23gold quality
peritoneumUBERON:000235885.19gold quality
right coronary arteryUBERON:000162585.09gold quality
lungUBERON:000204884.68gold quality

Single-cell (SCXA)

Detected in 31 experiment(s), a significant marker in 29.

ExperimentMarker?Max mean expression
E-CURD-112yes3767.08
E-MTAB-10432yes2990.09
E-MTAB-9067yes2672.10
E-CURD-98yes2281.72
E-MTAB-7407yes1880.54
E-GEOD-135922yes1745.66
E-CURD-6yes1564.42
E-GEOD-130473yes1465.43
E-MTAB-8884yes1427.00
E-HCAD-6yes1327.01
E-GEOD-75688yes1021.97
E-ANND-5yes619.18
E-HCAD-1yes84.78
E-CURD-122yes47.35
E-GEOD-84465yes39.41

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): FLI1, GATA1, LMO2, RUNX1, SPI1

miRNA regulators (miRDB)

54 targeting PLEK, 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-6758-5P100.0066.211470
HSA-MIR-6856-5P100.0065.471298
HSA-MIR-60799.9773.625593
HSA-MIR-548AA99.9670.643753
HSA-MIR-548AP-3P99.9670.643753
HSA-MIR-548T-3P99.9670.643753
HSA-MIR-141-3P99.9472.792421
HSA-MIR-200A-3P99.9472.682420
HSA-MIR-218-5P99.9372.222103
HSA-MIR-205-3P99.9269.923165
HSA-MIR-449399.9066.48977
HSA-MIR-391999.8769.452489
HSA-MIR-4728-5P99.8569.394718
HSA-MIR-4756-5P99.8464.981809
HSA-MIR-132399.8369.892471
HSA-MIR-3180-5P99.8269.122422
HSA-MIR-205-5P99.8170.051557
HSA-MIR-548O-3P99.7469.302228
HSA-MIR-1255A99.7468.09744
HSA-MIR-1255B-5P99.7468.16741
HSA-MIR-451699.6167.783390
HSA-MIR-1260A99.6166.671098
HSA-MIR-1260B99.6166.671098
HSA-MIR-1212299.5669.331672
HSA-MIR-6751-5P99.5664.991145
HSA-MIR-486-3P99.5166.821901
HSA-MIR-1213199.4868.721673
HSA-MIR-391599.4568.491905
HSA-MIR-446099.3768.52615
HSA-MIR-612899.3367.831581

Literature-anchored findings (GeneRIF, showing 12)

  • Translocation requires its phosphorylation and newly formed ligands (PMID:12054651)
  • A pleckstrin homology domain located in G protein-coupled receptor kinase-2 (GRK2) residue 548 to 660 plays a significant role in mediating interaction between protein kinase C beta 1 and GRK2. (PMID:12456365)
  • The human pleckstrin-1 solution nuclear magnetic resonance structure of the C-terminal pleckstrin homology domain was reported. (PMID:15698571)
  • Proteins beta3 integrin, Vav3, Plekhm1, and Src, implicated in attachment defects, had normal exon sequences in a new type of osteopetrosis. (PMID:19546854)
  • Idirect associations between plek and actin through 17 beta-hydroxysteroid dehydrogenase 4, alpha-actinin, moesin, radixin and factor XIIIA, is proposed. (PMID:19722192)
  • Here they show that the PH domain from Bcr-Abl binds a number of proteins involved in vital cellular processes in leukemogenesis. (PMID:19944685)
  • crystallization and preliminary X-ray diffraction analysis of the first 2 domains of pleckstrin (NPHDEP); work demonstrates that NPHDEP behaves as a monomer in solution and suggests that all 3 pleckstrin domains contribute to the dimerization interface (PMID:21393855)
  • These findings reveal a novel role of the PLD1-pleckstrin homology domain as a positive regulator of endocytosis and provide a link between PLD1 and HIF-1alpha in the EGFR endocytosis pathway. (PMID:26680696)
  • Only one gene, pleckstrin , was significantly overexpressed in periodontitis,cardiovascular disease, rheumatoid arthritis and ulcerative colitis , implicating this gene as an important networking link between these chronic inflammatory diseases (PMID:26686060)
  • A rare genomic duplication in 2p14 underlies autosomal dominant hearing loss DFNA58. (PMID:32337552)
  • Pleckstrin Levels Are Increased in Patients with Chronic Periodontitis and Regulated via the MAP Kinase-p38alpha Signaling Pathway in Gingival Fibroblasts. (PMID:35087525)
  • Higher expression of PLEK and LY86 as the potential biomarker of carotid atherosclerosis. (PMID:37861500)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_rerioplekENSDARG00000104325
mus_musculusPlekENSMUSG00000020120
rattus_norvegicusPlekENSRNOG00000005214

