PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
35399501-0	2022	AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	20-24
34693628-9	2022	CONCLUSIONS: We suggest that AZD5153, a novel dual-BRD4 inhibitor, can reduce MYCN levels in both anaplastic and nonanaplastic Wilms tumor cell lines, reduces tumor volume in Wilms tumor PDXs, and should be further explored for its therapeutic potential.	AZD5153	29-36	bromodomain containing 4	Mus musculus	51-55
34693628-9	2022	CONCLUSIONS: We suggest that AZD5153, a novel dual-BRD4 inhibitor, can reduce MYCN levels in both anaplastic and nonanaplastic Wilms tumor cell lines, reduces tumor volume in Wilms tumor PDXs, and should be further explored for its therapeutic potential.	AZD5153	29-36	MYCN proto-oncogene, bHLH transcription factor	Homo sapiens	78-82
35480096-7	2022	Moreover, addition of the bromodomain-containing protein 4 inhibitor AZD5153 increased the anticancer effect of talazoparib via MUS81 inhibition in gastric cancer cells, and this combination effect was largely impaired when MUS81 was knocked down.	AZD5153	69-76	bromodomain containing 4	Homo sapiens	26-58
35480096-7	2022	Moreover, addition of the bromodomain-containing protein 4 inhibitor AZD5153 increased the anticancer effect of talazoparib via MUS81 inhibition in gastric cancer cells, and this combination effect was largely impaired when MUS81 was knocked down.	AZD5153	69-76	MUS81 structure-specific endonuclease subunit	Homo sapiens	128-133
35480096-9	2022	Therefore, AZD5153 combined with talazoparib may represent a promising therapeutic strategy for patients with MUS81 proficient gastric cancer.	AZD5153	11-18	MUS81 structure-specific endonuclease subunit	Homo sapiens	110-115
35399501-10	2022	In conclusion, our results identified novel targets of BRD4 in the HCCLM3 cell genome and demonstrated anti-HCC efficacy of AZD5153, which was potentiated in combination with an NAMPT inhibitor.	AZD5153	124-131	bromodomain containing 4	Homo sapiens	55-59
34942306-0	2022	AZD5153 reverses palbociclib resistance in ovarian cancer by inhibiting cell cycle-related proteins and the MAPK/PI3K-AKT pathway.	AZD5153	0-7	AKT serine/threonine kinase 1	Homo sapiens	118-121
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	AZD5153	236-243	AKT serine/threonine kinase 1	Homo sapiens	72-75
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	AZD5153	236-243	bromodomain containing 4	Homo sapiens	197-218
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	AZD5153	236-243	bromodomain containing 4	Homo sapiens	220-224
34942306-7	2022	Based on these results, it is anticipated that this class of drugs, including AZD5153, which inhibit the cell cycle-related protein and MAPK/PI3K-AKT pathway, will exhibit synergistic effects with palbociclib in OC.	AZD5153	78-85	AKT serine/threonine kinase 1	Homo sapiens	146-149
34160250-4	2021	Introduction of BRD4 inhibitor AZD5153 to senescent epithelial cells reversed this effect and reduced SASP related inflammatory molecule release in TMNK-1 or EAhy926 as representative human endothelial cell line, when exposed to cell culture medium (CM) derived from A549 cells expressing SARS-CoV-2 spike protein, also exhibited a senescence phenotype with enhanced p16, p21, SA-beta-galactosidase expression, and triggered SASP pathways.	AZD5153	31-38	bromodomain containing 4	Homo sapiens	16-20
34160250-4	2021	Introduction of BRD4 inhibitor AZD5153 to senescent epithelial cells reversed this effect and reduced SASP related inflammatory molecule release in TMNK-1 or EAhy926 as representative human endothelial cell line, when exposed to cell culture medium (CM) derived from A549 cells expressing SARS-CoV-2 spike protein, also exhibited a senescence phenotype with enhanced p16, p21, SA-beta-galactosidase expression, and triggered SASP pathways.	AZD5153	31-38	surface glycoprotein	Severe acute respiratory syndrome coronavirus 2	300-305
