Assay Detail
Binding
CHEMBL3705511
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Binding Assay: The CRTH2 receptor binding assay is performed in a scintillation proximity assay (SPA) format with the radioligand [3H]-PGD2 (Perkin Elmer, NET616000MC). CHO-K1-hCRTH2 cell membranes are again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well). The SPA assay is set up in 96 well microtiter plates (Perkin Elmer, CatNo. 6005040) in SPA incubation buffer with a final volume of 200 ul per well and final concentration of 50 mM Tris-HCl, 10 mM MgCl2, 150 mM NaCl, 1 mM EDTA pH 7.4, 0.1% bovine serum albumin). The SPA assay mixture contains 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (GE Healthcare, RPNQ-0001, 0.3 mg/well), 40 ul of [3H]-PGD2 diluted in SPA buffer to a final concentration of 1 nM (50 000 dpm) and 20 ul of the test compound (dissolved in dimethylsulfoxid).
215
Total Activities
214
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1-hCRTH2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrazole compounds as CRTH2 antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 215 | 7.99 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181751 | — | — | 1 | 10.00 |
| CHEMBL3685933 | — | — | 1 | 10.00 |
| CHEMBL3685949 | — | — | 1 | 10.00 |
| CHEMBL3685952 | — | — | 1 | 10.00 |
| CHEMBL3686053 | — | — | 1 | 10.00 |
| CHEMBL3685926 | — | — | 1 | 10.00 |
| CHEMBL3685864 | — | — | 1 | 9.70 |
| CHEMBL3685885 | — | — | 1 | 9.70 |
| CHEMBL3685891 | — | — | 1 | 9.70 |
| CHEMBL3685924 | — | — | 1 | 9.70 |
| CHEMBL3685925 | — | — | 1 | 9.70 |
| CHEMBL3685936 | — | — | 1 | 9.70 |
| CHEMBL3685890 | — | — | 1 | 9.60 |
| CHEMBL3685943 | — | — | 1 | 9.52 |
| CHEMBL3685967 | — | — | 1 | 9.52 |
| CHEMBL3685921 | — | — | 1 | 9.40 |
| CHEMBL3685898 | — | — | 1 | 9.30 |
| CHEMBL3685935 | — | — | 1 | 9.30 |
| CHEMBL3685944 | — | — | 1 | 9.30 |
| CHEMBL3686017 | — | — | 1 | 9.30 |
| CHEMBL3685930 | — | — | 1 | 9.22 |
| CHEMBL3685932 | — | — | 1 | 9.22 |
| CHEMBL3685947 | — | — | 1 | 9.22 |
| CHEMBL3685977 | — | — | 1 | 9.22 |
| CHEMBL3685894 | — | — | 1 | 9.15 |
| CHEMBL3685920 | — | — | 1 | 9.15 |
| CHEMBL3685889 | — | — | 1 | 9.12 |
| CHEMBL3685910 | — | — | 1 | 9.10 |
| CHEMBL3685916 | — | — | 1 | 9.10 |
| CHEMBL3685970 | — | — | 1 | 9.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181751 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3685926 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3685933 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3685949 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3686053 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3685952 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3685924 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685925 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685864 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685891 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685885 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685936 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685890 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL3685943 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3685967 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3685921 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3685898 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3686017 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3685944 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3685935 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3685930 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3685977 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3685947 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3685932 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3685894 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3685920 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3685889 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL3685916 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3685910 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3685970 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3685973 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3686003 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3685922 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3685886 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3685863 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3685979 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3685968 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3685917 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3685975 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3685914 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3685888 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3685892 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3686055 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3685923 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3685976 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3685931 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3685915 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3685983 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3685899 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3685966 | — | Ki | = | 2.2 | nM | 8.66 |