Target (40)
Compound (646)
Article Title (70)
Assay (226)
Fan, L; Xu, K; Chen, K; Wang, F; Wu, X; Luo, T; Zhang, S; Li, X; Chen, Y BRD4 inhibitor US Patent US11572371 (2023) Chen, L; Yap, JL; Yoshioka, M; Lanning, ME; Fountain, RN; Raje, M; Scheenstra, JA; Strovel, JW; Fletcher, S BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett 6: 764 -9 (2015) Fan, L; Wang, F; Wu, X; Xu, K; Chen, K; Luo, T; Zhang, S; Huo, Y; Tu, Z; Li, X; Chen, Y BRD4 inhibitor as well as a preparative method and use thereof US Patent US12162878 (2024) Shen, C; Liu, Y; Bian, H; Wu, C; Wu, J BRD4 inhibitor compound in solid form and preparation method therefor and use thereof US Patent US12344620 (2025) Yu, P; Liu, W; Ren, J; Wang, Y; Ning, Y; Huang, M; Hu, X; Wei, L; Ji, M; Cai, J Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208. 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Bioorg Med Chem 93: (2023) Schönbrunn, E; Lawrence, NJ; Lawrence, HR; Reuther, G BRD4-JAK2 inhibitors US Patent US12391676 (2025) Liu, J; Huang, J; Wang, K; Li, Y; Li, C; Zhu, Y; He, X; Zhang, Y; Zhao, Y; Hu, C; Xi, Z; Tong, M; Li, Z; Gong, P; Hou, Y Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer. Bioorg Med Chem 101: (2024) Huang, QX; Fan, DM; Zheng, ZZ; Ran, T; Bai, A; Xiao, RQ; Hu, GS; Liu, W Peptide Inhibitor Targeting the Extraterminal Domain in BRD4 Potently Suppresses Breast Cancer Both In Vitro and In Vivo. J Med Chem 67: 6658 -6672 Rosse, G Dihydropteridinone Inhibitors of BRD4. ACS Med Chem Lett 7: 131 -131 (2016) Jung, M; Philpott, M; Müller, S; Schulze, J; Badock, V; Eberspächer, U; Moosmayer, D; Bader, B; Schmees, N; Fernández-Montalván, A; Haendler, B Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. 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Eur J Med Chem 227: (2022) Schönbrunn, E; Lawrence, NJ; Lawrence, HR BRD4-kinase inhibitors as cancer therapeutics US Patent US11643396 (2023) Chen, J; He, H; Wei, A; Li, Y; Cheng, G; Qin, H; Zhong, H; Liu, H; Geng, M; Shen, A; Hu, Y Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold. Eur J Med Chem 236: (2022) Abdel-Magid, AF Inhibitors of BRD4 as Potential Cancer Therapy. ACS Med Chem Lett 7: 728 -9 (2016) Zhou, J; Brasier, AR; Tian, B; Liu, Z; Chen, H; Rytting, E Inhibitors of bromodomain-containing protein 4 (BRD4) US Patent US11117865 (2021) Sabnis, RW Novel Bromodomain BRD4 Inhibitors for Treating Cancer. ACS Med Chem Lett 12: 951 -952 (2021) Ouyang, L; Zhang, L; Liu, J; Fu, L; Yao, D; Zhao, Y; Zhang, S; Wang, G; He, G; Liu, B Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. J Med Chem 60: 9990 -10012 (2017) Sabnis, RW Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors. ACS Med Chem Lett 12: 1530 -1531 (2021) Divakaran, A; Scholtz, CR; Zahid, H; Lin, W; Griffith, EC; Lee, RE; Chen, T; Harki, DA; Pomerantz, WCK Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader. ACS Med Chem Lett 13: 1621 -1627 (2022) Yang, SM; Urban, DJ; Yoshioka, M; Strovel, JW; Fletcher, S; Wang, AQ; Xu, X; Shah, P; Hu, X; Hall, MD; Jadhav, A; Maloney, DJ Discovery and lead identification of quinazoline-based BRD4 inhibitors. Bioorg Med Chem Lett 28: 3483 -3488 (2018) Engelhardt, H; Gianni, D; Smethurst, C Substituted [1,2,4]triazolo[4,3-a]pyrazines as BRD4 inhibitors US Patent US10328074 (2019) Amemiya, S; Yamaguchi, T; Hashimoto, Y; Noguchi-Yachide, T Synthesis and evaluation of novel dual BRD4/HDAC inhibitors. 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ChEMBL_853393 (CHEMBL2155213) Inhibition of human factor-13A ChEMBL_880180 (CHEMBL2214882) Inhibition of coagulation factor 13a ChEMBL_2275400 Inhibition of BRD4 BD1 (unknown origin) by chromatin/BRD4 displacement assay ChEMBL_2275401 Inhibition of BRD4 BD2 (unknown origin) by chromatin/BRD4 displacement assay ChEMBL_880968 (CHEMBL2216380) Inhibition of BRD4 ChEBML_1694131 Inhibition of BRD4 (unknown origin) ChEMBL_2271319 Inhibition of BRD4 (unknown origin) ChEMBL_2273374 Inhibition of BRD4 (unknown origin) ChEMBL_2275397 Inhibition of BRD4 (unknown origin) ChEMBL_2279926 Inhibition of BRD4 (unknown origin) ChEMBL_2285432 Inhibition of BRD4 (unknown origin) ChEMBL_2315625 Inhibition of BRD4 (unknown origin) ChEMBL_2327207 Inhibition of BRD4 (unknown origin) ChEMBL_2328176 Inhibition of BRD4 (unknown origin) ChEMBL_2434547 Inhibition of BRD4 (unknown origin) ChEMBL_2476277 Inhibition of BRD4 (unknown origin) ChEMBL_2488258 Inhibition of BRD4 (unknown origin) ChEMBL_2513633 Inhibition of BRD4 (unknown origin) ChEMBL_1692573 (CHEMBL4043463) Inhibition of BRD4 (unknown origin) ChEMBL_1694131 (CHEMBL4045021) Inhibition of BRD4 (unknown origin) ChEMBL_1712939 (CHEMBL4122988) Inhibition of BRD4 (unknown origin) ChEMBL_1822368 (CHEMBL4322132) Inhibition of BRD4 (unknown origin) ChEMBL_1830003 (CHEMBL4329877) Inhibition of BRD4 (unknown origin) ChEMBL_1854530 (CHEMBL4355259) Inhibition of BRD4 (unknown origin) ChEMBL_1864568 (CHEMBL4365543) Inhibition of BRD4 (unknown origin) ChEMBL_1902819 (CHEMBL4405041) Inhibition of BRD4 (unknown origin) ChEMBL_1994004 (CHEMBL4627899) Inhibition of BRD4 (unknown origin) ChEMBL_2070232 (CHEMBL4725766) Inhibition of BRD4 (unknown origin) ChEMBL_2072935 (CHEMBL4728469) Inhibition of BRD4 (unknown origin) ChEMBL_2089729 (CHEMBL4770992) Inhibition of BRD4 (unknown origin) ChEMBL_2101164 (CHEMBL4809560) Inhibition of BRD4 (unknown origin) ChEMBL_2145529 (CHEMBL5029809) Inhibition of BRD4 (unknown origin) ChEMBL_2184911 (CHEMBL5096993) Inhibition of BRD4 (unknown origin) ChEMBL_2224686 (CHEMBL5138199) Inhibition of BRD4 (unknown origin) ChEMBL_2251591 (CHEMBL5165801) Inhibition of BRD4 (unknown origin) ChEMBL_2251892 (CHEMBL5166102) Inhibition of BRD4 (unknown origin) ChEMBL_2267239 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2267240 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2281648 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2281659 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2282495 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2282496 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2285443 Inhibition of human full length BRD4 ChEMBL_2329794 Binding affinity to BRD4 (unknown origin) ChEMBL_2341192 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2341193 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2434297 Inhibition of BRD4 in HEK293T cells ChEMBL_2448581 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2448582 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2472930 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2472931 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2472933 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2472934 Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2496990 Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2496991 Inhibition of BRD4 BD2 (unknown origin) ChEBML_1696637 Binding affinity to BRD4 BD1 (unknown origin) ChEMBL_1584187 (CHEMBL3821505) Inhibition of BRD4(1) (unknown origin) ChEMBL_1842489 (CHEMBL4342916) Binding affinity to BRD4 (unknown origin) ChEMBL_1848888 (CHEMBL4349429) Binding affinity to BRD4 (unknown origin) ChEMBL_1897676 (CHEMBL4399711) Inhibition of BRD4 bromodomain (unknown origin) ChEMBL_1977430 (CHEMBL4610565) Inhibition of BRD4 BD1 (unknown origin) ChEMBL_1977431 (CHEMBL4610566) Inhibition of BRD4 BD2 (unknown origin) ChEMBL_1994005 (CHEMBL4627900) Binding affinity to BRD4 (unknown origin) ChEMBL_2069568 (CHEMBL4724821) Inhibition of BRD4-BD1 (unknown origin) ChEMBL_2184237 (CHEMBL5096319) Inhibition of BRD4-BD1 (unknown origin) ChEMBL_2184248 (CHEMBL5096330) Inhibition of BRD4-BD2 (unknown origin) ChEMBL_2209373 (CHEMBL5122322) Binding affinity to BRD4 (unknown origin) ChEMBL_2209378 (CHEMBL5122327) Inhibition of BRD4-BD1 (unknown origin) ChEMBL_2209379 (CHEMBL5122328) Inhibition of BRD4-BD2 (unknown origin) ChEMBL_2213606 (CHEMBL5126738) Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2213607 (CHEMBL5126739) Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2251592 (CHEMBL5165802) Inhibition of BRD4 BD1 (unknown origin) ChEMBL_2251593 (CHEMBL5165803) Inhibition of BRD4 BD2 (unknown origin) ChEMBL_2275399 Binding affinity to BRD4 BD2 (unknown origin) ChEMBL_2285445 Inhibition of BRD4 (unknown origin) BD1 domain ChEMBL_2285709 Binding affinity to BRD4 BD1 (unknown origin) ChEMBL_2285710 Binding affinity to BRD4 BD2 (unknown origin) ChEMBL_770211 (CHEMBL1833001) Inhibition of first bromodomain of BRD4 ChEMBL_874464 (CHEMBL2184787) Binding affinity to BRD4 isoform 1 In Vitro Enzyme Inhibition Assay-BRD4 Inhibition Inhibition of BRD4 was determined as previously described in U.S. Pat. No. 9,034,900. In Vitro Enzyme Inhibition Assay-BRD4 Inhibition Inhibition of BRD4 was determined as described previously. See, e.g., U.S. Pat. No. 9,034,900. ChEMBL_1569678 (CHEMBL3791151) Inhibition of BRD4 bromodomain 1 (unknown origin) ChEMBL_1694115 (CHEMBL4045005) Inhibition of human BRD4 bromo domain 2 ChEMBL_1694121 (CHEMBL4045011) Inhibition of human BRD4 bromo domain 1 ChEMBL_1696638 (CHEMBL4047528) Binding affinity to BRD4 BD2 (unknown origin) ChEMBL_1801594 (CHEMBL4273886) Binding affinity to human BRD4 bromodomain-1 ChEMBL_2069569 (CHEMBL4724822) Binding affinity to BRD4-BD1 (unknown origin) ChEMBL_2070239 (CHEMBL4725773) Inhibition of BRD4 BD2 domain (unknown origin) ChEMBL_2145174 (CHEMBL5029454) Binding affinity to human BRD4 bromodomain 1 ChEMBL_2184249 (CHEMBL5096331) Inhibition of BRD4 (unknown origin) by ELISA ChEMBL_2209377 (CHEMBL5122326) Binding affinity to BRD4-BD1 (unknown origin) ChEMBL_2209380 (CHEMBL5122329) Binding affinity to BRD4-BD2 (unknown origin) ChEMBL_2212963 (CHEMBL5125912) Binding affinity to BRD4-T (unknown origin) ChEMBL_2220941 (CHEMBL5134275) Inhibition of BRD4-BD1/2 (unknown origin) ChEMBL_2271310 Binding affinity to BRD4 BD1 domain (unknown origin) ChEMBL_2271311 Binding affinity to BRD4 BD2 domain (unknown origin) ChEMBL_2283137 Induction of BRD4 degradation in human 231MFP cells ChEMBL_2310092 Inhibition of BRD4 (unknown origin) by HTRF analysis ChEMBL_2577109 Inhibition of BRD4 (unknown origin) by FRET-assay ChEMBL_853604 (CHEMBL2154059) Binding affinity to first bromodomain of BRD4 ChEMBL_2457797 Inhibition of BRD4-BD1 (unknown origin) assessed as peptide-biotin titration - BRD4(1)/histone H4 peptide interaction by HTRF/EPIgeneous assay Inhibition Assay Several TP Scaffold compounds were tested for inhibition activity against isoforms of PI3K (alpha, beta, gamma, and delta isoforms) and the bromodomain protein BRD4 at regions 1 (BRD4-1) and 2 (BRD4-2). ChEMBL_2289457 Protac activity at FEM1B/BRD4 in human HEK293T cells assessed as degradation of BRD4 incubated for 8 hrs by Western blot analysis ChEMBL_1759898 (CHEMBL4194906) Binding affinity to BRD4 bromodomain 1 (K57 to E168 amino acids) (unknown origin) using Alexa647-labeled BET-inhibitor as fluorescent probe by bromodomain TR-FRET binding assay ChEMBL_1759899 (CHEMBL4194907) Binding affinity to BRD4 bromodomain 2 (E352 to M457 amino acids) (unknown origin) using Alexa647-labeled BET-inhibitor as fluorescent probe by bromodomain TR-FRET binding assay ChEBML_1662832 Inhibition of BRD4 (unknown origin) by fluorescence polarization assay ChEMBL_1469309 (CHEMBL3414206) Inhibition of BRD4 (unknown origin) by fluorescence anisotrophy ChEMBL_1561484 (CHEMBL3779621) Inhibition of human BRD4 by isothermal titration calorimetry ChEMBL_1586811 (CHEMBL3826496) Inhibition of human BRD4-BD1 by alpha assay ChEMBL_1662841 (CHEMBL4012522) Inhibition of human BRD4 by fluorescence polarization assay ChEMBL_1694129 (CHEMBL4045019) Inhibition of human BRD4 bromodomain2 by Alphascreen assay ChEMBL_1738681 (CHEMBL4154431) Inhibition of BRD4 (unknown origin) by Alphascreen assay ChEMBL_1750887 (CHEMBL4185647) Inhibition of BRD4 (unknown origin) by AlphaScreen assay ChEMBL_2281678 Binding affinity BRD4 (unknown origin) assessed as dissociation constant ChEMBL_2285437 Inhibition of BRD4 (unknown origin) assessed as dissociation constant ChEMBL_2337675 Inhibition of human BRD4 BD1 by TR-FRET assay ChEMBL_2337676 Inhibition of human BRD4 BD2 by TR-FRET assay ChEMBL_2348182 Inhibition of BRD4 (unknown origin) by alpha screen assay ChEMBL_2440168 Inhibition of BRD4 (unknown origin) by TR-FRET assay ChEMBL_2440172 Inhibition of BRD4 (unknown origin) by alpha-screen assay ChEMBL_2442968 Binding affinity to BRD4 (unknown origin) by SPR assay ChEMBL_2448976 Inhibition of BRD4 BD1 (unknown origin) by Alphascreen assay ChEMBL_2448977 Inhibition of BRD4 BD2 (unknown origin) by Alphascreen assay ChEMBL_2452589 Inhibition of BRD4 (unknown origin) by TR-FRET assay ChEMBL_2452675 Inhibition of BRD4 BD1 (unknown origin) by HTRF assay ChEMBL_2452676 Inhibition of BRD4 BD2 (unknown origin) by HTRF assay ChEMBL_2457796 Inhibition of BRD4 (unknown origin) by ALPHA screen assay ChEMBL_2458288 Inhibition of BRD4 BD1 (unknown origin) by Alphascreen assay ChEMBL_2458289 Inhibition of BRD4 BD2 (unknown origin) by Alphascreen assay ChEMBL_2459004 Inhibition of human BRD4 BD1 by TR-FRET assay ChEMBL_2459005 Inhibition of human BRD4 BD2 by TR-FRET assay ChEMBL_2468700 Inhibition of BRD4 BD1 (unknown origin) by alphascreen assay ChEMBL_2468701 Inhibition of BRD4 BD2 (unknown origin) by alphascreen assay ChEMBL_2491484 Inhibition of BRD4 BD1 (unknown origin) by Alphascreen assay ChEMBL_2491485 Inhibition of BRD4 BD2 (unknown origin) by Alphascreen assay ChEMBL_806308 (CHEMBL1959072) Binding affinity to BRD4 by isothermal titration calorimetry ChEMBL_878136 (CHEMBL2183681) Inhibition of BRD4 isoform 1 by AlphaScreen assay ChEMBL_2271300 Inhibition of BRD4-BD1 domain (unknown origin) assessed as inhibition of tetra-acetylated Histone H4 peptide binding to BRD4 by ALPHA-screen assay ChEMBL_2271301 Inhibition of BRD4-BD2 domain (unknown origin) assessed as inhibition of tetra-acetylated Histone H4 peptide binding to BRD4 by ALPHA-screen assay ChEMBL_2341712 Inhibition of full length BRD4 (unknown origin) transfected in HEK293 cells incubated for 20 hrs measured by NanoBRET BRD4/Histone H3.3 interaction assay kit ChEMBL_1434743 (CHEMBL3383412) Inhibition of human BRD4 bromodomain 1 by BROMOscan assay ChEMBL_1434744 (CHEMBL3383413) Inhibition of human BRD4 bromodomain 2 by BROMOscan assay ChEMBL_1513098 (CHEMBL3610435) Inhibition of BRD4 (unknown origin) by alpha screen assay ChEMBL_1569665 (CHEMBL3791138) Inhibition of BRD4 bromodomain1 in human MV4-11 cells ChEMBL_1662832 (CHEMBL4012513) Inhibition of BRD4 (unknown origin) by fluorescence polarization assay ChEMBL_1692586 (CHEMBL4043476) Inhibition of acetylated H4 binding to BRD4 (unknown origin) ChEMBL_1713098 (CHEMBL4123147) Inhibition of BRD4 (unknown origin) by fluorescence polarization assay ChEMBL_1899763 (CHEMBL4401878) Binding affinity to BRD4 (unknown origin) by isothermal calorimetry ChEMBL_2031100 (CHEMBL4685258) Inhibition of BRD4 (unknown origin) by alpha-screen assay ChEMBL_2046866 (CHEMBL4701565) Inhibition of BRD4 BD1 (unknown origin) by ALPHAScreen assay ChEMBL_2046869 (CHEMBL4701568) Inhibition of BRD4 BD2 (unknown origin) by ALPHAScreen assay ChEMBL_2159804 (CHEMBL5044554) Inhibition of BRD4 D1 (unknown origin) by alphascreen assay ChEMBL_2202254 (CHEMBL5114962) Inhibition of BRD4 BD1 (unknown origin) fluorescence polarization method ChEMBL_2202255 (CHEMBL5114963) Inhibition of BRD4 BD2 (unknown origin) fluorescence polarization method ChEMBL_2202256 (CHEMBL5114964) Inhibition of BRD4 BD1 (unknown origin) TR-FRET analysis ChEMBL_2202257 (CHEMBL5114965) Inhibition of BRD4 BD2 (unknown origin) TR-FRET analysis ChEMBL_2230521 (CHEMBL5144293) Inhibition of BRD4 (unknown origin) by alpha-screen assay ChEMBL_2267251 Binding affinity to BRD4 (unknown origin) assessed as dissociation constant ChEMBL_2280589 Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay ChEMBL_2283085 Binding affinity to BRD4 bromodomain 1 in human Ramos cells ChEMBL_2283098 Binding affinity to BRD4 (unknown origin) assessed as dissociation constant ChEMBL_2293025 Binding affinity to human recombinant BRD4 assessed as dissociation constant ChEMBL_2307844 Inhibition of BRD4-BD1 (unknown origin) by fluorescence polarization assay ChEMBL_2307845 Inhibition of BRD4-BD2 (unknown origin) by fluorescence polarization assay ChEMBL_2338330 Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay ChEMBL_2338331 Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay ChEMBL_2364622 Binding affinity to BRD4 BD1 (unknown origin) by ITC analysis ChEMBL_2369634 Binding affinity to BRD4 (unknown origin) assessed as dissociation constant ChEMBL_2440171 Inhibition of BRD4-BD1 (unknown origin) by fluorescence polarization method ChEMBL_2448965 Binding affinity to BRD4 BD1 (unknown origin) by ITC analysis ChEMBL_2448966 Binding affinity to BRD4 BD2 (unknown origin) by ITC analysis ChEMBL_2448967 Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay ChEMBL_2448968 Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay ChEMBL_2458290 Binding affinity to BRD4 BD1 (unknown origin) by ITC analysis ChEMBL_2458291 Binding affinity to BRD4 BD2 (unknown origin) by ITC analysis ChEMBL_2460781 Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay ChEMBL_2472900 Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay ChEMBL_2472901 Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay ChEMBL_2476279 Binding affinity to BRD4 (unknown origin) assessed as dissociation constant ChEMBL_806301 (CHEMBL1959065) Binding affinity to BRD4-BD1 by isothermal titration calorimetry ChEMBL_807439 (CHEMBL1958561) Binding affinity to BRD4-BD1 by isothermal titration calorimetry ChEMBL_807440 (CHEMBL1958562) Binding affinity to BRD4-BD2 by isothermal titration calorimetry ChEMBL_807444 (CHEMBL1958566) Binding affinity to BRD4-BD1,2 by isothermal titration calorimetry ChEMBL_988297 (CHEMBL2439863) Binding affinity to first bromodomain of BRD4 (unknown origin) Ligand KI Assay The labeled ligand specifically binds BRD4-1 and BRD4-2 and can be displaced by a small molecule inhibitor that shares a similar or overlapping binding site. BRD4-I and BRD4-2 were expressed and purified from Escherichia coli as N-terminal His6, tagged proteins. A Eu-cryptate labeled anti-His antibody (Perkin Elmer) was used to specifically bind BRD4. Binding of BRD4 to the labeled probe/ligand resulted in an increase in FRET signal whereas displacement of this labeled ligand from BRD4 with a small molecule inhibitor resulted in a decrease in FRET signal. Assays were performed in 50 mM Hepes (pH 7.5), 150 mM NaCl, 0.1 mg/ml BSA, 0.01% (v/v) Brij, 0.5% (v/v) DMSO and 10 nM labeled ligand at the following concentrations for each BRD4 isoform: 2 nM BRD4-1 and 0.5 nM BRD4-2. After an assay reaction time of 60 minutes at 25° C., binding was measured with 2 nM Eu-cryptate labeled anti-His antibody. TR-FRET signal was detected on an Envision plate reader (Ex: 320 nm; Em: 615/665 nm; 100 us delay and 200 us read window). Data were normalized based on a positive (2 uM I-BET) and negative (DMSO) controls and IC50 values were calculated from the fit of the dose-response curves to a four-parameter equation. All IC50 values represent geometric mean values of a minimum of four determinations. The IC50 values were converted to Ki values (dissociation constant for BRD4-inhibitor complex) using the Cheng and Prusoff equation for a competitive inhibitor mode of action. ChEMBL_1327497 (CHEMBL3226597) Inhibition of BRD4 bromodomain-1 (unknown origin) by AlphaScreen assay ChEMBL_1434747 (CHEMBL3383416) Inhibition of human BRD4 bromodomain 1/2 by BROMOscan assay ChEMBL_1442441 (CHEMBL3380071) Binding affinity to BRD4 (unknown origin) by isothermal titration colorimetry ChEMBL_1614102 (CHEMBL3855902) Inhibition of BRD4 bromodomain 1 (unknown origin) by Alphascreen assay ChEMBL_1739117 (CHEMBL4154867) Inhibition of BRD4 bromodomain-1 (unknown origin) by AlphaScreen assay ChEMBL_1739119 (CHEMBL4154869) Inhibition of BRD4 bromodomain-1 (unknown origin) by FRET assay ChEMBL_1754580 (CHEMBL4189340) Binding affinity to BRD4 BD1 (unknown origin) by ITC method ChEMBL_1816701 (CHEMBL4316275) Binding affinity to BRD4 BD1 (unknown origin) by ITC analysis ChEMBL_1845969 (CHEMBL4346396) Binding affinity to human BRD4 BD1 by isothermal calorimetry analysis ChEMBL_1845970 (CHEMBL4346397) Binding affinity to human BRD4 BD2 by isothermal calorimetry analysis ChEMBL_1988985 (CHEMBL4622532) Binding affinity to BRD4 BD2 (unknown origin) by SPR assay ChEMBL_1988986 (CHEMBL4622533) Binding affinity to BRD4 BD1 (unknown origin) by SPR assay ChEMBL_2069573 (CHEMBL4724826) Inhibition of BRD4-BD1 (unknown origin) by TR-FRET assay ChEMBL_2077525 (CHEMBL4733316) Binding affinity to human BRD4 bromodomain1 by isothermal titration calorimetry ChEMBL_2077526 (CHEMBL4733317) Binding affinity to human BRD4 bromodomain2 by isothermal titration calorimetry ChEMBL_2115129 (CHEMBL4824070) Binding affinity to BRD4 (unknown origin) by fluorescence polarization assay ChEMBL_2116289 (CHEMBL4825230) Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay ChEMBL_2119177 (CHEMBL4828243) Binding affinity to BRD4 BD1 (unknown origin) by BROMOscan method ChEMBL_2184252 (CHEMBL5096334) Inhibition of GST-tagged BRD4 (unknown origin) by HTRF assay ChEMBL_2185061 (CHEMBL5097143) Inhibition of BRD4 BD1 (unknown origin) by fluorescence based analysis ChEMBL_2200516 (CHEMBL5113032) Inhibition of BRD4-BD2 (unknown origin) measured by AlphaScreen assay ChEMBL_2224354 (CHEMBL5137867) Inhibition of BRD4 BD1 (unknown origin) by Alpha screen assay ChEMBL_2224355 (CHEMBL5137868) Inhibition of BRD4 BD2 (unknown origin) by Alpha screen assay ChEMBL_2224356 (CHEMBL5137869) Inhibition of BRD4 BD1 (unknown origin) by fluorescence based assay ChEMBL_2224357 (CHEMBL5137870) Inhibition of BRD4 BD2 (unknown origin) by fluorescence based assay ChEMBL_2224362 (CHEMBL5137875) Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay ChEMBL_2224363 (CHEMBL5137876) Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay ChEMBL_2267254 Inhibition of BRD4 (unknown origin) by radiometric ATP-competitive kinase assay ChEMBL_2267265 Binding affinity to BRD4 BD1 (unknown origin) assessed as dissociation constant ChEMBL_2267266 Binding affinity to BRD4 BD2 (unknown origin) assessed as dissociation constant ChEMBL_2272486 Binding affinity to BRD4 BD1 (unknown origin) by isothermal titration calorimetry ChEMBL_2285434 Inhibition of full length BRD4 (unknown origin) incubated for 18 hrs ChEMBL_2285435 Inhibition of BRD4 (unknown origin) BD1 domain incubated for 18 hrs ChEMBL_2295027 Inhibition of BRD4 bromodomain 1/2 (unknown origin) by Alphascreen assay ChEMBL_2315643 Inhibition of BRD4 bromodomain 1 (unknown origin) by Alphascreen based method ChEMBL_2315644 Inhibition of BRD4 bromodomain 2 (unknown origin) by Alphascreen based method ChEMBL_2315650 Binding affinity to BRD4 BD1 (unknown origin) by thermal denaturation assay ChEMBL_2315651 Binding affinity to BRD4 BD2 (unknown origin) by thermal denaturation assay ChEMBL_2559586 Binding affinity to BRD4 (unknown origin) assessed as apparent dissociation constant ChEMBL_1759876 (CHEMBL4194884) Binding affinity to His-tagged BRD4 bromodomain 1 to 2 (K57 to K550 amino acids) (unknown origin) using Alexa647-labeled BET-inhibitor as fluorescent probe by bromodomain TR-FRET binding assay Biochemical Activity Assay for BRD4 1) using BRD4-BD1 protein and BRD4-BD2 protein from BPS company for the experiments; as well as polypeptides from ANASPEC company; detection reagents from Perkinelmer company;2) screening compounds by applying the experimental principle of TR-FRET;3) testing the compounds.
