General Information of Target

Target ID LDTP12484
Target Name Potassium voltage-gated channel subfamily KQT member 5 (KCNQ5)
Gene Name KCNQ5
Gene ID 56479
Synonyms
Potassium voltage-gated channel subfamily KQT member 5; KQT-like 5; Potassium channel subunit alpha KvLQT5; Voltage-gated potassium channel subunit Kv7.5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVAKDYPFYLTVKRANCSLELPPASGPAKDAEEPSNKRVKPLSRVTSLANLIPPVKATPL
KRFSQTLQRSISFRSESRPDILAPRPWSRNAAPSSTKRRDSKLWSETFDVCVNQMLTSKE
IKRQEAIFELSQGEEDLIEDLKLAKKAYHDPMLKLSIMTEQELNQIFGTLDSLIPLHEEL
LSQLRDVRKPDGSTEHVGPILVGWLPCLSSYDSYCSNQVAAKALLDHKKQDHRVQDFLQR
CLESPFSRKLDLWNFLDIPRSRLVKYPLLLREILRHTPNDNPDQQHLEEAINIIQGIVAE
INTKTGESECRYYKERLLYLEEGQKDSLIDSSRVLCCHGELKNNRGVKLHVFLFQEVLVI
TRAVTHNEQLCYQLYRQPIPVKDLLLEDLQDGEVRLGGSLRGAFSNNERIKNFFRVSFKN
GSQSQTHSLQANDTFNKQQWLNCIRQAKETVLCAAGQAGVLDSEGSFLNPTTGSRELQGE
TKLEQMDQSDSESDCSMDTSEVSLDCERMEQTDSSCGNSRHGESNV
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Potassium channel family, KQT (TC 1.A.1.15) subfamily, Kv7.5/KCNQ5 sub-subfamily
Subcellular location
Cell membrane
Function
Associates with KCNQ3 to form a potassium channel which contributes to M-type current, a slowly activating and deactivating potassium conductance which plays a critical role in determining the subthreshold electrical excitability of neurons. Therefore, it is important in the regulation of neuronal excitability. May contribute, with other potassium channels, to the molecular diversity of a heterogeneous population of M-channels, varying in kinetic and pharmacological properties, which underlie this physiologically important current. Insensitive to tetraethylammonium, but inhibited by barium, linopirdine and XE991. Activated by niflumic acid and the anticonvulsant retigabine. As the native M-channel, the potassium channel composed of KCNQ3 and KCNQ5 is also suppressed by activation of the muscarinic acetylcholine receptor CHRM1.
TTD ID
T55068
Uniprot ID
Q9NR82
DrugMap ID
TTWVL5Q
Ensemble ID
ENST00000342056.6
HGNC ID
HGNC:6299
ChEMBL ID
CHEMBL2925

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
C32 SNV: p.T97P .
COLO320 SNV: p.L47M
Substitution: p.Q112G
.
DETROIT562 SNV: p.T392A .
DU145 SNV: p.R244H .
HCT15 SNV: p.R244C .
HT115 SNV: p.A182V; p.R426C .
HT1197 SNV: p.H4N
Substitution: p.A14C
.
IM95 SNV: p.R244C .
IPC298 SNV: p.E385D .
MCC13 SNV: p.R187Q; p.G273E; p.K408I .
MCC26 SNV: p.A899V .
MELJUSO SNV: p.K107Q DBIA    Probe Info 
NCIH196 SNV: p.A332E .
NUGC3 SNV: p.S416I .
PF382 SNV: p.A725V .
SISO SNV: p.C507Y .
SKMEL28 SNV: p.S724L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C641(2.52); C934(2.11)  LDD3332  [1]
AHL-Pu-1
 Probe Info 
C915(2.96)  LDD0170  [2]
IPM
 Probe Info 
C915(2.31)  LDD1701  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C915(2.96)  LDD0170  [2]
 LDCM0026  4SU-RNA+native RNA DM93 C819(2.17); C622(2.66)  LDD0171  [2]
 LDCM0022  KB02 A101D C934(1.95)  LDD2250  [1]
 LDCM0023  KB03 MDA-MB-231 C915(2.31)  LDD1701  [3]
 LDCM0024  KB05 MKN45 C641(2.52); C934(2.11)  LDD3332  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Enflurane Small molecular drug DB00228
Ezogabine Small molecular drug DB04953
Gabapentin Small molecular drug DB00996
Miconazole Small molecular drug DB01110
Promethazine Small molecular drug DB01069
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(S)-n-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide Small molecular drug D02BGR
Xe991 Small molecular drug D0P8PH
Zinc Pyrithione Small molecular drug D07FTI
[14c]Tea Small molecular drug D06PZZ
Ica-105665 . DB06089

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761