BDBM411364 US10774056, Compound 070 US11542242, Compound 070 US10385031, Compound 070
BDBM271759 US10065941, Compound R-070 US9732060, Compound R-070
BDBM476920 US11345716, Compound II-070 US10870660, Compound II-070
US10065941, Compound I-070 BDBM271569 US9732060, Compound I-070
US10870660, Compound I-070 US11345716, Compound I-070 BDBM476880
BDBM105560 US8575197, I-070
BDBM184436 US9150578, I-070
BDBM230226 US9340500, I-070
BDBM235460 US9359338, Exe. 070
BDBM550222 US11306081, Example 070
BDBM586152 US11530244, Compound 070
BDBM588355 US11542274, Compound 070
BDBM716632 US20250034135, Compound 070
BDBM719157 US20250051277, Compound 070
BDBM730857 US20250122183, Example 070
BDBM733664 US20250115609, Compound 070
US8575197, II-070 BDBM106127
US9212130, I-070 BDBM196193
BDBM152163 US8987474, HL2-070-1
BDBM152164 US8987474, HL2-070-2
BDBM152165 US8987474, HL2-070-3
BDBM152166 US8987474, HL2-070-4
BDBM152168 US8987474, HL2-070-6
BDBM152169 US8987474, HL2-070-7
BDBM152170 US8987474, HL2-070-9
BDBM306861 US10150728, Example I-070
BDBM50465914 Branaplam LMI-070 LMI070
BDBM593787 US11578084, Compound I-070
BDBM601820 US11643396, Example MA1-070
BDBM640525 US20230399319, Example 2-070
BDBM661800 US20240101572, Example 2-070
BDBM731352 US12281099, Example I-070
US12247004, Compound ANASIA-070 BDBM726215
US20230286948, Compound HYBI-070 BDBM617679
US20240083872, Compound I-070 BDBM657860
US20240383900, Compound PPA-070 BDBM706406
US20250026765, Compound I-070 BDBM715463
US20250092056, Compound I-070 BDBM728468
US9550763, Compound I-070 BDBM244321
BDBM152170 BDBM152167 US8987474, HL2-070-5
US11643396, Example SG2-070-01 BDBM601813
BDBM710612 US12187701, Compound FMF-05-070-1
US10202389, Compound I-070 US9796725, Compound I-070 US9663525, Compound I-070 (rac)-((1R,2R,3S,4R)-4-(2-(4-fluoro-2-methoxyphenyl)pyrazolo[1,5-a]pyrimidin-7- BDBM329862
CHEMBL302625 US9120744, CDE-070 BDBM50058812 N,N'-1,3-Propanediylbis(3,4,5-trihydroxybenzamide)Hydrate
BDBM346043 4-{2-[6-Methyl-2-(3- trifluoromethyl- phenyl)-3H- benzoimidazol-5- ylamino]-thiazol-4- yl}-benzonitrile US10202370, Example 070
2-[1H-benzimidazol-2-yl-(5-fluoro- 2-hydroxy-phenyl)methyl]-8-fluoro- 6-[4-(1-methyl-4-piperidyl)phenyl]- isoquinolin-1-one; hydrochloride BDBM765185 US12391671, Compound 070
US11542283, Compound Velcade Dipeptidyl boronic acid derivative LDP-341 BORTEZOMIB Peptidyl boronic acid derivative PS-341 Velcade cid_387447 N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE CHEMBL325041 (R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-6-carboxamido)propanamido)butylboronic acid BDBM50069989 (R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butylboronic acid
- Nguyen, M; Marcellus, RC; Roulston, A; Watson, M; Serfass, L; Murthy Madiraju, SR; Goulet, D; Viallet, J; Bélec, L; Billot, X; Acoca, S; Purisima, E; Wiegmans, A; Cluse, L; Johnstone, RW; Beauparlant, P; Shore, GC Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A 104: 19512-7 (2007)
- Supuran, CT Bortezomib inhibits mammalian carbonic anhydrases. Bioorg Med Chem 25: 5064-5067 (2017)
- Supuran, CT Bortezomib inhibits bacterial and fungalß-carbonic anhydrases. Bioorg Med Chem 24: 4406-4409 (2016)
- Xu, Y; Yang, X; Chen, Y; Chen, H; Sun, H; Li, W; Xie, Q; Yu, L; Shao, L Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib. Bioorg Med Chem Lett 28: 2148-2152 (2018)
- Robinson, RM; Reyes, L; Duncan, RM; Bian, H; Strobel, ED; Hyman, SL; Reitz, AB; Dolloff, NG Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor. Eur J Med Chem 186: (2020)
- Lee, MJ; Bhattarai, D; Yoo, J; Miller, Z; Park, JE; Lee, S; Lee, W; Driscoll, JJ; Kim, KB Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib. J Med Chem 62: 4444-4455 (2019)
- Siegel, MB; Liu, SQ; Davare, MA; Spurgeon, SE; Loriaux, MM; Druker, BJ; Scott, EC; Tyner, JW Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma. Oncotarget 6: 18921-32
- Zhou, Y; Liu, X; Xue, J; Liu, L; Liang, T; Li, W; Yang, X; Hou, X; Fang, H Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma. J Med Chem 63: 4701-4715 (2020)
- Asfaha, Y; Bollmann, LM; Skerhut, AJ; Fischer, F; Horstick, N; Roth, D; Wecker, M; Mammen, C; Smits, SHJ; Fluegen, G; Kassack, MU; Kurz, T 5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib. Eur J Med Chem 263:
- Pati, ML; Vitale, P; Ferorelli, S; Iaselli, M; Miciaccia, M; Boccarelli, A; Di Mauro, GD; Fortuna, CG; Souza Domingos, TF; Rodrigues Pereira da Silva, LC; de Pádula, M; Cabral, LM; Sathler, PC; Vacca, A; Scilimati, A; Perrone, MG Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Eur J Med Chem 164: 59-76 (2019)
