Target family: Chemokine receptors (type: gpcr)
Target: CCR2

Ligand: AZD2423 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.59000015258789 pIC50
Reference (Webpage): Slideset: CCR2 antagonists for the treatment of neuropathic pain. The discovery and development of AZD2423.

Ligand: BMS-681 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Published in: ACS Med Chem Lett

Ligand: BMS-741672 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Journal): Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Published in: ACS Med Chem Lett

Ligand: BMS-753426 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pIC50
Reference (Journal): Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Published in: ACS Med Chem Lett

Ligand: CCL11 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6.
Published in: J Biol Chem

Ligand: CCL11 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): High level expression, activation, and antagonism of CC chemokine receptors CCR2 and CCR3 in Chinese hamster ovary cells.
Published in: Cytokine

Ligand: CCL13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): High expression of the chemokine receptor CCR3 in human blood basophils. Role in activation by eotaxin, MCP-4, and other chemokines.
Published in: J Clin Invest

Ligand: CCL13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6.
Published in: J Biol Chem

Ligand: CCL16 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: CCL2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Characterisation of macrophage inflammatory protein-5/human CC cytokine-2, a member of the macrophage-inflammatory-protein family of chemokines.
Published in: Eur J Biochem

Ligand: CCL2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6.
Published in: J Biol Chem

Ligand: CCL2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.
Published in: J Biol Chem

Ligand: CCL2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): High expression of the chemokine receptor CCR3 in human blood basophils. Role in activation by eotaxin, MCP-4, and other chemokines.
Published in: J Clin Invest

Ligand: CCL2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): High level expression, activation, and antagonism of CC chemokine receptors CCR2 and CCR3 in Chinese hamster ovary cells.
Published in: Cytokine

Ligand: CCL24 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): High level expression, activation, and antagonism of CC chemokine receptors CCR2 and CCR3 in Chinese hamster ovary cells.
Published in: Cytokine

Ligand: CCL26 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): High level expression, activation, and antagonism of CC chemokine receptors CCR2 and CCR3 in Chinese hamster ovary cells.
Published in: Cytokine

Ligand: CCL7 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): High expression of the chemokine receptor CCR3 in human blood basophils. Role in activation by eotaxin, MCP-4, and other chemokines.
Published in: J Clin Invest

Ligand: CCL7 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6.
Published in: J Biol Chem

Ligand: CCL7 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Characterisation of macrophage inflammatory protein-5/human CC cytokine-2, a member of the macrophage-inflammatory-protein family of chemokines.
Published in: Eur J Biochem

Ligand: CCL8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6.
Published in: J Biol Chem

Ligand: CCR2-RA-[R] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pIC50
Reference (Patent): Pyrrolidinone derivatives

Ligand: CCR2-RA-[R] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pIC50
Reference (Journal): Novel, Acidic CCR2 Receptor Antagonists: Lead Optimization
Published in: Lett Drug Des Discov

Ligand: compound 39 [PMID: 31742400] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.
Published in: J Med Chem

Ligand: GSK Compound 34 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi

Ligand: HIV-Tat (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: HIV-Tat (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): HIV-1 Tat protein mimicry of chemokines.
Published in: Proc Natl Acad Sci USA

Ligand: ilacirnon (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Patent): Fused heteroaryl pyridyl and phenyl benzenesuflonamides as ccr2 modulators for the treament of inflammation

Ligand: INCB3284 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.430000305175781 pIC50
Reference (Journal): Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.
Published in: ACS Med Chem Lett

Ligand: INCB3344 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Published in: J Immunol

Ligand: INCB8761 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.279999732971191 pIC50
Reference (Journal): Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
Published in: ACS Med Chem Lett

Ligand: JNJ-27141491 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.019999980926514 pIC50
Reference (Journal): Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2.
Published in: J Pharmacol Exp Ther

Ligand: MC148R (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): Broad spectrum chemokine antagonistic activity of a human poxvirus chemokine homolog.
Published in: Proc Natl Acad Sci USA

Ligand: MK-0812 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist.
Published in: J Immunol Methods

Ligand: PF-04634817 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 pIC50
Reference (Patent): 3-aminocyclopentanecarboxamides as chemokine receptor agonists.

Ligand: plozalizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9.720000267028809 pEC50
Reference (Patent): Humanized anti-CCR2 antibodies and methods of use therefor.

Ligand: RS-102895 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.
Published in: J Biol Chem

Ligand: RS-136270 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.
Published in: J Biol Chem

Ligand: RS-504393 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Published in: J Med Chem

Ligand: SB-282241 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Published in: J Med Chem

Ligand: [125I]CCL2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: [125I]CCL7 (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: TAK-779 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity.
Published in: Proc Natl Acad Sci USA

Ligand: TAK-779 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Published in: J Med Chem

Ligand: TAK-779 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Published in: J Med Chem

Ligand: Teijin-lead_cmp_5 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Published in: J Med Chem

Ligand: vCCL4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6.
Published in: J Biol Chem

Ligand: vMIP-II (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pIC50
Reference (Journal): A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus.
Published in: Science