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Chemokine GPCR Assays

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Overview of Chemokine Receptors

Chemokines, a family of secreted cytokines, are involved in the regulation of various physiological and pathological processes. Chemokines are classified into four subfamilies according to the assembly of cysteine residues: CC, XC, CXC, and CX3C. Chemokines are composed of chemokine ligands and receptors. Chemokine receptors are expressed on all leukocytes and can be divided into two groups: G protein-coupled chemokine receptors (GPCRs) and atypical chemokine receptors (ACKRs). It is worth noting that many chemokine ligands can bind to multiple receptors and some receptors have many ligands.

Functions of chemokines and their receptors.Fig.1. Functions of chemokines and their receptors. (Hughes, 2028)

Chemokine Receptors and Diseases

Chemokines play multiple roles in a variety of life activities, such as chemotaxis, leukocyte migration, cell proliferation, and survival. Due to their vital roles, chemokines have always been relevant to many human disorders, such as inflammation, cancer, allergy, viral infections, atherosclerosis, and autoimmune diseases. Activation of chemokine-mediated signaling pathways requires selective binding of chemokines to receptors. Chemokines from four subfamilies activate diverse receptors. Chemokines and chemokine receptors are potential therapeutic targets for antagonists aimed at blocking chemokine receptor-ligand interactions.

The table lists the types of general chemokine receptors and their main mechanisms.

Receptor Gene Mechanism Agonists Antagonists
CC chemokine receptors 1 CCR1
  • CCR1 binds CC chemokines, including CCL4, CCL5, CCL6, CCL14, CCL15, CCL16 and CCL23.
  • CXCL4
  • CD26
  • LD78β
  • BX-471
  • BX 513 hydrochloride
CC chemokine receptors 2 CCR2
  • CCR2 can interact with CCL2, CCL8 and CCL16.
  • MCP-1
  • BMS CCR2 22
  • INCB 3284 dimesylate
CC chemokine receptors 3 CCR3
  • CCR3 binds CC chemokines, including CCL11, CCL26, CCL7, CCL13, CCL15, CCL24 and CCL5
  • CXCL11
  • RS 504393
  • SB 297006
CC chemokine receptors 4 CCR4
  • CCR4 binds CC chemokines, including CCL3, CCL5, CCL17 and CCL22
  • vMIP-III
  • CCL22
  • GSK 2239633A
  • AZD 2098
CC chemokine receptors 5 CCR5
  • CCR5 binds CC chemokines, including CCL2, CCL3, CCL4, CCL5, CCL11, CCL13, CCL14 and CCL16.
  • SDF-1
  • YM-370749
  • CCL5
  • DAPTA
  • Maraviroc
CC chemokine receptors 6 CCR6
  • CCR6 is a receptor for CCL20
  • CCL20
  • GSK3050002
CC chemokine receptors 7 CCR7
  • CCR7 binds CC chemokines, including CCL19 and CCL21
  • CCL21
  • CCL19
CC chemokine receptors 8 CCR8
  • The ligands for this receptor are CCL1 and CCL16
  • ZK 756326
  • vMIP-I
CC chemokine receptors 9 CCR9
  • The specific ligand of this receptor is CCL25
  • CCL25
CC chemokine receptors 10 CCR10
  • CCR10 is receptor for CCL27 and CCL28
  • CCL28
  • BI-6901
CX3C chemokine receptor 1 CX3CR1
  • This receptor binds the chemokine CX3CL1
  • CX3CL1
  • CCL26
CXC Chemokine receptor 1 CXCR1
  • CXCL8 and CXCL6 can both bind CXCR1
  • vCXCL1
CXC Chemokine receptor 2 CXCR2
  • CXCL1 to CXCL7 can bind CXCR2
  • vCXCL1
  • CXCL8-Arg6His
  • SB 332235
  • SB 265610
CXC Chemokine receptor 3 CXCR3
  • It has three highly related ligands, CXCL9, CXCL10, and CXCL11
  • CXCL10
  • CXCL11
  • VUF 11222
  • AMG487
  • NBI-74330
CXC Chemokine receptor 4 CXCR4
  • CXCR4 is the receptor for a chemokine known as CXCL12
  • NUCC-390
  • UCUF-728
  • AT-2341
  • AMD3100
  • BL-8040
  • CTCE 9908
CXC Chemokine receptor 5 CXCR5
  • Its principal ligand is CXCL13
  • CXCL13
CXC Chemokine receptor 6 CXCR6
  • CXCR6 binds the ligand CXCL16
  • CXCL16
  • ML 339
CXC Chemokine receptor 7 ACKR3
  • It can bind the chemokines CXCL12/SDF-1 and CXCL11
  • Amantamide
  • TC14012
  • AMD3100
  • TC 14012
  • CCX771
  • ACT-1004-1239

Assay List of Chemokine Receptors

Creative Biolabs can provide a range of assays of chemokine receptors. You can choose the assay in the list or contact us for more information:

CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9 CCR10 CX3CR1 CXCR1 CXCR2 CXCR3 CXCR4 CXCR5 CXCR6 ACKR1 ACKR3 ACKR4
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX285 Magic™ Mouse CCR1 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX281 Magic™ Human CCR1 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX283 Magic™ Human CCR1 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX284 Magic™ Human CCR1 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX291 Magic™ Human CCR2 In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX295 Magic™ Mouse CCR2 In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX300 Magic™ Rat CCR2 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX290 Magic™ Human CCR2 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX294 Magic™ Mouse CCR2 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX297 Magic™ Rhesus monkey CCR2 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX299 Magic™ Rat CCR2 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX292 Magic™ Human CCR2 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX293 Magic™ Human CCR2 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX296 Magic™ Mouse CCR2 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX298 Magic™ Rhesus monkey CCR2 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX301 Magic™ Rat CCR2 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-0722-KX12 Magic™ Human CCR3 In Vitro Agonist cAMP Assay, CHO CHO cAMP Assay
Calcium Flux Assay
S01YF-1122-KX302 Magic™ Human CCR3 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX305 Magic™ Mouse CCR3 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX303 Magic™ Human CCR3 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX304 Magic™ Human CCR3 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX306 Magic™ Human CCR4 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX309 Magic™ Mouse CCR4 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX307 Magic™ Human CCR4 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX308 Magic™ Human CCR4 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX321 Magic™ Rat CCR5 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX311 Magic™ Human CCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX315 Magic™ Mouse CCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX320 Magic™ Rat CCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX317 Magic™ Rabbit CCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX310 Magic™ Dog CCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX318 Magic™ Rhesus Macaque CCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX313 Magic™ Human CCR5 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX314 Magic™ Human CCR5 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX316 Magic™ Mouse CCR5 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX319 Magic™ Rhesus Macaque CCR5 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX322 Magic™ Rat CCR5 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX328 Magic™ Mouse CCR6 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX323 Magic™ Human CCR6 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX327 Magic™ Mouse CCR6 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX325 Magic™ Human CCR6 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX326 Magic™ Human CCR6 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX329 Magic™ Human CCR7 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX333 Magic™ Mouse CCR7 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX331 Magic™ Human CCR7 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX332 Magic™ Human CCR7 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX335 Magic™ Human CCR8 In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX339 Magic™ Mouse CCR8 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX334 Magic™ Human CCR8 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX338 Magic™ Mouse CCR8 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX336 Magic™ Human CCR8 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX337 Magic™ Human CCR8 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX340 Magic™ Human CCR9 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX341 Magic™ Mouse CCR9 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX286 Magic™ Human CCR10 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX289 Magic™ Mouse CCR10 In Vitro Calcium Flux Assay CHO-K1-Gqi5 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX288 Magic™ Human CCR10 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX343 Magic™ Human CX3CR1 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX342 Magic™ Human CX3CR1 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX346 Magic™ Mouse CX3CR1 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX348 Magic™ Rat CX3CR1 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX344 Magic™ Human CX3CR1 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
S01YF-1122-KX347 Magic™ Mouse CX3CR1 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX345 Magic™ Human CX3CR1 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-0722-KX94 Magic™ Human CXCR1 In Vitro cAMP Assay, HEK293 HEK293 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX349 Magic™ Human CXCR1 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX352 Magic™ Mouse CXCR1 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX350 Magic™ Human CXCR1 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX351 Magic™ Human CXCR1 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-0722-KX95 Magic™ Human CXCR2 In Vitro cAMP Assay, HEK293 HEK293 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX353 Magic™ Human CXCR2 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX357 Magic™ Mouse CXCR2 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX356 Magic™ Human CXCR2 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX358 Magic™ Human CXCR3a In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX361 Magic™ Human CXCR3b In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX362 Magic™ Mouse CXCR3 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX359 Magic™ Human CXCR3a In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX360 Magic™ Human CXCR3a In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX363 Magic™ Human CXCR4 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX367 Magic™ Mouse CXCR4 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX368 Magic™ Rat CXCR4 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX365 Magic™ Human CXCR4 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Radioligand Binding Assay
S01YF-1122-KX366 Magic™ Human CXCR4 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX369 Magic™ Human CXCR5 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
S01YF-1122-KX371 Magic™ Mouse CXCR5 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX370 Magic™ Human CXCR5 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX372 Magic™ Human CXCR6 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX375 Magic™ Mouse CXCR6 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX374 Magic™ Human CXCR6 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Radioligand Binding Assay
S01YF-1122-KX376 Magic™ Human ACKR3 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX378 Magic™ Human XCR1 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX377 Magic™ Human XCR1 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX379 Magic™ Human XCR1 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Radioligand Binding Assay
S01YF-1122-KX272 Magic™ Human CCRL2 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay

Published Data

Paper Title Chemokines and chemokine receptors during COVID-19 infection
Journal Computational and structural biotechnology journal
Published 2021
Abstract Chemokines play critical roles in the immune response to clear pathogens. However, their excessive release can lead to excessive inflammation. Studies have shown that in COVID-19, chemokines are a potential factor contributing to acute respiratory disease syndrome. In addition, there is evidence revealed that chemokines were directly involved in different stages of SARS-CoV-2 infection. This article reviewed the close association of chemokines and their receptors with the pathogenesis of COVID-19, which was beneficial for the development of possible therapeutic targets for infections.
Result This article summarized the top chemokines associated with COVID-19 progression, including CCL2, CXCL10, and CXCL8, and their importance as potential biomarkers. In addition, the article discussed the chemokine profiles involved in different stages of SARS-CoV-2 infection and their crucial roles in stratifying patients at risk of complications. This could be very beneficial in determining the correct regimen targeting chemokines to avoid complications and reduce mortality. Finally, the investigators have revealed potential targeted therapies against chemokines or their receptors in ongoing related clinical trials. Analysis of chemokines and their receptors at the stage of infection will contribute to the prediction of possible outcomes of disease and the likelihood of complications.

The chemokine profile in COVID-19 patients.Fig.2. The chemokine profile in COVID-19 patients. (Khalil, 2021)

References

  1. Hughes, C. E.; Nibbs, R. J. A guide to chemokines and their receptors. The FEBS journal. 2018; 285(16): 2944-2971.
  2. Khalil, B.A.; et al. Chemokines and chemokine receptors during COVID-19 infection. Computational and structural biotechnology journal. 2021; 19: 976-988.
Note: All of our products are for Research Use Only (RUO). NOT intended for diagnostic, therapeutic or clinical use. We DO NOT offer patients any direct products or services. No products from Creative Biolabs may be resold, modified for resale or used to manufacture commercial products without prior written approval from Creative Biolabs.
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