34160250-4	2021	Introduction of BRD4 inhibitor AZD5153 to senescent epithelial cells reversed this effect and reduced SASP related inflammatory molecule release in TMNK-1 or EAhy926 as representative human endothelial cell line, when exposed to cell culture medium (CM) derived from A549 cells expressing SARS-CoV-2 spike protein, also exhibited a senescence phenotype with enhanced p16, p21, SA-beta-galactosidase expression, and triggered SASP pathways.	AZD5153	31-38	cyclin dependent kinase inhibitor 2A	Homo sapiens	367-370
34160250-4	2021	Introduction of BRD4 inhibitor AZD5153 to senescent epithelial cells reversed this effect and reduced SASP related inflammatory molecule release in TMNK-1 or EAhy926 as representative human endothelial cell line, when exposed to cell culture medium (CM) derived from A549 cells expressing SARS-CoV-2 spike protein, also exhibited a senescence phenotype with enhanced p16, p21, SA-beta-galactosidase expression, and triggered SASP pathways.	AZD5153	31-38	H3 histone pseudogene 16	Homo sapiens	372-375
34160250-4	2021	Introduction of BRD4 inhibitor AZD5153 to senescent epithelial cells reversed this effect and reduced SASP related inflammatory molecule release in TMNK-1 or EAhy926 as representative human endothelial cell line, when exposed to cell culture medium (CM) derived from A549 cells expressing SARS-CoV-2 spike protein, also exhibited a senescence phenotype with enhanced p16, p21, SA-beta-galactosidase expression, and triggered SASP pathways.	AZD5153	31-38	galactosidase beta 1	Homo sapiens	380-398
35399501-0	2022	AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	80-84
35399501-2	2022	Here, we determined the anti-HCC efficacy of AZD5153, a potent bivalent BRD4 inhibitor, and elucidated its underlying molecular mechanism of action.	AZD5153	45-52	bromodomain containing 4	Homo sapiens	72-76
35399501-5	2022	Mapping of BRD4- chromosomal targets by ChIP-seq analysis identified the occupancy of BRD4 with the promoters, gene bodies, and super-enhancers of both mRNA and noncoding RNA genes, which were disrupted upon AZD5153 treatment.	AZD5153	208-215	bromodomain containing 4	Mus musculus	11-15
35399501-5	2022	Mapping of BRD4- chromosomal targets by ChIP-seq analysis identified the occupancy of BRD4 with the promoters, gene bodies, and super-enhancers of both mRNA and noncoding RNA genes, which were disrupted upon AZD5153 treatment.	AZD5153	208-215	bromodomain containing 4	Mus musculus	86-90
35399501-6	2022	RNA-seq analysis of polyadenylated RNAs showed several BRD4 target genes involved in DNA replication, cell proliferation, and anti-apoptosis were repressed in AZD5153-treated HCC cells.	AZD5153	159-166	bromodomain containing 4	Mus musculus	55-59
35399501-8	2022	Interestingly, AZD5153 treatment upregulated NAMPT, whose product is the rate-limiting enzyme for NAD+ synthesis from nicotinamide.	AZD5153	15-22	nicotinamide phosphoribosyltransferase	Mus musculus	45-50
35399501-9	2022	This may explain why AZD5153 acted in concert with FK866, a potent NAMPT inhibitor, in reducing HCC cell proliferation and clonogenic survival.	AZD5153	21-28	nicotinamide phosphoribosyltransferase	Mus musculus	67-72
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	29-61
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	63-67
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	85-89
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	85-89
33838899-11	2021	Dinaciclib-AZD5153 combination therapy can be effective against MYCN-amplified and TERT-overexpressing neuroblastoma tumors.	AZD5153	11-18	MYCN proto-oncogene, bHLH transcription factor	Homo sapiens	64-68
33838899-11	2021	Dinaciclib-AZD5153 combination therapy can be effective against MYCN-amplified and TERT-overexpressing neuroblastoma tumors.	AZD5153	11-18	telomerase reverse transcriptase	Homo sapiens	83-87
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	5'-nucleotidase ecto	Homo sapiens	92-96
33717143-5	2021	This is supported by pharmacological targeting where the first-generation pan-BET bromodomain inhibitor JQ1(+) displays anti-inflammatory effects and inhibit tumor cell eradication, while the novel bivalent BET bromodomain inhibitor AZD5153, which shows differential activity towards BET family members, does not.	AZD5153	233-240	delta/notch like EGF repeat containing	Homo sapiens	207-210
33717143-5	2021	This is supported by pharmacological targeting where the first-generation pan-BET bromodomain inhibitor JQ1(+) displays anti-inflammatory effects and inhibit tumor cell eradication, while the novel bivalent BET bromodomain inhibitor AZD5153, which shows differential activity towards BET family members, does not.	AZD5153	233-240	delta/notch like EGF repeat containing	Homo sapiens	207-210
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	POU class 5 homeobox 1	Homo sapiens	187-193
33574760-4	2020	Methods: We retrieved and reviewed published reports on the clinical trials of twelve BET inhibitors including AZD5153, ABBV-075, BMS-986158, CPI-0610, GSK525762, OTX-015, PLX51107, INCB054329, INCB057643, FT-1101, CC-90010, and ODM-207 for patients with hematological malignancies and solid tumors and summarized their published target genes.	AZD5153	111-118	delta/notch like EGF repeat containing	Homo sapiens	86-89
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	Thy-1 cell surface antigen	Homo sapiens	97-101
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	SRY-box transcription factor 2	Homo sapiens	194-198
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	platelet and endothelial cell adhesion molecule 1	Homo sapiens	108-112
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	Nanog homeobox	Homo sapiens	199-204
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	CD34 molecule	Homo sapiens	113-117
33407870-5	2021	RESULTS: We found the combination of LLY-507 and AZD5153 was sufficient for high-efficiency CD73+CD90+CD105+CD31-CD34-CD45-HLA-DR- MSC induction from both hESCs and hiPSCs with stemness (POU5F1/SOX2/NANOG).	AZD5153	49-56	protein tyrosine phosphatase receptor type C	Homo sapiens	118-122
29931583-0	2019	Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2.	AZD5153	46-53	bromodomain containing 4	Homo sapiens	18-42
31142662-6	2019	Furthermore, Mus81 promoted migration of gastric cancer cells both in vitro and in vivo We conducted a drug screen using a collection of preclinical and FDA-approved drugs and found that the BRD4 inhibitor AZD5153 inhibited the expression of Mus81 and ZEB1 by regulating the epigenetic factor Sirt5.	AZD5153	206-213	MUS81 structure-specific endonuclease subunit	Homo sapiens	13-18
31142662-6	2019	Furthermore, Mus81 promoted migration of gastric cancer cells both in vitro and in vivo We conducted a drug screen using a collection of preclinical and FDA-approved drugs and found that the BRD4 inhibitor AZD5153 inhibited the expression of Mus81 and ZEB1 by regulating the epigenetic factor Sirt5.	AZD5153	206-213	bromodomain containing 4	Homo sapiens	191-195
31142662-6	2019	Furthermore, Mus81 promoted migration of gastric cancer cells both in vitro and in vivo We conducted a drug screen using a collection of preclinical and FDA-approved drugs and found that the BRD4 inhibitor AZD5153 inhibited the expression of Mus81 and ZEB1 by regulating the epigenetic factor Sirt5.	AZD5153	206-213	MUS81 structure-specific endonuclease subunit	Homo sapiens	242-247
31142662-6	2019	Furthermore, Mus81 promoted migration of gastric cancer cells both in vitro and in vivo We conducted a drug screen using a collection of preclinical and FDA-approved drugs and found that the BRD4 inhibitor AZD5153 inhibited the expression of Mus81 and ZEB1 by regulating the epigenetic factor Sirt5.	AZD5153	206-213	zinc finger E-box binding homeobox 1	Homo sapiens	252-256
31142662-6	2019	Furthermore, Mus81 promoted migration of gastric cancer cells both in vitro and in vivo We conducted a drug screen using a collection of preclinical and FDA-approved drugs and found that the BRD4 inhibitor AZD5153 inhibited the expression of Mus81 and ZEB1 by regulating the epigenetic factor Sirt5.	AZD5153	206-213	sirtuin 5	Homo sapiens	293-298
31142662-7	2019	As expected, AZD5153 treatment significantly reduced the migration of gastric cancer cells overexpressing Mus81 in vitro and in vivo Collectively, we show that Mus81 is a regulator of ZEB1 and promotes metastasis in gastric cancer.	AZD5153	13-20	MUS81 structure-specific endonuclease subunit	Homo sapiens	106-111
31142662-7	2019	As expected, AZD5153 treatment significantly reduced the migration of gastric cancer cells overexpressing Mus81 in vitro and in vivo Collectively, we show that Mus81 is a regulator of ZEB1 and promotes metastasis in gastric cancer.	AZD5153	13-20	MUS81 structure-specific endonuclease subunit	Homo sapiens	160-165
31142662-7	2019	As expected, AZD5153 treatment significantly reduced the migration of gastric cancer cells overexpressing Mus81 in vitro and in vivo Collectively, we show that Mus81 is a regulator of ZEB1 and promotes metastasis in gastric cancer.	AZD5153	13-20	zinc finger E-box binding homeobox 1	Homo sapiens	184-188
31142662-8	2019	Importantly, we demonstrate that the BRD4 inhibitor AZD5153 can potentially be used as an effective antimetastasis drug because of its effect on Mus81.	AZD5153	52-59	bromodomain containing 4	Homo sapiens	37-41
31142662-8	2019	Importantly, we demonstrate that the BRD4 inhibitor AZD5153 can potentially be used as an effective antimetastasis drug because of its effect on Mus81.	AZD5153	52-59	MUS81 structure-specific endonuclease subunit	Homo sapiens	145-150
32184777-0	2020	BRD4 Inhibition by AZD5153 Promotes Antitumor Immunity via Depolarizing M2 Macrophages.	AZD5153	19-26	bromodomain containing 4	Homo sapiens	0-4
32184777-5	2020	AZD5153 inhibiting BRD4, as a potential therapeutic strategy for HGSOC, was demonstrated to confer controversial plasticity on TAMs, which shows the need to uncover its impact on TAMs in HGSOC.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	19-23
32184777-8	2020	This modification occurs on MAF transcripts in TAMs and modified by BRD4, which is the target of AZD5153.	AZD5153	97-104	MAF bZIP transcription factor	Homo sapiens	28-31
32184777-8	2020	This modification occurs on MAF transcripts in TAMs and modified by BRD4, which is the target of AZD5153.	AZD5153	97-104	bromodomain containing 4	Homo sapiens	68-72
32184777-9	2020	Importantly, the 3-D microfluid model demonstrates that AZD5153 sensitizes ovarian cancer to anti-PD-L1 therapy.	AZD5153	56-63	CD274 molecule	Homo sapiens	98-103
32184777-10	2020	Our results clarify that besides eliminating tumor cells directly, AZD5153 works as a regulator of the TAM phenotype, providing a novel strategy combining AZD5153 and PD-1/PD-L1 antibody that could benefit HGSOC patients.	AZD5153	67-74	CD274 molecule	Homo sapiens	172-177
31199520-6	2020	Two BET inhibitors, JQ1 and AZD5153, increased and prolonged AZD1775-induced DNA double-strand breaks (DSBs) and concomitantly repressed genes related to nonhomologous end joining (NHEJ), including XRCC4 and SHLD1.	AZD5153	28-35	X-ray repair cross complementing 4	Homo sapiens	198-203
30696721-14	2019	Panobinostat (IC50, 0.4-1.3 nmol/L) and a bivalent BET inhibitor, AZD5153 (IC50, 3.7-8.2 nmol/L), also showed remarkable efficacies.	AZD5153	66-73	delta/notch like EGF repeat containing	Homo sapiens	51-54
31523195-0	2019	BRD4 Inhibitor AZD5153 Suppresses the Proliferation of Colorectal Cancer Cells and Sensitizes the Anticancer Effect of PARP Inhibitor.	AZD5153	15-22	bromodomain containing 4	Homo sapiens	0-4
31523195-0	2019	BRD4 Inhibitor AZD5153 Suppresses the Proliferation of Colorectal Cancer Cells and Sensitizes the Anticancer Effect of PARP Inhibitor.	AZD5153	15-22	poly(ADP-ribose) polymerase 1	Homo sapiens	119-123
31523195-2	2019	AZD5153, a novel specific BRD4 inhibitor, showed potent anticancer effects in several cancer types, but its therapeutic potential has not been fully evaluated in colorectal cancer cells.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	26-30
31523195-3	2019	Objective: We sought to evaluate the therapeutic potential of BRD4 inhibition of by AZD5153 and its combined anticancer cancer effect with PARP inhibitor BMN673 in vitro and in vivo in colorectal cancer.	AZD5153	84-91	bromodomain containing 4	Homo sapiens	62-66
31523195-10	2019	The clonogenic and MTT assays and PI/Annexin V staining demonstrated that AZD5153 significantly suppressed cell proliferation and induced apoptosis in colorectal cancer cells HCT116 and LoVo.	AZD5153	74-81	annexin A5	Homo sapiens	37-46
31523195-11	2019	Western blotting showed that AZD5153 inhibited the expression of c-Myc and increased expression of the apoptosis markers, cleaved caspase-3 and poly(ADP-ribose) polymerase (PARP), besides, we found that BRD4 knockdown could also inhibited cell proliferation and induced cell apoptosis.	AZD5153	29-36	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	65-70
31523195-11	2019	Western blotting showed that AZD5153 inhibited the expression of c-Myc and increased expression of the apoptosis markers, cleaved caspase-3 and poly(ADP-ribose) polymerase (PARP), besides, we found that BRD4 knockdown could also inhibited cell proliferation and induced cell apoptosis.	AZD5153	29-36	caspase 3	Homo sapiens	130-139
31523195-11	2019	Western blotting showed that AZD5153 inhibited the expression of c-Myc and increased expression of the apoptosis markers, cleaved caspase-3 and poly(ADP-ribose) polymerase (PARP), besides, we found that BRD4 knockdown could also inhibited cell proliferation and induced cell apoptosis.	AZD5153	29-36	poly(ADP-ribose) polymerase 1	Homo sapiens	144-171
31523195-11	2019	Western blotting showed that AZD5153 inhibited the expression of c-Myc and increased expression of the apoptosis markers, cleaved caspase-3 and poly(ADP-ribose) polymerase (PARP), besides, we found that BRD4 knockdown could also inhibited cell proliferation and induced cell apoptosis.	AZD5153	29-36	poly(ADP-ribose) polymerase 1	Homo sapiens	173-177
31523195-11	2019	Western blotting showed that AZD5153 inhibited the expression of c-Myc and increased expression of the apoptosis markers, cleaved caspase-3 and poly(ADP-ribose) polymerase (PARP), besides, we found that BRD4 knockdown could also inhibited cell proliferation and induced cell apoptosis.	AZD5153	29-36	bromodomain containing 4	Homo sapiens	203-207
31523195-12	2019	Moreover, AZD5153 inhibited the expression of Wee1 and impaired G2M cell cycle checkpoint, thus sensitized the anticancer effect of BMN673 in vitro and in vivo.	AZD5153	10-17	WEE1 G2 checkpoint kinase	Homo sapiens	46-50
29931583-0	2019	Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2.	AZD5153	46-53	BCL2 apoptosis regulator	Homo sapiens	138-142
29931583-3	2019	We first used AZD5153, a novel bivalent inhibitor for bromodomain-containing 4 (BRD4), in DHL- and DEL-derived cell lines, because BRD4 regulates disease type-oriented key molecules for oncogenesis.	AZD5153	14-21	bromodomain containing 4	Homo sapiens	54-78
29931583-3	2019	We first used AZD5153, a novel bivalent inhibitor for bromodomain-containing 4 (BRD4), in DHL- and DEL-derived cell lines, because BRD4 regulates disease type-oriented key molecules for oncogenesis.	AZD5153	14-21	bromodomain containing 4	Homo sapiens	80-84
29931583-3	2019	We first used AZD5153, a novel bivalent inhibitor for bromodomain-containing 4 (BRD4), in DHL- and DEL-derived cell lines, because BRD4 regulates disease type-oriented key molecules for oncogenesis.	AZD5153	14-21	bromodomain containing 4	Homo sapiens	131-135
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	104-109
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	AKT serine/threonine kinase 2	Homo sapiens	111-115
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	CD19 molecule	Homo sapiens	180-184
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	B cell linker	Homo sapiens	186-190
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	CD79b molecule	Homo sapiens	195-200
