Potency data for probe GSK973 and control GSK943
In vitro potency
| Target name | Target information | Species | Assay description | GSK973 | GSK943 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BRD2 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD1) | pIC50 = 4.4 | PMID: 32832027 | |
| BRD2 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD2) | pIC50 = 7.5 | PMID: 32832027 | |
| BRD3 | BD1 | Homo sapiens | BET mutant TR-FRETassay (BRD3 BD1) | pIC50 = 4.5 | PMID: 32832027 | |
| BRD3 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD3 BD2) | pIC50 = 7.8 | PMID: 32832027 | |
| BRD4 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD1) | pIC50 = 4.6 ± 0.100 (n=19) | PMID: 32832027 | |
| BRD4 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD2) | pIC50 = 7.8 ± 0.200 (n=16) | PMID: 32832027 | |
| BRDT | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD1) | pIC50 = 4.5 | PMID: 32832027 | |
| BRDT | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD2) | pIC50 = 7.4 | PMID: 32832027 | |
| BRD2 | BD1 | Homo sapiens | BRD2 BD1 Bromoscan (DiscoverX) | pKd = 5.3 | PMID: 32832027 | |
| BRD2 | BD2 | Homo sapiens | BRD2 BD2 Bromoscan (DiscoverX) | pKd = 8.3 | PMID: 32832027 | |
| BRD3 | BD1 | Homo sapiens | BRD3 BD1 Bromoscan (DiscoverX) | pKd = 5.2 | PMID: 32832027 | |
| BRD3 | BD2 | Homo sapiens | BRD3 BD2 Bromoscan (DiscoverX) | pKd = 8.5 | PMID: 32832027 | |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 Bromoscan (DiscoverX) | pKd = 5.6 | PMID: 32832027 | |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 Bromoscan (DiscoverX) | pKd = 8.7 | PMID: 32832027 | |
| BRDT | BD1 | Homo sapiens | BRDT BD1 Bromoscan (DiscoverX) | pKd = 5.4 | PMID: 32832027 | |
| BRDT | BD2 | Homo sapiens | BRDT BD2 Bromoscan (DiscoverX) | pKd = 8.3 | PMID: 32832027 | |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 SPR | Kd > 3 µM | PMID: 32832027 | |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 SPR | Kd = 34 nM | PMID: 32832027 | |
| BRD4 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD1) | pIC50 = 4.3 | PMID: 32832027 | |
| BRD4 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD2) | pIC50 = 5.1 | PMID: 32832027 |
In cell potency
| Target name | Target information | Species | Assay description | GSK973 | GSK943 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| CCL2 | whole blood | Homo sapiens | In vitro inhibition of MCP-1 in Lipopolysaccharide-stimulated human whole blood | pIC50 = 7.3 | PMID: 32832027 |