Target family: Chemokine receptors (type: gpcr)
Target: CCR5

Ligand: ancriviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
Published in: J Med Chem

Ligand: ancriviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structural and molecular interactions of CCR5 inhibitors with CCR5.
Published in: J Biol Chem

Ligand: ancriviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.
Published in: Antimicrob Agents Chemother

Ligand: aplaviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Structural and molecular interactions of CCR5 inhibitors with CCR5.
Published in: J Biol Chem

Ligand: AZD5672 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.59000015258789 pIC50
Reference (Journal): Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.
Published in: Bioorg Med Chem Lett

Ligand: BMS-681 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.619999885559082 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: 6.110000133514404 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: 7.079999923706055 pIC50
Reference (Journal): Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Published in: ACS Med Chem Lett

Ligand: BP-CCL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Synthesis and characterization of fluorescent and photoactivatable MIP-1alpha ligands and interactions with chemokine receptors CCR1 and CCR5.
Published in: J Med Chem

Ligand: CCL11 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): CCR5 binds multiple CC-chemokines: MCP-3 acts as a natural antagonist.
Published in: Blood

Ligand: CCL13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): CCR5 has an expanded ligand-binding repertoire and is the primary receptor used by MCP-2 on activated T cells.
Published in: Cell Immunol

Ligand: CCL14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

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: 7.5 pKi
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: CCL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: CCL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and characterization of fluorescent and photoactivatable MIP-1alpha ligands and interactions with chemokine receptors CCR1 and CCR5.
Published in: J Med Chem

Ligand: CCL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): CCR5 has an expanded ligand-binding repertoire and is the primary receptor used by MCP-2 on activated T cells.
Published in: Cell Immunol

Ligand: CCL4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): CCR5 has an expanded ligand-binding repertoire and is the primary receptor used by MCP-2 on activated T cells.
Published in: Cell Immunol

Ligand: CCL4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: CCL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: CCL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  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: CCL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): CCR5 has an expanded ligand-binding repertoire and is the primary receptor used by MCP-2 on activated T cells.
Published in: Cell Immunol

Ligand: CCL7 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: CCL8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): CCR5 has an expanded ligand-binding repertoire and is the primary receptor used by MCP-2 on activated T cells.
Published in: Cell Immunol

Ligand: CCR5 antagonist 34 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.
Published in: J Med Chem

Ligand: cenicriviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans.
Published in: Antimicrob Agents Chemother

Ligand: compound 39 [PMID: 31742400] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.079999923706055 pIC50
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: E913 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5.
Published in: J Biol Chem

Ligand: Flu-CCL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Synthesis and characterization of fluorescent and photoactivatable MIP-1alpha ligands and interactions with chemokine receptors CCR1 and CCR5.
Published in: J Med Chem

Ligand: GSK2239633A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.
Published in: J Med Chem

Ligand: leronlimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Anti-CCR5 antibody

Ligand: maraviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA and FDA (2007)
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: MLN-3897 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): MLN3897, a novel CCR1 inhibitor, impairs osteoclastogenesis and inhibits the interaction of multiple myeloma cells and osteoclasts.
Published in: Blood

Ligand: MRK-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.
Published in: J Pharmacol Exp Ther

Ligand: R5-HIV-1 gp120 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: [125I]CCL3 (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: [125I]CCL4 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.6 pKd
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: [125I]CCL5 (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: [125I]CCL8 (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: [3H]ancriviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.
Published in: Antimicrob Agents Chemother

Ligand: [3H]maraviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human.
Published in: Biochem Pharmacol

Ligand: TAK-220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent Anti-HIV-1 activity.
Published in: J Med Chem

Ligand: TAK-779 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Structural and molecular interactions of CCR5 inhibitors with CCR5.
Published in: J Biol Chem

Ligand: vicriviroc (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.
Published in: Antimicrob Agents Chemother

Ligand: vMIP-II (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus.
Published in: Science