- ChEMBL_2581961 Inhibition of JAK in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581965 Inhibition of CSF1R in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581966 Inhibition of PKA in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581968 Inhibition of FLT3 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581969 Inhibition of PDGFRB in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581970 Inhibition of KIT in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581971 Inhibition of ALK5 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581973 Inhibition of RET in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581976 Inhibition of LCK in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581977 Inhibition of FYN in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581978 Inhibition of HCK in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581981 Inhibition of ERB2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581982 Inhibition of ERB4 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581985 Inhibition of PKCB in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581991 Inhibition of Hsp90 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581992 Inhibition of AKT in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582002 Inhibition of MEK1 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582006 Inhibition of PLK1 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582007 Inhibition of IKK in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582010 Inhibition of GSK3Beta in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582011 Inhibition of BET in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582017 Inhibition of IGF1R in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582018 Inhibition of ALK in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582019 Inhibition of IR in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582020 Inhibition of mTOR in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582025 Inhibition of AKT1 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582026 Inhibition of AKT2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582027 Inhibition of AKT3 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582028 Inhibition of IKKB in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582031 Inhibition of Src in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582033 Inhibition of PDPK1 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582034 Inhibition of Raf in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582036 Inhibition of Syk in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582038 Inhibition of STAT3 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582039 Inhibition of Abl in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582040 Inhibition of TNKS1 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582041 Inhibition of FGFR in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582042 Inhibition of survivin in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582044 Inhibition of VEGFR2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582045 Inhibition of JAK2V617F in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582046 Inhibition of TNKS2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582047 Inhibition of PKC in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582254 Inhibition of CDK2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581673 Inhibition of PKC in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581680 Inhibition of JAK in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581684 Inhibition of CSF1R in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581685 Inhibition of PKA in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581687 Inhibition of FLT3 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581688 Inhibition of PDGFRB in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581689 Inhibition of KIT in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581690 Inhibition of ALK5 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581692 Inhibition of RET in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581695 Inhibition of LCK in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581696 Inhibition of FYN in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581697 Inhibition of HCK in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581700 Inhibition of ERB2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581701 Inhibition of ERB4 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581704 Inhibition of PKCB in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581710 Inhibition of Hsp90 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581711 Inhibition of AKT in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581721 Inhibition of MEK1 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581725 Inhibition of PLK1 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581726 Inhibition of IKK in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581729 Inhibition of GSK3Beta in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581730 Inhibition of BET in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581736 Inhibition of IGF1R in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581738 Inhibition of IR in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581739 Inhibition of mTOR in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581745 Inhibition of AKT1 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581746 Inhibition of AKT2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581747 Inhibition of AKT3 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581748 Inhibition of IKKB in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581751 Inhibition of Src in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581754 Inhibition of PDPK1 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581755 Inhibition of Raf