Potency data for probe T-10430 and control T-10404
In vitro potency
| Target name | Target information | Species | Assay description | T-10430 | T-10404 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| LTB4R2 | CHO-K1 cells | Homo sapiens | Tag-lite displacement assay (LTB4R2): Uses a fluorescent BLT2 ligand; HTRF-based | IC50 = 31 nM | PMID: 34995452 |
In cell potency
| Target name | Target information | Species | Assay description | Compound conc. | T-10430 | T-10404 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| LTB4R2 | CHO-K1 cells overexpressing LTB4R2 and GNA | Homo sapiens | cAMP assay : cAMP HIRANGE kit (62AM6PEx Cisbio Bioassays, Codolet, France) | EC50 = 0.51 nM | EC50 = 560 nM | PMID: 39803894 | |
| LTB4R2 | CHO-K1 cells | Homo sapiens | IP-One assay (LTB4R2): The accumulation of IP-1 as a downstream effect of GPCR activation was detected in a displacement assay based on HTRF between FRET acceptor coupled IP-1 and terbium cryptate coupled anti-IP-1 antibody (IP-One assay kit, revvity) | up to 50 µM | EC50 = 19.4 nM | EC50 > 100 µM | PMID: 39803894 |
| LTB4R | CHO-K1 cells co-expressing BLT1 and GNA15/16 | Homo sapiens | IP-One assay (LTB4R), agonist mode | up to 50 µM | EC50 > 50 µM | PMID: 39803894 | |
| AGTR1 | CHO-K1 cells co-expressing AT1 and GNA14 | Homo sapiens | IP-One assay (AGTR1), agonist mode | up to 50 µM | EC50 > 50 µM | PMID: 39803894 | |
| AGTR1 | CHO-K1 cells co-expressing AT1 and GNA14 | Homo sapiens | IP-One assay (AGTR1), antagonist mode: vs. 10 nM Val5-Angiotensin II | up to 50 µM | EC50 > 50 µM | PMID: 39803894 | |
| LTB4R | CHO-K1 cells co-expressing BLT1 and GNA15/16 | Homo sapiens | IP-One assay (LTB4R), antagonist mode: vs. 300 nM LTB4 | up to 50 µM | EC50 > 50 µM | PMID: 39803894 |