KCNF1

Summary

KCNF1 (potassium voltage-gated channel modifier subfamily F member 1, HGNC:6246) is a protein-coding gene on chromosome 2p25.1, encoding Voltage-gated potassium channel regulatory subunit KCNF1 (Q9H3M0). Regulatory alpha-subunit of the voltage-gated potassium (Kv) channel which, when coassembled with KCNB1 or KCNB2, can modulate their expression and their gating kinetics by acting on deactivation upon repolarization and inactivation during maintained depolarization.

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 F. This gene is intronless and expressed in all tissues tested, including the heart, skeletal muscle, brain, kidney, and pancreas.

Source: NCBI Gene 3754 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 52 total — 1 pathogenic, 1 likely-pathogenic
• Druggable target: yes
• MANE Select transcript: NM_002236

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6246
Approved symbol	KCNF1
Name	potassium voltage-gated channel modifier subfamily F member 1
Location	2p25.1
Locus type	gene with protein product
Status	Approved
Aliases	Kv5.1, kH1, IK8
Ensembl gene	ENSG00000162975
Ensembl biotype	protein_coding
OMIM	603787
Entrez	3754

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000295082, ENST00000961110

RefSeq mRNA: 1 — MANE Select: NM_002236 NM_002236

CCDS: CCDS1676

Canonical transcript exons

ENST00000295082 — 1 exons

Exon	Start	End
ENSE00001070247	10911934	10914225

Expression profiles

Bgee: expression breadth ubiquitous, 135 present calls, max score 92.06.

FANTOM5 (CAGE): breadth broad, TPM avg 3.9671 / max 142.6659, expressed in 471 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter ID	TPM avg	Samples expressed
18862	2.5314	403
18861	0.7810	203
18858	0.2224	102
18860	0.1731	75
18864	0.0708	43
18863	0.0688	35
18865	0.0619	37
18859	0.0578	34

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
prefrontal cortex	UBERON:0000451	92.06	gold quality
putamen	UBERON:0001874	91.70	gold quality
nucleus accumbens	UBERON:0001882	91.06	gold quality
right frontal lobe	UBERON:0002810	89.95	gold quality
caudate nucleus	UBERON:0001873	89.87	gold quality
cingulate cortex	UBERON:0003027	89.84	gold quality
anterior cingulate cortex	UBERON:0009835	89.77	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	89.69	gold quality
frontal cortex	UBERON:0001870	89.59	gold quality
Brodmann (1909) area 9	UBERON:0013540	89.42	gold quality
neocortex	UBERON:0001950	89.04	gold quality
telencephalon	UBERON:0001893	88.26	gold quality
orbitofrontal cortex	UBERON:0004167	88.14	gold quality
cerebral cortex	UBERON:0000956	88.09	gold quality
Brodmann (1909) area 10	UBERON:0013541	88.08	gold quality
superior frontal gyrus	UBERON:0002661	87.01	gold quality
amygdala	UBERON:0001876	86.88	gold quality
cortical plate	UBERON:0005343	86.46	gold quality
temporal lobe	UBERON:0001871	86.10	gold quality
Brodmann (1909) area 46	UBERON:0006483	86.08	gold quality
parietal lobe	UBERON:0001872	85.90	gold quality
postcentral gyrus	UBERON:0002581	85.82	gold quality
Ammon’s horn	UBERON:0001954	85.41	gold quality
entorhinal cortex	UBERON:0002728	85.34	gold quality
frontal pole	UBERON:0002795	85.02	gold quality
vena cava	UBERON:0004087	84.59	silver quality
primary visual cortex	UBERON:0002436	84.58	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	84.52	silver quality
occipital lobe	UBERON:0002021	84.43	gold quality
forebrain	UBERON:0001890	84.12	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.40

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

24 targeting KCNF1, 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-4510	100.00	66.60	2050
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-6129	100.00	66.46	2080
HSA-MIR-6130	100.00	66.69	2012
HSA-MIR-6133	100.00	66.48	2064
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-6883-5P	99.69	68.05	3785
HSA-MIR-1912-3P	99.32	67.40	936
HSA-MIR-196A-3P	99.19	67.34	1204
HSA-MIR-7109-5P	99.18	66.13	1057
HSA-MIR-1295B-5P	99.03	67.50	810
HSA-MIR-7157-3P	98.95	68.70	1582
HSA-MIR-6737-3P	98.95	68.56	1577
HSA-MIR-4763-5P	98.75	63.89	854
HSA-MIR-5008-3P	98.73	67.50	1433
HSA-MIR-3188	98.58	65.60	878
HSA-MIR-5088-3P	98.29	66.63	1310
HSA-MIR-3130-5P	98.14	66.00	711
HSA-MIR-4482-5P	97.53	65.68	598
HSA-MIR-6849-3P	97.25	64.57	1371
HSA-MIR-6886-3P	96.96	66.36	844
HSA-MIR-5591-3P	96.23	67.03	489

Literature-anchored findings (GeneRIF, showing 1)

• KCNF1 promotes lung cancer by modulating ITGB4 expression. (PMID:36385523)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	kcnf1b	ENSDARG00000027285
danio_rerio	kcnf1a	ENSDARG00000027940
mus_musculus	Kcnf1	ENSMUSG00000051726
rattus_norvegicus	Kcnf1	ENSRNOG00000024310

Paralogs (31): KCNG1 (ENSG00000026559), KCNQ1 (ENSG00000053918), KCNQ2 (ENSG00000075043), KCND1 (ENSG00000102057), KCNA7 (ENSG00000104848), KCNA1 (ENSG00000111262), KCNC4 (ENSG00000116396), KCNQ4 (ENSG00000117013), KCNS1 (ENSG00000124134), KCNC1 (ENSG00000129159), KCNA5 (ENSG00000130037), KCNC3 (ENSG00000131398), KCNA10 (ENSG00000143105), KCNA6 (ENSG00000151079), KCNS2 (ENSG00000156486), KCNB1 (ENSG00000158445), KCNV1 (ENSG00000164794), KCNC2 (ENSG00000166006), KCNV2 (ENSG00000168263), KCNG4 (ENSG00000168418), KCNS3 (ENSG00000170745), KCNG3 (ENSG00000171126), KCND3 (ENSG00000171385), KCNA3 (ENSG00000177272), KCNA2 (ENSG00000177301), KCNG2 (ENSG00000178342), KCNA4 (ENSG00000182255), KCNB2 (ENSG00000182674), KCNQ3 (ENSG00000184156), KCND2 (ENSG00000184408), KCNQ5 (ENSG00000185760)

Protein

Protein identifiers

Voltage-gated potassium channel regulatory subunit KCNF1 — Q9H3M0 (reviewed: Q9H3M0)

Alternative names: Potassium voltage-gated channel subfamily F member 1, Voltage-gated potassium channel subunit Kv5.1, kH1

All UniProt accessions (1): Q9H3M0

UniProt curated annotations — full annotation on UniProt →

Function. Regulatory alpha-subunit of the voltage-gated potassium (Kv) channel which, when coassembled with KCNB1 or KCNB2, can modulate their expression and their gating kinetics by acting on deactivation upon repolarization and inactivation during maintained depolarization. Accelerates inactivation but has relatively little effect on deactivation. Coexpression with KCNB1 or KCNB2 markedly slows inactivation. Each modulatory subunit has its own specific properties of regulation, and can lead to extensive inhibitions, to large changes in kinetics, and/or to large shifts in the voltage dependencies of the inactivation process. The gating kinetics depends on the nature and stoichiometry of the associated regulatory sunbunit. Fails to produce a potassium current when expressed alone.

Subunit / interactions. Heterotetramer with KCNB1 or KCNB2.

Subcellular location. Cell membrane.

Tissue specificity. Detected in heart, brain, liver, skeletal muscle, kidney and pancreas.

Similarity. Belongs to the potassium channel family. F (TC 1.A.1.2) subfamily. Kv5.1/KCNF1 sub-subfamily.

RefSeq proteins (1): NP_002227* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR003131	T1-type_BTB	Domain
IPR003968	K_chnl_volt-dep_Kv	Family
IPR003971	K_chnl_volt-dep_Kv5/Kv9	Family
IPR005821	Ion_trans_dom	Domain
IPR011333	SKP1/BTB/POZ_sf	Homologous_superfamily
IPR027359	Volt_channel_dom_sf	Homologous_superfamily
IPR028325	VG_K_chnl	Family
IPR048010	KCNF1-like_BTB_POZ	Domain

Pfam: PF00520, PF02214

UniProt features (18 total): transmembrane region 6, topological domain 4, sequence conflict 4, chain 1, region of interest 1, short sequence motif 1, intramembrane region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9H3M0-F1	80.39	0.47

