rvx 208 profile

ID Source	ID
PubMed CID	135564749
SCHEMBL ID	145019
SCHEMBL ID	17002023
MeSH ID	M0547663

Synonym
AKOS016008772
1044870-39-4
rvx-208
rvx208
apabetalone [usan:inn]
apabetalone [inn]
8r4a7gdz1d ,
2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxy-4(1h)-quinazolinone
unii-8r4a7gdz1d
apabetalone
rvx000222
2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3h)-one
rvx 208
rvx 000222
rvx-000222
QC-216 ,
4MR6
4MR4
S7295
gtpl7034
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1,4-dihydroquinazolin-4-one
2-[4-(2-hydroxy-ethoxy)-3,5-dimethyl-phenyl]-5,7-dimethoxy-3h-quinazolin-4-one
NETXMUIMUZJUTB-UHFFFAOYSA-N
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3h)-one
1k0 ,
CS-3239
HY-16652
SCHEMBL145019
apabetalone [who-dd]
apabetalone [usan]
AC-28201
c20h22n2o5
DTXSID90146502
4J3I
4J1P
SCHEMBL17002023
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-3h-quinazolin-4-one
mfcd18633270
BP-23380
J-001182
AKOS026750505
EX-A1110
HMS3653C10
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-3,4-dihydroquinazolin-4-one
EN300-7408723
NCGC00356073-09
SW219327-1
DB12000
BCP07787
rvx-208(rvx-000222)
AS-35133
Q21099554
SB17171
HMS3886D13
HMS3744M09
CCG-268298
D11131
apabetalone (usan/inn)
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1h-quinazolin-4-one
2-[4-(2-hydroxyethoxy)-3,5-dimethyl-phenyl]-5,7-dimethoxy-3h-quinazolin-4-one
nsc771600
nsc-771600
NCGC00356073-11

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	16.2248	AID1645841
G	Vesicular stomatitis virus	Potency	11.3358	AID1645842
Interferon beta	Homo sapiens (human)	Potency	11.3358	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	11.3358	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	11.3358	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	11.3358	AID1645842

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Bromodomain-containing protein 4	Homo sapiens (human)	IC50	2.6223	AID1191950; AID1318693; AID1318694; AID1357987; AID1357988; AID1357989; AID1357990; AID1357991; AID1357992; AID1375117; AID1375118; AID1462214; AID1462220; AID1462228; AID1477943; AID1534669; AID1547245; AID1559489; AID1559490; AID1591809; AID1594404; AID1594406; AID1600708; AID1606738; AID1606739; AID1821724; AID1821725; AID1882324
Bromodomain-containing protein 2	Homo sapiens (human)	IC50	2.9935	AID1357993; AID1357994; AID1821726; AID1821727
Bromodomain-containing protein 3	Homo sapiens (human)	IC50	13.7543	AID1286397; AID1357995; AID1357996; AID1559423; AID1559424; AID1821728; AID1821729
Bromodomain testis-specific protein	Homo sapiens (human)	IC50	2.8168	AID1357997; AID1357998; AID1821730; AID1821731
CREB-binding protein	Homo sapiens (human)	IC50	10.0000	AID1357999; AID1821732

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Bromodomain-containing protein 4	Homo sapiens (human)	Kd	1.1301	AID1280137; AID1280138; AID1280141; AID1280142; AID1289235; AID1289236; AID1460619; AID1460620; AID1513787; AID1513788; AID1549006; AID1549007; AID1606740; AID1606741; AID1674518; AID1674519; AID1827504; AID1827505; AID1859896; AID1859897; AID1881998; AID1881999
Bromodomain-containing protein 2	Homo sapiens (human)	Kd	4.1268	AID1280135; AID1280136; AID1280139; AID1280140; AID1460669; AID1460671; AID1513797; AID1513798; AID1606742; AID1606743
Bromodomain-containing protein 3	Homo sapiens (human)	Kd	2.3736	AID1375174; AID1460668; AID1460670; AID1513794; AID1513795; AID1606744; AID1606745
Bromodomain testis-specific protein	Homo sapiens (human)	Kd	2.7720	AID1606746; AID1606747
CREB-binding protein	Homo sapiens (human)	Kd	10.0000	AID1606748

Assay ID	Title	Year	Journal	Article
AID977608	Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB	2013	PloS one, , Volume: 8, Issue:12 ISSN: 1932-6203	RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
AID1280142	Binding affinity to human BRD4 bromodomain 2 by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID752924	Drug metabolism in human liver microsomes assessed as M5 metabolite level at 100 uM after 4 hrs by LC/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1674518	Binding affinity to N-terminal His-tagged BRD4 BD2 (unknown origin) by isothermal calorimetric titration assay	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804	Design and Synthesis of a Highly Selective and
AID752992	Drug metabolism in Beagle dog liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1594410	Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID752965	Drug metabolism in cynomolgus monkey liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1547273	Inhibition of HDAC2 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1280140	Binding affinity to human BRD2 bromodomain 2 by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1375119	Selectivity ratio of IC50 for 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) to IC50 for 6H-Thr BRD4 Y97A mutant BD2 (unknown origin)	2018	Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804	Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
AID1513798	Inhibition of human 6x-His-tagged BRD2 bromodomain 2 expressed in Escherichia coli	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID752938	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per 4 mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1368373	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID1357987	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID752964	Drug metabolism in cynomolgus monkey liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1460669	Inhibition of recombinant human His6-tagged BRD2 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells	2017	Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 ISSN: 1520-4804	Drug Discovery Targeting Bromodomain-Containing Protein 4.
