Target & Activity
| Target | Activity | Value |
|---|---|---|
| MIP-1α-CCR5 | 1 nM (IC50, in CHO/CCR5 cells) | |
| MIP-1β-CCR5 | 1 nM (IC50, in CHO/CCR5 cells) | |
| RANTES-CCR5 | 1.4 nM (IC50, in CHO/CCR5 cells) | |
| MCP-1-CCR2b | 27 nM (IC50, in CHO/CCR5 cells) | |
| R5 HIV-1 (Ba-L) | 1.2 nM (EC50, in MAGI-CCR5 cells) | |
| R5 HIV-1 (KK) | 1.6 nM (EC50, in PBMCs) | |
| R5 HIV-1 (HHA) | 3.2 nM (EC50, in PBMCs) | |
| R5 HIV-1 (CTV) | 3.5 nM (EC50, in PBMCs) | |
| R5 HIV-1 (Ba-L) | 3.7 nM (EC50, in PBMCs) | |
| R5 HIV-1 (Ba-L) | 5.7 nM (EC90, in MAGI-CCR5 cells) | |
| R5 HIV-1 (HHA) | 7.5 nM (EC90, in PBMCs) | |
| R5 HIV-1 (Ba-L) | 12.8 nM (EC90, in PBMCs) | |
| R5 HIV-1 (KK) | 20.8 nM (EC90, in PBMCs) | |
| R5 HIV-1 (CTV) | 27 nM (EC90, in PBMCs) | |
| mCXCR3 | 369 nM (IC50, in PBMCs) |
15 targets · Scroll to view more
Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| HEK-293T | EC50 | 7 nM | Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay | [PMID: 28463783] |
| MOLT-4 | IC50 | 7.9 nM | Antagonist activity at human CCR5 receptor expressed in MOLT4/CCR5 cells assessed as inhibition of CCL5-induced intracellular calcium mobilization by spectrophotometry | [PMID: 21820898] |
| PC-3 | IC50 | 37.85 μM | Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay | [PMID: 24731275] |
| U2OS | IC50 | 23 μM | Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence ba | [PMID: 25766632] |
| U2OS | IC50 | 6 nM | Antagonist activity at human TEV cleavage site-linked CCR5 expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL3-induced beta-arrestin recruitment incubated for 30 mins followed by CCL3 stimulation and measure | [PMID: 31742400] |