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

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

MSigDB gene sets: 119 (showing top): BROWNE_HCMV_INFECTION_30MIN_DN, GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_MCMV_INFECTION_DN, GSE45365_NK_CELL_VS_CD8A_DC_MCMV_INFECTION_UP, ATF_B, GOBP_POTASSIUM_ION_TRANSPORT, chr2p25, BENPORATH_ES_WITH_H3K27ME3, REACTOME_VOLTAGE_GATED_POTASSIUM_CHANNELS, REACTOME_POTASSIUM_CHANNELS, GAUSSMANN_MLL_AF4_FUSION_TARGETS_E_UP, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CILIUM_ORGANIZATION, GOBP_ORGANELLE_ASSEMBLY, LASTOWSKA_COAMPLIFIED_WITH_MYCN, ARGGGTTAA_UNKNOWN

GO Biological Process (9): action potential (GO:0001508), potassium ion transport (GO:0006813), regulation of potassium ion transport (GO:0043266), protein homooligomerization (GO:0051260), potassium ion transmembrane transport (GO:0071805), non-motile cilium assembly (GO:1905515), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), transmembrane transport (GO:0055085)

GO Molecular Function (5): voltage-gated potassium channel activity (GO:0005249), potassium channel regulator activity (GO:0015459), monoatomic ion channel activity (GO:0005216), potassium channel activity (GO:0005267), protein binding (GO:0005515)

GO Cellular Component (5): plasma membrane (GO:0005886), voltage-gated potassium channel complex (GO:0008076), membrane (GO:0016020), ciliary base (GO:0097546), monoatomic ion channel complex (GO:0034702)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Potassium Channels	1
Neuronal System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
potassium ion transport	2
transport	2
potassium channel activity	2
cellular anatomical structure	2
regulation of membrane potential	1
metal ion transport	1
regulation of metal ion transport	1
protein complex oligomerization	1
monoatomic cation transmembrane transport	1
cilium assembly	1
monoatomic ion transport	1
transmembrane transport	1
cellular process	1
voltage-gated monoatomic cation channel activity	1
ion channel regulator activity	1
monoatomic ion transmembrane transporter activity	1
channel activity	1
monoatomic cation channel activity	1
potassium ion transmembrane transporter activity	1
binding	1
membrane	1
cell periphery	1
potassium channel complex	1
plasma membrane protein complex	1
cilium	1
ciliary transition zone	1
ciliary transition fiber	1
transmembrane transporter complex	1

Protein interactions and networks

STRING

2031 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
KCNF1	ATP6V1C2	Q8NEY4	800
KCNF1	HNRNPK	P61978	758
KCNF1	FXR2	P51116	688
KCNF1	NOVA2	Q9UNW9	686
KCNF1	CACNG2	Q9Y698	660
KCNF1	FXR1	P51114	630
KCNF1	KCNB1	Q14721	627
KCNF1	FMR1	Q06787	597
KCNF1	HNRNPDL	O14979	586
KCNF1	PCBP2	Q15366	583
KCNF1	NUFIP1	Q9UHK0	575
KCNF1	PCBP1	Q15365	571
KCNF1	NUFIP2	Q7Z417	554
KCNF1	KCNH3	Q9ULD8	544
KCNF1	RRM2	P31350	535

IntAct

29 interactions, top by confidence:

A	B	Type	Score
KCNF1	SERP1	psi-mi:“MI:0915”(physical association)	0.600
SLC39A7	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
TSPO	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
CLPTM1L	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
FARS2	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
ALOX15B	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
TCEA2	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
MCL1	KCNF1	psi-mi:“MI:0915”(physical association)	0.560
KCNF1	OPRM1	psi-mi:“MI:0915”(physical association)	0.490
KCNF1	TRIM13	psi-mi:“MI:0914”(association)	0.350
TCEA2	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
MCL1	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
SLC39A7	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
TSPO	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
CLPTM1L	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
FARS2	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
ALOX15B	KCNF1	psi-mi:“MI:0915”(physical association)	0.000
SERP1	KCNF1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (20): KCNF1 (Two-hybrid), KCNF1 (Two-hybrid), KCNF1 (Two-hybrid), KCNF1 (Two-hybrid), KCNF1 (Two-hybrid), KCNF1 (Two-hybrid), KCNF1 (Two-hybrid), TCEA2 (Two-hybrid), ALOX15B (Two-hybrid), KCNG3 (Two-hybrid), KCNH1 (Two-hybrid), KCNV2 (Two-hybrid), USP20 (Affinity Capture-MS), MTHFR (Affinity Capture-MS), KCNB2 (Affinity Capture-MS)

