Details of the Target

General Information of Target

Target ID LDTP10901
Target Name P2X purinoceptor 7 (P2RX7)
Gene Name P2RX7
Gene ID 5027
Synonyms
P2X purinoceptor 7; P2X7; ATP receptor; P2Z receptor; Purinergic receptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGCCAALAAFLFEYDTPRIVLIRSRKVGLMNRAVQLLILAYVIGWVFVWEKGYQETDSV
VSSVTTKVKGVAVTNTSKLGFRIWDVADYVIPAQEENSLFVMTNVILTMNQTQGLCPEIP
DATTVCKSDASCTAGSAGTHSNGVSTGRCVAFNGSVKTCEVAAWCPVEDDTHVPQPAFLK
AAENFTLLVKNNIWYPKFNFSKRNILPNITTTYLKSCIYDAKTDPFCPIFRLGKIVENAG
HSFQDMAVEGGIMGIQVNWDCNLDRAASLCLPRYSFRRLDTRDVEHNVSPGYNFRFAKYY
RDLAGNEQRTLIKAYGIRFDIIVFGKAGKFDIIPTMINIGSGLALLGMATVLCDIIVLYC
MKKRLYYREKKYKYVEDYEQGLASELDQ
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
P2X receptor family
Subcellular location
Cell membrane
Function
Receptor for ATP that acts as a ligand-gated ion channel. Responsible for ATP-dependent lysis of macrophages through the formation of membrane pores permeable to large molecules. Could function in both fast synaptic transmission and the ATP-mediated lysis of antigen-presenting cells. In the absence of its natural ligand, ATP, functions as a scavenger receptor in the recognition and engulfment of apoptotic cells.
TTD ID
T63414
Uniprot ID
Q99572
DrugMap ID
TT473XN
Ensemble ID
ENST00000328963.10
HGNC ID
HGNC:8537
ChEMBL ID
CHEMBL4805

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A3KAW SNV: p.L278F .
COLO792 SNV: p.S101P; p.S130F .
HT115 SNV: p.A296V .
KNS42 SNV: p.I315T .
KYSE30 SNV: p.C135F .
SKHEP1 Deletion: p.R544HfsTer11 .
TOV21G Deletion: p.V475SfsTer131 .

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
IA-alkyne
 Probe Info  		C506(8.70)  LDD2157  [1]
DBIA
 Probe Info  		C29(2.57); C82(2.83)  LDD3413  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 G-361 C82(2.29)  LDD2329  [2]
 LDCM0023  KB03 G-361 C82(5.45)  LDD2746  [2]
 LDCM0024  KB05 RVH-421 C29(2.57); C82(2.83)  LDD3413  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein RFP (TRIM27) TRIM/RBCC family P14373
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 655 (ZNF655) Krueppel C2H2-type zinc-finger protein family Q8N720
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
EGF-containing fibulin-like extracellular matrix protein 2 (EFEMP2) Fibulin family O95967
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Keratin, type I cuticular Ha4 (KRT34) Intermediate filament family O76011
Keratin-associated protein 10-8 (KRTAP10-8) KRTAP type 10 family P60410
Notch homolog 2 N-terminal-like protein C (NOTCH2NLC) NOTCH family P0DPK4
Heat shock factor 2-binding protein (HSF2BP) . O75031
Pleckstrin homology domain-containing family F member 2 (PLEKHF2) . Q9H8W4

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Promethazine Small molecular drug DB01069
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ce-224535 Small molecular drug D0F4JK
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd9056 Small molecular drug D0CS2C
Bil010t . D02AIZ
Phase 1
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Evt 401 . D01TLV
Gsk1482160 . D0I7BU
Jnj-54175446 . D0VI4N
Jnj-55308942 . D0OQ1A
Sgm-1019 . D02XAS
Clinical trial
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jnj-479655 Small molecular drug D07QTG
Investigative
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
A-740003 Small molecular drug D0U5ML
A438079 Small molecular drug D05QLT
A804598 Small molecular drug D0Q1PO
A839977 Small molecular drug D0M0XC
Az11645373 Small molecular drug D02EFX
Az11657312 (Salt Free) Small molecular drug D00REB
Chelerythrine Small molecular drug D0T9ZL
Decavanadate Small molecular drug D06KHR
Isoppads Small molecular drug D05BFC
Kn-62 Small molecular drug D0N6ES
Afc-5128 . D0N1ST
Az-11657312 . D03HJZ
Stylissadine A . D05DLI
Stylissadine B . D02TNK
Patented
Click To Hide/Show 34 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aminobenzoxazole Analog 1 Small molecular drug D0GQ6D
Benzamide Derivative 12 Small molecular drug D0N2TV
Benzamide Derivative 13 Small molecular drug D04QLC
Bicyclic Heteroaryl Amide Derivative 1 Small molecular drug D0PI1X
Bicyclic Heteroaryl Amide Derivative 2 Small molecular drug D08OKB
Bicyclic Heteroaryl Amide Derivative 3 Small molecular drug D0OG3Z
Chlorobenzamide Derivative 1 Small molecular drug D0RG4J
Chlorobenzamide Derivative 2 Small molecular drug D0FR8L
Dihydroisoquinoline Carboxamide Analog 1 Small molecular drug D0O8DL
Fluorophenyl-substituted Heterocyclic Amide Analog 1 Small molecular drug D07VLC
Fused Triazoloamino-phenyl Analog 1 Small molecular drug D0AI1I
Heterocyclic-fused Piperazine Derivative 1 Small molecular drug D0R4IT
Imidazolidine Derivative 1 Small molecular drug D0WI9M
Indole Carboxamide Derivative 1 Small molecular drug D0ZY5M
Isoindole 1,3-dione Analog 1 Small molecular drug D0EY5F
Isothiazolidine Derivative 1 Small molecular drug D04SHK
Piperazine Derivative 6 Small molecular drug D0QC5O
Piperidinone Derivative 1 Small molecular drug D0NG6O
Pmid27724045-compound-14 Small molecular drug D09REZ
Pmid27724045-compound-15 Small molecular drug D08SFW
Pmid27724045-compound-17 Small molecular drug D07EBW
Pmid27724045-compound-19 Small molecular drug D06MSZ
Pmid27724045-compound-29 Small molecular drug D0S9HE
Pmid27724045-compound-33 Small molecular drug D08PQU
Pyridazinone Derivative 1 Small molecular drug D0L8QD
Quinoline Derivative 10 Small molecular drug D05KRX
Quinoline Derivative 11 Small molecular drug D0L2KM
Quinoline Derivative 12 Small molecular drug D01EBW
Quinoline Derivative 13 Small molecular drug D0B7KM
Tetrazole Derivative 1 Small molecular drug D0UC8I
Thiazole Derivative 5 Small molecular drug D0T1JN
Thiazole-fused Cycloalkyl Carboxamide Derivative 1 Small molecular drug D0C9WD
Triazole Derivative 2 Small molecular drug D00PVH
Triazolo-pyrazinone Derivative 1 Small molecular drug D0N4RJ

References

1 From chemoproteomic-detected amino acids to genomic coordinates: insights into precise multi-omic data integration. Mol Syst Biol. 2021 Feb;17(2):e9840. doi: 10.15252/msb.20209840.
Mass spectrometry data entry: PXD022151
2 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