General Information of the Protein
Protein ID
PT04128
Protein Name
C-C chemokine receptor type 2
Secondarily
Protein Name
JE/FIC receptor
MCP-1 receptor
Gene Name
CCR2
Secondarily
Gene Name
Cmkbr2
Sequence
MEDNNMLPQFIHGILSTSHSLFTRSIQELDEGATTPYDYDDGEPCHKTSVKQIGAWILPPLYSLVFIFGFVGNMLVIIILIGCKKLKSMTDIYLLNLAISDLLFLLTLPFWAHYAANEWVFGNIMCKVFTGLYHIGYFGGIFFIILLTIDRYLAIVHAVFALKARTVTFGVITSVVTWVVAVFASLPGIIFTKSKQDDHHYTCGPYFTQLWKNFQTIMRNILSLILPLLVMVICYSGILHTLFRCRNEKKRHRAVRLIFAIMIVYFLFWTPYNIVLFLTTFQESLGMSNCVIDKHLDQAMQVTETLGMTHCCINPVIYAFVGEKFRRYLSIFFRKHIAKRLCKQCPVFYRETADRVSSTFTPSTGEQEVSVGL
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Organism
Mus musculus, Mouse
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Chemokine receptor
>
CC chemokine receptor
Function
Key functional receptor for CCL2 but can also bind CCL7 and CCL12 chemokines (PubMed:8631787, PubMed:8662823, PubMed:8996246). Its binding with CCL2 on monocytes and macrophages mediates chemotaxis and migration induction through the activation of the PI3K cascade, the small G protein Rac and lamellipodium protrusion (By similarity). Also acts as a receptor for the beta-defensin DEFB106A/DEFB106B (By similarity). Regulates the expression of T-cell inflammatory cytokines and T-cell differentiation, promoting the differentiation of T-cells into T-helper 17 cells (Th17) during inflammation (PubMed:28507030). Facilitates the export of mature thymocytes by enhancing directional movement of thymocytes to sphingosine-1-phosphate stimulation and up-regulation of S1P1R expression; signals through the JAK-STAT pathway to regulate FOXO1 activity leading to an increased expression of S1P1R (PubMed:29930553). Plays an important role in mediating peripheral nerve injury-induced neuropathic pain (PubMed:29993042). Increases NMDA-mediated synaptic transmission in both dopamine D1 and D2 receptor-containing neurons, which may be caused by MAPK/ERK-dependent phosphorylation of GRIN2B/NMDAR2B (PubMed:29993042). Mediates the recruitment of macrophages and monocytes to the injury site following brain injury (PubMed:24806994, PubMed:29632244).
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Uniprot ID
Primary ID:
P51683

Secondarily ID:
Q61172
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Ensembl ID
ENSG00000121807
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0437369
1-ethyl-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C30H34F4N2O
 1
1
IC50 = 3.5 nM
   TI
   LI
   LO
   TS
CP0444505
(1S,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(propan-2-yl)cyclopentane-1-carboxamide
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C31H36F4N2O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0428650
(1R,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-1-(2-methylpropyl)-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C32H38F4N2O
 1
1
IC50 = 7.5 nM
   TI
   LI
   LO
   TS
CP0425145
(1S,3R)-1-cyclopropyl-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C31H34F4N2O
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0425146
1-(cyclopropylmethyl)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C32H36F4N2O
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0442366
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(propan-2-yl)cyclopentane-1-carboxamide
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C32H36F6N2O
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0522581
N-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-propylcyclopentane-1-carboxamide
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C31H36F4N2O
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0525772
(1R,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-[(methylsulfanyl)methyl]cyclopentane-1-carboxamide
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C30H34F4N2OS
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0428649
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-ethyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C31H34F6N2O
 1
1
IC50 = 17.5 nM
   TI
   LI
   LO
   TS
CP0437367
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-1-(2-methylpropyl)-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C33H38F6N2O
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0420176
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-propylcyclopentane-1-carboxamide
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C32H36F6N2O
 1
1
IC50 = 44.3 nM
   TI
   LI
   LO
   TS
CP0535185
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-cyclopropyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C32H34F6N2O
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0373631
(1S,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-1-methyl-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C29H32F4N2O
 1
1
IC50 = 57 nM
   TI
   LI
   LO
   TS
CP0427178
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-(cyclopropylmethyl)-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C33H36F6N2O
 1
1
IC50 = 63.5 nM
   TI
   LI
   LO
   TS
CP0428648
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-1-(cyclobutylmethyl)-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C34H38F6N2O
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0428698
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-[(methylsulfanyl)methyl]cyclopentane-1-carboxamide
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C31H34F6N2OS
 1
1
IC50 = 65.5 nM
   TI
   LI
   LO
   TS
CP0522580
N-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-1-(methoxymethyl)-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C30H34F4N2O2
 1
1
IC50 = 74 nM
   TI
   LI
   LO
   TS
CP0535186
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-(methoxymethyl)-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C31H34F6N2O2
 1
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0437368
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-1-methyl-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C30H32F6N2O
 1
1
IC50 = 126 nM
   TI
   LI
   LO
   TS
CP0373628
N-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-1-hexyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C34H42F4N2O
 1
1
IC50 = 128 nM
   TI
   LI
   LO
   TS
CP0505434
(1R,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(methylsulfanyl)cyclopentane-1-carboxamide
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C29H32F4N2OS
 1
1
IC50 = 193 nM
   TI
   LI
   LO
   TS
CP0433969
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-hexyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C35H42F6N2O
 1
1
IC50 = 279 nM
   TI
   LI
   LO
   TS
CP0433968
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(methylsulfanyl)cyclopentane-1-carboxamide
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C30H32F6N2OS
 1
1
IC50 = 351 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04757 C-C chemokine receptor type 2 Rattus norvegicus, Rat
50% Identity
Protein ID Protein Name Protein Organism
PT01021 C-C chemokine receptor type 2 Homo sapiens, Human