Potency data for probe GSK620
In vitro potency
| Target name | Target information | Species | Assay description | GSK620 | Publication of assay conditions |
|---|---|---|---|---|---|
| BRD2 | BD1 | Homo sapiens | TR-FRET assay (BRD2 BD1) | IC50 = 25420 nM ± 2591.000 nM (n=13) | PMID: 32193360 |
| BRD2 | BD2 | Homo sapiens | TR-FRET assay (BRD2 BD2) | IC50 = 285 nM ± 20.000 nM (n=20) | PMID: 32193360 |
| BRD3 | BD1 | Homo sapiens | TR-FRET assay (BRD3 BD1) | IC50 = 25802 nM ± 6171.000 nM (n=6) | PMID: 32193360 |
| BRD3 | BD2 | Homo sapiens | TR-FRET assay (BRD3 BD2) | IC50 = 72 nM ± 4.000 nM (n=16) | PMID: 32193360 |
| BRD4 | BD1 | Homo sapiens | TR-FRET assay (BRD4 BD1) | IC50 = 17442 nM ± 1857.000 nM (n=14) | PMID: 32193360 |
| BRD4 | BD2 | Homo sapiens | TR-FRET assay (BRD4 BD2) | IC50 = 81 nM ± 9.000 nM (n=16) | PMID: 32193360 |
| BRDT | BD1 | Homo sapiens | TR-FRET assay (BRDT BD1) | IC50 = 22634 nM ± 2353.000 nM (n=9) | PMID: 32193360 |
| BRDT | BD2 | Homo sapiens | TR-FRET assay (BRDT BD2) | IC50 = 184 nM ± 19.000 nM (n=18) | PMID: 32193360 |
| BRD2 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD1) | pIC50 = 4.6 (n=13) | PMID: 32702236 |
| BRD2 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD2) | pIC50 = 6.5 (n=20) | PMID: 32702236 |
| BRD3 | BD1 | Homo sapiens | BET mutant TR-FRETassay (BRD3 BD1) | pIC50 = 4.6 (n=6) | PMID: 32702236 |
| BRD3 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD3 BD2) | pIC50 = 7.1 (n=16) | PMID: 32702236 |
| BRD4 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD1) | pIC50 = 4.8 (n=14) | PMID: 32702236 |
| BRD4 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD2) | pIC50 = 7.1 (n=16) | PMID: 32702236 |
| BRDT | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD1) | pIC50 = 4.6 (n=9) | PMID: 32702236 |
| BRDT | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD2) | pIC50 = 6.7 (n=18) | PMID: 32702236 |
| BRD2 | BD1 | Homo sapiens | BRD2 BD1 Bromoscan (DiscoverX) | pKd = 4.9 | PMID: 32702236 |
| BRD2 | BD2 | Homo sapiens | BRD2 BD2 Bromoscan (DiscoverX) | pKd = 7.8 | PMID: 32702236 |
| BRD3 | BD1 | Homo sapiens | BRD3 BD1 Bromoscan (DiscoverX) | pKd = 5.1 | PMID: 32702236 |
| BRD3 | BD2 | Homo sapiens | BRD3 BD2 Bromoscan (DiscoverX) | pKd = 7.9 | PMID: 32702236 |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 Bromoscan (DiscoverX) | pKd = 5.6 | PMID: 32702236 |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 Bromoscan (DiscoverX) | pKd = 8.2 | PMID: 32702236 |
| BRDT | BD1 | Homo sapiens | BRDT BD1 Bromoscan (DiscoverX) | pKd = 5.3 | PMID: 32702236 |
| BRDT | BD2 | Homo sapiens | BRDT BD2 Bromoscan (DiscoverX) | pKd = 7.8 | PMID: 32702236 |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 SPR | pKd = 5 | PMID: 32702236 |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 SPR | pKd = 7.3 | PMID: 32702236 |
In cell potency
| Target name | Target information | Species | Assay description | GSK620 | Publication of assay conditions |
|---|---|---|---|---|---|
| CCL2 | whole blood | Homo sapiens | In vitro inhibition of MCP-1 in Lipopolysaccharide-stimulated human whole blood | pIC50 = 6.1 ± 0.200 (n=8) | PMID: 32702236 |
| CCL2 | Peripheral blood mononuclear cell | Homo sapiens | LPS-PBMC assay (MCP-1) | pIC50 = 7.2 ± 0.300 (n=8) | PMID: 32702236 |