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TargetC-C chemokine receptor type 2
LigandBDBM50382941
Substrate/Competitorn/a
Meas. Tech.ChEMBL_819955 (CHEMBL2032542)
IC50 3.4±n/a nM
Citation Xue, CBWang, AHan, QZhang, YCao, GFeng, HHuang, TZheng, CXia, MZhang, KKong, LGlenn, JAnand, RMeloni, DRobinson, DJShao, LStorace, LLi, MHughes, RODevraj, RMorton, PARogier, DJCovington, MScherle, PDiamond, SEmm, TYeleswaram, SContel, NVaddi, KNewton, RHollis, GMetcalf, B Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. ACS Med Chem Lett2:913-918 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
C-C chemokine receptor type 2
Name:C-C chemokine receptor type 2
Synonyms:C-C chemokine receptor type 2 (CCR2) | CCR2 | CCR2_HUMAN | CMKBR2 | Chemoattractant Cytokine Receptor 2 (CCR2) | Chemokine Receptor Type 2b (CCR2b) | Monocyte chemotactic protein-1 (MCP-1)
Type:Enzyme
Mol. Mass.:41932.32
Organism:Homo sapiens (Human)
Description:P41597
Residue:374
Sequence:
MLSTSRSRFIRNTNESGEEVTTFFDYDYGAPCHKFDVKQIGAQLLPPLYSLVFIFGFVGN
MLVVLILINCKKLKCLTDIYLLNLAISDLLFLITLPLWAHSAANEWVFGNAMCKLFTGLY
HIGYFGGIFFIILLTIDRYLAIVHAVFALKARTVTFGVVTSVITWLVAVFASVPGIIFTK
CQKEDSVYVCGPYFPRGWNNFHTIMRNILGLVLPLLIMVICYSGILKTLLRCRNEKKRHR
AVRVIFTIMIVYFLFWTPYNIVILLNTFQEFFGLSNCESTSQLDQATQVTETLGMTHCCI
NPIIYAFVGEKFRSLFHIALGCRIAPLQKPVCGGPGVRPGKNVKVTTQGLLDGRGKGKSI
GRAPEASLQDKEGA
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  Blast E-value cutoff:
BDBM50382941
n/a
NameBDBM50382941
Synonyms:CHEMBL2029424
TypeSmall organic molecule
Emp. Form.C28H30F3N5O4
Mol. Mass.557.5641
SMILESO[C@]1(CC[C@@H](CC1)N[C@H]1CCN(C1)C(=O)CNC(=O)c1cccc(c1)C(F)(F)F)c1ccc(cn1)-c1ncco1 |r,wU:4.7,wD:8.8,1.0,(24.38,-2.82,;25.71,-3.59,;27.04,-4.36,;28.37,-3.59,;28.37,-2.05,;27.04,-1.28,;25.71,-2.05,;29.71,-1.29,;31.04,-2.06,;31.06,-3.6,;32.53,-4.05,;33.42,-2.8,;32.5,-1.56,;34.75,-2.02,;34.74,-.48,;36.09,-2.78,;37.42,-2,;38.75,-2.76,;38.77,-4.3,;40.08,-1.98,;40.06,-.45,;41.38,.33,;42.73,-.43,;42.74,-1.97,;41.42,-2.75,;44.08,-2.73,;44.09,-4.27,;45.41,-1.95,;45.33,-3.62,;24.38,-4.37,;23.05,-3.59,;21.72,-4.37,;21.72,-5.91,;23.06,-6.68,;24.39,-5.9,;20.39,-6.68,;18.97,-6.07,;17.95,-7.21,;18.72,-8.54,;20.23,-8.22,)|
Structure
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