KCNG3

Summary

KCNG3 (potassium voltage-gated channel modifier subfamily G member 3, HGNC:18306) is a protein-coding gene on chromosome 2p21, encoding Voltage-gated potassium channel regulatory subunit KCNG3 (Q8TAE7). Regulatory subunit of the voltage-gated potassium (Kv) channel which, when coassembled with KCNB1, modulates the kinetics parameters of the heterotetrameric channel namely the inactivation and deactivation rate.

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 G. This member is a gamma subunit functioning as a modulatory molecule. Alternative splicing results in two transcript variants encoding distinct isoforms.

Source: NCBI Gene 170850 — RefSeq curated summary.

At a glance

• GWAS associations: 11
• Clinical variants (ClinVar): 51 total
• Druggable target: yes
• MANE Select transcript: NM_133329

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:18306
Approved symbol	KCNG3
Name	potassium voltage-gated channel modifier subfamily G member 3
Location	2p21
Locus type	gene with protein product
Status	Approved
Aliases	Kv6.3
Ensembl gene	ENSG00000171126
Ensembl biotype	protein_coding
OMIM	606767
Entrez	170850

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000306078, ENST00000394973

RefSeq mRNA: 2 — MANE Select: NM_133329 NM_133329, NM_172344

CCDS: CCDS1809, CCDS42674

Canonical transcript exons

ENST00000306078 — 2 exons

Exon	Start	End
ENSE00001168755	42492837	42493982
ENSE00001216024	42442017	42444579

Expression profiles

Bgee: expression breadth broad, 80 present calls, max score 72.60.

FANTOM5 (CAGE): breadth broad, TPM avg 1.0838 / max 62.8118, expressed in 306 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
28016	1.0838	306

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
islet of Langerhans	UBERON:0000006	72.60	gold quality
adrenal tissue	UBERON:0018303	65.22	gold quality
endothelial cell	CL:0000115	62.52	silver quality
prefrontal cortex	UBERON:0000451	61.13	gold quality
right adrenal gland	UBERON:0001233	60.80	gold quality
left adrenal gland	UBERON:0001234	60.19	gold quality
right adrenal gland cortex	UBERON:0035827	60.08	gold quality
middle temporal gyrus	UBERON:0002771	59.98	silver quality
endometrium	UBERON:0001295	59.77	gold quality
adrenal gland	UBERON:0002369	59.52	gold quality
left adrenal gland cortex	UBERON:0035825	58.99	gold quality
Brodmann (1909) area 23	UBERON:0013554	58.42	silver quality
adrenal cortex	UBERON:0001235	57.89	gold quality
entorhinal cortex	UBERON:0002728	57.88	silver quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	56.70	silver quality
superior frontal gyrus	UBERON:0002661	56.59	gold quality
Brodmann (1909) area 9	UBERON:0013540	56.06	gold quality
frontal cortex	UBERON:0001870	55.74	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	55.59	gold quality
mucosa of transverse colon	UBERON:0004991	55.47	gold quality
nucleus accumbens	UBERON:0001882	54.71	gold quality
neocortex	UBERON:0001950	54.13	gold quality
cerebral cortex	UBERON:0000956	54.06	gold quality
dorsal root ganglion	UBERON:0000044	53.66	gold quality
caudate nucleus	UBERON:0001873	53.31	gold quality
putamen	UBERON:0001874	52.73	gold quality
Ammon’s horn	UBERON:0001954	51.97	gold quality
anterior cingulate cortex	UBERON:0009835	51.96	gold quality
forebrain	UBERON:0001890	51.73	gold quality
temporal lobe	UBERON:0001871	51.32	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.61

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

141 targeting KCNG3, 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-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-3162-3P	100.00	65.37	363
HSA-MIR-3689D	100.00	66.14	1181
HSA-MIR-6851-5P	100.00	65.63	1294
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-6740-5P	100.00	65.64	932
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-6870-5P	99.99	68.55	2115
HSA-MIR-511-3P	99.99	68.85	1467
HSA-LET-7F-2-3P	99.98	70.98	2588
HSA-MIR-1185-1-3P	99.98	71.04	2593
HSA-MIR-1185-2-3P	99.98	71.04	2593
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-4723-5P	99.97	68.70	2034

Literature-anchored findings (GeneRIF, showing 5)