alpha-ketoamide inhibitor 13a BDBM420293
US9266895, 13a BDBM143192 US11040980, Example 13a US8940744, 13a US9994576, 13a
BDBM136709 US8865911, 13a US9918985, Example 13a US10231967, Example 13a
US9029399, 13A BDBM158439 US9339501, 13A
US11560368, Example 13a US10683279, Example 13a US10988458, Example 13a BDBM445416
BDBM150823 USRE47267, Compound 13a US8981106, 13a
US9598410, Compound 13a BDBM179730 US9127001, 13a
BDBM497390 US11007200, Example 13a US11426411, Example 13a
BDBM50189945 CHEMBL3828502 US11111253, Compound 13a US10618914, Compound 13a
BDBM127968 US8796310, 13A
BDBM186017 US9168255, 13a
BDBM192245 US9187441, 13a
BDBM194660 US9206162, 13a
BDBM236613 US9365589, 13a
BDBM239123 US9403810, 13a
BDBM29086 cyclopropanolamide, 13a
US9102670, 13a BDBM174587
US9221796, 13a BDBM198680
US9266878, 13a BDBM208790
US9487490, 13A BDBM256390
US9493474, 13A BDBM254081
BDBM180296 US9133168, Example 13a
BDBM194660 US8835464, 13a BDBM131794
BDBM304246 US10143695, Compound 13A
BDBM316060 US9616064, Compound 13a
BDBM34050 iodinated benzimidazole, 13a
BDBM34073 benzamide derivative, 13a
BDBM35636 5-chloroindolecarboxamide, 13a
BDBM35715 benzazepine derivative, 13a
BDBM35956 acyclic compound, 13a
BDBM404651 US10344000, Example 13A
BDBM408046 US10336774, Example 13a
BDBM412671 US10399979, Compound 13a
BDBM448155 US10689369, Example 13A
BDBM462244 US10766893, Example 13a
BDBM523183 US11161864, Example 13A
BDBM541790 US11267824, Example 13a
BDBM548020 WO2022091056, Example 13a
BDBM553819 US11325884, Compound 13a
BDBM590203 US11560385, Compound 13A
BDBM613581 US11731944, Example 13a
BDBM619167 US20230295119, Compound 13A
BDBM668391 US20240124478, Example 13a
BDBM685652 US20240239813, Compound 13a
BDBM700722 US12115157, Ex. 13a
BDBM81376 Amine compound, 13a
US10201546, Example 13a BDBM339051
US10287272, Example 13A BDBM385521
US11236046, Example 13a BDBM534943
US11505523, Compound 13a BDBM581352
US11691969, Example 13A BDBM608122
US11718589, Compound 13a BDBM611590
US11834440, Compound 13A BDBM637809
US20230287003, Example 13a BDBM618583
US20230331683, Compound 13a BDBM627452
US20240043442, Example 13A BDBM650929
US20240166642, Example 13a BDBM676523
US20240246932, Example 13A BDBM686316
US20240336629, Compound 13A BDBM700451
US20250197424, Compound 13a' BDBM752801
US9845308, Example 13a BDBM362890
benzothienopyrimidinone deriv., 13a BDBM35013
tetrahydrobenzothiophene (THBT), 13a BDBM31638
US9259422, 13a, R = Ph-BU126 US9480684, 13a, R = Ph- BU126 BDBM50014995 CHEMBL3262090
BDBM553819 BDBM453313 US10730826, Compound 13a
BDBM577495 US11472838, Compound 13a/b
Bicyclic core, rac-13a BDBM36576
US11643436, Compound TM-13A BDBM602187
US9388210, 15a US9388210, 13a BDBM238238
BDBM280346 US11053216, Compound 13a US10030004, Compound 13a 4-[[2-(5-chloro-2-fluoro-phenyl)-5-methoxy-4-pyridyl]amino]-N-[(2S)-2-hydroxypropyl]pyridine-3-carboxamide US10501436, Compound 13a US11702401, Compound 13a
BDBM35125 5-vinyl-3-pyridinecarbonitrile, 13a
BDBM748946 US20250188078, Ref. PA1-13A-3
BDBM748947 US20250188078, Ref. PA1-13A-7
Dansyl derivatives 13A, (R) isomer BDBM36675
US10195181, Example 13a BDBM239113 US9403810, 13b
US20250188078, Ref. PA1-13A-2 BDBM748945
US10196354, Example 13A US9745265, 13A BDBM332473 4-(6-(3-aminoprop-1-ynyl)-1-(2-chloro-6-(trifluoromethyl)benzoyl)-1H-indazol-3-yl)-3-fluorobenzoic acid (13A)
BDBM180295 US9133168, Example 13a US9133168, Example 12a
BDBM218942 US9303033, W4, Table 13A, Compound 31
BDBM29578 isatin Michael acceptor (IMA) analogue, 13a
BDBM408044 US10336774, Example 12a US10336774, Example 13a
US11104675, Example 13b US11104675, Example 13a BDBM516923
US11685719, Example 13B US11685719, Example 13A BDBM606230
US11702409, Example 13a BDBM608852 US11702409, Example 13b
US20240124450, Example 13A BDBM668159 US20240124450, Example 13B
US9346782, 13c US9346782, 13a US9346782, 13b BDBM231233
US9745289, Compound 13B US9745289, Compound 13A BDBM336850
racemic cyclopropanolamide, rac-10a BDBM29078 cyclopropanolamide, 13a
US11001568, Example 13A BDBM270518 US10059687, Example 13A US11731954, Example 13A and 13B (R)-3-(((6-((4-ethylphenyl)(methyl)amino)-2-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)methyl)amino)isonico-tinic acid
US20240327418, Comparative example 2 LP97/13a BDBM50584228 CHEMBL4597954
1,1-Bis[3-bromo-4-methoxy-5-(methoxycarbonyl)phenyl]-5-phenyl-1-pentene Alkenyldiarylmethanes (ADAM) 13a BDBM2772 Alkenyldiarylmethane (ADAM) 13a
US11673864, Compound 20 BDBM161235 US10087143, Compound 20 US10787472, Compound 13a US9051270, 20 US9758483, Compound 20 US10738009, Compound 20 US9163042, 13a
BDBM235700 L-Isoseryl-L-leucyl-L-phenylalanine methyl ester hydrochloride (13a)
Dansyl derivatives 13A, (R) isomer Dansyl derivatives 12A, (S) isomer BDBM36674
BDBM15067 6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]pyridin-3-yl}isoquinoline isoquinoline-pyridine, 1 isoquinoline-pyridine, 3 (2S)-1-(1H-indol-3-yl)-3-(5-isoquinolin-6-ylpyridin-3-yl)oxy-propan-2-amine 13a (S-) 5-isoquinolinyl pyridine 2 pyridine-base inhibitor 13a
4-(3-Morpholinopropoxy)-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide (13a) BDBM152774
BDBM4398 N-(3-chlorophenyl)-6-methylquinazolin-4-amine 4-Anilidoquinazoline deriv. 13a
BDBM601447 (S)-2-(3-(3,5-dimethyl-1H-pyrazol-1- US11634418, Compound 13a
US10696672, Compound 13a BDBM448776 (S)-2-(3-(3,5-dimethyl-1H-pyrazol-1-
BDBM218920 US9303033, M7, Table 22A, Compound 7 US9303033, A4, Table 13A, Compound 9
BDBM218921 US9303033, B4, Table 13A, Compound 10 US9303033, B8, Table 22A, Compound 22
BDBM218929 US9303033, J4, Table 13A, Compound 18 US9303033, Q7, Table 22A, Compound 11
