Details of the Target

General Information of Target

Target ID LDTP04896
Target Name C-X-C chemokine receptor type 4 (CXCR4)
Gene Name CXCR4
Gene ID 7852
Synonyms
C-X-C chemokine receptor type 4; CXC-R4; CXCR-4; FB22; Fusin; HM89; LCR1; Leukocyte-derived seven transmembrane domain receptor; LESTR; Lipopolysaccharide-associated protein 3; LAP-3; LPS-associated protein 3; NPYRL; Stromal cell-derived factor 1 receptor; SDF-1 receptor; CD antigen CD184
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEGISIYTSDNYTEEMGSGDYDSMKEPCFREENANFNKIFLPTIYSIIFLTGIVGNGLVI
LVMGYQKKLRSMTDKYRLHLSVADLLFVITLPFWAVDAVANWYFGNFLCKAVHVIYTVNL
YSSVLILAFISLDRYLAIVHATNSQRPRKLLAEKVVYVGVWIPALLLTIPDFIFANVSEA
DDRYICDRFYPNDLWVVVFQFQHIMVGLILPGIVILSCYCIIISKLSHSKGHQKRKALKT
TVILILAFFACWLPYYIGISIDSFILLEIIKQGCEFENTVHKWISITEALAFFHCCLNPI
LYAFLGAKFKTSAQHALTSVSRGSSLKILSKGKRGGHSSVSTESESSSFHSS
Target Type
Successful
Target Bioclass
Cytokine and receptor
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for the C-X-C chemokine CXCL12/SDF-1 that transduces a signal by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation. Involved in the AKT signaling cascade. Plays a role in regulation of cell migration, e.g. during wound healing. Acts as a receptor for extracellular ubiquitin; leading to enhanced intracellular calcium ions and reduced cellular cAMP levels. Binds bacterial lipopolysaccharide (LPS) et mediates LPS-induced inflammatory response, including TNF secretion by monocytes. Involved in hematopoiesis and in cardiac ventricular septum formation. Also plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Involved in cerebellar development. In the CNS, could mediate hippocampal-neuron survival.; (Microbial infection) Acts as a coreceptor (CD4 being the primary receptor) for human immunodeficiency virus-1/HIV-1 X4 isolates and as a primary receptor for some HIV-2 isolates. Promotes Env-mediated fusion of the virus.
TTD ID
T96079
Uniprot ID
P61073
DrugMap ID
TTBID49
Ensemble ID
ENST00000241393.4
HGNC ID
HGNC:2561
ChEMBL ID
CHEMBL2107

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
FADU SNV: p.L150V .
HCT116 SNV: p.Y76C .
KYSE510 SNV: p.G323W .
MCAS SNV: p.E15Ter .
MOLT4 SNV: p.V242I .
RKO SNV: p.T43N .

