Assay Detail
Binding
CHEMBL3705226
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, Cat No. 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 dimethylsulfoxide). The SPA assay mixture is incubated for 3 h at room temperature.
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrazole compounds as CRTH2 antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 59 | 9.29 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3690165 | — | — | 1 | 10.00 |
| CHEMBL3690164 | — | — | 1 | 10.00 |
| CHEMBL3690191 | — | — | 1 | 10.00 |
| CHEMBL3690177 | — | — | 1 | 10.00 |
| CHEMBL3690185 | — | — | 1 | 10.00 |
| CHEMBL3639847 | — | — | 1 | 10.00 |
| CHEMBL3690178 | — | — | 1 | 10.00 |
| CHEMBL3690192 | — | — | 1 | 9.70 |
| CHEMBL3690168 | — | — | 1 | 9.70 |
| CHEMBL3685833 | — | — | 1 | 9.70 |
| CHEMBL3690167 | — | — | 1 | 9.70 |
| CHEMBL3690172 | — | — | 1 | 9.70 |
| CHEMBL3685840 | — | — | 1 | 9.70 |
| CHEMBL3690190 | — | — | 1 | 9.70 |
| CHEMBL3690189 | — | — | 1 | 9.70 |
| CHEMBL3690155 | — | — | 1 | 9.70 |
| CHEMBL3690161 | — | — | 1 | 9.70 |
| CHEMBL3690158 | — | — | 1 | 9.70 |
| CHEMBL3685842 | — | — | 1 | 9.70 |
| CHEMBL3685841 | — | — | 1 | 9.70 |
| CHEMBL3690170 | — | — | 1 | 9.52 |
| CHEMBL3690181 | — | — | 1 | 9.52 |
| CHEMBL3690180 | — | — | 1 | 9.52 |
| CHEMBL3685838 | — | — | 1 | 9.52 |
| CHEMBL3685844 | — | — | 1 | 9.52 |
| CHEMBL3690156 | — | — | 1 | 9.52 |
| CHEMBL3690157 | — | — | 1 | 9.52 |
| CHEMBL3690159 | — | — | 1 | 9.52 |
| CHEMBL3690171 | — | — | 1 | 9.52 |
| CHEMBL3690175 | — | — | 1 | 9.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3690165 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3690178 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3639847 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3690185 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3690191 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3690164 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3690177 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3685840 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690168 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685833 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690167 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690172 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690192 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685841 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690190 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690189 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690155 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690161 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690158 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3685842 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3690181 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690180 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3685838 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3685844 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690157 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690159 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690170 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690171 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690156 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3690175 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3690187 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3690186 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3690176 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3685846 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3685832 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3690174 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3685836 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3690163 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3690188 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3685831 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3690162 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3685845 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3685835 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3685834 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3690183 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3690166 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3690184 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3685839 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3685837 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3690173 | — | Ki | = | 2.2 | nM | 8.66 |