Compound,SMILES,PBRM1-BD2 NMR Kd (µM),PBRM1-BD2 LE (Ligand Efficiency),PBRM1-BD2 DSF Tm (¡C),PBRM1-BD1 DSF Tm (¡C),PBRM1-BD3 DSF Tm (¡C),PBRM1-BD4 DSF Tm (¡C),PBRM1-BD5 DSF Tm (¡C),PBRM1-BD6 DSF Tm (¡C),SMARCA2B DSF Tm (¡C),SMARCA4 DSF Tm (¡C),ASH1L DSF Tm (¡C),TAF1L BD2 DSF Tm (¡C),BAZ2B DSF Tm (¡C),TRIM33A DSF Tm (¡C),ATAD2B DSF Tm (¡C),BRD1 DSF Tm (¡C),BRD7 DSF Tm (¡C),BRPF1B DSF Tm (¡C),BRWD1 BD2 DSF Tm (¡C),CREBBP DSF Tm (¡C),PHIP BD2 DSF Tm (¡C),p300 DSF Tm (¡C),BRD2-BD2 DSF Tm (¡C),BRD3-BD1 DSF Tm (¡C),BRD3-BD2 DSF Tm (¡C),BRD4-BD1 DSF Tm (¡C),BRD4-BD2 DSF Tm (¡C),BRDT-BD1 DSF Tm (¡C),BPTF DSF Tm (¡C),CECR2 DSF Tm (¡C),GCN5 DSF Tm (¡C),PCAF DSF Tm (¡C),PBRM1-BD2 AlphaScreen IC50 (µM),PBRM1-BD2 ITC Kd (µM) ,PBRM1-BD5 ITC Kd (µM) ,SMARCA2B ITC Kd (µM) ,SMARCA4 ITC Kd (µM) ,ASH1L ITC Kd (µM) ,LNCaP CellTiter-Glo IC50 (µM) Exp1,LNCaP CellTiter-Glo IC50 (µM) Exp2,PC3 CellTiter-Glo IC50 (µM) Exp1,PC3 CellTiter-Glo IC50 (µM) Exp2,HEK293 T CellTiter-Glo IC50 (µM) Exp1,HEK293 T CellTiter-Glo IC50 (µM) Exp2 2,ClC1=C(C2=O)C(N(CC/C3=C\N(C)C)C3=N2)=CC=C1,,,3.3 ± 0.4,-0.1,2.6,0.3,7.7,-1.4,2.2,2,-0.7,,,-0.9,,,1.2,,,0.1,,-0.6,-0.2,0.1,0.5,0.1,-0.6,-0.1,,2,,-0.2,,,,,,,,,,,, 5,O=C1C2=CC=CC=C2NC(C3=C(Cl)C=CC=C3F)N1,45.3 ± 8.1,0.31,1.0 ± 0.2 ,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,4.2 ± 1.3,18.4 ± 3.7,179 ± 92,15.9 ± 9.7,~142,NB,,,,,, 6,OC(C1=CC=CC2=C1NC3=CC=CC=C3C2=O)=O,79 ± 35,0.33,1.5 ± 1.0 ,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,127 ± 30,,,,,,,,,,, 6a,O=C1CC(C)OC2=CC=C(Br)C=C21,170 ± 35,0.4,1.0 ± 0.1,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,30.7 ± 4.5,,,,,,,,,,, 6b,O=C1C2=CC(O)=CC=C2CC1,902 ± 270,0.4,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6c,O=C(C1=CC=CC=C1)C2=CC=CC(N)=C2,709 ± 211,0.29,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6d,C1(C2=NC(C3=CC=CN=C3)=CS2)=CC=CN=C1,1387 ± 262,0.23,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6e,O=C(C)C1=CNC2=CC=CC=C21,1195 ± 250,0.33,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6f,BrC1=C(C2=NN=NN2)C=CC=C1,1446 ± 599,0.32,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6g,CC1C(C2=CC=CS2)=NNC(C1)=O,1210 ± 267,0.3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6h,NC(C1=CC=C(F)C=C1)=S,>2000,N/A,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6i,COC1=C(C#N)C(OCC(F)(F)F)=CC=C1,>2000,N/A,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 