ccr1

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

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

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.

CCR1 antagonist 9 is an effective and selective CCR1 antagonist (IC50: 6.8 nM in calcium flux assay).

CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist that acts on hCCR1 (IC50: 0/.03 μM), mCCR1 (IC50: 0.58 μM), rCCR1 (IC50: 0.32 μM). 11 hydrochloride can be used to study rheumatoid arthritis and other related inflammatory diseases.

CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay).

CCR1 antagonist 7 (compound 16r) is an antagonist of chemokine receptor 1 (CCR1) with an IC 50 of 4 nM [1].

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

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.

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

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

Trans-J-113863 serves as a potent antagonist of chemokine receptors CCR1 and CCR3, effectively inhibiting MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, with respective half-maximal inhibitory concentrations (IC50) of 9.57 nM and 93.8 nM [1] [2].

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.

Cis-J-113863 is a competitive antagonist for the chemokine receptor 1 (CCR1), demonstrating inhibitory concentration 50 (IC50) values of 0.9 nM for human CCR1 receptors and 5.8 nM for mouse CCR1 receptors, respectively [1].

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

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

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

BMS-457 is a potent, CCR1-selective antagonist.

chemokine CCR1 and CCR3 receptor antagonist

BAY-3153 is a selective CCR1 ( C-C motif chemokine receptor 1 ) antagonist (human IC 50 =3 nM ; rat IC 50 =11 nM ; mice IC 50 =81 nM) .

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.

MLN-3897 citrate is a C-C Motif Chemokine Receptor 1 (CCR1) antagonist potentially for the treatment of multiple sclerosis and rheumatoid arthritis.

BX-513 HCl is a selective CCR1 receptor antagonist.

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

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent CCR9 antagonist. It effectively inhibits CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells, exhibiting IC50 values of 5.4 nM and 3.4 nM, respectively. Demonstrating high selectivity, Vercirnon sodium does not significantly affect CCR1-12 or CX3CR1-7, with IC50 values exceeding 10 µM for these receptors. Additionally, it inhibits CCL25-directed chemotaxis equally well in both CCR9 splice variants, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively.

RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).