Details of the Target

General Information of Target

Target ID LDTP04447
Target Name C-C chemokine receptor type 5 (CCR5)
Gene Name CCR5
Gene ID 1234
Synonyms
CMKBR5; C-C chemokine receptor type 5; C-C CKR-5; CC-CKR-5; CCR-5; CCR5; CHEMR13; HIV-1 fusion coreceptor; CD antigen CD195
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDYQVSSPIYDINYYTSEPCQKINVKQIAARLLPPLYSLVFIFGFVGNMLVILILINCKR
LKSMTDIYLLNLAISDLFFLLTVPFWAHYAAAQWDFGNTMCQLLTGLYFIGFFSGIFFII
LLTIDRYLAVVHAVFALKARTVTFGVVTSVITWVVAVFASLPGIIFTRSQKEGLHYTCSS
HFPYSQYQFWKNFQTLKIVILGLVLPLLVMVICYSGILKTLLRCRNEKKRHRAVRLIFTI
MIVYFLFWAPYNIVLLLNTFQEFFGLNNCSSSNRLDQAMQVTETLGMTHCCINPIIYAFV
GEKFRNYLLVFFQKHIAKRFCKCCSIFQQEAPERASSVYTRSTGEQEISVGL
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for a number of inflammatory CC-chemokines including CCL3/MIP-1-alpha, CCL4/MIP-1-beta and RANTES and subsequently transduces a signal by increasing the intracellular calcium ion level. May play a role in the control of granulocytic lineage proliferation or differentiation. Participates in T-lymphocyte migration to the infection site by acting as a chemotactic receptor.; (Microbial infection) Acts as a coreceptor (CD4 being the primary receptor) of human immunodeficiency virus-1/HIV-1.
TTD ID
T09960
Uniprot ID
P51681
DrugMap ID
TTH91NV
Ensemble ID
ENST00000292303.5
HGNC ID
HGNC:1606
ChEMBL ID
CHEMBL274

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
IA-alkyne
 Probe Info  		C323, C324(8.52)  LDD1707  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell C323, C324(8.52)  LDD1707  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

GPCR
Click To Hide/Show 1 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
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
T-cell surface glycoprotein CD4 (CD4) . P01730
Cytokine and receptor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
C-X-C chemokine receptor type 4 (CXCR4) G-protein coupled receptor 1 family P61073
C-C motif chemokine 17 (CCL17) Intercrine beta (chemokine CC) family Q92583
C-C motif chemokine 5 (CCL5) Intercrine beta (chemokine CC) family P13501
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Epithelial membrane protein 1 (EMP1) PMP-22/EMP/MP20 family P54849

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Maraviroc Small molecular drug D0NR6S
Ibalizumab . DB12698
Phase 3
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pro 140 Antibody D1M8GC
E-913 Small molecular drug D0J7QU
Vicriviroc Small molecular drug D09JLI
Pro-140 . D0CG0N
Phase 2
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cenicriviroc Small molecular drug D0YQ7U
Incb9471 Small molecular drug D0Y7NA
Pf-232798 Small molecular drug D0F7PZ
Bms-813160 . D0B1SG
Cal-1 . D0A0BK
Gsk-706769 . D0UV4H
Sb-728-t . D06FIT
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ccr5 Mab Antibody D0K1OK
Tak-220 Small molecular drug D0O9UC
Incb15050 . D06KNE
Vch-286 . D09XXH
Investigative
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ccr5 Mab Antibody DB05906
Leronlimab Monoclonal antibody DB05941
(2-(4-chlorobenzyloxy)-5-bromophenyl)Methanamine Small molecular drug D0I3IZ
4-(2-(4-chlorobenzyloxy)-5-bromobenzyl)Morpholine Small molecular drug D0BD3G
Amd-070 Small molecular drug DB05501
Anibamine Small molecular drug D01LRC
Cmpd-167 Small molecular drug D06TQD
Gt-1282 Small molecular drug D0BD6A
Incb-9471 Small molecular drug DB12960
N-(2-(4-chlorobenzyloxy)-5-bromobenzyl)Ethanamine Small molecular drug D06XRS
Nifeviroc Small molecular drug D0J3BT
Sch-210971 Small molecular drug D01TYO
Variecolin Small molecular drug D06XIC
Aplaviroc . DB06497
Discontinued
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd5672 Small molecular drug D07GIB
Gw873140 Small molecular drug D0G6SZ
Sch-c Small molecular drug D0G6JE
Tak-779 Small molecular drug D0W0LS
Ccr5qb Vaccine D0O9AZ
Azd8566 . D06EMW

References

1 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.