BDBM218930 US9303033, R7, Table 22A, Compound 12 US9303033, K4, Table 13A, Compound 19
BDBM218931 US9303033, L4, Table 13A, Compound 20 US9303033, G8, Table 22A, Compound 27
BDBM218934 US9303033, O4, Table 13A, Compound 23 US9303033, J8, Table 22A, Compound 30
BDBM218940 US9303033, U4, Table 13A, Compound 29 US9303033, W7, Table 22A, Compound 17
BDBM218943 US9303033, N8, Table 22A, Compound 34 US9303033, X4, Table 13A, Compound 32
BDBM218944 US9303033, Y4, Table 13A, Compound 33 US9303033, O8, Table 22A, Compound 35
BDBM218946 US9303033, A5, Table 13A, Compound 35 US9303033, X7, Table 22A, Compound 18
Diethylsulfonamide Derivative, 13a 2-{[4-bromo-3-(diethylsulfamoyl)benzene]amido}benzoic acid BDBM23570
US9303033, B5, Table 13A, Compound 36 US9303033, Y7, Table 22A, Compound 19 BDBM218947
US9303033, C8, Table 22A, Compound 23 BDBM218922 US9303033, C4, Table 13A, Compound 11
US9303033, D4, Table 13A, Compound 12 BDBM218923 US9303033, D8, Table 22A, Compound 24
US9303033, E4, Table 13A, Compound 13 BDBM218924 US9303033, E8, Table 22A, Compound 25
US9303033, F8, Table 22A, Compound 26 US9303033, F4, Table 13A, Compound 14 BDBM218925
US9303033, G4, Table 13A, Compound 15 US9303033, N7, Table 22A, Compound 8 BDBM218926
US9303033, G7, Table 22A, Compound 1 US9303033, S3, Table 13A, Compound 1 BDBM218912
US9303033, H8, Table 22A, Compound 28 BDBM218932 US9303033, M4, Table 13A, Compound 21
US9303033, I4, Table 13A, Compound 17 BDBM218928 US9303033, P7, Table 22A, Compound 10
US9303033, I7, Table 22A, Compound 3 BDBM218916 US9303033, W3, Table 13A, Compound 5
US9303033, K7, Table 22A, Compound 5 BDBM218918 US9303033, Y3, Table 13A, Compound 7
US9303033, L8, Table 22A, Compound 32 BDBM218941 US9303033, V4, Table 13A, Compound 30
US9303033, N4, Table 13A, Compound 22 BDBM218933 US9303033, I8, Table 22A, Compound 29
US9303033, O7, Table 22A, Compound 9 BDBM218927 US9303033, H4, Table 13A, Compound 16
US9303033, P4, Table 13A, Compound 24 BDBM218935 US9303033, K8, Table 22A, Compound 31
US9303033, P8, Table 22A, Compound 36 BDBM218945 US9303033, Z4, Table 13A, Compound 34
US9303033, Q4, Table 13A, Compound 25 BDBM218936 US9303033, S7, Table 22A, Compound 13
US9303033, Q8, Table 22A, Compound 37 BDBM218948 US9303033, C5, Table 13A, Compound 37
US9303033, S4, Table 13A, Compound 27 US9303033, U7, Table 22A, Compound 15 BDBM218938
US9303033, T3, Table 13A, Compound 2 BDBM218913 US9303033, H7, Table 22A, Compound 2
US9303033, T7, Table 22A, Compound 14 BDBM218937 US9303033, R4, Table 13A, Compound 26
US9303033, U3, Table 13A, Compound 3 US9303033, Z7, Table 22A, Compound 20 BDBM218914
US9303033, V3, Table 13A, Compound 4 US9303033, A8, Table 22A, Compound 21 BDBM218915
US9303033, V7, Table 22A, Compound 16 BDBM218939 US9303033, T4, Table 13A, Compound 28
US9303033, X3, Table 13A, Compound 6 BDBM218917 US9303033, J7, Table 22A, Compound 4
US9303033, Z3, Table 13A, Compound 8 BDBM218919 US9303033, L7, Table 22A, Compound 6
pyrimidine deriv. 13a 6-(cyclohexylmethoxy)-5-[(1E)-(hydroxyimino)methyl]pyrimidine-2,4-diamine BDBM5582
US10221142, Example 13A-A US10221142, Example 13A-B BDBM359512 4-(1-(2-chloro-6-(1- cyanocyclopropyl) benzoyl)-6-(3- methoxyazetidine-1- carbonyl)-4,5,6,7- tetrahydro-1H- indazol-3-yl)-3- fluorobenzoic acid
2-[(3-chlorophenyl)methoxy]-3-methyl-4-(piperidin-4-yl)pyridine pyridylpiperidine, 13a BDBM28607
BDBM175368 1,3-Dimethyl-8-[4-{2-(dimethylaminoethylamino)-2-oxoethoxy}-phenyl]xanthine (13a, RB-420)
US20250197396, Compound 13a 1'-isobutyryl-2-oxospiro[indoline-3,4'-piperidine]-5-carboxylic acid BDBM752301
US10745364, Example 13A BDBM352513 US9809561, 13A (S)-1,1,1-trifluoro-2-methylpropan-2-yl (4-((4-fluorophenyl)sulfonyl)-2- ((morpholine-4-sulfonamido)methyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin-6- yl)carbamate
BDBM349895 2-{[4-{6-[(4-Chloro-2-fluorobenzyl)oxy]pyridin-2-yl}-2-methylpiperidin-1-yl]methyl}-1-(2-methoxyethyl)-1H-benzimidazole-6-carboxylic acid US10208019, Example 13A-01 US10208019, Example 13A-04
BDBM419131 3CLpro inhibitor 7j 3CLpro inhibitor 6j
Cyclophilin Inhibitor, 15 Cyclophilin Inhibitor, 3b BDBM85116
Nicotinamidase Inhibitor, 23 BDBM92856 PncA Inhibitor, 5
PDE5 Inhibitor, 8 BDBM93134 PDE5 Inhibitor, 5
(3-Pyridylmethylene)tetrahydronaphthalene 13a BDBM8595 3-{[(1E)-6-methoxy-1,2,3,4-tetrahydronaphthalen-1-ylidene]methyl}pyridine
(5Z)-5-{[3-(trifluoromethoxy)phenyl]methylidene}-1,3-thiazolidine-2,4-dione BDBM26635 thiazolidine-2,4-dione, 13a
1-amino-2,3-dihydro-1H-inden-4-yl N,N-dimethylcarbamate BDBM10742 Aminoindan deriv. 13a
Benzimidazole compound, 13a BDBM24202 2-{4-[2-(pyrrolidin-1-yl)ethoxy]phenoxy}-1H-1,3-benzodiazole
thiolate analogue, 13a tert-butyl N-[(1S)-1-[(3-phenylphenyl)carbamoyl]-6-sulfanylhexyl]carbamate BDBM19132
4-hydroxy thyromimetic, 13a BDBM18938 2-[3,5-dibromo-4-(4-hydroxy-3-phenoxyphenoxy)phenyl]acetic acid
N-(di-p-tolylmethyl)-6-oxo- 2-(trifluoromethyl)-1,6- dihydropyrimidine-5- carboxamide US11957687, Compound 13A BDBM667322
pyrrolopyrimidine, 13a BDBM24846 1-{7H-pyrrolo[2,3-d]pyrimidin-4-yl}-1,2-dihydrospiro[indole-3,4'-piperidine]
N-[2-(13a,14-Dihydro-6H,13H-pyrazino[1,2-a;4,5-a']diindol-7-yl)-ethyl]-acetamide N-[2-(13a,14-Dihydro-6H,13H-pyrazino[1,2-a:4,5-a']diindol-7-yl)-ethyl]-acetamide BDBM50273283 CHEMBL455909
BDBM103579 ATX inhibitor 10 analogue 9 ATX inhibitor 9
BDBM93428 PHD Inhibitor, 12{2,3,4} PHD Inhibitor, 12{2,4,4}
PHD Inhibitor, 12{2,3,2} PHD Inhibitor, 12{2,4,2} BDBM93423
ATX inhibitor 10 Monosubstituted aryl-Me ATX inhibitor 5 Disubstituted aryl-Me ATX inhibitor 3 BDBM103961