ESM2 similar proteins: A4K2M4, A4K2N8, A4K2P6, A4K2Q6, A4K2R3, A4K2S2, A4K2T1, A4K2V2, A4K2W6, A4K2X4, A4K2Y2, D4ADX7, O35173, O35174, O88758, P15384, P15388, P16390, P17658, P17659, P19024, P22001, P22460, P22462, P25122, P48547, P50638, P59053, P59994, P79197, Q03719, Q03721, Q14B80, Q17ST2, Q61762, Q61923, Q63734, Q7TSH7, Q8CFS6, Q8R1C0

Diamond homologs: A2BDX4, A4K2M4, A4K2N8, A4K2P6, A4K2Q6, A4K2R3, A4K2S2, A4K2T1, A4K2V2, A4K2W6, A4K2X4, A4K2Y2, A6H8H5, D4AD53, D4ADX7, G5EFC3, O18868, O35173, O35174, O73606, O88758, O88759, P10499, P15384, P15385, P15387, P15388, P16388, P16390, P17970, P17971, P17972, P22001, P22459, P22739, P25122, P48547, P59053, P59994, P59995

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	1
Uncertain significance	47
Likely benign	1
Benign	2

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
148848	GRCh38/hg38 2p25.3-24.1(chr2:1664615-23664142)x3	Pathogenic
982230	NM_002236.5(KCNF1):c.845T>C (p.Leu282Pro)	Likely pathogenic

SpliceAI

69 predictions. Top by Δscore:

Variant	Effect	Δscore
2:10912146:GGG:G	donor_gain	0.9300
2:10912147:GGG:G	donor_gain	0.9300
2:10912147:GG:G	donor_gain	0.8900
2:10912148:GG:G	donor_gain	0.8900
2:10912145:CGGGG:C	donor_loss	0.8800
2:10912148:GGTGA:G	donor_loss	0.8800
2:10912150:T:G	donor_loss	0.8800
2:10912151:G:GT	donor_loss	0.8800
2:10912152:AGTG:A	donor_loss	0.8700
2:10912153:G:C	donor_loss	0.8300
2:10912149:G:GG	donor_gain	0.7900
2:10912154:T:G	donor_loss	0.5900
2:10912106:G:GT	donor_gain	0.5300
2:10912711:CGGGG:C	acceptor_gain	0.5100
2:10912144:CCGGG:C	donor_gain	0.4900
2:10912145:CGGG:C	donor_gain	0.4800
2:10912146:GGGG:G	donor_gain	0.4800
2:10912507:C:CT	acceptor_gain	0.4300
2:10912645:C:CT	acceptor_gain	0.4300
2:10912276:C:A	acceptor_gain	0.4000
2:10912522:G:GT	acceptor_gain	0.3800
2:10912275:G:GA	acceptor_gain	0.3600
2:10912282:G:GA	acceptor_gain	0.3600
2:10912667:AG:A	acceptor_gain	0.3600
2:10912668:GG:G	acceptor_gain	0.3600
2:10912627:C:CA	acceptor_gain	0.3400
2:10912715:G:C	acceptor_gain	0.3300
2:10912524:G:GT	acceptor_gain	0.3000
2:10912667:A:AG	acceptor_gain	0.3000
2:10912668:G:GG	acceptor_gain	0.3000

AlphaMissense

3260 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:10912668:G:T	R81M	1.000
2:10912772:T:A	W116R	1.000
2:10912772:T:C	W116R	1.000
2:10912773:G:C	W116S	1.000
2:10913513:T:A	W363R	1.000
2:10913513:T:C	W363R	1.000
2:10913594:A:C	S390R	1.000
2:10913596:C:A	S390R	1.000
2:10913596:C:G	S390R	1.000
2:10913607:G:A	G394D	1.000
2:10912506:T:A	V27D	0.999
2:10912510:C:A	N28K	0.999
2:10912510:C:G	N28K	0.999
2:10912515:G:A	G30E	0.999
2:10912581:T:C	L52P	0.999
2:10912625:T:C	C67R	0.999
2:10912626:G:A	C67Y	0.999
2:10912627:C:G	C67W	0.999
2:10912662:T:C	F79S	0.999
2:10912668:G:C	R81T	0.999
2:10912669:G:C	R81S	0.999
2:10912669:G:T	R81S	0.999
2:10912739:T:C	C105R	0.999
2:10912740:G:A	C105Y	0.999
2:10912741:C:G	C105W	0.999
2:10912752:T:C	F109S	0.999
2:10912769:T:C	F115L	0.999
2:10912771:C:A	F115L	0.999
2:10912771:C:G	F115L	0.999
2:10912774:G:C	W116C	0.999

