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KCNH6

gene
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Also known as Kv11.2erg2HERG2

Summary

KCNH6 (potassium voltage-gated channel subfamily H member 6, HGNC:18862) is a protein-coding gene on chromosome 17q23.3, encoding Voltage-gated inwardly rectifying potassium channel KCNH6 (Q9H252). Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel.

Voltage-gated potassium (Kv) channels represent the most complex class of voltage-gated ion channels from both functional and structural standpoints. Their diverse functions include regulating neurotransmitter release, heart rate, insulin secretion, neuronal excitability, epithelial electrolyte transport, smooth muscle contraction, and cell volume. This gene encodes a member of the potassium channel, voltage-gated, subfamily H. This member is a pore-forming (alpha) subunit. Alternative splicing results in multiple transcript variants that encode different isoforms.

Source: NCBI Gene 81033 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 199 total
  • Druggable target: yes
  • MANE Select transcript: NM_001278919

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:18862
Approved symbolKCNH6
Namepotassium voltage-gated channel subfamily H member 6
Location17q23.3
Locus typegene with protein product
StatusApproved
AliasesKv11.2, erg2, HERG2
Ensembl geneENSG00000173826
Ensembl biotypeprotein_coding
OMIM608168
Entrez81033

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 7 protein_coding, 1 nonsense_mediated_decay

ENST00000314672, ENST00000456941, ENST00000580652, ENST00000581784, ENST00000583023, ENST00000583465, ENST00000913416, ENST00000913417

RefSeq mRNA: 4 — MANE Select: NM_001278919 NM_001278919, NM_001278920, NM_030779, NM_173092

CCDS: CCDS11638, CCDS11639, CCDS62290

Canonical transcript exons

ENST00000314672 — 13 exons

ExonStartEnd
ENSE000011806656352413963524369
ENSE000026855626354560963546727
ENSE000027076476352335863523489
ENSE000035115056353841063538662
ENSE000036060946353566963536068
ENSE000036097696353033763530542
ENSE000036107416354424963544411
ENSE000036284686354357663543660
ENSE000036432616353388663534311
ENSE000036554526353806563538264
ENSE000036655936354507863545264
ENSE000036845886354224163542434
ENSE000036932236353009163530252

Expression profiles

Bgee: expression breadth broad, 96 present calls, max score 90.87.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.4556 / max 971.9161, expressed in 71 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
1621981.297366
1621970.141816
2083120.01656

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
olfactory bulbUBERON:000226490.87gold quality
type B pancreatic cellCL:000016990.20gold quality
buccal mucosa cellCL:000233687.57silver quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099183.59gold quality
cervix squamous epitheliumUBERON:000692282.76gold quality
skeletal muscle tissue of biceps brachiiUBERON:000450278.99gold quality
vastus lateralisUBERON:000137977.34gold quality
quadriceps femorisUBERON:000137776.44gold quality
gluteal muscleUBERON:000200075.09silver quality
biceps brachiiUBERON:000150774.81gold quality
diaphragmUBERON:000110373.62gold quality
adult mammalian kidneyUBERON:000008272.41gold quality
tongue squamous epitheliumUBERON:000691972.03gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047371.99silver quality
upper arm skinUBERON:000426371.89gold quality
hair follicleUBERON:000207371.52gold quality
epithelial cell of pancreasCL:000008371.18gold quality
cervix epitheliumUBERON:000480171.04gold quality
mucosa of paranasal sinusUBERON:000503069.92gold quality
adenohypophysisUBERON:000219669.62gold quality
pituitary glandUBERON:000000769.53gold quality
islet of LangerhansUBERON:000000669.03gold quality
jejunal mucosaUBERON:000039968.75silver quality
heart right ventricleUBERON:000208068.55gold quality
kidneyUBERON:000211368.09gold quality
secondary oocyteCL:000065567.93gold quality
cardiac muscle of right atriumUBERON:000337967.22gold quality
left ventricle myocardiumUBERON:000656667.21gold quality
myocardiumUBERON:000234967.17gold quality
cerebellar vermisUBERON:000472067.05gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 4.

