Potency data for probe GSK778
In vitro potency
| Target name | Target information | Species | Assay description | GSK778 | Publication of assay conditions |
|---|---|---|---|---|---|
| BRD2 | BD1 | Homo sapiens | TR-FRET assay (BRD2 BD1) | IC50 = 75 nM ± 4.000 nM (n=6) | PMID: 32193360 |
| BRD2 | BD2 | Homo sapiens | TR-FRET assay (BRD2 BD2) | IC50 = 3950 nM ± 290.000 nM (n=8) | PMID: 32193360 |
| BRD3 | BD1 | Homo sapiens | TR-FRET assay (BRD3 BD1) | IC50 = 41 nM ± 5.000 nM (n=6) | PMID: 32193360 |
| BRD3 | BD2 | Homo sapiens | TR-FRET assay (BRD3 BD2) | IC50 = 1210 nM ± 65.000 nM (n=6) | PMID: 32193360 |
| BRD4 | BD1 | Homo sapiens | TR-FRET assay (BRD4 BD1) | IC50 = 41 nM ± 3.000 nM (n=16) | PMID: 32193360 |
| BRD4 | BD2 | Homo sapiens | TR-FRET assay (BRD4 BD2) | IC50 = 5843 nM ± 304.000 nM (n=16) | PMID: 32193360 |
| BRDT | BD1 | Homo sapiens | TR-FRET assay (BRDT BD1) | IC50 = 143 nM ± 14.000 nM (n=6) | PMID: 32193360 |
| BRDT | BD2 | Homo sapiens | TR-FRET assay (BRDT BD2) | IC50 = 17451 nM ± 1938.000 nM (n=6) | PMID: 32193360 |
| BRD2 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD1) | pIC50 = 7.1 ± 0.060 (n=8) | PMID: 32787145 |
| BRD2 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD2 BD2) | pIC50 = 5.5 ± 0.260 (n=10) | PMID: 32787145 |
| BRD3 | BD1 | Homo sapiens | BET mutant TR-FRETassay (BRD3 BD1) | pIC50 = 7.4 ± 0.090 (n=8) | PMID: 32787145 |
| BRD3 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD3 BD2) | pIC50 = 6 ± 0.170 (n=8) | PMID: 32787145 |
| BRD4 | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD1) | pIC50 = 7.4 ± 0.150 (n=16) | PMID: 32787145 |
| BRD4 | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRD4 BD2) | pIC50 = 5.2 ± 0.090 (n=16) | PMID: 32787145 |
| BRDT | BD1 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD1) | pIC50 = 6.8 ± 0.090 (n=8) | PMID: 32787145 |
| BRDT | BD2 | Homo sapiens | BET mutant TR-FRET assay (BRDT BD2) | pIC50 = 4.8 ± 0.130 (n=8) | PMID: 32787145 |
| BRD2 | BD1 | Homo sapiens | BRD2 Bromoscan (DiscoverX) | Kd = 13 nM | PMID: 32787145 |
| BRD3 | BD1 | Homo sapiens | BRD3 Bromoscan (DiscoverX) | Kd = 5 nM | PMID: 32787145 |
| BRD4 | BD1 | Homo sapiens | BRD4 Bromoscan (DiscoverX) | Kd = 5.9 nM | PMID: 32787145 |
| BRDT | BD1 | Homo sapiens | BRDT Bromoscan (DiscoverX) | Kd = 18 nM | PMID: 32787145 |
| BRD4 | BD1 | Homo sapiens | BRD4 BD1 SPR | pKd = 8 | PMID: 32787145 |
| BRD4 | BD2 | Homo sapiens | BRD4 BD2 SPR | pKd = 5.9 | PMID: 32787145 |
In cell potency
| Target name | Target information | Species | Assay description | GSK778 | Publication of assay conditions |
|---|---|---|---|---|---|
| HEK293 cells | Homo sapiens | NanoBRET | pIC50 = 7.3 | PMID: 32787145 | |
| AML cell line MV-4−11 with MLL-AF4 rearrangement | Homo sapiens | Cell proliferation assay: Growth inhibition after 3 days | pIC50 = 7 | PMID: 32787145 |