Human CMKLR1

Figure. Concentration-dependent activation of CMKLR1 by chemerin

Reporter cells were transfected with either the expression plasmid for human chemerin chemokine-like receptor 1 (CMKLR1) or the mock plasmid and treated with various concentrations of chemerin. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 15 nM.

chemerin chemokine-like receptor 1
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Urology/Reproduction, Human non-orphan GPCRs

Chemerin receptors

The chemoattractant protein and adipokine, chemerin, has been shown to be the endogenous ligand for both chemerin family receptors. Chemerin1 was the founding family member, and when GPR1 was de-orphanised it was re-named Chermerin2 [1]. Chemerin1 is also activated by the lipid-derived, anti-inflammatory ligand resolvin E1 (RvE1), which is formed via the sequential metabolism of EPA by aspirin-modified cyclooxygenase and lipoxygenase [2,3]. In addition, two GPCRs for resolvin D1 (RvD1) have been identified: FPR2/ALX, the lipoxin A4 receptor, and GPR32, an orphan receptor [4].


  1. Kennedy AJ, Davenport AP. International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function. Pharmacol Rev 2018;70:174-196.
  2. Arita M, Bianchini F, Aliberti J, et al. Stereochemical assignment, antiinflammatory properties, and receptor for the omega-3 lipid mediator resolvin E1. J Exp Med 2005;201:713-22.
  3. Arita M, Ohira T, Sun YP, et al. Resolvin E1 selectively interacts with leukotriene B4 receptor BLT1 and ChemR23 to regulate inflammation. J Immunol 2007;178:3912-7.
  4. Krishnamoorthy S, Recchiuti A, Chiang N, et al. Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc Natl Acad Sci USA 2010;107:1660-5.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

Filters Sort results
Reset Apply