Details of the Target

General Information of Target

Target ID LDTP04189
Target Name G protein-activated inward rectifier potassium channel 4 (KCNJ5)
Gene Name KCNJ5
Gene ID 3762
Synonyms
GIRK4; G protein-activated inward rectifier potassium channel 4; GIRK-4; Cardiac inward rectifier; CIR; Heart KATP channel; Inward rectifier K(+) channel Kir3.4; IRK-4; KATP-1; Potassium channel, inwardly rectifying subfamily J member 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGDSRNAMNQDMEIGVTPWDPKKIPKQARDYVPIATDRTRLLAEGKKPRQRYMEKSGKC
NVHHGNVQETYRYLSDLFTTLVDLKWRFNLLVFTMVYTVTWLFFGFIWWLIAYIRGDLDH
VGDQEWIPCVENLSGFVSAFLFSIETETTIGYGFRVITEKCPEGIILLLVQAILGSIVNA
FMVGCMFVKISQPKKRAETLMFSNNAVISMRDEKLCLMFRVGDLRNSHIVEASIRAKLIK
SRQTKEGEFIPLNQTDINVGFDTGDDRLFLVSPLIISHEINQKSPFWEMSQAQLHQEEFE
VVVILEGMVEATGMTCQARSSYMDTEVLWGHRFTPVLTLEKGFYEVDYNTFHDTYETNTP
SCCAKELAEMKREGRLLQYLPSPPLLGGCAEAGLDAEAEQNEEDEPKGLGGSREARGSV
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Inward rectifier-type potassium channel (TC 1.A.2.1) family, KCNJ5 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.
TTD ID
T78692
Uniprot ID
P48544
DrugMap ID
TTEO25X
Ensemble ID
ENST00000338350.4
HGNC ID
HGNC:6266
ChEMBL ID
CHEMBL1914278

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C60(1.61)  LDD2377  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 HuP-T3 C60(1.61)  LDD2377  [1]
 LDCM0023  KB03 DAN-G C60(1.42)  LDD2730  [1]
 LDCM0024  KB05 DAN-G C60(1.26)  LDD3147  [1]

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