Assay Detail
Binding
CHEMBL3706252
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorometric Imaging Plate Reader (FLIPR) Assay: Cell Culture Conditions: CHO-K1 cells previously transfected with G-alpha 16 were subsequently transfected with the human CRTH2 receptor and the neomycin resistance gene. Following selection in 800 ug/mL G418 (geneticin), individual clones were assayed for their receptor expression based on staining with an anti human CRTH2 IgG, followed by assaying for their response to 13,14-dihydro-15-keto Prostaglandin D2 (DK-PDG2) (ligand) in the Ca2+ Flux assay. Positive clones were then cloned by limiting dilution cloning. The transfected cells were cultured in Ham's F-12 medium supplemented with 10% fetal bovine serum, 2 mM glutamine, 100 U/mL penicillin/100 ug/mL streptomycin, 200 ug/mL hygromycin B, and 800 ug/mL G418 (geneticin). Cells were harvested with trypsin-EDTA (trypsin-ethylenediaminetetraacetic acid) and counted using ViaCount reagent (from Guava Technologies, Inc. which contains two DNA-binding dyes.
55
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted naphthylacetic acids
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 8.46 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3667662 | — | — | 1 | 10.00 |
| CHEMBL3667608 | — | — | 1 | 9.52 |
| CHEMBL3667653 | — | — | 1 | 9.40 |
| CHEMBL3667639 | — | — | 1 | 9.30 |
| CHEMBL3667609 | — | — | 1 | 9.15 |
| CHEMBL3667648 | — | — | 1 | 9.15 |
| CHEMBL3667631 | — | — | 1 | 9.15 |
| CHEMBL3667637 | — | — | 1 | 9.10 |
| CHEMBL3667638 | — | — | 1 | 9.05 |
| CHEMBL3667645 | — | — | 1 | 9.05 |
| CHEMBL3667646 | — | — | 1 | 9.05 |
| CHEMBL3667613 | — | — | 1 | 9.00 |
| CHEMBL3667632 | — | — | 1 | 8.96 |
| CHEMBL3667617 | — | — | 1 | 8.92 |
| CHEMBL3667618 | — | — | 1 | 8.92 |
| CHEMBL3667655 | — | — | 1 | 8.89 |
| CHEMBL3667612 | — | — | 1 | 8.89 |
| CHEMBL3667647 | — | — | 1 | 8.82 |
| CHEMBL3667651 | — | — | 1 | 8.82 |
| CHEMBL3667641 | — | — | 1 | 8.82 |
| CHEMBL3667642 | — | — | 1 | 8.80 |
| CHEMBL3667621 | — | — | 1 | 8.80 |
| CHEMBL3667652 | — | — | 1 | 8.77 |
| CHEMBL3667650 | — | — | 1 | 8.74 |
| CHEMBL3667624 | — | — | 1 | 8.64 |
| CHEMBL3639664 | — | — | 1 | 8.64 |
| CHEMBL3667633 | — | — | 1 | 8.57 |
| CHEMBL3667644 | — | — | 1 | 8.51 |
| CHEMBL3667611 | — | — | 1 | 8.49 |
| CHEMBL3667654 | — | — | 1 | 8.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3667662 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3667608 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3667653 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3667639 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3667609 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3667648 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3667631 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3667637 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3667638 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3667645 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3667646 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3667613 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3667632 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3667617 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3667618 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3667655 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3667612 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3667647 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3667651 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3667641 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3667642 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3667621 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3667652 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3667650 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3639664 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3667624 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3667633 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3667644 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3667611 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3667654 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3667616 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3667610 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3667649 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3667627 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3667636 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3667620 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3667658 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3667640 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3667659 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3667635 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3667623 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3667622 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3667622 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3667615 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3667626 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL3667643 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3667619 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3667614 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL3667625 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL3667630 | — | IC50 | = | 22.1 | nM | 7.66 |