CCR

ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations.

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

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

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

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).

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

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

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

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

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

Zn-DPA-maytansinoid 1 targets checkpoints, shrinks tumors, and heats TME.

Met-RANTES (human) acetate is the acetate salt form of Met-RANTES (human). It acts as an antagonist for CCR1 and CCR5 receptors. This compound inhibits the human chemokines MIP-1α and MIP-1β, with respective IC50 values of 5 and 2 nM. Additionally, Met-RANTES (human) acetate reduces bone destruction and alleviates adjuvant-induced arthritis (AIA) in rats.

MLN-3897 TFA is a potent CCR1 antagonist that inhibits the binding of 125I-MIP-1α to THP-1 cell membranes.

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

CAP-100 is a monoclonal antibody targeting CCR7. It neutralizes the ligand binding site and signaling of CCR7. This compound effectively inhibits migration, extravasation, homing, and survival in chronic lymphocytic leukemia (CLL) samples induced by CCR7. CAP-100 can mediate potent tumor cell killing through host immune mechanisms and exhibits favorable toxicity profiles in related hematopoietic cell subsets. It is involved in research on antitumor activity and diseases like chronic lymphocytic leukemia (CLL).

Orally active CCR4 antagonist with piperidinyl-azetidine; IC50: 22 nM (calcium flux), 50 nM (CTX); antitumor effects.

PF-232798 is a second generation oral CCR5 antagonist with potent broad-spectrum anti-HIV-1 activity.

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).

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.

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