General Information of Target

Target ID LDTP03313
Target Name Atypical chemokine receptor 3 (ACKR3)
Gene Name ACKR3
Gene ID 57007
Synonyms
CMKOR1; CXCR7; GPR159; RDC1; Atypical chemokine receptor 3; C-X-C chemokine receptor type 7; CXC-R7; CXCR-7; Chemokine orphan receptor 1; G-protein coupled receptor 159; G-protein coupled receptor RDC1 homolog; RDC-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDLHLFDYSEPGNFSDISWPCNSSDCIVVDTVMCPNMPNKSVLLYTLSFIYIFIFVIGMI
ANSVVVWVNIQAKTTGYDTHCYILNLAIADLWVVLTIPVWVVSLVQHNQWPMGELTCKVT
HLIFSINLFGSIFFLTCMSVDRYLSITYFTNTPSSRKKMVRRVVCILVWLLAFCVSLPDT
YYLKTVTSASNNETYCRSFYPEHSIKEWLIGMELVSVVLGFAVPFSIIAVFYFLLARAIS
ASSDQEKHSSRKIIFSYVVVFLVCWLPYHVAVLLDIFSILHYIPFTCRLEHALFTALHVT
QCLSLVHCCVNPVLYSFINRNYRYELMKAFIFKYSAKTGLTKLIDASRVSETEYSALEQS
TK
Target Type
Preclinical
Target Bioclass
Cytokine and receptor
Family
G-protein coupled receptor 1 family, Atypical chemokine receptor subfamily
Subcellular location
Cell membrane
Function
Atypical chemokine receptor that controls chemokine levels and localization via high-affinity chemokine binding that is uncoupled from classic ligand-driven signal transduction cascades, resulting instead in chemokine sequestration, degradation, or transcytosis. Also known as interceptor (internalizing receptor) or chemokine-scavenging receptor or chemokine decoy receptor. Acts as a receptor for chemokines CXCL11 and CXCL12/SDF1. Chemokine binding does not activate G-protein-mediated signal transduction but instead induces beta-arrestin recruitment, leading to ligand internalization and activation of MAPK signaling pathway. Required for regulation of CXCR4 protein levels in migrating interneurons, thereby adapting their chemokine responsiveness. In glioma cells, transduces signals via MEK/ERK pathway, mediating resistance to apoptosis. Promotes cell growth and survival. Not involved in cell migration, adhesion or proliferation of normal hematopoietic progenitors but activated by CXCL11 in malignant hemapoietic cells, leading to phosphorylation of ERK1/2 (MAPK3/MAPK1) and enhanced cell adhesion and migration. Plays a regulatory role in CXCR4-mediated activation of cell surface integrins by CXCL12. Required for heart valve development. Regulates axon guidance in the oculomotor system through the regulation of CXCL12 levels.; (Microbial infection) Acts as a coreceptor with CXCR4 for a restricted number of HIV isolates.
TTD ID
T10491
Uniprot ID
P25106
DrugMap ID
TTRQJTC
Ensemble ID
ENST00000272928.4
HGNC ID
HGNC:23692
ChEMBL ID
CHEMBL2010631

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 
C196(2.24)  LDD2469  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 MGG123 C196(2.24)  LDD2469  [1]
 LDCM0023  KB03 MGG123 C196(2.96)  LDD2886  [1]
 LDCM0024  KB05 MGG123 C196(2.93)  LDD3303  [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