ccr1

CCR1 antagonist 6 is a CCR1 antagonist (IC50: 3 nM).

CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 (CCR1) antagonist with an IC50 of 4 nM [1].

CCX354 (CCR1 antagonist 1) is a potent small molecule CCR1 antagonist with anti-inflammatory activity for the treatment of rheumatoid arthritis.

MLN-3897 (CCR1 antagonist 10) is an orally active antagonist of CCR1 with a Ki of 2.3 nM for 125I-MIP-1α binding to THP-1 cell membranes. MLN-3897 inhibits Akt signaling and MM cell survival and proliferation.

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). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

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

BI 639667, a compound belonging to the azaindazole class, functions as a potent inhibitor of CCR1 activity, a property quantitatively demonstrated by its half-maximal inhibitory concentration (IC50) of 1.8 nM in standardized calcium flux assays.

YM022 is a highly effective and selective gastrin/cholecystokinin (CCK)-B receptor antagonist. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively.

AZD-4818 (CCR1 antagonist) is a chemokine CCR1 antagonist for the treatment of chronic obstructive pulmonary disease.

NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

CCR1 antagonist 9 (compound 19e) is a selective CCR1 antagonist based on aziridine. It exhibits an IC50 of 6.8 nM for CCR1 inhibition in calcium flux assays and an IC50 of 30 μM for hERG.

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with a Ki of 1 nM for human CCR1, exhibiting 250-fold selectivity over CCR2, CCR5, and CXCR4.

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.

CCR1/5/8 activator 1 is a cytoplasmic phospholipase A inhibitor with antifungal activity.

CCR1 antagonist13 is a selective small molecule antagonist of CCR1.

CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with IC50 values of 0.03 μM for hCCR1, 0.58 μM for mCCR1, and 0.32 μM for rCCR1. This compound is useful for studying rheumatoid arthritis and other related inflammatory diseases.

CCR1 antagonist12 (Compound 12) is an antagonist of CCR1, exhibiting an IC50 of 3 nM against human CCR1. It inhibits the chemotaxis through pores induced by CCL3, with an IC50 of 0.009 µM. Additionally, CCR1 antagonist12 demonstrates favorable pharmacokinetic properties in a rat model.

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

BMS-817399 is an orally active antagonist of CCR1 with IC50s of binding affinity and chemotaxis inhibition potencies and can be used in studies about rheumatoid arthritis.

CCR-11 is a tannin-containing derivative with antimicrobial activity. CCR-11 inhibits the proliferation of B. subtilis and HeLa cells. CCR-11 inhibits bacterial proliferation and bacterial cytoplasmic division by inhibiting FtsZ assembly and GTPase activity. CCR-11 has potential anti-tumor activity and can be used to study breast cancer and pediatric myelodysplasia.

BX 513 hydrochloride (VUF 2274 HCl) is a selective CCR1 antagonist (Ki=0.04 µM) that concentration-dependently inhibits CCL18-induced acidification in THP-1 monocytes and suppresses RANTES- and CCL18-induced chemotaxis in peripheral blood mononuclear cells (PBMCs).

CP 481715 is an effective selective CCR1 antagonist with potential therapeutic significance for inflammatory diseases.

BI-6901 is a CCR10 antagonist. In a mouse model of DNFB exposure hypersensitivity, BI 6901 displays its anti-inflammatory response in a dose-dependent manner.