• These results indicate that Kv6.3 is a novel member of the voltage-gated K(+) channel which functions as a modulatory subunit of the Kv2.1 channel. (PMID:11852086)
• Obligatory heterotetramerization of three previously uncharacterized Kv channel subunits identified in human genome (Kv6.3)(Kv10.1) (Kv11.1) (PMID:12060745)
• [review] an overview of the current status of data linking K(V)10.1 to cancer, and techniques that could exploit K(V)10.1’s properties for the management of cancer (PMID:22204340)
• the correlation between dismal prognosis and Kv10.1 expression to patients with brain metastases or glioblastoma multiforme and, moreover, they strongly suggest a role of tricyclic antidepressants for personalized therapy of brain malignancies. (PMID:26530050)
• Original association of ion transporters mediates the ECM-induced breast cancer cell survival: Kv10.1-Orai1-SPCA2 partnership. (PMID:30718673)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	kcng3	ENSDARG00000061622
mus_musculus	Kcng3	ENSMUSG00000045053
rattus_norvegicus	Kcng3	ENSRNOG00000004535

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), KCNF1 (ENSG00000162975), KCNV1 (ENSG00000164794), KCNC2 (ENSG00000166006), KCNV2 (ENSG00000168263), KCNG4 (ENSG00000168418), KCNS3 (ENSG00000170745), 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 KCNG3 — Q8TAE7 (reviewed: Q8TAE7)

Alternative names: Potassium voltage-gated channel subfamily G member 3, Voltage-gated potassium channel subunit Kv10.1, Voltage-gated potassium channel subunit Kv6.3

All UniProt accessions (1): Q8TAE7

UniProt curated annotations — full annotation on UniProt →

Function. Regulatory subunit of the voltage-gated potassium (Kv) channel which, when coassembled with KCNB1, modulates the kinetics parameters of the heterotetrameric channel namely the inactivation and deactivation rate. Potassium channel subunit that does not form functional channels by itself. Reduces the deactivation rate. Moderately accelerates activation.

Subunit / interactions. Heterotetramer with KCNB1. Does not form homomultimers.

Subcellular location. Cell membrane. Cytoplasm.

Tissue specificity. Expressed in the brain, liver, testis, small intestine, colon, thymus and adrenal gland.

Domain organisation. The transmembrane segment S4 functions as a voltage-sensor and is characterized by a series of positively charged amino acids at every third position. Channel opening and closing is effected by a conformation change that affects the position and orientation of the voltage-sensor paddle formed by S3 and S4 within the membrane. A transmembrane electric field that is positive inside would push the positively charged S4 segment outwards, thereby opening the pore, while a field that is negative inside would pull the S4 segment inwards and close the pore. Changes in the position and orientation of S4 are then transmitted to the activation gate formed by the inner helix bundle via the S4-S5 linker region.

Similarity. Belongs to the potassium channel family. G (TC 1.A.1.2) subfamily. Kv6.3/KCNG3 sub-subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
Q8TAE7-1	1, Kv10.1b	yes
Q8TAE7-2	2, Kv10.1a

RefSeq proteins (2): NP_579875, NP_758847 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000210	BTB/POZ_dom	Domain
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

Pfam: PF00520, PF02214

UniProt features (19 total): topological domain 8, transmembrane region 6, intramembrane region 2, chain 1, short sequence motif 1, splice variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8TAE7-F1	80.07	0.32

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: 102 (showing top): GOBP_POTASSIUM_ION_TRANSPORT, REACTOME_VOLTAGE_GATED_POTASSIUM_CHANNELS, REACTOME_POTASSIUM_CHANNELS, GOBP_MONOATOMIC_CATION_TRANSPORT, HFH4_01, AACTTT_UNKNOWN, TGGNNNNNNKCCAR_UNKNOWN, GOBP_PROTEIN_HOMOOLIGOMERIZATION, GOBP_REGULATION_OF_TRANSPORT, GOBP_REGULATION_OF_MONOATOMIC_ION_TRANSPORT, GOBP_TRANSMEMBRANE_TRANSPORT, GOBP_REGULATION_OF_POTASSIUM_ION_TRANSPORT, GOBP_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOCC_POTASSIUM_CHANNEL_COMPLEX, GOBP_REGULATION_OF_MEMBRANE_POTENTIAL

GO Biological Process (9): action potential (GO:0001508), regulation of potassium ion transport (GO:0043266), protein homooligomerization (GO:0051260), potassium ion transmembrane transport (GO:0071805), regulation of potassium ion transmembrane transport (GO:1901379), monoatomic ion transport (GO:0006811), potassium ion transport (GO:0006813), 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 (6): endoplasmic reticulum (GO:0005783), plasma membrane (GO:0005886), voltage-gated potassium channel complex (GO:0008076), membrane (GO:0016020), cytoplasm (GO:0005737), 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
regulation of metal ion transport	1
protein complex oligomerization	1
monoatomic cation transmembrane transport	1
regulation of potassium ion transport	1
potassium ion transmembrane transport	1
regulation of monoatomic cation transmembrane transport	1
metal ion transport	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
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1
membrane	1
cell periphery	1
potassium channel complex	1
plasma membrane protein complex	1
intracellular anatomical structure	1
transmembrane transporter complex	1

Protein interactions and networks

STRING

1432 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
KCNG3	PRR35	P0CG20	582
KCNG3	PKDCC	Q504Y2	561
KCNG3	KBTBD12	Q3ZCT8	529
KCNG3	CACNA1S	Q13698	508
KCNG3	RRP36	Q96EU6	499
KCNG3	KLHDC8B	Q8IXV7	477
KCNG3	SPMIP7	A4D263	475
KCNG3	TOGARAM1	Q9Y4F4	474
KCNG3	KCNK12	Q9HB15	472
KCNG3	TRAPPC6B	Q86SZ2	467
KCNG3	IHO1	Q8IYA8	459
KCNG3	KCNN1	Q92952	459
KCNG3	SIPA1L2	Q9P2F8	450
KCNG3	VWC2	Q2TAL6	448
KCNG3	LRRTM1	Q86UE6	447

IntAct

4 interactions, top by confidence:

A	B	Type	Score
MYC		psi-mi:“MI:0914”(association)	0.350
ATG16L1	ESYT2	psi-mi:“MI:0914”(association)	0.350
SLC27A6	NBAS	psi-mi:“MI:0914”(association)	0.350

BioGRID (16): KCNG3 (Affinity Capture-RNA), KCNG3 (Affinity Capture-RNA), KCNG3 (Two-hybrid), KCNG3 (Two-hybrid), KCNG3 (Two-hybrid), KCNG3 (Affinity Capture-Western), KCNG3 (Affinity Capture-RNA), KCNV1 (Negative Genetic), KCNG3 (Affinity Capture-MS), KCNG3 (Affinity Capture-RNA), KCNB1 (Affinity Capture-Western), KCNG3 (Two-hybrid), KCNG3 (Two-hybrid), KCNG3 (FRET), KCNB2 (Two-hybrid)

ESM2 similar proteins: A2BDX4, A4K2T1, A4K2Y2, D4AD53, O15554, O73606, O88454, O89109, P15388, P17971, P17972, P35739, P48547, P59053, P59994, P59995, P97557, Q03719, Q0P583, Q17ST2, Q52PG9, Q5RC10, Q60565, Q63881, Q6IVV8, Q6PIU1, Q7TN37, Q80XM3, Q8BZN2, Q8CFS6, Q8HYZ1, Q8IV77, Q8R1P5, Q8R523, Q8TAE7, Q8TD43, Q8TDN1, Q8TDN2, Q96RP8, Q9ERS0

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

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	49
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

513 predictions. Top by Δscore:

Variant	Effect	Δscore
2:42444575:TTATC:T	acceptor_gain	1.0000
2:42444576:TATC:T	acceptor_gain	1.0000
2:42444577:ATC:A	acceptor_gain	1.0000
2:42444578:TC:T	acceptor_gain	1.0000
2:42444578:TCCTG:T	acceptor_loss	1.0000
2:42444579:CC:C	acceptor_gain	1.0000
2:42444580:C:CC	acceptor_gain	1.0000
2:42444580:C:G	acceptor_loss	1.0000
2:42444584:C:CT	acceptor_gain	1.0000
2:42444585:A:T	acceptor_gain	1.0000
2:42444592:C:CT	acceptor_gain	0.9900
2:42491747:C:CA	donor_gain	0.9900
2:42444593:A:T	acceptor_gain	0.9800
2:42444580:C:T	acceptor_gain	0.9700
2:42492868:ACC:A	donor_loss	0.9700
2:42492869:CCTGC:C	donor_loss	0.9700
2:42491744:ACTC:A	donor_gain	0.9400
2:42491745:CTCC:C	donor_gain	0.9400
2:42485970:A:AC	donor_gain	0.9200
2:42485971:C:CC	donor_gain	0.9200
2:42444576:TATCC:T	acceptor_gain	0.9100
2:42491746:TCCC:T	donor_gain	0.8800
2:42492869:CCTG:C	donor_gain	0.8800
2:42492872:G:A	donor_gain	0.8800
2:42485966:G:A	donor_gain	0.8700
2:42485972:T:C	donor_gain	0.8600
2:42444577:ATCC:A	acceptor_gain	0.8500
2:42444577:ATCCT:A	acceptor_gain	0.8500
2:42444578:TCCT:T	acceptor_gain	0.8500
2:42487680:CAAT:C	donor_gain	0.8500