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	IKAROS family zinc finger 1	Homo sapiens	256-261
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	IKAROS family zinc finger 3	Homo sapiens	263-268
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	paired box 5	Homo sapiens	270-274
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	POU class 2 homeobox associating factor 1	Homo sapiens	276-283
29931583-6	2019	At the molecular level, AZD5153 was potent in downregulating various molecules for oncogenesis, such as c-MYC, AKT2 and MAP3K; those involved in the BCR signaling pathway, such as CD19, BLNK and CD79B; and those associated with B-cell development, such as IKZF1, IKZF3, PAX5, POU2AF1 and EBF1.	AZD5153	24-31	EBF transcription factor 1	Homo sapiens	288-292
29931583-9	2019	These results provide a rationale for dual targeting of BRD4 and BCL2 using AZD5153 and AZD4320 as a therapeutic strategy against DHL and DEL.	AZD5153	76-83	BCL2 apoptosis regulator	Homo sapiens	65-69
30304769-8	2018	Marked cytotoxicity was found following bromodomain-containing protein 4 (BRD4) inhibition with AZD5153, suggesting a strict dependency of this particular subtype of T-ALL on the activity of super-enhancers.	AZD5153	96-103	bromodomain containing 4	Homo sapiens	40-72
30304769-8	2018	Marked cytotoxicity was found following bromodomain-containing protein 4 (BRD4) inhibition with AZD5153, suggesting a strict dependency of this particular subtype of T-ALL on the activity of super-enhancers.	AZD5153	96-103	bromodomain containing 4	Homo sapiens	74-78
30036377-6	2018	Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector.	AZD5153	56-63	bromodomain containing 4	Homo sapiens	85-89
30036377-6	2018	Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector.	AZD5153	56-63	delta/notch like EGF repeat containing	Homo sapiens	41-44
29636547-4	2018	Inhibition of BRD4 by JQ1 or AZD5153 resulted in a rapid, time-dependent reduction in CHK1 phosphorylation and aberrant DNA replication re-initiation.	AZD5153	29-36	bromodomain containing 4	Homo sapiens	14-18
29636547-4	2018	Inhibition of BRD4 by JQ1 or AZD5153 resulted in a rapid, time-dependent reduction in CHK1 phosphorylation and aberrant DNA replication re-initiation.	AZD5153	29-36	checkpoint kinase 1	Homo sapiens	86-90
30036377-6	2018	Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector.	AZD5153	56-63	neuregulin 1	Homo sapiens	139-151
29596834-0	2018	AZD5153, a novel BRD4 inhibitor, suppresses human thyroid carcinoma cell growth in vitro and in vivo.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	17-21
29596834-2	2018	AZD5153 is a novel and specific Bromodomain-containing protein 4 (BRD4) inhibitor.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	32-64
29596834-2	2018	AZD5153 is a novel and specific Bromodomain-containing protein 4 (BRD4) inhibitor.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	66-70
30036377-6	2018	Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector.	AZD5153	56-63	bromodomain containing 4	Homo sapiens	163-167
28378926-0	2017	Translational Modeling of Drug-Induced Myelosuppression and Effect of Pretreatment Myelosuppression for AZD5153, a Selective BRD4 Inhibitor.	AZD5153	104-111	bromodomain containing 4	Homo sapiens	125-129
29596834-3	2018	Here, we show that AZD5153 dose-dependently inhibited survival, proliferation and cell cycle progression in TPC-1 cells and primary human thyroid carcinoma cells.	AZD5153	19-26	two pore segment channel 1	Homo sapiens	108-113
29596834-5	2018	AZD5153 induced caspase-3/-9 and apoptosis activation in TPC-1 cells and primary cancer cells.	AZD5153	0-7	caspase 3	Homo sapiens	16-28
29596834-5	2018	AZD5153 induced caspase-3/-9 and apoptosis activation in TPC-1 cells and primary cancer cells.	AZD5153	0-7	two pore segment channel 1	Homo sapiens	57-62
29596834-8	2018	BRD4-regulated proteins, including c-Myc, Bcl-2 and cyclin D1, were significantly downregulated following AZD5153 treatment in TPC-1 and primary cancer cells.	AZD5153	106-113	bromodomain containing 4	Homo sapiens	0-4
29596834-8	2018	BRD4-regulated proteins, including c-Myc, Bcl-2 and cyclin D1, were significantly downregulated following AZD5153 treatment in TPC-1 and primary cancer cells.	AZD5153	106-113	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	35-40
29596834-8	2018	BRD4-regulated proteins, including c-Myc, Bcl-2 and cyclin D1, were significantly downregulated following AZD5153 treatment in TPC-1 and primary cancer cells.	AZD5153	106-113	BCL2 apoptosis regulator	Homo sapiens	42-47
29596834-8	2018	BRD4-regulated proteins, including c-Myc, Bcl-2 and cyclin D1, were significantly downregulated following AZD5153 treatment in TPC-1 and primary cancer cells.	AZD5153	106-113	cyclin D1	Homo sapiens	52-61
29596834-8	2018	BRD4-regulated proteins, including c-Myc, Bcl-2 and cyclin D1, were significantly downregulated following AZD5153 treatment in TPC-1 and primary cancer cells.	AZD5153	106-113	two pore segment channel 1	Homo sapiens	127-132
29596834-9	2018	In vivo, oral administration of AZD5153 at well-tolerated doses significantly inhibited TPC-1 xenograft growth in severe combined immunodeficient (SCID) mice.	AZD5153	32-39	two pore channel 1	Mus musculus	88-93
29596834-10	2018	BRD4-dependent proteins, Myc, Bcl-2 and cyclin D1, were also downregulated in AZD5153-treated tumor tissues.	AZD5153	78-85	bromodomain containing 4	Homo sapiens	0-4
29596834-10	2018	BRD4-dependent proteins, Myc, Bcl-2 and cyclin D1, were also downregulated in AZD5153-treated tumor tissues.	AZD5153	78-85	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	25-28
29596834-10	2018	BRD4-dependent proteins, Myc, Bcl-2 and cyclin D1, were also downregulated in AZD5153-treated tumor tissues.	AZD5153	78-85	BCL2 apoptosis regulator	Homo sapiens	30-35
29596834-10	2018	BRD4-dependent proteins, Myc, Bcl-2 and cyclin D1, were also downregulated in AZD5153-treated tumor tissues.	AZD5153	78-85	cyclin D1	Homo sapiens	40-49
29596834-11	2018	Collectively, the results suggest that targeting BRD4 by AZD5153 inhibits human thyroid carcinoma cell growth in vitro and in vivo.	AZD5153	57-64	bromodomain containing 4	Homo sapiens	49-53
30308485-2	2018	AZD5153 is a novel BRD4 inhibitor.	AZD5153	0-7	bromodomain containing 4	Mus musculus	19-23
30308485-13	2018	AZD5153 downregulated BRD4 targets (cyclin D1, Myc, Bcl-2, FOSL1 and CDK4) in PC-3 and primary prostate cancer cells.	AZD5153	0-7	bromodomain containing 4	Mus musculus	22-26
30308485-13	2018	AZD5153 downregulated BRD4 targets (cyclin D1, Myc, Bcl-2, FOSL1 and CDK4) in PC-3 and primary prostate cancer cells.	AZD5153	0-7	cyclin D1	Mus musculus	36-45
30308485-13	2018	AZD5153 downregulated BRD4 targets (cyclin D1, Myc, Bcl-2, FOSL1 and CDK4) in PC-3 and primary prostate cancer cells.	AZD5153	0-7	myelocytomatosis oncogene	Mus musculus	47-50
30308485-13	2018	AZD5153 downregulated BRD4 targets (cyclin D1, Myc, Bcl-2, FOSL1 and CDK4) in PC-3 and primary prostate cancer cells.	AZD5153	0-7	B cell leukemia/lymphoma 2	Mus musculus	52-57
30308485-13	2018	AZD5153 downregulated BRD4 targets (cyclin D1, Myc, Bcl-2, FOSL1 and CDK4) in PC-3 and primary prostate cancer cells.	AZD5153	0-7	fos-like antigen 1	Mus musculus	59-64
30308485-13	2018	AZD5153 downregulated BRD4 targets (cyclin D1, Myc, Bcl-2, FOSL1 and CDK4) in PC-3 and primary prostate cancer cells.	AZD5153	0-7	cyclin-dependent kinase 4	Mus musculus	69-73
30308485-14	2018	Further studies show that AKT could be the primary resistance factor of AZD5153.	AZD5153	72-79	thymoma viral proto-oncogene 1	Mus musculus	26-29
30308485-15	2018	Pharmacological inhibition or genetic depletion of AKT induced BRD4 downregulation, sensitizing AZD5153-induced cytotoxicity in PC-3 cells.	AZD5153	96-103	thymoma viral proto-oncogene 1	Mus musculus	51-54
30308485-18	2018	CONCLUSION: Together, our results indicate a promising therapeutic value of the novel BRD4 inhibitor AZD5153 against prostate cancer cells.	AZD5153	101-108	bromodomain containing 4	Mus musculus	86-90