ExperimentMarker?Max mean expression
E-MTAB-11121yes365.54
E-MTAB-5061yes129.86
E-ENAD-27yes4.93
E-ANND-3yes4.77

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

21 targeting KCNH6, 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-477599.9875.006394
HSA-MIR-6778-3P99.9667.292693
HSA-MIR-590-3P99.9674.346478
HSA-MIR-76599.8468.242442
HSA-MIR-1212299.5669.331672
HSA-MIR-766-3P99.4765.241811
HSA-MIR-504-3P99.3067.181745
HSA-MIR-450599.2767.812678
HSA-MIR-324-3P99.2666.311034
HSA-MIR-578799.2267.862628
HSA-MIR-3135B98.6165.331470
HSA-MIR-619-5P98.5764.971988
HSA-MIR-1199-5P98.4466.51829
HSA-MIR-6751-3P98.4466.35835
HSA-MIR-5008-5P98.4265.871019
HSA-MIR-6826-3P98.1966.321153
HSA-MIR-430398.0168.132304
HSA-MIR-6765-3P97.8364.591165
HSA-MIR-2467-5P97.3667.71991
HSA-MIR-34697.0166.97662
HSA-MIR-367497.0168.861171

Literature-anchored findings (GeneRIF, showing 7)

  • Transcripts for HERG1 were present in all adenomas and although transcripts for HERG2 and HERG3 were also detected, their expression level was more variable. (PMID:12634931)
  • results indicated that downregulation of miR-224 suppressed cell growth and resulted in the enhancement of cell apoptosis through activation of the ERG2-BAK-induced apoptosis pathway (PMID:25783051)
  • dysfunction of KCNH6 causes overstimulation of insulin secretion in the short term and beta cell failure in the long term. (PMID:30590050)
  • Prostate tumors of native men from West Africa show biologically distinct pathways-A comparative genomic study. (PMID:34529278)
  • Berberine is an insulin secretagogue targeting the KCNH6 potassium channel. (PMID:34556670)
  • Potassium Ion Channel Protein (KCNH) Levels in Patients with Fibromyalgia Syndrome. (PMID:35818223)
  • KCNH6 Enhanced Hepatic Glucose Metabolism through Mitochondrial Ca(2+) Regulation and Oxidative Stress Inhibition. (PMID:36217412)

Cross-species orthologs

8 orthologs

OrganismSymbolGene ID
mus_musculusKcnh6ENSMUSG00000001901
rattus_norvegicusKcnh6ENSRNOG00000008078
drosophila_melanogasterseiFBGN0003353
drosophila_melanogasterCngAFBGN0261612
caenorhabditis_elegansWBGENE00000487
caenorhabditis_elegansWBGENE00006526
caenorhabditis_elegansWBGENE00006830
caenorhabditis_elegansWBGENE00022295

Paralogs (17): KCNH2 (ENSG00000055118), CNGB1 (ENSG00000070729), KCNH4 (ENSG00000089558), HCN2 (ENSG00000099822), CNGA4 (ENSG00000132259), KCNH3 (ENSG00000135519), HCN4 (ENSG00000138622), KCNH5 (ENSG00000140015), KCNH1 (ENSG00000143473), HCN3 (ENSG00000143630), CNGA3 (ENSG00000144191), HCN1 (ENSG00000164588), CNGB3 (ENSG00000170289), CNGA2 (ENSG00000183862), KCNH8 (ENSG00000183960), KCNH7 (ENSG00000184611), CNGA1 (ENSG00000198515)

Protein

Protein identifiers

Voltage-gated inwardly rectifying potassium channel KCNH6 — Q9H252 (reviewed: Q9H252)

Alternative names: Ether-a-go-go-related gene potassium channel 2, Potassium voltage-gated channel subfamily H member 6, Voltage-gated potassium channel subunit Kv11.2

All UniProt accessions (2): Q9H252, J3KSC2

UniProt curated annotations — full annotation on UniProt →

Function. Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Characterized by unusual gating kinetics by producing relatively small outward currents during membrane depolarization and large inward currents during subsequent repolarization which reflect a rapid inactivation during depolarization and quick recovery from inactivation but slow deactivation (closing) during repolarization. Activates even more slowly than KCNH2.

Subunit / interactions. The potassium channel is probably composed of a homo- or heterotetrameric complex of pore-forming alpha subunits that can associate only within their subfamily.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in prolactin-secreting adenomas.

Domain organisation. The S4-S5 linker acts as a signal integrator where it both couples voltage-sensor domain (VSD) movement to pore opening and closure, as well as providing a binding site for other domains that regulate activation and/or deactivation of the channel.

Similarity. Belongs to the potassium channel family. H (Eag) (TC 1.A.1.20) subfamily. Kv11.2/KCNH6 sub-subfamily.