6j,N#CC1=NC=CC=C1N2CCCCC2,>2000,N/A,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, 7,O=C1C2=CC=CC=C2N(CC/C3=C\C(CC)CC)C3=N1,,,7.7 ± 0.2,-0.9,2.8,3.9,11,-1.5,3,3.1,-0.7,,0.9,0.3,0.8,0.1,0.4,0.8,-0.4,-0.7,-5.6,-0.5,0.6,-0.3,0.4,-0.2,-1.1,-0.8,-1.2,-0.9,-0.4,0.4,0.2 ± 0.02,0.7 ± 0.2,0.35 ± 0.04,8.1 ± 4.4,5.0 ± 0.7,NB,,,,,, 8,ClC1=C(C2=O)C(N(CC/C3=C\C(CC)CC)C3=N2)=CC=C1,,,1.9 ± 0.3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,6.3 ± 1.4,6.9 ± 3.1,3.3 ± 0.4,ND,NB,NB,,,,,, 11,O=C1C2=C(Cl)C=CC=C2NC(C3=C(Cl)C=CC=C3F)N1,,,4.4 ± 0.4,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,1.0 ± 0.2,9.3 ± 1.1,10.1 ± 1.2,18.4 ± 9.9,69 ± 34,NB,,,,,, 12,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC=C3)N1,,,3.8 ± 0.4,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,1.1 ± 0.2,,,,,,,,,,, 13,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC=C3F)N1,,,3.3 ± 0.5,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,1.7 ± 0.3,,,,,,,,,,, 14,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC=C3Cl)N1,,,3.7 ± 0.2,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,2.1 ± 0.4,,,,,,,,,,, 15,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC=C3C)N1,,,5.4 ± 0.1,-0.8,2.7,0.9,2.9,-2,0.5,0.4,-0.6,,,0.8,,,0.2,,,0.5,,0.2,0.6,0.3,0.4,0.1,-3.3,-0.7,,-0.5,,0.5,0.2 ± 0.04,5.5 ± 1.0,11.1 ± 1.2,NB,30 ± 11,,,,,,, 16,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC(C)=C3)N1,,,5.4 ± 0.2,-0.1,1.8,0.8,1.8,-1.9,0.4,0.3,-0.6,0.1,-0.7,0.9,-0.2,-0.5,0,1.1,0.2,0.4,-8.2,-0.2,0.6,0.3,0.4,0.3,-3.9,-0.1,-2.3,-1.3,-0.2,0.5,0.26 ± 0.04,1.5 ± 0.9,3.9 ± 2.6,NB,NB,,9.3,8.8,,,, 17,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=C(C)C=C3)N1,,,2.8 ± 0.2,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,0.87 ± 0.14,,,,,,,,,,, 18,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=C(OC)C=C3)N1,,,3.4 ± 0.3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,2.3 ± 0.3,,,,,,,,,,, 19,O=C1C2=CC=CC=C2NC(C3=CC=CC=C3C)N1,,,1.5 ± 0.8,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,49.6 ± 11,,,,,,,,,,, 20,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC(C(F)(F)F)=C3)N1,,,2.9 ± 0.3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,5.6 ± 1.0,,,,,,,,,,, 21,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=C(C)C=C3C)N1,,,4.5 ± 0.9,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,0.86 ± 0.15,,,,,,,,,,, 22,O=C1C2=C(Cl)C=CC=C2NC(C3=C(C)C=C(C)C=C3C)N1,,,5.5 ± 