#	Aladdin ID	Assay Type	Description	Organism	Compounds	Reference	BAO Format	Source
1.	ALA3423914	Binding	Agonist activity at CCR5 (unknown origin) at 12.5 uM relative to control	Homo sapiens	1	ALA3421577	single protein format	Scientific Literature
2.	ALA3424053	Binding	Antagonist activity at CCR5 (unknown origin) at 10 uM relative to control	Homo sapiens	1	ALA3421577	single protein format	Scientific Literature
3.	ALA3579780	Binding	Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs	Homo sapiens	9	ALA3576800	cell-based format	Scientific Literature
4.	ALA3579947	Binding	Antagonist activity against CCR5 in whole blood (unknown origin) assessed as reduction in CD11b upregulation	Homo sapiens	1	ALA3576800	single protein format	Scientific Literature
5.	ALA3606534	Functional	Antagonist activity at CCR5 (unknown origin) expressed in human MOLT4 cells assessed as inhibition of CCL5-induced calcium mobilization after 1 hr	Homo sapiens	17	ALA3603778	cell-based format	Scientific Literature
6.	ALA3610409	Binding	Inhibition of CCR5 assessed as reduction in fusion of effector cells expressing JRFL envelope (CCR5-tropic/CD4-dependent) with human HeLa-C14 target cells expressing CD4, CCR5, and CXCR4) by luciferase readout	Homo sapiens	1	ALA3608277	cell-based format	Scientific Literature
7.	ALA3610410	Binding	Displacement of [125I]-MIP-1beta form CCR5 (unknown origin) at 100 uM	Homo sapiens	1	ALA3608277	single protein format	Scientific Literature
8.	ALA3610411	Binding	Displacement of [125I]-MIP-1beta form CCR5 (unknown origin) at 1 mM	Homo sapiens	1	ALA3608277	single protein format	Scientific Literature
9.	ALA3610412	Binding	Displacement of [125I]-MIP-1beta form CCR5 (unknown origin)	Homo sapiens	1	ALA3608277	single protein format	Scientific Literature
10.	ALA3635207	Functional	Antagonist activity at CCR5 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of CCl5-induced calcium release at 1 uM by FLIPR assay	Homo sapiens	2	ALA3632509	cell-based format	Scientific Literature
11.	ALA3706103	Binding	Radioligand Binding Assay: Afterwards, the pharmacological profile of bivalent ligand 1 at the chemokine receptor CCR5 was characterized similarly. The competitive radioligand binding assay was conducted in CCR5 rhesus macaque membrane preparations from Chem-1 cells. Monovalent ligand 3 and compound 4, an analogue of maraviroc, were tested along under the same condition. Introduction of the 4-NH2 group onto the phenyl ring of maraviroc, as seen in compound 4, caused approximately 65-fold decrease in the binding affinity, compared to maraviroc. The decrease of the binding affinity was even more profound for bivalent ligand 1 and monovalent ligand 3, as their Ki values dropped to submicromolar range, respectively.		4	ALA3638635	cell membrane format	BindingDB Database
12.	ALA3706104	Functional	Flux Assay: Then the Ca2+ functional activity of bivalent ligand 1 was evaluated in the Gqi5 transfected CCR5-MOLT-4 cells as described in the literature.3 As expected, no CCR5 agonism was detected for the bivalent ligand 1 (data not shown). In the RANTES induced Ca2+ flux inhibition assay (Table 3), the bivalent ligand 1 was approximately 60-fold less potent than maraviroc. A more significant potency decrease (nearly 300 times) was observed for the monovalent ligand 3, compared to maraviroc. In order to figure out the possible reasons for such a dramatic drop of their potency, two analogues (4 and 5, FIG. 14) of mavaviroc carrying gradient steric hindrance characters at the same substitution position were evaluated under the same condition. Compound 4 showed a modest reduction of the potency (Table 2). However, the inhibition potency of the N-t-Boc protected analogue 5 dropped to micromolar (IC50=1.57+/-0.18 uM). It thus appeared that steric hindrance may play an essential role.		4	ALA3638635	assay format	BindingDB Database
13.	ALA3802810	Binding	Inhibition of human recombinant CCR5 encoding an HIV-1-longterminal-repeat-regulated beta-galactosidase reporter gene expressed in human HeLaP4 cells assessed as reduction of interaction with HIV-1 gp160 expressed in CHO cells by cell-cell fusion assay	Homo sapiens	1	ALA3797033	cell-based format	Scientific Literature
14.	ALA656492	Functional	Antagonistic activity against monkey C-C chemokine receptor type 5.	Cercopithecidae	26	ALA1149140	assay format	Scientific Literature
15.	ALA656493	Functional	Antagonistic activity against monkey C-C chemokine receptor type 5; nd denotes not determined	Cercopithecidae	8	ALA1149140	assay format	Scientific Literature
16.	ALA656494	Functional	Antagonistic activity against monkey chemokine receptor C-C chemokine receptor type 5; nd denotes not determined	Cercopithecidae	2	ALA1149140	assay format	Scientific Literature
17.	ALA656495	Functional	Antagonistic activity against monkey chemokine receptor CCR5; nd denotes not determined	Cercopithecidae	1	ALA1149140	assay format	Scientific Literature
18.	ALA873192	Binding	Ability of compound to inhibit [125I]-labeled RANTES binding to the CCR5 receptor expressed in membrane preparations from CHO cells	Cricetulus griseus	1	ALA1136572	cell-based format	Scientific Literature
19.	ALA656496	Binding	Ability to displace [125 I]-MIP-1alpha from C-C chemokine receptor type 5 expressed on CHO cell membranes	Homo sapiens	8	ALA1134084	cell-based format	Scientific Literature
20.	ALA654032	Binding	Ability to inhibit binding of [125I]-MIP-1 alpha to C-C chemokine receptor type 5 in Chinese hamster ovary (CHO) cell membranes		8	ALA1134148	assay format	Scientific Literature