AID1357989	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID752991	Drug metabolism in cynomolgus monkey liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1606742	Binding affinity to recombinant BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID1462220	Inhibition of human BRD4 bromo domain 1	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 ISSN: 1464-3405	Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1280139	Binding affinity to human BRD2 bromodomain 1 by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1827533	Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID1460670	Inhibition of recombinant human His6-tagged BRD3 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells	2017	Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 ISSN: 1520-4804	Drug Discovery Targeting Bromodomain-Containing Protein 4.
AID752969	Drug metabolism in Beagle dog liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752974	Drug metabolism in calf liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1460620	Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide substrate addition after 30 mins by alphas	2017	Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 ISSN: 1520-4804	Drug Discovery Targeting Bromodomain-Containing Protein 4.
AID1357990	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID752961	Drug metabolism in Sprague-Dawley rat liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1606748	Binding affinity to recombinant CBP (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752989	Drug metabolism in cynomolgus monkey liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752977	Drug metabolism in human liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752932	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per 4 mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1357995	Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1547245	Inhibition of GST-tagged BRD4 bromodomain (unknown origin) using biotinylated histone H4KAc peptide (1 to 21 residues) as substrate by HTRF assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1594415	Antifibrotic activity against human LX2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1357993	Inhibition of BRD2 BD1 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID752981	Drug metabolism in New Zealand White rabbit liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1460619	Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac peptide substrate addition after 30 mins by alphascreen assay	2017	Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 ISSN: 1520-4804	Drug Discovery Targeting Bromodomain-Containing Protein 4.
AID752933	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per 4 mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1594407	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1358022	Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mISG54 expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimula	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1286397	Inhibition of human His-tagged BRD3 bromodomain 2 using biotin-H4K5acK8acK12acK16ac as substrate incubated for 30 mins by alphascreen assay	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.
AID1477997	Induction of autophagy in GFP/mRFP treated human MCF7 cells assessed as induction of LC3 puncta at 150 uM by fluorescence microscopic analysis	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID752993	Drug metabolism in Beagle dog liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752955	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1318696	Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254	Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.