0.3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,1.27 ± 0.26,,,,,,,,,,, 23,O=C1C2=C(Cl)C=CC=C2NC(C3=CC(C)=CC(C)=C3)N1,,,0.23 ± 0.03,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,>70 ,,,,,,,,,,, 24,O=C1C2=C(Cl)C=CC=C2NC(C3=CC(C)=CC=C3C)N1,,,5.4 ± 1.2,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,0.43 ± 0.04,,,,,,,,,,, 25,O=C1C2=C(Cl)C=CC=C2NC(C3=CC=CC(C)=C3C)N1,,,3.9 ± 0.3,-0.3,1.9,0.2,0.9,-1.3,0,-0.4,-0.8,,,0.3,,,0,,,0.6,,0.6,0.2,0.4,0.4,0.6,-4.2,0.1,,0.8,,0.1,0.22 ± 0.02,,,,,,0.66,0.66,0.77,0.8,0.32, 26,O=C1C2=C(Cl)C=CC=C2NC(C3=C(C)C=CC=C3C)N1,,,5.2 ± 0.3,-0.5,5,1,4.4,-1.2,0.5,0.6,-0.8,,,0.5,,,0.1,,,0.2,,0.2,0.5,0,0.3,0,-4.4,-0.6,,1.3,,0.6,0.29 ± 0.05,,,,,,2.2,2.1,2.2,2.4,³10,³10 27,O=C(N)C1=CC=CC=C1/N=C/C2=C(Cl)C=CC=C2F,,,0,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,118.6 ± 2.9,,,,,,,,,,, 28,O=C(N)C1=C(Cl)C=CC=C1/N=C/C2=C(Cl)C=CC=C2F,,,0.3 ± 0.2,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,17 ± 4,,,,,,,,,,, 29,O=C1C2=C(Cl)C=CC=C2N=C(C3=CC=CC(C)=C3)O1,,,0,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,236 ± 38,,,,,,,,,,, 30,O=C1C2=C(Cl)C=CC=C2N=C(C3=CC=CC(C)=C3)N1,,,0,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,89.9 ± 14.8,,,,,,,,,,, 31,O=C1C2=C(OC)C=CC=C2NC(C3=CC=CC=C3C)N1,,,0,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,>70 ,,,,,,,,,,, 32,O=C1C2=C(F)C=CC=C2NC(C3=CC=CC(C)=C3)N1,,,1.8 ± 0.2,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,5.6 ± 1.5,,,,,,,,,,, 33,O=C1C2=C(C)C=CC=C2NC(C3=CC=CC(C)=C3)N1,,,2.6 ± 0.3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,1.3 ± 0.4,,,,,,,,,,, 34,O=C1C2=C(Br)C=CC=C2NC(C3=CC=CC(C)=C3)N1,,,6.4 ± 0.2,1.4,0.6,0.2,1.5,-2.4,0.3,-0.2,-0.4,,,0.1,,,-0.4,,,-0.2,,-0.1,0.5,0.4,0.5,0.3,-1.1,-0.4,,-0.6,,0.6,0.16 ± 0.02,4.4 ± 1.3,25 ± 17,NB,NB,,9.5,9.3,,,, 35,O=C1C2=C(Br)C=CC=C2NC(C3=CC=CC=C3C)N1,,,4.0 ± 0.5,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,0.29 ± 0.04 ,,,,,,,,,,, 36,OC(C1=CC=CC=C1NC2=CC=CC(Cl)=C2C(O)=O)=O,,,1.4 ± 0.2,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,26,,,,,,,,,,, 37,OC(C1=CC=CC2=C1NC3=CC=CC(Cl)=C3C2=O)=O,,,3.0 ± 0.1,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,7,,,,,,,,,,, 38,OC(C1=CC=C(Cl)C=C1NC2=CC=CC=C2C(O)=O)=O,,,0.3 ± 0.02,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,>250,,,,,,,,,,, 39,OC(C1=CC=C(Cl)C2=C1NC3=CC=CC=C3C2=O)=O,,,0,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,>250,,,,,,,,,,,