US8815951, Epoxide Hydrolase Inhibitor 22 BDBM129339 US8815951, Epoxide Hydrolase Inhibitor 21 US8815951, Epoxide Hydrolase Inhibitor 20
BDBM234335 Inhibitor A
Inhibitor, 16 BDBM92446
Inhibitor, 17 BDBM92447
Inhibitor, 18 BDBM92448
Inhibitor, 19 BDBM92449
BDBM32378 adenosine-derived inhibitor, 12 adenosine-derived inhibitor (Grp78), 13
MurC/D inhibitor (compound 25) MurD inhibitor (compound 35) BDBM119086
adenosine-derived inhibitor (Grp78), 14 adenosine-derived inhibitor, 15 BDBM32381
adenosine-derived inhibitor (Grp78), 8 BDBM32373 adenosine-derived inhibitor, 7
adenosine-derived inhibitor, 10 adenosine-derived inhibitor (Grp78), 11 BDBM32376
adenosine-derived inhibitor, 11 BDBM32377 adenosine-derived inhibitor (Grp78), 12
adenosine-derived inhibitor, 4 adenosine-derived inhibitor (Grp78), 2 BDBM32370
adenosine-derived inhibitor, 5 adenosine-derived inhibitor (Grp78), 3 BDBM32371
adenosine-derived inhibitor, 9 adenosine-derived inhibitor (Grp78), 9 BDBM32375
BDBM26709 benzothiazole analogue, 13a 1-(ethanesulfonyl)-N-[4-(6-methyl-1,3-benzothiazol-2-yl)phenyl]piperidine-4-carboxamide
CHEMBL193856 3-(4-methanesulfonylphenyl)-1-phenylprop-2-yn-1-one BDBM22344 1,3-Diarylprop-2-yn-1-one, 13a
N,12-dimethyl-14,15,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,15}]heptadeca-1,3,5,7,9,11,13,16-octaen-16-amine BDBM25924 benzopyrazoloquinazoline analogue, 13a
N-(4-{2,4-diamino-6-[(benzyloxy)methyl]pyrimidin-5-yl}phenyl)acetamide 2,4-diaminopyrimidine-based antagonist, 13a BDBM19355
[2-[(5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazol-3-yl]methylthio]acetic acid (13a) BDBM234284
aminomethylpyridine-based compound, 13a N-(2-aminophenyl)-4-[5-(azetidin-1-ylmethyl)-3-methylpyridin-2-yl]benzamide BDBM25232
CHEMBL515696 N-[2-(2,9-Dimethoxy-13a,14-dihydro-6H,13H-pyrazino[1,2-a;4,5-a']diindol-7-yl)-ethyl]-acetamide N-[2-(2,9-Dimethoxy-13a,14-dihydro-6H,13H-pyrazino[1,2-a:4,5-a']diindol-7-yl)-ethyl]-acetamide BDBM50266407
N-[2-(9-Methoxy-13a,14-dihydro-6H,13H-pyrazino[1,2-a;4,5-a']diindol-7-yl)-ethyl]-acetamide CHEMBL514413 N-[2-(9-Methoxy-13a,14-dihydro-6H,13H-pyrazino[1,2-a:4,5-a']diindol-7-yl)-ethyl]-acetamide BDBM50266406
BDBM136287 US8853212, DDP-4 Inhibitor 4 US8853212, DDP-4 Inhibitor 3
Pyridine-3-carbaldehyde BDBM50026863 Nicotinamidase Inhibitor, 16 PncA Inhibitor, 2 CHEMBL268493
US8815951, Epoxide Hydrolase Inhibitor 18 US8815951, Epoxide Hydrolase Inhibitor 19 BDBM129337
3CLpro inhibitor 7h BDBM419130
AANAT Inhibitor, 8c BDBM85586
AANAT Inhibitor, 8d BDBM85587
AANAT Inhibitor, 8e BDBM85588
AANAT Inhibitor, 8g BDBM85589
AANAT Inhibitor, 8h BDBM85590
ALR2 inhibitor, 8 BDBM228821
Aminopyrazole inhibitor, 3528 BDBM92523
Aminopyrazole inhibitor, 3576 BDBM92524
Aminopyrazole inhibitor, 3583 BDBM92525
Aminopyrazole inhibitor, 4018 BDBM92529
Aminopyrazole inhibitor, 4326 BDBM92526
Aminopyrazole inhibitor, 4642 BDBM92527
Aminopyrazole inhibitor, 4643 BDBM92528
BDBM104043 PDI inhibitor P6
BDBM104049 PDI inhibitor P12
BDBM104050 PDI inhibitor P13
BDBM104051 PDI inhibitor P14
BDBM104052 PDI inhibitor P15
BDBM104053 PDI inhibitor P16
BDBM104054 PDI inhibitor P17
BDBM104055 PDI inhibitor P18
BDBM104056 PDI inhibitor P19
BDBM104060 PDI inhibitor P23
BDBM104061 PDI inhibitor P24
BDBM104062 PDI inhibitor P25
BDBM104894 US8569313, Inhibitor 1
BDBM104895 US8569313, Inhibitor 2
BDBM104896 US8569313, Inhibitor 3
BDBM104897 US8569313, Inhibitor 4
BDBM104898 US8569313, Inhibitor 5
BDBM104899 US8569313, Inhibitor 6
BDBM104900 US8569313, Inhibitor 7
BDBM104901 US8569313, Inhibitor 8
BDBM104902 US8569313, Inhibitor 9
BDBM104903 US8569313, Inhibitor 10
BDBM104904 US8569313, Inhibitor 11
BDBM104905 US8569313, Inhibitor 13
BDBM104906 US8569313, Inhibitor 14
BDBM104909 US8569313, Inhibitor 18
BDBM104910 US8569313, Inhibitor 19
BDBM104915 US8569313, Inhibitor 29
BDBM104916 US8569313, Inhibitor 30
BDBM104917 US8569313, Inhibitor 31
BDBM104924 US8569313, Inhibitor 41
BDBM104927 US8569313, Inhibitor 44
BDBM104933 US8569313, Inhibitor 50
BDBM104934 US8569313, Inhibitor 51
BDBM104935 US8569313, Inhibitor 52
BDBM190662 LOX inhibitor, MLS000545091
BDBM190663 LOX inhibitor, 5
BDBM195610 KDM inhibitor, 3
BDBM205464 PPiase inhibitor, 1
BDBM205465 PPiase inhibitor, 6
BDBM205466 PPiase inhibitor, 9
BDBM205467 PPiase inhibitor, 11
BDBM205468 PPiase inhibitor, 12
BDBM205469 PPiase inhibitor, 13
BDBM205470 PPiase inhibitor, 14
BDBM205475 PPiase inhibitor, 19
BDBM205476 PPiase inhibitor, 20
BDBM214778 OPRT inhibitor, 1 
BDBM214779 OPRT inhibitor, 2
BDBM214780 OPRT inhibitor, 3
BDBM214787 OPRT inhibitor, 10
BDBM214788 OPRT inhibitor, 11
BDBM214789 OPRT inhibitor, 12
BDBM214790 OPRT inhibitor, 13
BDBM214791 OPRT inhibitor, 14
BDBM225236 BTK inhibitor, 1
BDBM225238 BTK inhibitor, 3
BDBM227631 MTH1 inhibitor, 14
BDBM227635 MTH1 inhibitor, 122
BDBM227636 MTH1 inhibitor, 123
BDBM227637 MTH1 inhibitor, 131
BDBM227638 MTH1 inhibitor, 132
BDBM228817 IspH inhibitor, 8
BDBM228822 ALR2 inhibitor, 11
BDBM233061 mtFabH inhibitor, 12
BDBM233062 mtFabH inhibitor, 15
BDBM233064 mtFabH inhibitor, 17
BDBM233065 mtFabH inhibitor, 19
BDBM233070 mtFabH inhibitor, 24
BDBM233071 mtFabH inhibitor, 25
BDBM233072 mtFabH inhibitor, 26
BDBM233073 mtFabH inhibitor, 27
BDBM233075 mtFabH inhibitor, 6
BDBM233076 mtFabH inhibitor, 7
BDBM233080 mtFabH inhibitor, 18
BDBM233081 mtFabH inhibitor, 28
BDBM233082 mtFabH inhibitor, 29
BDBM233084 mtFabH inhibitor, 31
BDBM233088 mtFabH inhibitor, 35
BDBM233090 mtFabH inhibitor, 37
BDBM233091 mtFabH inhibitor, 38
BDBM233092 mtFabH inhibitor, 39
BDBM234413 NA inhibitor, 1
BDBM234414 NA inhibitor, 3a