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  		C274(0.73)  LDD1492  [1]
Acrolein
 Probe Info  		H350(0.00); H337(0.00); H315(0.00)  LDD0217  [2]
Crotonaldehyde
 Probe Info  		H337(0.00); H350(0.00)  LDD0219  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0270  AC15 HEK-293T C274(0.98)  LDD1513  [1]
 LDCM0281  AC21 HEK-293T C274(0.81)  LDD1520  [1]
 LDCM0283  AC23 HEK-293T C274(0.95)  LDD1522  [1]
 LDCM0289  AC29 HEK-293T C274(0.97)  LDD1528  [1]
 LDCM0292  AC31 HEK-293T C274(0.99)  LDD1531  [1]
 LDCM0298  AC37 HEK-293T C274(0.89)  LDD1537  [1]
 LDCM0300  AC39 HEK-293T C274(1.14)  LDD1539  [1]
 LDCM0307  AC45 HEK-293T C274(0.78)  LDD1546  [1]
 LDCM0309  AC47 HEK-293T C274(1.02)  LDD1548  [1]
 LDCM0312  AC5 HEK-293T C274(0.86)  LDD1551  [1]
 LDCM0316  AC53 HEK-293T C274(0.89)  LDD1555  [1]
 LDCM0318  AC55 HEK-293T C274(1.12)  LDD1557  [1]
 LDCM0325  AC61 HEK-293T C274(1.02)  LDD1564  [1]
 LDCM0327  AC63 HEK-293T C274(0.98)  LDD1566  [1]
 LDCM0334  AC7 HEK-293T C274(0.98)  LDD1568  [1]
 LDCM0248  AKOS034007472 HEK-293T C274(0.99)  LDD1511  [1]
 LDCM0108  Chloroacetamide HeLa H350(0.00); H315(0.00); H337(0.00)  LDD0222  [2]
 LDCM0369  CL100 HEK-293T C274(0.90)  LDD1573  [1]
 LDCM0371  CL102 HEK-293T C274(1.06)  LDD1575  [1]
 LDCM0373  CL104 HEK-293T C274(0.88)  LDD1577  [1]
 LDCM0375  CL106 HEK-293T C274(1.20)  LDD1579  [1]
 LDCM0377  CL108 HEK-293T C274(0.91)  LDD1581  [1]
 LDCM0379  CL11 HEK-293T C274(1.48)  LDD1583  [1]
 LDCM0380  CL110 HEK-293T C274(1.06)  LDD1584  [1]
 LDCM0382  CL112 HEK-293T C274(1.01)  LDD1586  [1]
 LDCM0384  CL114 HEK-293T C274(1.26)  LDD1588  [1]
 LDCM0386  CL116 HEK-293T C274(0.83)  LDD1590  [1]
 LDCM0388  CL118 HEK-293T C274(0.99)  LDD1592  [1]
 LDCM0391  CL120 HEK-293T C274(0.85)  LDD1595  [1]
 LDCM0393  CL122 HEK-293T C274(1.02)  LDD1597  [1]
 LDCM0395  CL124 HEK-293T C274(0.92)  LDD1599  [1]
 LDCM0397  CL126 HEK-293T C274(1.09)  LDD1601  [1]
 LDCM0399  CL128 HEK-293T C274(0.89)  LDD1603  [1]
 LDCM0401  CL14 HEK-293T C274(1.06)  LDD1605  [1]
 LDCM0403  CL16 HEK-293T C274(1.02)  LDD1607  [1]
 LDCM0407  CL2 HEK-293T C274(1.16)  LDD1611  [1]
 LDCM0409  CL21 HEK-293T C274(2.77)  LDD1613  [1]
 LDCM0411  CL23 HEK-293T C274(1.66)  LDD1615  [1]
 LDCM0414  CL26 HEK-293T C274(0.94)  LDD1618  [1]
 LDCM0416  CL28 HEK-293T C274(1.01)  LDD1620  [1]
 LDCM0422  CL33 HEK-293T C274(3.06)  LDD1626  [1]
 LDCM0424  CL35 HEK-293T C274(1.57)  LDD1628  [1]
 LDCM0429  CL4 HEK-293T C274(1.71)  LDD1633  [1]
 LDCM0430  CL40 HEK-293T C274(1.11)  LDD1634  [1]
 LDCM0435  CL45 HEK-293T C274(1.62)  LDD1639  [1]
 LDCM0437  CL47 HEK-293T C274(1.51)  LDD1641  [1]
 LDCM0441  CL50 HEK-293T C274(0.97)  LDD1645  [1]
 LDCM0443  CL52 HEK-293T C274(0.99)  LDD1646  [1]
 LDCM0448  CL57 HEK-293T C274(1.85)  LDD1651  [1]
 LDCM0450  CL59 HEK-293T C274(1.63)  LDD1653  [1]
 LDCM0454  CL62 HEK-293T C274(0.99)  LDD1657  [1]
 LDCM0456  CL64 HEK-293T C274(1.21)  LDD1659  [1]
 LDCM0461  CL69 HEK-293T C274(1.57)  LDD1664  [1]
 LDCM0464  CL71 HEK-293T C274(1.44)  LDD1667  [1]
 LDCM0467  CL74 HEK-293T C274(0.94)  LDD1670  [1]
 LDCM0469  CL76 HEK-293T C274(0.91)  LDD1672  [1]
 LDCM0475  CL81 HEK-293T C274(1.45)  LDD1678  [1]
 LDCM0477  CL83 HEK-293T C274(1.43)  LDD1680  [1]
 LDCM0480  CL86 HEK-293T C274(1.14)  LDD1683  [1]
 LDCM0482  CL88 HEK-293T C274(0.93)  LDD1685  [1]
 LDCM0484  CL9 HEK-293T C274(2.17)  LDD1687  [1]
 LDCM0488  CL93 HEK-293T C274(1.58)  LDD1691  [1]
 LDCM0490  CL95 HEK-293T C274(1.51)  LDD1693  [1]
 LDCM0493  CL98 HEK-293T C274(1.18)  LDD1696  [1]
 LDCM0427  Fragment51 HEK-293T C274(0.94)  LDD1631  [1]
 LDCM0107  IAA HeLa H350(0.00); H337(0.00); H315(0.00)  LDD0221  [2]
 LDCM0022  KB02 HEK-293T C274(0.73)  LDD1492  [1]
 LDCM0023  KB03 HEK-293T C274(0.96)  LDD1497  [1]
 LDCM0024  KB05 HEK-293T C274(0.71)  LDD1502  [1]
 LDCM0109  NEM HeLa H337(0.00); H350(0.00); H315(0.00)  LDD0223  [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
Myosin-9 (MYH9) Myosin family P35579
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Toll-like receptor 2 (TLR2) Toll-like receptor family O60603
HLA class II histocompatibility antigen gamma chain (CD74) . P04233
GPCR
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
C-C chemokine receptor type 5 (CCR5) G-protein coupled receptor 1 family P51681
C-X-C chemokine receptor type 3 (CXCR3) G-protein coupled receptor 1 family P49682
C-X-C chemokine receptor type 5 (CXCR5) G-protein coupled receptor 1 family P32302
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Atypical chemokine receptor 3 (ACKR3) G-protein coupled receptor 1 family P25106
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sialomucin core protein 24 (CD164) CD164 family Q04900
Drebrin (DBN1) . Q16643

