Table 1.
Compound | Ni-DTPA (mM) | T1 (msec) | T2* (msec) |
---|---|---|---|
5-fluoroindole | 0 | 4890 | 208 |
20 | 528 | 107 | |
50 | 202 | 80 | |
4FF | 0 | 1870 | 77 |
20 | 216 | 97 | |
40 | 113 | 80 | |
W75 (+ JQ1) | 0 | 508 (552) | 7.5 (7.1) |
20 | 269 (399) | 7.2 (6.2) | |
40 | 294 (346) | 6.4 (6.9) | |
W120 (+ JQ1) | 0 | 721 (685) | 8.4 (6.1) |
20 | 146 (212) | 8.0 (7.2) | |
40 | 86 (156) | 8.4 (8.1) | |
W81 (+ JQ1) | 0 | 837 (772) | 8.8 (7.0) |
20 | 196 (289) | 8.6 (5.4) | |
40 | 192 (149) | 8.6 (2.9) |
Small molecules used in this study were 5-fluoroindole and 4-fluorophenylalanine (4FF). T1 and T2* values were also measured for 5-fluorotryptophan residues within the protein Brd4 with and without the addition of Brd4 ligand, JQ1, that binds near W81.