Isoforms (4)

UniProt IDNamesCanonical?
Q9H252-41yes
Q9H252-12
Q9H252-23
Q9H252-34

RefSeq proteins (4): NP_001265848, NP_001265849, NP_110406, NP_775115 (=MANE)

Domains & families (InterPro)

IDNameType
IPR000014PASDomain
IPR000595cNMP-bd_domDomain
IPR003938K_chnl_volt-dep_EAG/ELK/ERGFamily
IPR003967K_chnl_volt-dep_ERGFamily
IPR005821Ion_trans_domDomain
IPR014710RmlC-like_jellyrollHomologous_superfamily
IPR018490cNMP-bd_dom_sfHomologous_superfamily
IPR035965PAS-like_dom_sfHomologous_superfamily
IPR050818KCNH_animal-typeFamily

Pfam: PF00027, PF00520, PF13426

Catalyzed reactions (Rhea), 1 shown:

  • K(+)(in) = K(+)(out) (RHEA:29463)

UniProt features (31 total): topological domain 8, transmembrane region 6, splice variant 4, region of interest 3, domain 2, sequence variant 2, chain 1, intramembrane region 1, short sequence motif 1, compositionally biased region 1, glycosylation site 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9H252-F169.420.32

Functional residue map

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

Glycosylation sites (1): 449

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-1296072Voltage gated Potassium channels
R-HSA-112316Neuronal System
R-HSA-1296071Potassium Channels

MSigDB gene sets: 97 (showing top): GOBP_POTASSIUM_ION_TRANSPORT, GOBP_CIRCULATORY_SYSTEM_PROCESS, REACTOME_VOLTAGE_GATED_POTASSIUM_CHANNELS, REACTOME_POTASSIUM_CHANNELS, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_REGULATION_OF_CARDIAC_MUSCLE_CELL_MEMBRANE_REPOLARIZATION, AP1_Q4_01, GOBP_REGULATION_OF_HEART_RATE, GOBP_REGULATION_OF_SYSTEM_PROCESS, GOBP_REGULATION_OF_HEART_RATE_BY_CARDIAC_CONDUCTION, GOBP_CARDIAC_MUSCLE_CELL_ACTION_POTENTIAL, GOBP_HEART_PROCESS, HNF1_01, GOBP_MEMBRANE_REPOLARIZATION, GOBP_CARDIAC_CONDUCTION

GO Biological Process (8): regulation of ventricular cardiac muscle cell membrane repolarization (GO:0060307), potassium ion transmembrane transport (GO:0071805), membrane repolarization during cardiac muscle cell action potential (GO:0086013), regulation of heart rate by cardiac conduction (GO:0086091), monoatomic ion transport (GO:0006811), potassium ion transport (GO:0006813), monoatomic ion transmembrane transport (GO:0034220), transmembrane transport (GO:0055085)

GO Molecular Function (4): inward rectifier potassium channel activity (GO:0005242), monoatomic ion channel activity (GO:0005216), voltage-gated potassium channel activity (GO:0005249), potassium channel activity (GO:0005267)

GO Cellular Component (3): plasma membrane (GO:0005886), monoatomic ion channel complex (GO:0034702), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Potassium Channels1
Neuronal System1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
transport2
regulation of cardiac muscle cell membrane repolarization1
ventricular cardiac muscle cell membrane repolarization1
potassium ion transport1
monoatomic cation transmembrane transport1
cardiac muscle cell action potential1
membrane repolarization during action potential1
cardiac muscle cell membrane repolarization1
regulation of heart rate1
cardiac conduction1
metal ion transport1
monoatomic ion transport1
transmembrane transport1
cellular process1
voltage-gated potassium channel activity1
ligand-gated monoatomic cation channel activity1
monoatomic ion transmembrane transporter activity1
channel activity1
potassium channel activity1
voltage-gated monoatomic cation channel activity1
monoatomic cation channel activity1
potassium ion transmembrane transporter activity1
membrane1
cell periphery1
transmembrane transporter complex1
cellular anatomical structure1

Protein interactions and networks

STRING

680 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
KCNH6SIGMAR1Q99720944
KCNH6EBPQ15125901
KCNH6KCNA4P22459742
KCNH6ERGP11308727
KCNH6ETS1P14921560
KCNH6NSDHLQ15738553
KCNH6PRLP01236546
KCNH6ETS2P15036536
KCNH6MSMO1Q15800526
KCNH6EGR2P11161512
KCNH6DHCR7Q9UBM7435
KCNH6TMPRSS2O15393432
KCNH6TMBIM4Q9HC24427
KCNH6SRSF10O75494413
KCNH6CYP51A1Q16850400

IntAct

0 interactions, top by confidence:

BioGRID (2): KCNH6 (Protein-peptide), KCNH6 (Negative Genetic)

ESM2 similar proteins: A2AJ88, B3MRI9, B3NY03, B4H3U8, B4IL64, B4JLX2, B4L535, B4M709, B4N1W9, B4Q0P3, B5DKS8, D3ZEF4, O08703, O08962, O35219, O54853, P25848, P59111, P97414, Q02331, Q12809, Q14999, Q17QV9, Q21534, Q3TRM4, Q5BK26, Q5R667, Q5RCJ3, Q5RDS0, Q5TEA3, Q67E00, Q67E01, Q6CF18, Q6ZV29, Q7TNL3, Q7TT23, Q8IY17, Q8N2I9, Q8RY24, Q8VE73

Diamond homologs: A5K0N4, G5EFJ9, O08703, O08962, O18965, O35219, O54852, O54853, O89047, O95259, P29281, P59111, Q02280, Q12809, Q60603, Q63472, Q8I719, Q8NCM2, Q8WNY2, Q920E3, Q96L42, Q9EPI9, Q9ER47, Q9H252, Q9NS40, Q9PT84, Q9QWS8, Q9R1T9, Q9TSZ3, Q9TUI4, Q9ULD8, Q9UQ05, Q9WVJ0, W7JX98, A0A509AKL0, O64511, P93025, Q1M667, Q2NCA3, Q2QYY8

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance184
Likely benign11
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

2888 predictions. Top by Δscore:

VariantEffectΔscore
17:63523490:G:GGdonor_gain1.0000
17:63524365:GGATG:Gdonor_gain1.0000
17:63524366:GATGG:Gdonor_gain1.0000
17:63524367:A:Tdonor_gain1.0000
17:63530335:AGAG:Aacceptor_gain1.0000
17:63530336:GAGG:Gacceptor_gain1.0000
17:63534310:AGGTG:Adonor_loss1.0000
17:63534312:G:GCdonor_loss1.0000
17:63534313:T:Gdonor_loss1.0000
17:63536065:GGCT:Gdonor_gain1.0000
17:63536066:GCT:Gdonor_gain1.0000
17:63536066:GCTG:Gdonor_gain1.0000
17:63536069:G:GGdonor_gain1.0000
17:63536073:G:GGdonor_gain1.0000
17:63538060:CCCA:Cacceptor_loss1.0000
17:63538061:CCAGC:Cacceptor_loss1.0000
17:63538063:A:AGacceptor_gain1.0000
17:63538064:G:GTacceptor_gain1.0000
17:63538064:GCCC:Gacceptor_gain1.0000
17:63538064:GCCCT:Gacceptor_gain1.0000
17:63542403:G:GGdonor_gain1.0000
17:63542430:GGGAC:Gdonor_gain1.0000
17:63542431:GGAC:Gdonor_gain1.0000
17:63542431:GGACG:Gdonor_gain1.0000
17:63542432:G:GTdonor_gain1.0000
17:63542432:G:Tdonor_gain1.0000
17:63542432:GAC:Gdonor_gain1.0000
17:63542435:G:GGdonor_gain1.0000
17:63544247:A:AGacceptor_gain1.0000
17:63544248:G:GGacceptor_gain1.0000

AlphaMissense

6269 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
17:63524147:T:CF29L1.000
17:63524149:C:AF29L1.000
17:63524149:C:GF29L1.000
17:63535875:G:CW436C1.000
17:63535875:G:TW436C1.000
17:63536002:T:CF479L1.000
17:63536004:C:AF479L1.000
17:63536004:C:GF479L1.000
17:63536065:G:CG500R1.000
17:63536066:G:AG500D1.000
17:63538079:A:CS506R1.000
17:63538081:C:AS506R1.000
17:63538081:C:GS506R1.000
17:63538088:G:AG509R1.000
17:63538088:G:CG509R1.000
17:63538089:G:AG509E1.000
17:63523466:T:AI18N0.999
17:63523477:T:CF22L0.999
17:63523479:C:AF22L0.999
17:63523479:C:GF22L0.999
17:63524148:T:CF29S0.999
17:63524151:T:CL30P0.999
17:63524157:C:AA32D0.999
17:63530163:T:CL127P0.999
17:63533978:G:CK256N0.999
17:63533978:G:TK256N0.999
17:63533985:T:AW259R0.999
17:63533985:T:CW259R0.999
17:63533989:A:CD260A0.999
17:63533989:A:TD260V0.999