Paralogs (1): PLEK2 (ENSG00000100558)

Protein

Protein identifiers

PleckstrinP08567 (reviewed: P08567)

Alternative names: Platelet 47 kDa protein

All UniProt accessions (1): P08567

UniProt curated annotations — full annotation on UniProt →

Function. Major protein kinase C substrate of platelets.

RefSeq proteins (1): NP_002655* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000591DEP_domDomain
IPR001849PH_domainDomain
IPR011993PH-like_dom_sfHomologous_superfamily
IPR036388WH-like_DNA-bd_sfHomologous_superfamily
IPR036390WH_DNA-bd_sfHomologous_superfamily
IPR037370PleckstrinFamily
IPR037371PLEK_DEPDomain

Pfam: PF00169, PF00610

UniProt features (47 total): strand 24, helix 7, sequence variant 5, domain 3, turn 3, modified residue 3, chain 1, sequence conflict 1

Structure

Experimental structures (PDB)

8 structures.

PDBMethodResolution (Å)
2I5FX-RAY DIFFRACTION1.35
2I5CX-RAY DIFFRACTION1.75
1ZM0X-RAY DIFFRACTION2.1
1PLSSOLUTION NMR
1W4MSOLUTION NMR
1X05SOLUTION NMR
1XX0SOLUTION NMR
2CSOSOLUTION NMR

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P08567-F182.290.39

Functional residue map

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

Post-translational modifications (3): 64, 113, 117

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

IDPathway
R-HSA-114608Platelet degranulation

MSigDB gene sets: 443 (showing top): GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_HEMATOPOIETIC_PROGENITOR_CELL_DIFFERENTIATION, WALLACE_PROSTATE_CANCER_RACE_UP, GOBP_ACTIN_FILAMENT_BUNDLE_ORGANIZATION, GOBP_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING, MCLACHLAN_DENTAL_CARIES_UP, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, chr2p14, GOBP_PLATELET_ACTIVATION, MODULE_45, GOBP_INOSITOL_PHOSPHATE_METABOLIC_PROCESS, GOBP_POLYOL_METABOLIC_PROCESS, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, GOBP_NEGATIVE_REGULATION_OF_ALCOHOL_BIOSYNTHETIC_PROCESS, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS

GO Biological Process (25): hematopoietic progenitor cell differentiation (GO:0002244), platelet degranulation (GO:0002576), obsolete vesicle docking involved in exocytosis (GO:0006904), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), integrin-mediated signaling pathway (GO:0007229), positive regulation of platelet activation (GO:0010572), negative regulation of inositol phosphate biosynthetic process (GO:0010920), cell projection organization (GO:0030030), actin cytoskeleton organization (GO:0030036), positive regulation of actin filament depolymerization (GO:0030836), phospholipase C-inhibiting G protein-coupled receptor signaling pathway (GO:0030845), cortical actin cytoskeleton organization (GO:0030866), ruffle organization (GO:0031529), positive regulation of actin filament bundle assembly (GO:0032233), positive regulation of integrin activation (GO:0033625), intracellular signal transduction (GO:0035556), inositol phosphate metabolic process (GO:0043647), negative regulation of G protein-coupled receptor signaling pathway (GO:0045744), negative regulation of calcium-mediated signaling (GO:0050849), regulation of cell diameter (GO:0060305), thrombin-activated receptor signaling pathway (GO:0070493), negative regulation of thrombin-activated receptor signaling pathway (GO:0070495), platelet aggregation (GO:0070527), protein secretion by platelet (GO:0070560), positive regulation of cellular component biogenesis (GO:0044089)

GO Molecular Function (5): protein kinase C binding (GO:0005080), phosphatase activator activity (GO:0019211), protein homodimerization activity (GO:0042803), phosphatidylinositol-3,4-bisphosphate binding (GO:0043325), protein binding (GO:0005515)

GO Cellular Component (6): extracellular region (GO:0005576), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020), ruffle membrane (GO:0032587)

Reactome top-level categories

Rollup of top-1 pathways:

CategoryPathways
Response to elevated platelet cytosolic Ca2+1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure4
G protein-coupled receptor signaling pathway3
positive regulation of cytoskeleton organization2
positive regulation of supramolecular fiber organization2
intracellular anatomical structure2
hemopoiesis1
cell differentiation1
regulated exocytosis1
establishment of localization in cell1
phospholipase C activator activity1
cell surface receptor signaling pathway1
regulation of platelet activation1
platelet activation1
positive regulation of cell activation1
negative regulation of phosphorus metabolic process1
regulation of inositol phosphate biosynthetic process1
inositol phosphate biosynthetic process1
negative regulation of carbohydrate metabolic process1
negative regulation of alcohol biosynthetic process1
cellular component organization1
cytoskeleton organization1
actin filament-based process1
actin filament depolymerization1
regulation of actin filament depolymerization1
positive regulation of protein depolymerization1
phospholipase C inhibitor activity1
actin cytoskeleton organization1
cortical cytoskeleton organization1
plasma membrane bounded cell projection organization1
regulation of actin filament bundle assembly1
positive regulation of cellular component biogenesis1
actin filament bundle assembly1
positive regulation of protein-containing complex assembly1
integrin activation1
regulation of integrin activation1
signal transduction1
organophosphate metabolic process1
polyol metabolic process1
regulation of G protein-coupled receptor signaling pathway1
negative regulation of signal transduction1

Protein interactions and networks

STRING

4092 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PLEKMCF2P10911977
PLEKOSBPP22059908
PLEKCYTH1Q15438905
PLEKPLCD1P51178893
PLEKSRCP12931877
PLEKAKT1P31749867
PLEKBTKQ06187867
PLEKRABIFP47224861
PLEKCDC42P21181844
PLEKRHOAP06749835
PLEKCYTH3O43739814
PLEKANK1P16157800
PLEKANK3Q12955799
PLEKANK2Q01484797
PLEKRASA1P20936791

IntAct

17 interactions, top by confidence:

ABTypeScore
PLEKINPP5Apsi-mi:“MI:0407”(direct interaction)0.630
PLEKINPP5Apsi-mi:“MI:0914”(association)0.630
INPP5APLEKpsi-mi:“MI:0914”(association)0.630
PLEKWDR75psi-mi:“MI:0915”(physical association)0.590
CAVIN2PLEKpsi-mi:“MI:0915”(physical association)0.560
PLEKCAVIN2psi-mi:“MI:0914”(association)0.560
PLEKPF4psi-mi:“MI:0914”(association)0.460
PLEKpsi-mi:“MI:0915”(physical association)0.400
PLEKARHGEF1psi-mi:“MI:0915”(physical association)0.400
PLEKF13A1psi-mi:“MI:0914”(association)0.350
ENO1psi-mi:“MI:0914”(association)0.350
SARAFA2ML1psi-mi:“MI:0914”(association)0.350

BioGRID (10): PLEK (Reconstituted Complex), WDR75 (Affinity Capture-MS), PLEK (Affinity Capture-MS), PLEK (Affinity Capture-MS), PLEK (Proximity Label-MS), WDR75 (Affinity Capture-MS), PLEK (Affinity Capture-MS), ARHGEF1 (Affinity Capture-MS), PLEK (Cross-Linking-MS (XL-MS)), PLEK (Proximity Label-MS)

ESM2 similar proteins: O00170, O08915, O75689, O97627, O97628, P08487, P08567, P10686, P16885, P19174, P21146, P24135, P25098, P26817, P26818, P26819, P34512, P35626, P41229, P49619, P49620, P70392, Q09639, Q22070, Q24145, Q38JA7, Q3UYH7, Q4KM33, Q4PMC9, Q5F3R2, Q5FWY5, Q62077, Q64682, Q6IQX0, Q6Q308, Q7YRC1, Q8CIG3, Q8CIH5, Q8NB78, Q8R2V5

