Target
C-C chemokine receptor type 2
Ligand
BDBM50337604
Substrate
n/a
Meas. Tech.
ChEMBL_728647 (CHEMBL1685777)
IC50
3.1±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:
BDBM50337604
Synonyms:
CHEMBL1683059 | Cis-((1S,3R)-1-isopropyl-3-(3-methyl-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)methanone
Type:
Small organic molecule
Emp. Form.:
C26H38F3N3O2
Mol. Mass.:
481.594
SMILES:
CC(C)[C@@]1(CC[C@H](C1)N[C@H]1CCOC[C@H]1C)C(=O)N1CCN(CC1)c1cccc(c1)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: