Details of the Target

General Information of Target

Target ID LDTP06491
Target Name ATP-sensitive inward rectifier potassium channel 8 (KCNJ8)
Gene Name KCNJ8
Gene ID 3764
Synonyms
ATP-sensitive inward rectifier potassium channel 8; Inward rectifier K(+) channel Kir6.1; Potassium channel, inwardly rectifying subfamily J member 8; uKATP-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLARKSIIPEEYVLARIAAENLRKPRIRDRLPKARFIAKSGACNLAHKNIREQGRFLQDI
FTTLVDLKWRHTLVIFTMSFLCSWLLFAIMWWLVAFAHGDIYAYMEKSGMEKSGLESTVC
VTNVRSFTSAFLFSIEVQVTIGFGGRMMTEECPLAITVLILQNIVGLIINAVMLGCIFMK
TAQAHRRAETLIFSRHAVIAVRNGKLCFMFRVGDLRKSMIISASVRIQVVKKTTTPEGEV
VPIHQLDIPVDNPIESNNIFLVAPLIICHVIDKRSPLYDISATDLANQDLEVIVILEGVV
ETTGITTQARTSYIAEEIQWGHRFVSIVTEEEGVYSVDYSKFGNTVKVAAPRCSARELDE
KPSILIQTLQKSELSHQNSLRKRNSMRRNNSMRRNNSIRRNNSSLMVPKVQFMTPEGNQN
TSES
Target Bioclass
Transporter and channel
Family
Inward rectifier-type potassium channel (TC 1.A.2.1) family, KCNJ8 subfamily
Subcellular location
Membrane
Function
This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. Can be blocked by external barium.
Uniprot ID
Q15842
Ensemble ID
ENST00000240662.3
HGNC ID
HGNC:6269
ChEMBL ID
CHEMBL4770

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C43(2.44)  LDD3443  [1]
IPM
 Probe Info  		N.A.  LDD2156  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C43(1.12)  LDD1508  [3]
 LDCM0226  AC11 HEK-293T C43(1.14)  LDD1509  [3]
 LDCM0277  AC18 HEK-293T C43(0.92)  LDD1516  [3]
 LDCM0278  AC19 HEK-293T C43(1.06)  LDD1517  [3]
 LDCM0279  AC2 HEK-293T C43(0.92)  LDD1518  [3]
 LDCM0284  AC24 HEK-293T C43(1.00)  LDD1523  [3]
 LDCM0286  AC26 HEK-293T C43(1.02)  LDD1525  [3]
 LDCM0287  AC27 HEK-293T C43(1.09)  LDD1526  [3]
 LDCM0290  AC3 HEK-293T C43(1.02)  LDD1529  [3]
 LDCM0293  AC32 HEK-293T C43(1.06)  LDD1532  [3]
 LDCM0295  AC34 HEK-293T C43(1.06)  LDD1534  [3]
 LDCM0296  AC35 HEK-293T C43(1.17)  LDD1535  [3]
 LDCM0302  AC40 HEK-293T C43(0.95)  LDD1541  [3]
 LDCM0304  AC42 HEK-293T C43(1.12)  LDD1543  [3]
 LDCM0305  AC43 HEK-293T C43(1.00)  LDD1544  [3]
 LDCM0310  AC48 HEK-293T C43(1.09)  LDD1549  [3]
 LDCM0313  AC50 HEK-293T C43(0.97)  LDD1552  [3]
 LDCM0314  AC51 HEK-293T C43(1.05)  LDD1553  [3]
 LDCM0319  AC56 HEK-293T C43(1.07)  LDD1558  [3]
 LDCM0321  AC58 HEK-293T C43(1.01)  LDD1560  [3]
 LDCM0322  AC59 HEK-293T C43(1.09)  LDD1561  [3]
 LDCM0328  AC64 HEK-293T C43(0.97)  LDD1567  [3]
 LDCM0345  AC8 HEK-293T C43(1.10)  LDD1569  [3]
 LDCM0275  AKOS034007705 HEK-293T C43(1.00)  LDD1514  [3]
 LDCM0390  CL12 HEK-293T C43(0.97)  LDD1594  [3]
 LDCM0405  CL18 HEK-293T C43(1.11)  LDD1609  [3]
 LDCM0406  CL19 HEK-293T C43(1.17)  LDD1610  [3]
 LDCM0412  CL24 HEK-293T C43(0.95)  LDD1616  [3]
 LDCM0419  CL30 HEK-293T C43(1.02)  LDD1623  [3]
 LDCM0420  CL31 HEK-293T C43(1.16)  LDD1624  [3]
 LDCM0425  CL36 HEK-293T C43(1.08)  LDD1629  [3]
 LDCM0432  CL42 HEK-293T C43(0.93)  LDD1636  [3]
 LDCM0433  CL43 HEK-293T C43(1.06)  LDD1637  [3]
 LDCM0438  CL48 HEK-293T C43(1.04)  LDD1642  [3]
 LDCM0445  CL54 HEK-293T C43(1.42)  LDD1648  [3]
 LDCM0446  CL55 HEK-293T C43(1.00)  LDD1649  [3]
 LDCM0451  CL6 HEK-293T C43(1.02)  LDD1654  [3]
 LDCM0452  CL60 HEK-293T C43(1.02)  LDD1655  [3]
 LDCM0458  CL66 HEK-293T C43(1.13)  LDD1661  [3]
 LDCM0459  CL67 HEK-293T C43(0.98)  LDD1662  [3]
 LDCM0462  CL7 HEK-293T C43(1.04)  LDD1665  [3]
 LDCM0465  CL72 HEK-293T C43(1.06)  LDD1668  [3]
 LDCM0471  CL78 HEK-293T C43(0.98)  LDD1674  [3]
 LDCM0472  CL79 HEK-293T C43(1.05)  LDD1675  [3]
 LDCM0478  CL84 HEK-293T C43(1.22)  LDD1681  [3]
 LDCM0485  CL90 HEK-293T C43(1.22)  LDD1688  [3]
 LDCM0486  CL91 HEK-293T C43(1.03)  LDD1689  [3]
 LDCM0491  CL96 HEK-293T C43(1.14)  LDD1694  [3]
 LDCM0022  KB02 HuH-1 C43(2.50)  LDD2374  [1]
 LDCM0023  KB03 HuH-1 C43(2.68)  LDD2791  [1]
 LDCM0024  KB05 SNU-449 C43(2.44)  LDD3443  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transmembrane protein 54 (TMEM54) TMEM54 family Q969K7
Emerin (EMD) . P50402
Transmembrane protein 140 (TMEM140) . Q9NV12

The Drug(s) Related To This Target

Approved
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gliquidone Small molecular drug DB01251
Glyburide Small molecular drug DB01016
Levosimendan Small molecular drug DB00922
Phenformin Small molecular drug DB00914
Ritodrine Small molecular drug DB00867
Thiamylal Small molecular drug DB01154
Yohimbine Small molecular drug DB01392
Butamben . DB11148
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Glisoxepide Small molecular drug DB01289

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 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
3 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402