Target
C-C chemokine receptor type 2
Ligand
BDBM50337620
Substrate
n/a
Meas. Tech.
ChEMBL_728650 (CHEMBL1685780)
IC50
17±n/a nM
Citation
 Zheng, CCao, GXia, MFeng, HGlenn, JAnand, RZhang, KHuang, TWang, AKong, LLi, MGalya, LHughes, RODevraj, RMorton, PARogier, DJCovington, MBaribaud, FShin, NScherle, PDiamond, SYeleswaram, SVaddi, KNewton, RHollis, GFriedman, SMetcalf, BXue, CB Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist. Bioorg Med Chem Lett 21:1442-6 (2011) [PubMed]  Article
Target
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:
MLSTSRSRFIRNTNESGEEVTTFFDYDYGAPCHKFDVKQIGAQLLPPLYSLVFIFGFVGNMLVVLILINCKKLKCLTDIYLLNLAISDLLFLITLPLWAHSAANEWVFGNAMCKLFTGLYHIGYFGGIFFIILLTIDRYLAIVHAVFALKARTVTFGVVTSVITWLVAVFASVPGIIFTKCQKEDSVYVCGPYFPRGWNNFHTIMRNILGLVLPLLIMVICYSGILKTLLRCRNEKKRHRAVRVIFTIMIVYFLFWTPYNIVILLNTFQEFFGLSNCESTSQLDQATQVTETLGMTHCCINPIIYAFVGEKFRSLFHIALGCRIAPLQKPVCGGPGVRPGKNVKVTTQGLLDGRGKGKSIGRAPEASLQDKEGA
  
Inhibitor
Name:
BDBM50337620
Synonyms:
((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(4-(trifluoromethyl)pyrimidin-2-yl)piperazin-1-yl)methanone | CHEMBL1683075
Type:
Small organic molecule
Emp. Form.:
C24H36F3N5O3
Mol. Mass.:
499.5695
SMILES:
CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCN(CC1)c1nccc(n1)C(F)(F)F |r|
Structure:
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