CCR

Leronlimab (PRO 140), a humanized IgG4 monoclonal antibody, targets CCR5 to combat HIV and cancer.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM).

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations.

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

Mogamulizumab is a monoclonal antibody targeting CC chemokine receptor 4 with anticancer effects, used in ATLL and CTCL studies.

AZ084 is a potent, selective, allosteric, and oral active CCR8 antagonist (Ki: 0.9 nM). It has the potential to treat asthma.

MK-0812 Succinate is an effective and selective CCR2 antagonist.

INCB-9471 is a CCR5 antagonist with anti-HIV activity and inhibits the interaction between HIV-1 gp120.

Bertilimumab (CAT 213; iCo-008), humanized anti-eotaxin-1 mAb, inhibits eosinophil chemotaxis/activation for allergic disease research.

VZMC013 is a potent chemical probe targeting the MOR-CCR5 heterodimer, effectively inhibiting HIV-1 entry exacerbated by opioid compounds. It exhibits nanomolar binding affinity to both MOR and CCR5, inhibits CCL5-activated calcium mobilization, and significantly enhances anti-HIV-1BaL activity compared to previously reported bivalent ligands. In TZM-bl cells co-expressing CCR5 and MOR, VZMC013 demonstrates greater inhibition of viral infection than in cells expressing only CCR5. Additionally, VZMC013 blocks HIV-1 entry into peripheral blood mononuclear cells (PBMC) in a concentration-dependent manner and more effectively inhibits opioid-accelerated HIV-1 entry in phytohemagglutinin-activated PBMC than in opioid-free environments.

INCB3344 is a potent CCR2 antagonist. INCB3344 R-isomer is the R-isomer of INCB3344.

BMS-753426 is a potent and orally bioavailable antagonist of CCR2 .

Orally active CCR4 antagonist 3 hydrochloride with potent selectivity, IC50s: 22/50 nM; has antitumor properties.

TBK1degrader-4 (Compound 30) is a molecular glue degrader targeting TBK1. It effectively inhibits cyst growth, reduces inflammation, and lowers levels of pro-inflammatory factors such as Ccl2, IFNβ, and IL-6. TBK1degrader-4 shows potential for research in autosomal dominant polycystic kidney disease (ADPKD).

PROTAC CCR9 Degrader 1 is a PROTAC-based degrader specifically targeting CCR9. It functions by recruiting the VHL E3 ligase, leading to the ubiquitination and proteasomal degradation of CCR9, thereby reducing its intracellular levels. The compound has a Ki value of 78.0 nM for human CCR9. Additionally, PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the allosteric site within CCR9 and is applicable in research related to Crohn's disease.

INCB 3284 dimesylate: oral CCR2 antagonist, blocks MCP-1/hCCR2 binding (IC50: 3.7 nM), potential in acute liver failure research.

Aplaviroc, a potent CCR5 inhibitor, binds selectively, blocking HIV entry and specific monoclonal antibody attachment in vitro.

GSK163929 (compound 122) is an orally active CCR5 antagonist with anti-HIV properties and demonstrates low inhibitory potency against hEGR. Administered at a dosage of 2000 mg/kg/day (i.v., 7 d), it shows no adverse effects in rats, and at 250 mg/kg/day (i.v., 7 d), it is similarly non-toxic in dogs.