Table 1 ITC of human BRDs with BSP.

Titrations were carried out in 50 mM Hepes buffer (pH 7.5; 25°C) and 150 mM NaCl at 15°C while stirring at 1000 rpm. Proteins were titrated into the ligand solution (reverse titration). Values are means ± SD.

Protein[P] (μM)[L] (μM)KD (nM)ΔHobs (kcal/mol)NTΔS (kcal/mol)ΔG (kcal/mol)
BAZ2A433153,745 ± 291−3.04 ± 0.0951.05 ± 0.0254.12−7.16
BAZ2B60715Weak binding
BRD1440131,653 ± 66−7.32 ± 0.0781.01 ± 0.0080.30−7.62
BRD2(1)2712597.1 ± 6.7−7.90 ± 0.0341.00 ± 0.0031.34−9.25
BRD2(2)2352550.3 ± 5.0−5.46 ± 0.0281.10 ± 0.0034.18−9.64
BRD3(1)2752091.7 ± 5.3−10.02 ± 0.0391.00 ± 0.002−0.95−9.08
BRD3(2)3052550.0 ± 4.7−8.62 ± 0.0411.11 ± 0.0031.01−9.63
BRD4(1)2582041.8 ± 2.8−11.09 ± 0.0380.94 ± 0.002−1.36−9.73
BRD4(2)2702039.7 ± 2.2−6.60 ± 0.0180.94 ± 0.0013.17−9.77
BRDT(1)2282040.2 ± 2.8−13.16 ± 0.0471.02 ± 0.002−3.40−9.76
BRDT(2)27120172.1 ± 10.6−5.61 ± 0.0281.00 ± 0.0033.31−8.92
BRD92512541.7 ± 3.8−8.75 ± 0.0391.00 ± 0.0020.98−9.73
BRPF1B40620311.5 ± 11.2−6.12 ± 0.0211.00 ± 0.0032.45−8.57
BRPF3400158,621 ± 381−4.20 ± 0.1231.08 ± 0.0252.48−6.68
CECR2202168.0 ± 1.0−17.28 ± 0.0621.04 ± 0.002−6.60−10.68
CREBBP617251,524 ± 116−2.91 ± 0.0411.03 ± 0.0114.72−7.64
EP300460157,194 ± 501−5.65 ± 0.2650.97 ± 0.0361.13−6.78
BPTF230151,887 ± 53−10.09 ± 0.0741.07 ± 0.005−3.28−6.80
GCN5L233615Weak binding
PB1(3)38915Weak binding
PB1(5)6041514,225 ± 802−3.19 ± 0.1831.09 ± 0.0533.20−6.39
PCAF610134,762 ± 459−7.85 ± 0.4540.95 ± 0.044−0.83−7.02
SMARCA222225Weak binding
SMARCA44001319,685 ± 838−9.05 ± 0.5800.99 ± 0.055−2.84−6.21
TAF1(1)460235,525 ± 199−3.34 ± 0.0460.98 ± 0.0103.60−6.94
TAF1(2)2302016.6 ± 2.7−14.05 ± 0.0950.98 ± 0.003−3.80−10.25
TAF1L(1)6101325,000 ± 2,027−4.78 ± 0.7781.00 ± 0.1461.29−6.07
TAF1L(2)2502042.7 ± 4.4−12.48 ± 0.0690.99 ± 0.003−2.76−9.72
TIF1A400158,475 ± 431−2.61 ± 0.0881.09 ± 0.0294.06−6.67