dbSNP variants (sampled 300 via entrez): RS1000031491 (17:63548881 A>G), RS1000083419 (17:63549102 G>A), RS1000110265 (17:63525729 A>G), RS1000192342 (17:63523305 T>C), RS1000305435 (17:63532224 C>A), RS1000375566 (17:63530610 G>A,C), RS1000503560 (17:63524483 CCT>C), RS1000605584 (17:63530521 C>G,T), RS1000676986 (17:63531990 G>A), RS1000744987 (17:63536259 C>T), RS1000754594 (17:63543820 C>T), RS1000872464 (17:63549018 C>T), RS1001038359 (17:63530821 G>A), RS1001164654 (17:63534660 C>T), RS1001198788 (17:63547221 G>T)

Disease associations

OMIM: gene MIM:608168 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

StudyTraitp-value
GCST001438_9Crohn’s disease7.000000e-09
GCST010002_128Refractive error2.000000e-13

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2362996 (PROTEIN FAMILY), CHEMBL2363011 (SINGLE PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: vgic — Voltage-gated potassium channels (Kv)

Most potent curated ligand interactions (5 total), top 5:

LigandActionAffinityParameter
γ-KTx1.7Gating inhibitor8.8pKd
BeKm-1Gating inhibitor8.1pKd
E4031Channel blocker6.9pKd
ErgTx-1Inhibition6.7pKd
NS1643Activator4.9pEC50

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.82Ki0.15nMCHEMBL5722941
9.74IC500.18nMCHEMBL5722941

PubChem BioAssay actives

2 with measured affinity, of 38 total; 1 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-[(1R,2aS,4S,5aS,8aS,10S,11aR,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,87R,93S,96S,99S)-17a,20a,23a,53a,63-pentakis(4-aminobutyl)-31-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-5-carbamimidamido-2-[[(2S)-1-[(2S)-5-oxopyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]pentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-16,29a,72,78-tetrakis(2-amino-2-oxoethyl)-14a,26a-bis(3-amino-3-oxopropyl)-2a,38a,66-tribenzyl-28,50a,57-tris[(2S)-butan-2-yl]-4,5a,19,42,45,69-hexakis(3-carbamimidamidopropyl)-51,54-bis(2-carboxyethyl)-56a,99-bis(carboxymethyl)-36-[[(2S,3S)-1-(carboxymethylamino)-3-methyl-1-oxopentan-2-yl]carbamoyl]-39,60-bis[(1R)-1-hydroxyethyl]-75,93-bis(hydroxymethyl)-32a,35a,59a-tris[(4-hydroxyphenyl)methyl]-22-(1H-imidazol-4-ylmethyl)-96-(1H-indol-3-ylmethyl)-41a-methyl-25-(2-methylpropyl)-1a,3,4a,6,7a,9,10a,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,5,6a,8,9a,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.010,14.0144,148]nonahexacontahectan-8a-yl]propanoic acid2198828: Binding affinity to KV channel (unknown origin) assessed as inhibition constantki0.0001uM

CTD chemical–gene interactions

18 total (human), top 18 by PubMed support.

ChemicalActions (top 5)PubMed papers
chloropicrinincreases expression2
Benzo(a)pyrenedecreases expression, affects methylation2
Aflatoxin B1increases methylation2
ethyl-p-hydroxybenzoatedecreases expression1
aflatoxin B2increases methylation1
CGP 52608affects binding, increases reaction1
2-palmitoylglycerolincreases expression1
erucylphospho-N,N,N-trimethylpropylammoniumincreases expression1
ICG 001increases expression1
N-(1-(2,3-dimethoxyphenyl)-4-methyl-3-penten-1-yl)-1-(5-bromofurfuryl)-1-piperidyl-4-aminedecreases activity1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acidincreases expression1
Acetaminophenincreases expression1
Calcitriolincreases expression, affects cotreatment1
Copperincreases expression, affects binding1
Testosteroneincreases expression, affects cotreatment1
Thiosemicarbazonesaffects binding, increases expression1
8-Bromo Cyclic Adenosine Monophosphatedecreases expression1
1-Methyl-4-phenylpyridiniumincreases expression1

ChEMBL screening assays

23 unique, capped per target: 21 binding, 2 toxicity

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1787442BindingInhibition of human recombinant Kv channel at 10 uM by radioligand binding assayStructure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement. — Bioorg Med Chem Lett
CHEMBL5522525ToxicityInhibition of human K+ channel by automated electrophysiologyDiscovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure. — J Med Chem

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 79

This page pulls from 79 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot