Assay Detail
Functional
CHEMBL4005264
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 7.66 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494 | ILOPROST | 4.0 | 1 | 8.62 |
| CHEMBL3893346 | — | — | 1 | 8.48 |
| CHEMBL3926078 | — | — | 1 | 8.47 |
| CHEMBL3935924 | — | — | 1 | 8.41 |
| CHEMBL3932106 | — | — | 1 | 8.28 |
| CHEMBL238804 | SELEXIPAG | 4.0 | 1 | 8.22 |
| CHEMBL3975122 | — | — | 1 | 8.18 |
| CHEMBL3983767 | — | — | 1 | 8.11 |
| CHEMBL3301604 | RALINEPAG | 3.0 | 1 | 8.07 |
| CHEMBL3933704 | — | — | 1 | 8.06 |
| CHEMBL3981509 | — | — | 1 | 8.00 |
| CHEMBL3928729 | — | — | 1 | 7.92 |
| CHEMBL3914174 | — | — | 1 | 7.73 |
| CHEMBL3966307 | — | — | 1 | 7.72 |
| CHEMBL3952237 | — | — | 1 | 7.68 |
| CHEMBL239226 | LASELIPAG | 2.0 | 1 | 7.66 |
| CHEMBL3943791 | — | — | 1 | 7.64 |
| CHEMBL3896580 | — | — | 1 | 7.60 |
| CHEMBL3890685 | — | — | 1 | 7.42 |
| CHEMBL3952439 | — | — | 1 | 7.39 |
| CHEMBL3919269 | — | — | 1 | 7.34 |
| CHEMBL3900038 | — | — | 1 | 7.27 |
| CHEMBL3922000 | — | — | 1 | 7.21 |
| CHEMBL3917503 | — | — | 1 | 6.03 |
| CHEMBL4061744 | — | — | 1 | 5.98 |
| CHEMBL3930990 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494 | ILOPROST | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3893346 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3926078 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3935924 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3932106 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL238804 | SELEXIPAG | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3975122 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3983767 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3301604 | RALINEPAG | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3933704 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3981509 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3928729 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3914174 | — | EC50 | = | 18.5 | nM | 7.73 |
| CHEMBL3966307 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3952237 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL239226 | LASELIPAG | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3943791 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3896580 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3890685 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3952439 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3919269 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3900038 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3922000 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3917503 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4061744 | — | EC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3930990 | — | EC50 | = | 1630.0 | nM | 5.79 |