in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581757 Inhibition of Syk in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581759 Inhibition of STAT3 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581760 Inhibition of Abl in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581761 Inhibition of TNKS1 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581762 Inhibition of FGFR in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581763 Inhibition of survivin in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581765 Inhibition of VEGFR2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581766 Inhibition of JAK2V617F in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581767 Inhibition of TNKS2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581959 Inhibition of Aurora B in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581975 Inhibition of Src family in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581979 Inhibition of c-JUN in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581980 Inhibition of JAK1/JAK2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581984 Inhibition of ERB2/EGFR in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581989 Inhibition of EGFR/ERB2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581994 Inhibition of Bcl-2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582001 Inhibition of JAK-2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582012 Inhibition of PDGFRA/B in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582016 Inhibition of MEK1/2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582029 Inhibition of Aurora A in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582030 Inhibition of BCR-ABL in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582032 Inhibition of c-Met in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582035 Inhibition of BRAF-V600E in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2582247 Inhibition of CDK2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581678 Inhibition of Aurora B in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581694 Inhibition of Src family in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581698 Inhibition of c-JUN in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581699 Inhibition of JAK1/JAK2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581703 Inhibition of ERB2/EGFR in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581708 Inhibition of EGFR/ERB2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581713 Inhibition of Bcl-2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581720 Inhibition of JAK-2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581731 Inhibition of PDGFRA/B in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581735 Inhibition of MEK1/2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581749 Inhibition of Aurora A in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581750 Inhibition of BCR-ABL in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581756 Inhibition of BRAF-V600E in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581974 Inhibition of p-38a MAPK in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- ChEMBL_2581693 Inhibition of p-38a MAPK in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
- E3 Ligase dose-response_384 Molecular Library Screening Center Network (MLSCN) Penn Center for Molecular Discovery (PCMD) Assay Provider: Brent Stockwell, Columbia University MLSCN Grant: R03MH082369-01 The E3 ligases are involved in regulating other proteins by covalent ligation to the 76 amino acid protein ubiquitin. This post-translational modification can result in altered conformation, altered activity, or degradation of the substrate protein. Thus, E3 ligases are effectors of a major means of post-translational modification of proteins in many species, including mammals. The dipeptide boronic acid bortezomib is a potent proteasome inhibitor, has selective anticancer activity in tumor cells and in mice and was recently approved for clinical use in multiple myeloma. MDM2 E3 ligase is involved in numerous types of human cancer. Selective E3 ligase inhibitors would be preferable as they would be more selective and less toxic. Inhibitors of the MDM2-UBCH5 interaction should disrupt the E3 ligase activity of M
- E3 Ligase_Mutant_Dose Response Molecular Library Screening Center Network (MLSCN) Penn Center for Molecular Discovery (PCMD) Assay Provider: Brent Stockwell, Columbia University MLSCN Grant: R03MH082369-01 The E3 ligases are involved in regulating other proteins by covalent ligation to the 76 amino acid protein ubiquitin. This post-translational modification can result in altered conformation, altered activity, or degradation of the substrate protein. Thus, E3 ligases are effectors of a major means of post-translational modification of proteins in many species, including mammals. The dipeptide boronic acid bortezomib is a potent proteasome inhibitor, has selective anticancer activity in tumor cells and in mice and was recently approved for clinical use in multiple myeloma. MDM2 E3 ligase is involved in numerous types of human cancer. Selective E3 ligase inhibitors would be preferable as they would be more selective and less toxic. Inhibitors of the MDM2-UBCH5 interaction should disrupt the E3 ligase activity of M