AlphaMissense

2847 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:42444009:A:C	F412L	1.000
2:42444009:A:T	F412L	1.000
2:42444011:A:G	F412L	1.000
2:42444149:A:G	W366R	1.000
2:42444149:A:T	W366R	1.000
2:42444498:A:C	F249L	1.000
2:42444498:A:T	F249L	1.000
2:42444500:A:G	F249L	1.000
2:42444529:C:A	R239M	1.000
2:42444549:G:C	F232L	1.000
2:42444549:G:T	F232L	1.000
2:42444551:A:G	F232L	1.000
2:42493199:C:A	W101C	1.000
2:42493199:C:G	W101C	1.000
2:42493201:A:G	W101R	1.000
2:42493201:A:T	W101R	1.000
2:42493314:A:G	F63S	1.000
2:42493316:G:C	F62L	1.000
2:42493316:G:T	F62L	1.000
2:42493318:A:G	F62L	1.000
2:42493350:C:T	C51Y	1.000
2:42444010:A:C	F412C	0.999
2:42444034:G:C	P404R	0.999
2:42444034:G:T	P404H	0.999
2:42444055:C:T	G397E	0.999
2:42444056:C:G	G397R	0.999
2:42444056:C:T	G397R	0.999
2:42444057:A:C	S396R	0.999
2:42444057:A:T	S396R	0.999
2:42444059:T:G	S396R	0.999

dbSNP variants (sampled 300 via entrez): RS1000053224 (2:42406841 AAAAG>A), RS1000078288 (2:42463776 A>G), RS1000085021 (2:42437780 A>G), RS1000115702 (2:42451472 C>A), RS1000148023 (2:42422131 T>A,C), RS1000149556 (2:42459691 T>C), RS1000207782 (2:42416653 T>C), RS1000222898 (2:42459120 C>A,T), RS1000248141 (2:42491897 G>A), RS1000254782 (2:42411499 G>C,T), RS1000268914 (2:42486976 G>C), RS1000278849 (2:42487119 T>G), RS1000320907 (2:42416950 T>C,G), RS1000321284 (2:42416900 T>C), RS1000335608 (2:42448653 T>C)

Disease associations

OMIM: gene MIM:606767 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

11 associations (top):

Study	Trait	p-value
GCST002783_308	Body mass index	4.000000e-07
GCST002783_613	Body mass index	8.000000e-07
GCST003390_8	Thrombosis	2.000000e-07
GCST006190_7	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	8.000000e-11
GCST006190_76	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	3.000000e-13
GCST006192_62	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	5.000000e-11
GCST006192_78	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	1.000000e-08
GCST006193_40	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	1.000000e-11
GCST006193_78	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	1.000000e-14
GCST006195_30	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	5.000000e-09
GCST006195_40	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	9.000000e-12

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index
EFO:0003907	deep vein thrombosis
EFO:0006336	diastolic blood pressure
EFO:0006527	smoking status measurement
EFO:0006335	systolic blood pressure

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
Valproic Acid	increases expression, affects cotreatment, decreases expression, affects expression	6
trichostatin A	decreases expression, affects cotreatment	3
Benzo(a)pyrene	decreases methylation, decreases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
propionaldehyde	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
terbufos	increases methylation	1
sodium arsenite	increases expression	1
butyraldehyde	increases expression	1
nickel sulfate	increases expression	1
S-(1,2-dichlorovinyl)cysteine	decreases reaction, increases expression	1
pentanal	increases expression	1
CGP 52608	affects binding, increases reaction	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
NSC 689534	affects binding, decreases expression	1
(+)-JQ1 compound	decreases expression	1
PCI 5002	affects cotreatment, increases expression	1
bisphenol AF	increases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Leflunomide	increases expression	1
Aldehydes	increases expression	1
Carbamazepine	affects expression	1
Copper	affects binding, decreases expression	1
Diethylhexyl Phthalate	decreases expression	1
Fonofos	increases methylation	1
Lipopolysaccharides	decreases reaction, increases expression	1
Parathion	increases methylation	1
Silicon Dioxide	increases expression	1
Tobacco Smoke Pollution	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)

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