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Baclofen Small molecular drug DB00181
Framycetin Small molecular drug DB00452
Plerixafor Small molecular drug D0L5RW
Ibalizumab . DB12698
Phase 3
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ulocuplumab Monoclonal antibody D0C3LQ
Balixafortide Peptide D0GG9P
Bl-8040 Peptide D0T6CN
Amd-070 Small molecular drug D0O2XQ
Phase 2
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ctce-9908 . D01TJM
Pol-6326 . D0FV8P
Tg-0054 . D06KGI
Usl311 . D08XQV
Phase 1
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ly2624587 Antibody D3KZ6M
Gmi-1359 Small molecular drug DBDW09
Msx-122 Small molecular drug D0E5JC
Alx-0651 . D09MPD
Bms-936564 . D0Z8JR
Ctce-0214 . D0AZ3Y
Pf-06747143 . D0LC5L
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mab173 Antibody D2NU0H
Investigative
Click To Hide/Show 41 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cx-02 Antibody D06EBJ
Cxcl8 Small molecular drug D07PHS
Cyclo(-d-ala-d-arg-l-arg-l-nal-gly-) Small molecular drug D0K9KQ
Cyclo(-d-metyr-d-arg-l-arg-l-nal-gly-) Small molecular drug D00XBM
Cyclo(-d-metyr-l-arg-l-arg-l-nal-gly-) Small molecular drug D0S0GV
Cyclo(-d-tyr-arg-arg-nal-gly-) Small molecular drug D04TIO
Cyclo(-d-tyr-d-ala-l-arg-l-nal-gly-) Small molecular drug D0FQ3G
Cyclo(-d-tyr-d-arg-l-arg-l-menal-gly-) Small molecular drug D04BVW
Cyclo(-d-tyr-d-arg-l-arg-l-nal-beta-ala-) Small molecular drug D04XHX
Cyclo(-d-tyr-d-arg-l-arg-l-nal-d-ala-) Small molecular drug D0K0SO
Cyclo(-d-tyr-d-arg-l-arg-l-nal-gly-) Small molecular drug D0ZO3C
Cyclo(-d-tyr-d-arg-l-arg-l-nal-l-ala-) Small molecular drug D0BH8K
Cyclo(-d-tyr-d-arg-l-arg-l-nal-l-pic-) Small molecular drug D0ST1U
Cyclo(-d-tyr-d-arg-l-arg-l-nal-sar-) Small molecular drug D05YHT
Cyclo(-d-tyr-d-arg-l-mearg-l-nal-gly-) Small molecular drug D08YYV
Cyclo(-d-tyr-d-mearg-l-arg-l-nal-gly-) Small molecular drug D02UES
Cyclo(-d-tyr-l-ala-l-arg-l-nal-gly-) Small molecular drug D0M6RQ
Cyclo(-d-tyr-l-arg-l-arg-l-ala-sar-) Small molecular drug D08XRM
Cyclo(-d-tyr-l-arg-l-arg-l-menal-gly-) Small molecular drug D0B8VW
Cyclo(-d-tyr-l-arg-l-arg-l-nal-beta-ala-) Small molecular drug D0P7UV
Cyclo(-d-tyr-l-arg-l-arg-l-nal-d-ala-) Small molecular drug D0S0PU
Cyclo(-d-tyr-l-arg-l-arg-l-nal-gly-) Small molecular drug D0Q3MM
Cyclo(-d-tyr-l-arg-l-arg-l-nal-l-ala-) Small molecular drug D04PDF
Cyclo(-d-tyr-l-arg-l-mearg-l-nal-gly-) Small molecular drug D00GII
Cyclo(-d-tyr-l-mearg-l-arg-l-nal-gly-) Small molecular drug D04TED
Gsk-812397 Small molecular drug D03QJA
Isothiourea-1a Small molecular drug D06MBD
Isothiourea-1t Small molecular drug D05VQJ
Nb-325 Small molecular drug D0R4WT
T134 Small molecular drug D08NJD
T140 Small molecular drug D0I6AN
T22 Small molecular drug D0TL6C
Viral Macrophage Inflammatory Protein-ii Small molecular drug D09PZD
At-009 . D04ATE
Ati-2341 . D0A7GH
Ctce-0324 . D0L3GH
Cxcr4 Gene Disrupted T Cells . D07VDF
Kur-cxcr4 . D05IXH
Lp-0067 . D0Q7XS
Nd-401 . D07IZP
Tn-14003 . D0Y3OX
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Garnocestim . D0H5KK
Krh-2731 . D00FJS
Suradista . D0I4OX

References

1 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
2 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.