28378926-1	2017	In this work, we evaluate the potential risk of thrombocytopenia in man for a BRD4 inhibitor, AZD5153, based on the platelet count decreases from a Han Wistar rat study.	AZD5153	94-101	bromodomain containing 4	Homo sapiens	78-82
28073847-1	2017	Purpose: AZD5153 is a novel BRD4/BET inhibitor with a distinctive bivalent bromodomain binding mode.	AZD5153	9-16	bromodomain containing 4	Homo sapiens	28-32
28073847-1	2017	Purpose: AZD5153 is a novel BRD4/BET inhibitor with a distinctive bivalent bromodomain binding mode.	AZD5153	9-16	delta/notch like EGF repeat containing	Homo sapiens	33-36
28073847-3	2017	MYC and HEXIM1 mRNAs were also evaluated.Results: RNA-sequencing data showed consistent decreases in CCR2/CD180 expression across multiple hematologic cell lines upon AZD5153 treatment.	AZD5153	167-174	C-C motif chemokine receptor 2	Homo sapiens	101-105
28073847-3	2017	MYC and HEXIM1 mRNAs were also evaluated.Results: RNA-sequencing data showed consistent decreases in CCR2/CD180 expression across multiple hematologic cell lines upon AZD5153 treatment.	AZD5153	167-174	CD180 molecule	Homo sapiens	106-111
28073847-5	2017	In vivo downregulation of CCR2/CD180 mRNAs (>80%) was demonstrated in MV4,11 and KMS-11 xenograft tumors at efficacious AZD5153 doses.	AZD5153	123-130	C-C motif chemokine receptor 2	Homo sapiens	26-30
28073847-5	2017	In vivo downregulation of CCR2/CD180 mRNAs (>80%) was demonstrated in MV4,11 and KMS-11 xenograft tumors at efficacious AZD5153 doses.	AZD5153	123-130	CD180 molecule	Homo sapiens	31-36
27573426-0	2016	AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.	AZD5153	0-7	delta/notch like EGF repeat containing	Homo sapiens	26-29
27573426-3	2016	Herein, we report AZD5153, a potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode.	AZD5153	18-25	delta/notch like EGF repeat containing	Homo sapiens	69-72
27573426-3	2016	Herein, we report AZD5153, a potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode.	AZD5153	18-25	bromodomain containing 4	Homo sapiens	73-77
27573426-4	2016	Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously.	AZD5153	51-58	bromodomain containing 4	Homo sapiens	87-91
27573426-7	2016	The relationship between AZD5153 exposure and efficacy suggests that prolonged BRD4 target coverage is a primary efficacy driver.	AZD5153	25-32	bromodomain containing 4	Homo sapiens	79-83
27573426-8	2016	AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR.	AZD5153	0-7	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	63-66
27573426-8	2016	AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR.	AZD5153	0-7	mechanistic target of rapamycin kinase	Homo sapiens	77-81
27573426-9	2016	Of note, mTOR pathway modulation is associated with cell line sensitivity to AZD5153.	AZD5153	77-84	mechanistic target of rapamycin kinase	Homo sapiens	9-13
27573426-10	2016	Transcriptional modulation of MYC and HEXIM1 was confirmed in AZD5153-treated human whole blood, thus supporting their use as clinical pharmacodynamic biomarkers.	AZD5153	62-69	MYC proto-oncogene, bHLH transcription factor	Homo sapiens	30-33
27573426-10	2016	Transcriptional modulation of MYC and HEXIM1 was confirmed in AZD5153-treated human whole blood, thus supporting their use as clinical pharmacodynamic biomarkers.	AZD5153	62-69	HEXIM P-TEFb complex subunit 1	Homo sapiens	38-44
27573426-11	2016	This study establishes AZD5153 as a highly potent, orally available BET/BRD4 inhibitor and provides a rationale for clinical development in hematologic malignancies.	AZD5153	23-30	delta/notch like EGF repeat containing	Homo sapiens	68-71
27573426-11	2016	This study establishes AZD5153 as a highly potent, orally available BET/BRD4 inhibitor and provides a rationale for clinical development in hematologic malignancies.	AZD5153	23-30	bromodomain containing 4	Homo sapiens	72-76
16833545-5	2005	The rapid halogen abstraction of XnH*(D1) from some halogen donors such as carbon tetrachloride (CCl4) was found to occur.	AZD5153	33-36	C-C motif chemokine ligand 4	Homo sapiens	97-101