dbSNP variants (sampled 300 via entrez): RS1001641558 (2:10913245 G>A,T), RS1001910453 (2:10912028 G>C), RS1001983388 (2:10910410 G>A,T), RS1002245728 (2:10914465 C>A,G), RS1002276717 (2:10914307 G>A), RS1004419809 (2:10910690 A>T), RS1004854929 (2:10910454 G>A), RS1004981669 (2:10910487 G>A), RS1005195431 (2:10914104 G>A,T), RS1007951611 (2:10912357 C>A,T), RS1008129049 (2:10911782 G>C,T), RS1008639084 (2:10911206 G>A,C,T), RS1009100371 (2:10914231 C>T), RS1009200147 (2:10911748 C>T), RS1009544545 (2:10914033 C>T)

Disease associations

OMIM: gene MIM:603787 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): prostate cancer (MONDO:0008315)

Orphanet (2): Familial prostate cancer (Orphanet:1331), Moyamoya angiopathy (Orphanet:477768)

HPO phenotypes

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

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2362996 (PROTEIN FAMILY)

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 (K_v)

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
9.82	Ki	0.15	nM	CHEMBL5722941
9.74	IC50	0.18	nM	CHEMBL5722941

PubChem BioAssay actives

2 with measured affinity, of 34 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.

Compound	Assay	Type	Value	Unit
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 acid	2198828: Binding affinity to KV channel (unknown origin) assessed as inhibition constant	ki	0.0001	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Estradiol	increases expression, affects binding	4
bisphenol A	increases expression	2
pentanal	increases methylation, increases expression	2
Benzo(a)pyrene	affects methylation, increases expression	2
Zearalenone	increases expression	2
Genistein	increases expression	2
propionaldehyde	increases methylation	1
nonanal	increases methylation	1
n-hexanal	increases methylation	1
ethyl-p-hydroxybenzoate	increases expression	1
methylparaben	increases expression	1
butyraldehyde	increases methylation	1
caprylic aldehyde	increases methylation	1
butylparaben	increases expression	1
S-(1,2-dichlorovinyl)cysteine	decreases expression, affects response to substance, increases expression, affects cotreatment	1
heptanal	increases methylation	1
abrine	increases expression	1
(+)-JQ1 compound	decreases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Temozolomide	increases expression	1
Air Pollutants	increases abundance, increases expression	1
Diethylstilbestrol	increases expression	1
Lipopolysaccharides	increases expression, affects cotreatment, decreases expression, affects response to substance	1
Niclosamide	increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Dronabinol	decreases expression	1
Valproic Acid	increases methylation	1
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	affects expression	1
Uranium Compounds	increases expression	1
Acrylamide	decreases expression	1

ChEMBL screening assays

21 unique, capped per target: 20 binding, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1787442	Binding	Inhibition of human recombinant Kv channel at 10 uM by radioligand binding assay	Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement. — Bioorg Med Chem Lett
CHEMBL5522525	Toxicity	Inhibition of human K+ channel by automated electrophysiology	Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure. — J Med Chem

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00029224	PHASE4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	PHASE4	COMPLETED	Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609	PHASE4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	PHASE4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	PHASE4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	PHASE4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	PHASE4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	PHASE4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	PHASE4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	PHASE4	COMPLETED	Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554	PHASE4	COMPLETED	Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098	PHASE4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	PHASE4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	PHASE4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	PHASE4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	PHASE4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	PHASE4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	PHASE4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	PHASE4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	PHASE4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	PHASE4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	PHASE4	COMPLETED	Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027	PHASE4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	PHASE4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	PHASE4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	PHASE4	COMPLETED	Does Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199	PHASE4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	PHASE4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	PHASE4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	PHASE4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	PHASE4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	PHASE4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	PHASE4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563	PHASE4	COMPLETED	Hydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874	PHASE4	COMPLETED	Efficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472	PHASE4	TERMINATED	Firmagon (Degarelix) Intermittent Therapy
NCT01547416	PHASE4	COMPLETED	The Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544	PHASE4	COMPLETED	The Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749	PHASE4	UNKNOWN	Evaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635	PHASE4	COMPLETED	Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer