Potency data for probe GSK789 and control GSK791
In vitro potency
| Target name | Target information | Species | Assay description | GSK789 | GSK791 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BRD2 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD1) | pIC50 = 7 | pIC50 = 5.6 ± 0.010 (n=2) | PMID: 32691589 |
| BRD2 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD2) | pIC50 = 4.7 | pIC50 = 4.8 | PMID: 32691589 |
| BRD3 | BD1 | Homo sapiens | BET mutant TR-FRETassay (BRD3 BD1) | pIC50 = 6.8 | pIC50 = 5.4 (n=2) | PMID: 32691589 |
| BRD3 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD3 BD2) | pIC50 = 4.7 | pIC50 = 4.7 ± 0.090 (n=2) | PMID: 32691589 |
| BRD4 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD1) | pIC50 = 7.5 ± 0.260 (n=4) | pIC50 = 5.8 ± 0.140 (n=4) | PMID: 32691589 |
| BRD4 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD2) | pIC50 = 4.5 ± 0.090 (n=2) | pIC50 = 4.5 ± 0.140 (n=3) | PMID: 32691589 |
| BRDT | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD1) | pIC50 = 6.2 | pIC50 = 5.2 ± 0.010 (n=2) | PMID: 32691589 |
| BRDT | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD2) | pIC50 = 4.9 | pIC50 = 5.1 ± 0.030 (n=2) | PMID: 32691589 |
| BRD2 | BD1 | Homo sapiens | BRD2 BD1 Bromoscan (DiscoverX) | pKd = 7.7 | PMID: 32691589 | |
| BRD2 | BD2 | Homo sapiens | BRD2 BD2 Bromoscan (DiscoverX) | pKd = 4.6 | PMID: 32691589 | |
| BRD3 | BD1 | Homo sapiens | BRD3 BD1 Bromoscan (DiscoverX) | pKd = 7.8 | PMID: 32691589 | |
| BRD3 | BD2 | Homo sapiens | BRD3 BD2 Bromoscan (DiscoverX) | pKd = 4.7 | PMID: 32691589 | |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 Bromoscan (DiscoverX) | pKd = 7.7 | PMID: 32691589 | |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 Bromoscan (DiscoverX) | pKd = 4.5 | PMID: 32691589 | |
| BRDT | BD1 | Homo sapiens | BRDT BD1 Bromoscan (DiscoverX) | pKd = 7.7 | PMID: 32691589 | |
| BRDT | BD2 | Homo sapiens | BRDT BD2 Bromoscan (DiscoverX) | pKd = 4.7 | PMID: 32691589 | |
| BRD2 | BD1 (full-length protein) | Homo sapiens | BRD2 BD1 Chemoproteomics | pKd = 8.4 | PMID: 32691589 | |
| BRD2 | BD2 (full-length protein) | Homo sapiens | BRD2 BD2 Chemoproteomics | pKd < 4.6 | PMID: 32691589 | |
| BRD3 | BD1 (full-length protein) | Homo sapiens | BRD3 BD1 Chemoproteomics | pKd = 8.4 | PMID: 32691589 | |
| BRD3 | BD2 (full-length protein) | Homo sapiens | BRD3 BD2 Chemoproteomics | pKd = 5.2 | PMID: 32691589 | |
| BRD4 | BD1 (full-length protein) | Homo sapiens | BRD4 BD1 Chemoproteomics | pKd = 8.2 | PMID: 32691589 | |
| BRD4 | BD2 (full-length protein) | Homo sapiens | BRD4 BD2 Chemoproteomics | pKd < 4.7 | PMID: 32691589 | |
| BRDT | BD1 (full-length protein) | Homo sapiens | BRDT BD1 Chemoproteomics | pKd = 8 | PMID: 32691589 | |
| BRDT | BD2 (full-length protein) | Homo sapiens | BRDT BD2 Chemoproteomics | pKd < 4.5 | PMID: 32691589 |
In cell potency
| Target name | Target information | Species | Assay description | GSK789 | GSK791 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MV-4−11 cells | Homo sapiens | Proliferation assay (MV-4−11 cells) | IC50 = 125 nM | PMID: 32691589 | ||
| HL60 cells | Homo sapiens | Proliferation assay (HL60 cells) | IC50 = 390 nM | PMID: 32691589 | ||
| THP-1 cells | Homo sapiens | Proliferation assay (THP-1 cells) | IC50 = 258 nM | PMID: 32691589 | ||
| CCL2 | whole blood | Homo sapiens | In vitro inhibition of MCP-1 in Lipopolysaccharide-stimulated human whole blood | IC50 = 0.67 µM ± 0.030 µM (n=6) | PMID: 32691589 | |
| TNF | whole blood | Homo sapiens | In vitro inhibition of TNFalpha in Lipopolysaccharide-stimulated human whole blood | IC50 = 0.87 µM ± 0.190 µM (n=5) | PMID: 32691589 | |
| IL6 | whole blood | Homo sapiens | In vitro inhibition of IL-6 in Lipopolysaccharide-stimulated human whole blood | IC50 = 3.55 µM ± 1.740 µM (n=5) | PMID: 32691589 | |
| CCL2 | Peripheral blood mononuclear cell | Homo sapiens | LPS-PBMC assay (MCP-1) | pIC50 = 7.7 | PMID: 32691589 |