TY82 |
Function assay |
0.2 to 1 uM |
24 hrs |
Inhibition of BRD4 in human TY82 cells assessed as reduction in c-Myc protein expression at 0.2 to 1 uM after 24 hrs by Western blot analysis |
29525435 |
TY82 |
Function assay |
0.2 to 1 uM |
24 hrs |
Inhibition of BRD4 in human TY82 cells assessed as reduction in c-Myc mRNA expression at 0.2 to 1 uM after 24 hrs by RT-PCR analysis |
29525435 |
TY82 or NCI-H1299 |
Function assay |
0.2 to 1 uM |
24 hrs |
Inhibition of BRD4 in human TY82 or NCI-H1299 cells assessed as reduction in PD-L1 protein expression at 0.2 to 1 uM after 24 hrs by Western blot analysis |
29525435 |
TY82 or NCI-H1299 |
Function assay |
0.2 to 1 uM |
24 hrs |
Inhibition of BRD4 in human TY82 or NCI-H1299 cells assessed as reduction in PD-L1 mRNA expression at 0.2 to 1 uM after 24 hrs by RT-PCR analysis |
29525435 |
HepG2 |
Function assay |
|
18 hrs |
Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay, EC50 = 0.7 μM. |
21568322 |
HepG2 |
Function assay |
|
6 hrs |
Induction of human ApoA1 protein synthesis in human HepG2 cells assessed as neosynthesised radiolabeled protein secretion after 6 hrs by SDS PAGE analysis in presence of [35S]methionine |
21568322 |
HepG2 |
Function assay |
|
18 hrs |
Upregulation of ApoA1 expression in human HepG2 cells assessed as concentration required to increase 70% of luciferase activity after 18 hrs by luciferase reporter gene assay, EC170 = 0.2 μM. |
22386529 |
HepG2 |
Function assay |
|
18 hrs |
Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay, EC50 = 0.7 μM. |
22924434 |
Raji |
Function assay |
|
4 hrs |
Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs, IC50 = 0.19 μM. |
24900758 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0303 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0323 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0388 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0492 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0539 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0568 μM. |
26080064 |
MV4-11 |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay, IC50 = 0.093 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50 = 0.0984 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50 = 0.156 μM. |
26080064 |
MOLM13 |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay, IC50 = 0.241 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, Ki = 0.023 μM. |
28463487 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, Ki = 0.0464 μM. |
28463487 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, IC50 = 0.0775 μM. |
28463487 |
MV4-11 |
Growth inhibition assay |
|
4 days |
Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay, IC50 = 0.093 μM. |
28463487 |
Rosetta2 DE3 |
Function assay |
|
30 mins |
Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, IC50 = 0.145 μM. |
28463487 |
MOLM13 |
Growth inhibition assay |
|
4 days |
Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay, IC50 = 0.241 μM. |
28463487 |
TY82 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.2 μM. |
28586718 |
MM1S |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay, IC50 = 0.23 μM. |
28586718 |
BL21 (DE3)-codon plus-RIL |
Function assay |
|
4 hrs |
Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay, IC50 = 0.26 μM. |
28586718 |
NALM16 |
Cytotoxicity assay |
|
5 days |
Cytotoxicity against human NALM16 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 0.27 μM. |
29170024 |
NALM6 |
Cytotoxicity assay |
|
5 days |
Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 0.39 μM. |
29170024 |
697 |
Cytotoxicity assay |
|
5 days |
Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 1.17 μM. |
29170024 |
HD-MB03 |
Cytotoxicity assay |
|
5 days |
Cytotoxicity against human HD-MB03 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 3.5 μM. |
29170024 |
TY82 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.3043 μM. |
29525435 |
MM1S |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay, IC50 = 0.3492 μM. |
29525435 |
C4-2B |
Antiproliferative assay |
|
96 hrs |
Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay |
29541371 |
22Rv1 |
Antiproliferative assay |
|
96 hrs |
Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay |
29541371 |
LNCAP |
Antiproliferative assay |
|
96 hrs |
Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay |
29541371 |
MV411 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human MV411 cells after 72 hrs by CellTiter-Glo assay, IC50 = 0.8 μM. |
30268702 |
PBMC |
Antiinflammatory assay |
|
|
Antiinflammatory activity against human PBMC cells assessed as LPS-induced IL-6 production by chemiluminescence assay, IC50 = 0.31623 μM. |
24015967 |
Rosetta2 DE3 |
Function assay |
|
|
Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0407 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
|
Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0454 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
|
Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0476 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
|
Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0607 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
|
Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0994 μM. |
26080064 |
Rosetta2 DE3 |
Function assay |
|
|
Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.159 μM. |
26080064 |
BL21(DE3) |
Function assay |
|
|
Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.065 μM. |
26367539 |
BL21(DE3) |
Function assay |
|
|
Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.095 μM. |
26367539 |
BL21(DE3) |
Function assay |
|
|
Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.1 μM. |
26367539 |
BL21(DE3) |
Function assay |
|
|
Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.23 μM. |
26367539 |
BL21(DE3)-R3-pRARE2 |
Function assay |
|
|
Inhibition of human His-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay, IC50 = 0.036 μM. |
26731490 |
BL21(DE3)-R3-pRARE2 |
Function assay |
|
|
Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay, IC50 = 0.036 μM. |
26731490 |
THP1 |
Antiproliferative assay |
|
|
Antiproliferative activity against human THP1 cells, IC50 = 0.29 μM. |
28939121 |
TY82 |
Antiproliferative assay |
|
|
Antiproliferative activity against human TY82 cells, IC50 = 0.39 μM. |
28939121 |
A673 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells |
29435139 |
DAOY |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells |
29435139 |
Saos-2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells |
29435139 |
BT-37 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells |
29435139 |
RD |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells |
29435139 |
MG 63 (6-TG R) |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells |
29435139 |
NB1643 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells |
29435139 |
OHS-50 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells |
29435139 |
Rh41 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells |
29435139 |
SJ-GBM2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells |
29435139 |
SK-N-MC |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells |
29435139 |
NB-EBc1 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells |
29435139 |
LAN-5 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells |
29435139 |
HL60 |
Cytotoxicity assay |
|
|
Cytotoxicity against human HL60 cells by MTS assay, IC50 = 0.12 μM. |
29657099 |
Raji |
Function assay |
|
|
Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method, IC50 = 0.132 μM. |
29657099 |
LNCAP |
Antiproliferative assay |
|
|
Antiproliferative activity against human LNCAP cells, IC50 = 0.3565 μM. |
29758518 |