BDBM234415 NA inhibitor, 3b
BDBM234416 NA inhibitor, 3c
BDBM237233 hCA inhibitor, 4
BDBM237285 CA inhibitor, 5c
BDBM237286 CA inhibitor, 5d
BDBM237290 CA inhibitor, 5l
BDBM237291 CA inhibitor, 2
BDBM237340 CA inhibitor, 14
BDBM243049 PTP inhibitor, 4a
BDBM243059 PTP inhibitor, 4k
BDBM243060 PTP inhibitor, 4l
BDBM243061 PTP inhibitor, 4m
BDBM246596 TIM inhibitor, 1
BDBM27807 fluorescently labelled inhibitor
BDBM419121 3CLpro inhibitor 6a
BDBM419123 3CLpro inhibitor 7a
BDBM419124 3CLpro inhibitor 6c
BDBM419126 3CLpro inhibitor 7c
BDBM419127 3CLpro inhibitor 6e
BDBM419128 3CLpro inhibitor 7e
BDBM419129 3CLpro inhibitor 6h
BDBM419132 3CLpro inhibitor 7j
BDBM60960 hDDAH inhibitor, 2f
BDBM60969 CA inhibitor, 1
BDBM65493 eIF4A3 inhibitor, 2
BDBM65494 eIF4A3 inhibitor, 3
BDBM65495 SmNACE inhibitor, 1
BDBM65496 SmNACE inhibitor, 2
BDBM731600 US20250114359, Inhibitor 1
BDBM731630 US20250114359, Inhibitor 6
BDBM731631 US20250114359, Inhibitor 7
BDBM731657 US20250114359, Inhibitor 8
BDBM731658 US20250114359, Inhibitor 9
BDBM731661 US20250114359, Inhibitor 11
BDBM731665 US20250114359, Inhibitor 13
BDBM731673 US20250114359, Inhibitor 14
BDBM731675 US20250114359, Inhibitor 15
BDBM731676 US20250114359, Inhibitor 16
BDBM731677 US20250114359, Inhibitor 17
BDBM731684 US20250114359, Inhibitor 18
BDBM731688 US20250114359, Inhibitor 19
BDBM731750 US20250114359, Inhibitor 25
BDBM731757 US20250114359, Inhibitor 26
BDBM731763 US20250114359, Inhibitor 29
BDBM731772 US20250114359, Inhibitor 30
BDBM731982 US20250114359, Inhibitor 41
BDBM81435 CDK Inhibitor, 8
BDBM81436 CDK Inhibitor, 9
BDBM81437 CDK Inhibitor, 10
BDBM81438 CDK Inhibitor, 11
BDBM81439 CDK Inhibitor, 12
BDBM81440 CDK Inhibitor, 13
BDBM81441 CDK Inhibitor, 14
BDBM81624 MurF inhibitor, 3
BDBM81627 MurF inhibitor, 6
BDBM81628 MurF inhibitor, 12
BDBM81629 MurF inhibitor, 13
BDBM81630 MurF inhibitor, 14
BDBM81700 LpxC Inhibitor, L1
BDBM81701 LpxC Inhibitor, L2
BDBM81706 LpxC Inhibitor, L7
BDBM81708 LpxC Inhibitor, L9
BDBM81709 LpxC Inhibitor, L10
BDBM81710 LpxC Inhibitor, L11
BDBM81711 LpxC Inhibitor, L12
BDBM81712 LpxC Inhibitor, L13
BDBM81713 LpxC Inhibitor, L14
BDBM81714 LpxC Inhibitor, L15
BDBM81732 HSP90 Inhibitor, 6
BDBM81733 HSP90 Inhibitor, 7
BDBM84878 Fucosidase Inhibitor, 4
BDBM85115 Cyclophilin Inhibitor, 3a
BDBM85121 Cyclophilin Inhibitor, 15
BDBM85122 Thr1 inhibitor, 1
BDBM85294 Glucosidase inhibitor, 6a
BDBM85295 Glucosidase inhibitor, 6b
BDBM85296 Glucosidase inhibitor, 6c
BDBM85297 Glucosidase inhibitor, 6d
BDBM85298 Glucosidase inhibitor, 6e
BDBM85299 Glucosidase inhibitor, 6f
BDBM85300 Glucosidase inhibitor, 11
BDBM85428 NEP inhibitor, 6h
BDBM85429 NEP inhibitor, 6i
BDBM85430 NEP inhibitor, 6j
BDBM85437 NEP inhibitor, 6q
BDBM85438 NEP inhibitor, 6r
BDBM85439 NEP inhibitor, 6s
BDBM85591 AANAT Inhibitor, 8i
BDBM85592 AANAT Inhibitor, 12d
BDBM85773 Tyrosinase Inhibitor, 8
BDBM85774 Tyrosinase Inhibitor, 10
BDBM86112 LDHA Inhibitor, 1
BDBM86116 LDHA Inhibitor, 11
BDBM86121 LDHA Inhibitor, 16
BDBM86122 LDHA Inhibitor, 17
BDBM86123 LDHA Inhibitor, 18
BDBM86124 LDHA Inhibitor, 20
BDBM86125 LDHA Inhibitor, 21
BDBM86126 LDHA Inhibitor, 22
BDBM86130 LDHA Inhibitor, 26
BDBM86131 LDHA Inhibitor, 27
BDBM86132 LDHA Inhibitor, 28
BDBM86133 LDHA Inhibitor, 29
BDBM86134 LDHA Inhibitor, 30
BDBM86135 LDHA Inhibitor, 31
BDBM86136 LDHA Inhibitor, 32
BDBM86137 LDHA Inhibitor, 33
BDBM91592 dUTPase inhibitor, 3
BDBM92346 GSK3 Inhibitor, 2
BDBM92357 HGXPRT Inhibitor, 2
BDBM92442 MMP Inhibitor, 2
BDBM92444 MMP Inhibitor, 6
BDBM92522 Aminopyrazole inhibitor, 3451
BDBM92530 Aminopyrazole inhibitor, 4276
BDBM92850 Nicotinamidase Inhibitor, 17
BDBM92851 Nicotinamidase Inhibitor, 18
BDBM92852 Nicotinamidase Inhibitor, 19
BDBM92854 Nicotinamidase Inhibitor, 21
BDBM92859 PncA Inhibitor, 3
BDBM92860 PncA Inhibitor, 4
BDBM92861 PncA Inhibitor, 6
BDBM92865 KSP Inhibitor, 4d
BDBM92905 DDAH Inhibitor, 15
BDBM93029 CB2 Inhibitor, 5
BDBM93030 CB2 Inhibitor, 6
BDBM93031 CB2 Inhibitor, 7
BDBM93032 CB2 Inhibitor, 8
BDBM93106 COX inhibitor, 9
BDBM93109 PTP1B Inhibitor, 5
BDBM93112 PTP1B Inhibitor, 10
BDBM93113 PTP1B Inhibitor, 11
BDBM93117 PTP1B Inhibitor, 15
BDBM93118 PTP1B Inhibitor, 19
BDBM93139 PDE5 Inhibitor, 8
BDBM93140 PDE5 Inhibitor, 12
BDBM93207 Kinase inhibitor, 5
BDBM93227 Kinase inhibitor, C2
BDBM93228 Kinase inhibitor, D1
BDBM93229 Kinase inhibitor, F3
BDBM93254 CypA Inhibitor, 1d
BDBM93255 CypA Inhibitor, 1e
BDBM93260 CypA Inhibitor, 4a
BDBM93266 CypA Inhibitor, 4g
BDBM97453 FAAH Inhibitor, 2b
BDBM97454 FAAH Inhibitor, 2c
BDBM97455 FAAH Inhibitor, 2d
BDBM97456 FAAH Inhibitor, 2e
BDBM97460 FAAH Inhibitor, 2i
BDBM97461 FAAH Inhibitor, 2j
BDBM97462 FAAH Inhibitor, 2k
BDBM97463 FAAH Inhibitor, 2l
BTK inhibitor, 2 BDBM225237
Benzimidazole Inhibitor, 1 BDBM93208
Benzimidazole Inhibitor, 2 BDBM93209
Benzimidazole Inhibitor, 3 BDBM93210
Benzimidazole Inhibitor, 4 BDBM93211
Benzimidazole Inhibitor, 5 BDBM93212
Benzimidazole Inhibitor, 6 BDBM93213
Benzodiazepine Inhibitor, 7 BDBM93214
Bisanilinopyrimidine inhibitor, 3 BDBM87049
CA inhibitor, 12 BDBM237339
CA inhibitor, 5 BDBM236510
CA inhibitor, 5e BDBM237287
CA inhibitor, 5f BDBM237288
CA inhibitor, 5i BDBM237289
CA inhibitor, 6 BDBM236511
CB2 Inhibitor, 1 BDBM93025
CB2 Inhibitor, 10 BDBM93034
CB2 Inhibitor, 11 BDBM93035
CB2 Inhibitor, 12 BDBM93036
CB2 Inhibitor, 13 BDBM93037
CB2 Inhibitor, 2 BDBM93026
CB2 Inhibitor, 3 BDBM93027
CB2 Inhibitor, 4 BDBM93028
CB2 Inhibitor, 9 BDBM93033
CDK Inhibitor, 2 BDBM81429
CDK Inhibitor, 3 BDBM81430
CDK Inhibitor, 4 BDBM81431
CDK Inhibitor, 5 BDBM81432
CDK Inhibitor, 6 BDBM81433