Diamond homologs: A0A0G2JUG7, A2A5R2, A5PKW4, A6H7I5, B6RSP1, D3ZL52, D4A631, E1JIT7, F1MUS9, F4IXW2, F4JN05, F4JSZ5, F4K2K3, G3X9K3, G5EET6, G5EGS5, O08967, O13817, O43739, O46382, P08567, P11075, P31749, P31751, P34512, P39052, P39054, P39993, P47102, P47196, P50570, P54644, P60669, P63034, P63035, P97694, P97696, Q00IB7, Q01314, Q10491

SIGNOR signaling

3 interactions.

AEffectBMechanism
PRKCAup-regulatesPLEKphosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance40
Likely benign0
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1455 predictions. Top by Δscore:

VariantEffectΔscore
2:68365390:GAAG:Gdonor_gain1.0000
2:68365394:GTGA:Gdonor_loss1.0000
2:68365395:T:Adonor_loss1.0000
2:68380322:TTACA:Tacceptor_loss1.0000
2:68380323:TACA:Tacceptor_loss1.0000
2:68380326:A:AGacceptor_gain1.0000
2:68380326:AG:Aacceptor_gain1.0000
2:68380326:AGG:Aacceptor_gain1.0000
2:68380327:G:GGacceptor_gain1.0000
2:68380327:G:GTacceptor_loss1.0000
2:68380327:GG:Gacceptor_gain1.0000
2:68380327:GGG:Gacceptor_gain1.0000
2:68380327:GGGGA:Gacceptor_gain1.0000
2:68380479:GGATG:Gdonor_gain1.0000
2:68380480:GATG:Gdonor_gain1.0000
2:68380480:GATGG:Gdonor_gain1.0000
2:68380481:ATGG:Adonor_loss1.0000
2:68380484:G:Adonor_loss1.0000
2:68380721:A:AGacceptor_gain1.0000
2:68380721:AGTTT:Aacceptor_gain1.0000
2:68380722:G:GCacceptor_gain1.0000
2:68380722:GT:Gacceptor_gain1.0000
2:68380722:GTT:Gacceptor_gain1.0000
2:68380722:GTTT:Gacceptor_gain1.0000
2:68380722:GTTTG:Gacceptor_gain1.0000
2:68380857:G:GTdonor_gain1.0000
2:68380858:A:Tdonor_gain1.0000
2:68380869:G:GTdonor_gain1.0000
2:68382531:T:Gacceptor_gain1.0000
2:68386682:ACTTT:Adonor_gain1.0000

AlphaMissense

2338 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
2:68388488:G:CK253N1.000
2:68388488:G:TK253N1.000
2:68380346:T:AW21R0.999
2:68380346:T:CW21R0.999
2:68380798:T:AW92R0.999
2:68380798:T:CW92R0.999
2:68388486:A:GK253E0.999
2:68393190:G:CR264T0.999
2:68393191:G:CR264S0.999
2:68393191:G:TR264S0.999
2:68395775:T:AW338R0.999
2:68395775:T:CW338R0.999
2:68393180:T:AW261R0.998
2:68393180:T:CW261R0.998
2:68393190:G:TR264M0.998
2:68393223:T:CL275P0.998
2:68395777:G:CW338C0.998
2:68395777:G:TW338C0.998
2:68386502:G:AG158D0.997
2:68386580:T:CL184P0.997
2:68393182:G:CW261C0.997
2:68393182:G:TW261C0.997
2:68393189:A:GR264G0.997
2:68393228:T:GY277D0.997
2:68365383:T:CL11P0.996
2:68386523:T:CL165P0.996
2:68386678:T:GY217D0.996
2:68388481:T:CL251S0.996
2:68388487:A:CK253T0.996
2:68393163:G:AG255E0.996

dbSNP variants (sampled 300 via entrez): RS1000097883 (2:68393568 G>A), RS1000111924 (2:68373226 A>C,G), RS1000201784 (2:68367252 T>C), RS1000257480 (2:68379034 T>C), RS1000355893 (2:68395213 T>C), RS1000399596 (2:68390874 A>G), RS1000415580 (2:68384491 G>A,T), RS1000527370 (2:68396735 T>C), RS1000533110 (2:68373416 G>A,T), RS1000557788 (2:68373289 G>A), RS1000677038 (2:68378854 G>C,T), RS1000742443 (2:68396719 A>G,T), RS1000846564 (2:68390640 G>A), RS1001089655 (2:68396480 T>A), RS1001130070 (2:68374668 A>G)

