Assay

#	Aladdin ID	Assay Type	Description	Organism	Compounds	Reference	BAO Format	Source
1.	ALA3423885	Binding	Agonist activity at CCR2B (unknown origin) at 12.5 uM relative to control	Homo sapiens	1	ALA3421577	single protein format	Scientific Literature
2.	ALA3424021	Binding	Antagonist activity at CCR2B (unknown origin) at 10 uM relative to control	Homo sapiens	1	ALA3421577	single protein format	Scientific Literature
3.	ALA3579778	Binding	Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature	Homo sapiens	27	ALA3576800	single protein format	Scientific Literature
4.	ALA3579779	Binding	Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC	Homo sapiens	18	ALA3576800	single protein format	Scientific Literature
5.	ALA3579946	Binding	Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation	Homo sapiens	1	ALA3576800	single protein format	Scientific Literature
6.	ALA3591341	Binding	Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells at 1 uM incubated for 150 mins by scintillation spectrometry	Homo sapiens	14	ALA3588778	cell-based format	Scientific Literature
7.	ALA3591342	Binding	Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry	Homo sapiens	1	ALA3588778	cell-based format	Scientific Literature
8.	ALA3591343	Functional	Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay	Homo sapiens	15	ALA3588778	cell-based format	Scientific Literature
9.	ALA3706065	Binding	Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and GalphaÂ±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the GalphaÂ±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).		68	ALA3638389	cell-based format	BindingDB Database
10.	ALA3705526	Binding	Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.		10	ALA3638728	assay format	BindingDB Database
11.	ALA3705527	Binding	Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).		52	ALA3638678	cell-based format	BindingDB Database
12.	ALA3758041	Binding	Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay	Homo sapiens	33	ALA3751831	single protein format	Scientific Literature
13.	ALA3758042	Functional	Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux	Homo sapiens	1	ALA3751831	single protein format	Scientific Literature
14.	ALA3758043	Binding	Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis	Homo sapiens	1	ALA3751831	single protein format	Scientific Literature
15.	ALA3758058	Functional	Partial agonist activity at CCR2 in human PBMC assessed as inhibition of calcium flux in absence of MCP1	Homo sapiens	1	ALA3751831	single protein format	Scientific Literature
16.	ALA3772537	Functional	Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay	Homo sapiens	12	ALA3769374	cell-based format	Scientific Literature
17.	ALA3791932	Binding	Displacement of [125I]MCP-1 from human recombinant CCR2 expressed in HEK293 cells assessed as remaining radioligand binding at 10 uM after 60 mins by scintillation counting method relative to control	Homo sapiens	1	ALA3784976	cell-based format	Scientific Literature
18.	ALA856950	Binding	Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells		5	ALA1145994	cell-based format	Scientific Literature
19.	ALA651921	Binding	Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells		2	ALA1145994	cell-based format	Scientific Literature
20.	ALA651922	Binding	Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells: Inactive		1	ALA1145994	cell-based format	Scientific Literature