AID1513833	Inhibition of BRD4 bromodomain 2 in human A549 cells assessed as reduction in TNFalpha-induced IL8 levels at 1 uM after 24 hrs by ELISA relative to control	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID752973	Drug metabolism in Yucatan minipig liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1827504	Inhibition of BRD4-BD1 (unknown origin) assessed as dissociation constant by ITC method	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID752925	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per 20 mg of protein at 1 mM after 24 hrs by LC/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752983	Drug metabolism in ICR/CD1 mouse liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1559490	Displacement of tetra-acetylated histone H4 peptide from recombinant human N-terminal His-tagged BRD4 BD2 incubated for 2 hrs by TR-FRET assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID752954	Drug metabolism in human liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1375174	Binding affinity to human BRD3 BD2 by ITC method	2018	Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804	Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
AID1368371	Cytotoxicity against human BJ cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID752951	Drug metabolism in Yucatan minipig liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1827530	Downregulation of Myc expression in human MOLM-14 cells incubated for 2 hrs by RT-PCR analysis	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID752927	Drug metabolism in calf liver microsomes assessed per 4 mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1357992	Inhibition of BRD4 BD2 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1547271	Inhibition of HDAC7 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1559424	Displacement of tetra-acetylated histone H4 peptide from recombinant human His-tagged BRD3 BD1 expressed in bacterial expression system by alphascreen assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID1547272	Inhibition of HDAC6 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1513797	Inhibition of human 6x-His-tagged BRD2 bromodomain 1 expressed in Escherichia coli	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID1559491	Selectivity index, ratio of IC50 for recombinant human N-terminal His-tagged BRD4 BD2 to IC50 for recombinant human N-terminal His-tagged BRD4 BD1 by TR-FRET assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID1827505	Inhibition of BRD4-BD2 (unknown origin) assessed as dissociation constant by ITC method	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID752952	Drug metabolism in human liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752940	Drug metabolism in New Zealand White rabbit liver microsomes assessed per mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1289236	Binding affinity to BRD4 bromodomain 2 (unknown origin) by isothermal titration calorimetric analysis	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
AID1318695	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254	Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.
AID1827532	Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID752982	Drug metabolism in New Zealand White rabbit liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752944	Drug metabolism in New Zealand White rabbit liver microsomes assessed per mg/ml of protein at 0.2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1375117	Displacement of (+)-JQ1 from 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) after 30 mins by TR-FRET assay	2018	Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804	Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
AID1368370	Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID1559422	Selectivity index, ratio of IC50 for recombinant human His-tagged BRD3 BD1 expressed in bacterial expression system to IC50 for recombinant human His-tagged BRD3 BD2 expressed in bacterial expression system	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID1513794	Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coli	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID752957	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752967	Drug metabolism in Beagle dog liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1606736	Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible CIG5 gene expression at 10 uM pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis relative to control	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752987	Drug metabolism in Sprague-Dawley rat liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1547284	Effect on histone H3 expression level in human HCT116 cells measured after 24 hrs by Western blot analysis	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID752966	Drug metabolism in cynomolgus monkey liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1845925	Reversal of HIV-1 latency infected in GFP-fused human J-Lat C11 cells assessed as increase in GFP expression at 100 uM incubated for 72 hrs by flow cytometry	2021	European journal of medicinal chemistry, Mar-05, Volume: 213ISSN: 1768-3254	HIV latency reversal agents: A potential path for functional cure?
AID1358020	Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in neutrophils recruitment into bronchoalveolar lavage fluid at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1368367	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID1547286	Inhibition of BRD4 in human HCT116 cells assessed as reduction in C-myc level measured after 24 hrs by Western blot analysis	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID752986	Drug metabolism in Sprague-Dawley rat liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1821724	Binding affinity recombinant human BRD4 BD1 (42 to 168 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1318693	Inhibition of human His-tagged BRD4 BD1 (49 to 170 residues) using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254	Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.
AID1513787	Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coli	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID1462223	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 ISSN: 1464-3405	Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1591814	Antihyperlipidemic activity in po dosed Sprague-Dawley rat assessed as decrease in triglyceride level administered twice daily for 1 week measured 2 hrs post-last dose by GPO-PAP analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
AID1594419	Selectivity index, ratio of IC50 for cytotoxicity against human LO2 cells to IC50 for antifibrotic activity against human LX2 cells	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1821731	Binding affinity BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1606738	Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible CIG5 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID1674517	Selectivity ratio of Kd for N-terminal His-tagged BRD4 BD1 (unknown origin) to Kd for N-terminal His-tagged BRD4 BD2 (unknown origin) by isothermal calorimetric titration assay	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804	Design and Synthesis of a Highly Selective and
