Assay Detail
Functional
CHEMBL2390624
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CRTh2 receptor (unknown origin) overexpressed in CHOK1 cell membranes assessed as inhibition of [35S]-GTPgammaS binding preincubated for 1 hr followed by 50 nM PGD2 and 0.1 nM [35S]-GTPgammaS addition measured after 2 hrs by liquid scintillation counting analysis
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.46 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2385113 | — | — | 1 | 8.40 |
| CHEMBL2387692 | — | — | 1 | 8.15 |
| CHEMBL2385124 | — | — | 1 | 7.80 |
| CHEMBL2385112 | — | — | 1 | 7.62 |
| CHEMBL2387698 | — | — | 1 | 7.44 |
| CHEMBL2385115 | — | — | 1 | 7.34 |
| CHEMBL2387700 | — | — | 1 | 7.18 |
| CHEMBL2385125 | — | — | 1 | 7.09 |
| CHEMBL2387699 | — | — | 1 | 7.05 |
| CHEMBL2387694 | — | — | 1 | 7.00 |
| CHEMBL560993 | TIMAPIPRANT | 3.0 | 1 | 6.89 |
| CHEMBL2385114 | — | — | 1 | 6.80 |
| CHEMBL2387691 | — | — | 1 | 6.64 |
| CHEMBL2385117 | — | — | 1 | 6.54 |
| CHEMBL2385118 | — | — | 1 | 6.51 |
| CHEMBL2387693 | — | — | 1 | 6.31 |
| CHEMBL2385109 | — | — | 1 | 6.07 |
| CHEMBL2387688 | — | — | 1 | 6.06 |
| CHEMBL2385120 | — | — | 1 | 5.96 |
| CHEMBL2387695 | — | — | 1 | 5.85 |
| CHEMBL2385131 | — | — | 1 | 5.80 |
| CHEMBL2385122 | — | — | 1 | 5.80 |
| CHEMBL2385116 | — | — | 1 | 5.72 |
| CHEMBL2387697 | — | — | 1 | 5.70 |
| CHEMBL2385110 | — | — | 1 | 5.54 |
| CHEMBL2385108 | — | — | 1 | 5.30 |
| CHEMBL2387689 | — | — | 1 | 5.30 |
| CHEMBL2387696 | — | — | 1 | 5.30 |
| CHEMBL2387690 | — | — | 1 | 5.30 |
| CHEMBL2385121 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2385113 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2387692 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2385124 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2385112 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2387698 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2385115 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2387700 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2385125 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2387699 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2387694 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL560993 | TIMAPIPRANT | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2385114 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2387691 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2385117 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2385118 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2387693 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2385109 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL2387688 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL2385120 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2387695 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2385131 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2385122 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2385116 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2387697 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2385110 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2385108 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2387689 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2387696 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2387690 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2385121 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2385123 | — | IC50 | - | — | - | |
| CHEMBL2385111 | — | IC50 | - | — | - | |
| CHEMBL2387687 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2385119 | — | IC50 | - | — | - |