Assay Detail
Binding
CHEMBL1069759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of[3H]PGD2 from human CRTH2 receptor expressed in african green monkey COS7 cells
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 6.56 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603158 | — | — | 1 | 8.43 |
| CHEMBL601621 | — | — | 1 | 7.62 |
| CHEMBL602322 | — | — | 1 | 7.62 |
| CHEMBL603659 | — | — | 1 | 7.42 |
| CHEMBL600475 | — | — | 1 | 7.40 |
| CHEMBL589502 | — | — | 1 | 7.39 |
| CHEMBL607423 | — | — | 1 | 7.39 |
| CHEMBL597725 | — | — | 1 | 7.31 |
| CHEMBL605351 | — | — | 1 | 7.30 |
| CHEMBL592458 | — | — | 1 | 7.14 |
| CHEMBL596712 | — | — | 1 | 7.08 |
| CHEMBL599176 | — | — | 1 | 7.06 |
| CHEMBL596915 | — | — | 1 | 7.05 |
| CHEMBL590090 | — | — | 1 | 7.03 |
| CHEMBL603658 | — | — | 1 | 7.03 |
| CHEMBL591519 | — | — | 1 | 7.00 |
| CHEMBL598965 | — | — | 1 | 6.89 |
| CHEMBL602925 | — | — | 1 | 6.85 |
| CHEMBL591042 | — | — | 1 | 6.80 |
| CHEMBL591517 | — | — | 1 | 6.80 |
| CHEMBL590395 | — | — | 1 | 6.80 |
| CHEMBL592217 | — | — | 1 | 6.77 |
| CHEMBL591516 | — | — | 1 | 6.77 |
| CHEMBL591984 | — | — | 1 | 6.75 |
| CHEMBL598964 | — | — | 1 | 6.68 |
| CHEMBL591359 | — | — | 1 | 6.68 |
| CHEMBL605138 | — | — | 1 | 6.66 |
| CHEMBL600040 | — | — | 1 | 6.60 |
| CHEMBL597524 | — | — | 1 | 6.51 |
| CHEMBL590309 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603158 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL601621 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL602322 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL603659 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL600475 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL589502 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL607423 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL597725 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL605351 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL592458 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL596712 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL599176 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL596915 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL590090 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL603658 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL591519 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL598965 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL602925 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL591042 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL591517 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL590395 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL592217 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL591516 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL591984 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL591359 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL598964 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL605138 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL600040 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL597524 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL590309 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL603187 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL589175 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL590397 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL599177 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL591119 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL599879 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL603163 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL601278 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL589092 | FENTIAZAC | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL600477 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL602386 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL597118 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL590310 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL599784 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL600261 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL603949 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL592001 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL603869 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL596711 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL596911 | — | IC50 | = | 960.0 | nM | 6.02 |