Disease associations

OMIM: gene MIM:173570 | disease phenotypes:

GenCC curated gene-disease

DiseaseClassificationInheritance
autosomal dominant nonsyndromic hearing loss 58LimitedAutosomal dominant

Mondo (1): autosomal dominant nonsyndromic hearing loss 58 (MONDO:0014293)

Orphanet (0):

HPO phenotypes

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

GWAS associations

20 associations (top):

StudyTraitp-value
GCST000274_1Metabolite levels2.000000e-09
GCST000612_20Celiac disease8.000000e-09
GCST001198_69Multiple sclerosis5.000000e-11
GCST001341_19Multiple sclerosis2.000000e-07
GCST002324_1Anger4.000000e-06
GCST004607_216Plateletcrit2.000000e-14
GCST004627_77Lymphocyte count3.000000e-13
GCST005531_106Multiple sclerosis1.000000e-13
GCST009030_1Venous thromboembolism3.000000e-10
GCST009597_9Multiple sclerosis5.000000e-16
GCST90002379_23Basophil count4.000000e-09
GCST90002388_72Lymphocyte count6.000000e-28
GCST90002392_205Mean corpuscular volume2.000000e-12
GCST90002393_191Monocyte count1.000000e-14
GCST90002395_327Mean platelet volume2.000000e-21
GCST90002397_806Mean spheric corpuscular volume8.000000e-13
GCST90002399_145Neutrophil percentage of white cells7.000000e-11
GCST90002400_567Plateletcrit1.000000e-27
GCST90002401_377Platelet distribution width2.000000e-21
GCST90002407_51White blood cell count2.000000e-12

EFO canonical traits (7, from GWAS)

EFO IDTrait name
EFO:0003015aggressive behavior
EFO:0007985platelet crit
EFO:0004587lymphocyte count
EFO:0005090basophil count
EFO:0005091monocyte count
EFO:0007990neutrophil percentage of leukocytes
EFO:0007984platelet component distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523171 (SINGLE PROTEIN)

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

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Tretinoinincreases expression3
tamibaroteneincreases expression2
Resveratrolaffects cotreatment, increases expression, decreases reaction, increases phosphorylation2
Benzo(a)pyrenedecreases expression, increases expression2
Smokeincreases expression, decreases expression, increases abundance2
triphenyl phosphateaffects expression1
bisphenol Adecreases expression1
nickel sulfateincreases expression1
dioleoylphosphatidic acidincreases phosphorylation, increases reaction1
S-(1,2-dichlorovinyl)cysteineaffects response to substance, increases expression1
phosphatidylethanolincreases phosphorylation, increases reaction1
CGP 52608affects binding, increases reaction1
nutlin 3affects cotreatment, increases expression1
hexabrominated diphenyl ether 153decreases expression1
licochalcone Bincreases expression1
Pioglitazonedecreases expression1
Zoledronic Acidincreases expression1
Acetaminophenincreases expression1
Air Pollutantsincreases abundance, increases expression1
Cisplatinincreases expression1
Coalincreases abundance, increases expression1
Dactinomycinaffects cotreatment, increases expression1
Diurondecreases expression1
Ivermectindecreases expression1
Lipopolysaccharidesincreases expression, affects response to substance1
Nickelincreases expression1
Plant Extractsaffects cotreatment, increases expression1
Quercetindecreases reaction, increases phosphorylation1
Tetradecanoylphorbol Acetatedecreases reaction, increases phosphorylation1
Tobacco Smoke Pollutiondecreases expression1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL4419286BindingBinding affinity to PLEK PH-domain (unknown origin) at 0.01 to 50 uM by SPR spectroscopyMethods and compositions for inhibiting cnksr1

Clinical trials (associated diseases)

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