- E3 Ligase_WT_Dose Response Molecular Library Screening Center Network (MLSCN) Penn Center for Molecular Discovery (PCMD) Assay Provider: Brent Stockwell, Columbia University MLSCN Grant: R03MH082369-01 The E3 ligases are involved in regulating other proteins by covalent ligation to the 76 amino acid protein ubiquitin. This post-translational modification can result in altered conformation, altered activity, or degradation of the substrate protein. Thus, E3 ligases are effectors of a major means of post-translational modification of proteins in many species, including mammals. The dipeptide boronic acid bortezomib is a potent proteasome inhibitor, has selective anticancer activity in tumor cells and in mice and was recently approved for clinical use in multiple myeloma. MDM2 E3 ligase is involved in numerous types of human cancer. Selective E3 ligase inhibitors would be preferable as they would be more selective and less toxic. Inhibitors of the MDM2-UBCH5 interaction should disrupt the E3 ligase activity of M
- Evaluation of NLRP3 Inflammasome Inhibitory Activity Assay The NLRP3 inflammasome inhibitory activity of test compounds were evaluated CM the basis of the inhibitory activity of the IL-1β, production in THP1-Null cells (Product Number: thp-null, InvivoGen). Cells were maintained for culture in RPMI-1640 media containing 10% (v/v) fetal bovine serum, 25 mmol/1. RUES, 100 U/mL penicillin, 100 μg/mL streptomycin, 100 μg/ml normocin, and 200 μg/mL hygromycin B (set at 37° C., 5% CO2/95% air). Cells were suspended with media for assay containing 0.5 μmol/L PMA (RPMI-1640 media containing 10% (v/v) fetal bovine serum, 100 U/mL penicillin, and 100 μg/mL streptomycin), and the suspended cells were seeded on Corning (registered trademark) 384-well Flat. Clear Bottom Black Polystyrene TC-treated Microplates (25,000 cells/25 μL/well)(followed by incubation (set at 37° C., 5% CO2/95% air) overnight supernatant of the culture was removed, and thereto was added media for assay (25 UL/well) containing 1 μg/mL Lipopolysaccharides (Product Number: L2654, Sigma-Aldrich (registered trademark)). Then, the culture was further incubated for 3 hours (set at 37° C., 5% CO2/91% air). The supernatant of the culture was removed. Then, a vehicle solution prepared from Opti-MEM (trademark) medium (Product Number: 31985-070, Invitrogen) was added to blank-setting wells and control-setting wells (20 μL/well), followed by incubation for 15 minutes (set at 37° C., 5% CO2/91% air). A solution containing a test compound (20 μL/well) was added to test compound-setting wells. Further, Opti-MEM (trademark) medium containing Nigericin (Product Number: N7143, Sigma-Aldrich (registered trademark)) was added to the control-setting wells and test compound-setting wells (5 μL/well), followed by incubation for 1.5 hours (set at 37° C., 5% CO2/95% air). The final concentration of Nigericin was adjusted to be 7.5 μmol/L, 5 μL/well of Opti-MEM (trademark) medium was added to the blank setting wells. The supernatant of the culture was cryonically stored (set at −20° C.) until measurement of IL-1β.
- Evaluation of NLRP3 Inflammasome Inhibitory Activity Assay The NLRP3 inflammasome inhibitory activity of test compounds were evaluated on the basis of the inhibitory activity of the IL-1β production in THP1-Null cells (Product Number: thp-null, InvivoGen). Cells were maintained for culture in RPMI-1640 media containing 10% (v/v) fetal bovine serum, 25 mmol/L HEPES, 100 U/mL penicillin, 100 μg/mL streptomycin, 100 μg/mL normocin, and 200 μg/mL hygromycin B (set at 37° C., 5% CO2/95% air). Cells were suspended with media for assay containing 0.5 μmol/L PMA (RPMI-1640 media containing 10% (v/v) fetal bovine serum, 100 U/mL penicillin, and 100 μg/mL streptomycin), and the suspended cells were seeded on Corning (registered trademark) 384-well Flat Clear Bottom Black Polystyrene TC-treated Microplates (25,000 cells/25 μL/well), followed by incubation (set at 37° C., 5% CO2/95% air) overnight. The supernatant of the culture was removed, and thereto was added media for assay (25 μL/well) containing 1 μg/mL Lipopolysaccharides (Product Number: L2654, Sigma-Aldrich (registered trademark)). Then, the culture was further incubated for 3 hours (set at 37° C., 5% CO2/95% air). The supernatant of the culture was removed. Then, a vehicle solution prepared from Opti-MEM (trademark) medium (Product Number: 31985-070, Invitrogen) was added to blank-setting wells and control-setting wells (20 μL/well), followed by incubation for 15 minutes (set at 37° C., 5% CO2/95% air). A solution containing a test compound (20 μL/well) was added to test compound-setting wells. Further, Opti-MEM (trademark) medium containing Nigericin (Product Number: N7143, Sigma-Aldrich (registered trademark)) was added to the control-setting wells and test compound-setting wells (5 μL/well), followed by incubation for 1.5 hours (set at 37° C., 5% CO2/95% air). The final concentration of Nigericin was adjusted to be 7.5 μmol/L. 5 μL/well of Opti-MEM (trademark) medium was added to the blank-setting wells. The supernatant of the culture was cryonically stored (set at −20° C.) until measurement of IL-1β.