Potency data for probe GSK046
In vitro potency
| Target name | Target information | Species | Assay description | GSK046 | Publication of assay conditions |
|---|---|---|---|---|---|
| BRD2 | BD1 | Homo sapiens | TR-FRET assay (BRD2 BD1) | IC50 = 10965 nM (n=1) | PMID: 32193360 |
| BRD2 | BD2 | Homo sapiens | TR-FRET assay (BRD2 BD2) | IC50 = 264 nM ± 53.000 nM (n=9) | PMID: 32193360 |
| BRD3 | BD1 | Homo sapiens | TR-FRET assay (BRD3 BD1) | IC50 = 36317 nM ± 1182.000 nM (n=2) | PMID: 32193360 |
| BRD3 | BD2 | Homo sapiens | TR-FRET assay (BRD3 BD2) | IC50 = 98 nM ± 6.000 nM (n=8) | PMID: 32193360 |
| BRD4 | BD1 | Homo sapiens | TR-FRET assay (BRD4 BD1) | IC50 = 70558 nM ± 51783.000 nM (n=3) | PMID: 32193360 |
| BRD4 | BD2 | Homo sapiens | TR-FRET assay (BRD4 BD2) | IC50 = 49 nM ± 4.000 nM (n=12) | PMID: 32193360 |
| BRDT | BD1 | Homo sapiens | TR-FRET assay (BRDT BD1) | IC50 > 50119 nM (n=8) | PMID: 32193360 |
| BRDT | BD2 | Homo sapiens | TR-FRET assay (BRDT BD2) | IC50 = 214 nM ± 53.000 nM (n=8) | PMID: 32193360 |
| BRD2 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD1) | pIC50 = 5 | PMID: 32691591 |
| BRD2 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD2) | pIC50 = 6.6 ± 0.200 (n=9) | PMID: 32691591 |
| BRD3 | BD1 | Homo sapiens | BET mutant TR-FRETassay (BRD3 BD1) | pIC50 = 4.4 ± 0.010 (n=2) | PMID: 32691591 |
| BRD3 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD3 BD2) | pIC50 = 7 ± 0.080 (n=8) | PMID: 32691591 |
| BRD4 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD1) | pIC50 = 4.2 ± 0.440 (n=3) | PMID: 32691591 |
| BRD4 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD2) | pIC50 = 7.3 ± 0.130 (n=12) | PMID: 32691591 |
| BRDT | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD1) | pIC50 = 4.3 (n=8) | PMID: 32691591 |
| BRDT | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD2) | pIC50 = 6.7 ± 0.250 (n=8) | PMID: 32691591 |
| BRD2 | BD1 | Homo sapiens | BRD2 BD1 Bromoscan (DiscoverX) | Kd = 1621 nM | PMID: 32691591 |
| BRD2 | BD2 | Homo sapiens | BRD2 BD2 Bromoscan (DiscoverX) | Kd = 35 nM | PMID: 32691591 |
| BRD3 | BD1 | Homo sapiens | BRD3 BD1 Bromoscan (DiscoverX) | Kd = 2082 nM | PMID: 32691591 |
| BRD3 | BD2 | Homo sapiens | BRD3 BD2 Bromoscan (DiscoverX) | Kd = 32 nM | PMID: 32691591 |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 Bromoscan (DiscoverX) | Kd = 769 nM | PMID: 32691591 |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 Bromoscan (DiscoverX) | Kd = 9 nM | PMID: 32691591 |
| BRDT | BD1 | Homo sapiens | BRDT BD1 Bromoscan (DiscoverX) | Kd = 2454 nM | PMID: 32691591 |
| BRDT | BD2 | Homo sapiens | BRDT BD2 Bromoscan (DiscoverX) | Kd = 15 nM | PMID: 32691591 |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 SPR | Kd > 10 µM | PMID: 32691591 |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 SPR | Kd = 30 nM | PMID: 32691591 |
In cell potency
| Target name | Target information | Species | Assay description | GSK046 | Publication of assay conditions |
|---|---|---|---|---|---|
| CCL2 | whole blood | Homo sapiens | In vitro inhibition of MCP-1 in Lipopolysaccharide-stimulated human whole blood | pIC50 = 6.5 ± 0.100 (n=6) | PMID: 32691591 |
| CCL2 | Peripheral blood mononuclear cell | Homo sapiens | LPS-PBMC assay (MCP-1) | pIC50 = 7.5 ± 0.300 (n=4) | PMID: 32691591 |