# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
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1. | ALA3705172 | Binding | Radio Ligand Binding Assay: Serial dilutions of compounds (stock in 10 mM DMSO) are prepared by first diluting the compounds in DMSO followed by a 1:50 dilution into assay buffer (10 mM HEPES, pH 8.0, 100 mM NaCl, 5 mM MgCl2, 1 mM CaCl2, 0.5% fatty acid-free BSA, 0.05% Tween-20). The radioligand [3H]4 (example 39) (specific activity 1500 GBq/mmol) is diluted directly into the assay buffer immediately before use to obtain a 20 nM solution. The desired amount of membranes (20 μg/well) is diluted with assay buffer. 50 μL of pre-diluted compound and 50 μL of [3H]4 (example 39) is placed into the bottom of a 96-well well plate. 100 μL of the membrane-suspension is added and the plate stirred for 60 minutes. The reaction is stopped by transfer onto the filter of a 96-well GF/C filter plate (soaked for 1 hour in 0.25% PEI) using a cell harvester. | Homo sapiens | 37 | ALA3638598 | assay format | BindingDB Database | |
2. | ALA3734137 | Functional | Antagonist activity at human GPR4 expressed in KJMGER8 cells assessed as inhibition of 17beta-estradiol-induced response after 6 hrs by steady glo luciferase reporter assay | Homo sapiens | 9 | ALA3727352 | cell-based format | Patent Bioactivity Data | |
3. | ALA3811134 | Functional | Antagonist activity at N-terminal HA-tagged GPR4 (unknown origin) expressed in HEK293 cells assessed as pH dependent cAMP response element-driven transcriptional activity ratio at 10 uM at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay relative to untreated control | Homo sapiens | 18 | ALA3808277 | cell-based format | Scientific Literature | |
4. | ALA3813382 | Functional | Antagonist activity at N-terminal HA-tagged GPR4 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent cAMP response element-driven transcriptional activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay | Homo sapiens | 7 | ALA3808277 | cell-based format | Scientific Literature | |
5. | ALA4044420 | Functional | Antagonist activity at human GPR4 expressed in human HeLa cells assessed as inhibition of pH-induced cAMP accumulation preincubated for 15 mins followed by cAMP addition measured after 60 mins by HTRF method | Homo sapiens | 22 | ALA4043105 | cell-based format | Scientific Literature | |
6. | ALA4044450 | Functional | Antagonist activity at human GPR4 expressed in African green monkey COS7 cells assessed as inhibition of pH 6.5-induced cAMP accumulation at 5 uM after 30 mins by HTRF method relative to control | Homo sapiens | 2 | ALA4043105 | cell-based format | Scientific Literature | |
7. | ALA4044451 | Functional | Antagonist activity at human GPR4 expressed in African green monkey COS7 cells assessed as inhibition of pH 6.5-induced cAMP accumulation after 30 mins by HTRF method | Homo sapiens | 2 | ALA4043105 | cell-based format | Scientific Literature | |
8. | ALA4178741 | Functional | Antagonist activity at human GPR4 expressed in human HeLa cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins by HTRF assay | Homo sapiens | 13 | ALA4177561 | cell-based format | Scientific Literature | |
9. | ALA4178757 | Functional | Antagonist activity at human GPR4 expressed in human HeLa cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins in presence of 40% rat plasma by HTRF assay | Homo sapiens | 3 | ALA4177561 | cell-based format | Scientific Literature | |
10. | ALA4178758 | Binding | Ratio of IC50 for human GPR4 expressed in human HeLa cells in presence of 40% rat plasma to IC50 for human GPR4 expressed in human HeLa in absence of 40% rat plasma | Homo sapiens | 3 | ALA4177561 | cell-based format | Scientific Literature | |
11. | ALA4407313 | Functional | Positive allosteric modulation of human GPR4 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production at higher concentration in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measured after 20 to 30 mins in presence of PDE inhibitor Ro 20-1724 by luciferase-glo reporter gene assay | Homo sapiens | 4 | ALA4406806 | cell-based format | Scientific Literature | |
12. | ALA4407338 | Functional | Positive allosteric modulation of human GPR4 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measured after 20 to 30 mins in presence of PDE inhibitor Ro 20-1724 by luciferase-glo reporter gene assay | Homo sapiens | 3 | ALA4406806 | cell-based format | Scientific Literature | |
13. | ALA4883452 | Binding | PRESTO-Tango GPCRome screening (GPR4) | 1 | ALA4507309 | single protein format | Donated Chemical Probes - SGC Frankfurt |