CDK Inhibitor, 7 BDBM81434
COX inhibitor, 5a BDBM93103
COX inhibitor, 5b BDBM93104
COX inhibitor, 8 BDBM93105
Cyclophilin Inhibitor, 3c BDBM85117
Cyclophilin Inhibitor, 3d BDBM85118
Cyclophilin Inhibitor, 3e BDBM85119
Cyclophilin Inhibitor, 3f BDBM85120
CypA Inhibitor, 1a BDBM93251
CypA Inhibitor, 1b BDBM93252
CypA Inhibitor, 1c BDBM93253
CypA Inhibitor, 2a BDBM93256
CypA Inhibitor, 2b BDBM93257
CypA Inhibitor, 3a BDBM93258
CypA Inhibitor, 3b BDBM93259
CypA Inhibitor, 4b BDBM93261
CypA Inhibitor, 4c BDBM93262
CypA Inhibitor, 4d BDBM93263
CypA Inhibitor, 4e BDBM93264
CypA Inhibitor, 4f BDBM93265
FAAH Inhibitor, 2a BDBM97452
FAAH Inhibitor, 2f BDBM97457
FAAH Inhibitor, 2g BDBM97458
FAAH Inhibitor, 2h BDBM97459
HGXPRT Inhibitor, 3 BDBM92358
HSP90 Inhibitor, 4 BDBM81730
HSP90 Inhibitor, 5 BDBM81731
KSP Inhibitor, 4c BDBM92864
KSP Inhibitor, 4g BDBM92866
Kinase inhibitor, A1 BDBM93224
Kinase inhibitor, A2 BDBM93225
Kinase inhibitor, B1 BDBM93226
LDHA Inhibitor, 12 BDBM86117
LDHA Inhibitor, 13 BDBM86118
LDHA Inhibitor, 14 BDBM86119
LDHA Inhibitor, 15 BDBM86120
LDHA Inhibitor, 23 BDBM86127
LDHA Inhibitor, 24 BDBM86128
LDHA Inhibitor, 25 BDBM86129
LDHA Inhibitor, 34 BDBM86138
LDHA Inhibitor, 7 BDBM86113
LDHA Inhibitor, 8 BDBM86114
LDHA Inhibitor, 9 BDBM86115
LOX inhibitor, 13 BDBM190664
LpxC Inhibitor, L16 BDBM81715
LpxC Inhibitor, L17 BDBM81716
LpxC Inhibitor, L18 BDBM81717
LpxC Inhibitor, L3 BDBM81702
LpxC Inhibitor, L4 BDBM81703
LpxC Inhibitor, L5 BDBM81704
LpxC Inhibitor, L6 BDBM81705
MTH1 inhibitor, 120 BDBM227633
MTH1 inhibitor, 121 BDBM227634
MTH1 inhibitor, 53 BDBM227632
MgrA inhibitor, 2 BDBM81553
MgrA inhibitor, 3 BDBM81554
MgrA inhibitor, 4 BDBM81555
MurF inhibitor, 4 BDBM81625
MurF inhibitor, 5 BDBM81626
NA inhibitor, 3d BDBM234417
NEP inhibitor, 6g BDBM85427
NEP inhibitor, 6k BDBM85431
NEP inhibitor, 6l BDBM85432
NEP inhibitor, 6m BDBM85433
NEP inhibitor, 6n BDBM85434
NEP inhibitor, 6o BDBM85435
NEP inhibitor, 6p BDBM85436
Nicotinamidase Inhibitor, 20 BDBM92853
Nicotinamidase Inhibitor, 22 BDBM92855
Nicotinamidase Inhibitor, 24 BDBM92857
OPRT inhibitor, 15 BDBM214792
OPRT inhibitor, 16 BDBM214793
OPRT inhibitor, 17 BDBM214794
OPRT inhibitor, 18 BDBM214795
OPRT inhibitor, 19 BDBM214796
OPRT inhibitor, 20 BDBM214797
OPRT inhibitor, 4 BDBM214781
OPRT inhibitor, 5 BDBM214782
OPRT inhibitor, 6 BDBM214783
OPRT inhibitor, 7 BDBM214784
OPRT inhibitor, 8 BDBM214785
OPRT inhibitor, 9 BDBM214786
PDE5 Inhibitor, 1 BDBM93135
PDE5 Inhibitor, 19 BDBM93141
PDE5 Inhibitor, 4 BDBM93138
PDE5 Inhibitor, 6 BDBM93136
PDE5 Inhibitor, 9 BDBM93137
PDI inhibitor P1 BDBM104038
PDI inhibitor P10 BDBM104047
PDI inhibitor P11 BDBM104048
PDI inhibitor P2 BDBM104039
PDI inhibitor P20 BDBM104057
PDI inhibitor P21 BDBM104058
PDI inhibitor P22 BDBM104059
PDI inhibitor P7 BDBM104044
PDI inhibitor P8 BDBM104045
PDI inhibitor P9 BDBM104046
PDK1 inhibitor, 2 BDBM92402
PDK1 inhibitor, 4 BDBM92403
PDK1 inhibitor, 6 BDBM92405
PDK1 inhibitor, 7 BDBM92406
PHD Inhibitor, 5 BDBM93410
PPiase inhibitor, 15 BDBM205471
PPiase inhibitor, 16 BDBM205472
PPiase inhibitor, 17 BDBM205473
PPiase inhibitor, 18 BDBM205474
PPiase inhibitor, 21 BDBM205477
PTP inhibitor, 4b BDBM243050
PTP inhibitor, 4c BDBM243051
PTP inhibitor, 4d BDBM243052
PTP inhibitor, 4e BDBM243053
PTP inhibitor, 4f BDBM243054
PTP inhibitor, 4g BDBM243055
PTP inhibitor, 4h BDBM243056
PTP inhibitor, 4i BDBM243057
PTP inhibitor, 4j BDBM243058
PTP inhibitor, 4n BDBM243062
PTP1B Inhibitor, 12 BDBM93114
PTP1B Inhibitor, 13 BDBM93115
PTP1B Inhibitor, 14 BDBM93116
PTP1B Inhibitor, 6 BDBM93110
PTP1B Inhibitor, 7 BDBM93111
Phosphinate inhibitor 1 BDBM81615
Phosphinate inhibitor 2 BDBM81616
PncA Inhibitor, 1 BDBM92858
SmNACE inhibitor, 3 BDBM65500
TIM inhibitor, 2 BDBM246597
TIM inhibitor, 3 BDBM246598
Thr1 inhibitor, 4 BDBM85124
Thr1 inhibitor, 5 BDBM85125
Thr1 inhibitor, 6 BDBM85126
US11980631, Inhibitor Avibactam BDBM674469
US20250114359, Inhibitor 10 BDBM731659
US20250114359, Inhibitor 12 BDBM731664
US20250114359, Inhibitor 20 BDBM731727
US20250114359, Inhibitor 21 BDBM731732
US20250114359, Inhibitor 22 BDBM731735
US20250114359, Inhibitor 23 BDBM731749
US20250114359, Inhibitor 3 BDBM731606
US20250114359, Inhibitor 31 BDBM731791
US20250114359, Inhibitor 32 BDBM731824
US20250114359, Inhibitor 33 BDBM731895
US20250114359, Inhibitor 39 BDBM731914
US20250114359, Inhibitor 4 BDBM731611
US20250114359, Inhibitor 40 BDBM731921
US20250114359, Inhibitor 5 BDBM731627
US8569313, Inhibitor 15 BDBM104907
US8569313, Inhibitor 33 BDBM104919
US8569313, Inhibitor 35 BDBM104920
US8569313, Inhibitor 36 BDBM104921
US8569313, Inhibitor 38 BDBM104922
US8569313, Inhibitor 46 BDBM104929
US8569313, Inhibitor 47 BDBM104930
US8569313, Inhibitor 48 BDBM104931
US8569313, Inhibitor 49 BDBM104932
eIF4A3 inhibitor, 1 BDBM65492
hCA inhibitor, 1 BDBM237231
hCA inhibitor, 2 BDBM236545
hCA inhibitor, 2 BDBM60962
hCA inhibitor, 3 BDBM237232
hCA inhibitor, 5 BDBM237234
mtFabH inhibitor, 10 BDBM233059
mtFabH inhibitor, 11 BDBM233060
mtFabH inhibitor, 13 BDBM233078
mtFabH inhibitor, 14 BDBM233079
mtFabH inhibitor, 16 BDBM233063
mtFabH inhibitor, 2 BDBM233055
mtFabH inhibitor, 20 BDBM233066
mtFabH inhibitor, 21 BDBM233067
mtFabH inhibitor, 22 BDBM233068
mtFabH inhibitor, 23 BDBM233069
mtFabH inhibitor, 3 BDBM233056
mtFabH inhibitor, 30 BDBM233083
mtFabH inhibitor, 32 BDBM233085
mtFabH inhibitor, 33 BDBM233086
mtFabH inhibitor, 34 BDBM233087
mtFabH inhibitor, 36 BDBM233089
mtFabH inhibitor, 4 BDBM233057
mtFabH inhibitor, 40 BDBM233093
mtFabH inhibitor, 5 BDBM233074
mtFabH inhibitor, 8 BDBM233058
mtFabH inhibitor, 9 BDBM233077