AID752934	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per mg/ml of protein at 0.2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1594418	Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1606744	Binding affinity to recombinant BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752994	Drug metabolism in Beagle dog liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1547353	Decrease in BRD4 expression in human HCT116 cells incubated for 24 hrs by western blot analysis	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID752959	Drug metabolism in ICR/CD1 mouse liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1357996	Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1368366	Cytotoxicity against human HD-MB03 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID1591810	Up regulation of ApoA1 mRNA expression in human HepG2 cells at 100 uM by RT-PCR analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
AID1594413	Inhibition of BRD4 in human A375 cells assessed as reduction in c-MYC mRNA expression at 10 uM measured after 24 hrs by RT-PCR analysis	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1477944	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID752984	Drug metabolism in ICR/CD1 mouse liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1821730	Binding affinity BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID752988	Drug metabolism in Sprague-Dawley rat liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1375175	Selectivity ratio of Kd for human BRD3 BD2 to Kd for human BRD3 BD1	2018	Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804	Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
AID1594417	Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1881998	Binding affinity to BRD4 BD1 (unknown origin) by isothermal titration calorimetry	2022	European journal of medicinal chemistry, Jan-05, Volume: 227ISSN: 1768-3254
AID752978	Drug metabolism in human liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1547246	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID752945	Drug metabolism in New Zealand White rabbit liver microsomes assessed per mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752942	Drug metabolism in New Zealand White rabbit liver microsomes assessed per 4 mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1559436	Inhibition of BRD4 BD1 in HUVEC assessed as downregulation of NF-kappaB activity at 0.1 to 10 uM incubated for 24 hrs by dual luciferase reporter gene assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID752972	Drug metabolism in Yucatan minipig liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752939	Drug metabolism in New Zealand White rabbit liver microsomes assessed per mg/ml of protein at 0.2 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1358021	Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mKC expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimulatio	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1594421	Inhibition of BRD4 in human HLF1 cells assessed as reduction in collagen-1 protein expression at 10 uM measured after 24 hrs by Western blot analysis	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1280137	Binding affinity to human BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1594409	Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1460668	Inhibition of recombinant human His6-tagged BRD3 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells	2017	Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 ISSN: 1520-4804	Drug Discovery Targeting Bromodomain-Containing Protein 4.
AID752985	Drug metabolism in ICR/CD1 mouse liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752937	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per 4 mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1280141	Binding affinity to human BRD4 bromodomain 1 by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1827529	Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID752949	Drug metabolism in Yucatan minipig liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752956	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1409614	Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound	2020	Nature, 07, Volume: 583, Issue:7816 ISSN: 1476-4687	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID752947	Drug metabolism in New Zealand White rabbit liver microsomes assessed per 4 mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1318694	Inhibition of human BRD4 BD2 (342 to 460 residues) at 30 uM preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254	Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.
AID1477943	Inhibition of His/thioredoxin-tagged human recombinant BRD4 bromodomain-1 (43 to 166 residues) expressed in Escherichia coli BL21 Star (DE3) pre-incubated for 30 mins followed by biotinylated histone peptide H4 addition measured after 30 mins by AlphaScre	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID1191950	Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay	2015	Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 ISSN: 1464-3391	Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
AID1547282	Inhibition of HDAC in human HCT116 cells assessed as increase in acetylated histone H3 expression level measured after 24 hrs by Western blot analysis	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1821722	Antiinflammatory activity in human SAEC assessed as inhibition of Poly(I:C) induced IL-6 expression pretreated for 24 hrs followed by Poly(I:C) addition for 4 hrs by qRT-PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1594408	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID752931	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1674519	Binding affinity to N-terminal His-tagged BRD4 BD1 (unknown origin) by isothermal calorimetric titration assay	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804	Design and Synthesis of a Highly Selective and
AID752936	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1859896	Binding affinity to human BRD4 BD1 assessed as dissociation constant by ITC analysis	2022	European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254	Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
AID752928	Drug metabolism in calf liver microsomes assessed per mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1358024	Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mCIG5 expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimulat	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1606747	Binding affinity to recombinant BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752979	Drug metabolism in human liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1559423	Displacement of tetra-acetylated histone H4 peptide from recombinant human His-tagged BRD3 BD2 expressed in bacterial expression system by alphascreen assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID1409609	Cytotoxicity of compound against Vero E6 cells by MTT assay.	2020	Nature, 07, Volume: 583, Issue:7816 ISSN: 1476-4687	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1821729	Binding affinity BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1280144	Selectivity ratio of Kd for human BRD2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells to Kd for human BRD2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1462222	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 ISSN: 1464-3405	Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1462217	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 ISSN: 1464-3405	Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID752976	Drug metabolism in calf liver microsomes assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1821726	Binding affinity BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1289235	Binding affinity to BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetric analysis	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
AID1477952	Inhibition of BRD4 bromodomain-1 interaction with AMPK in human MCF7 cells assessed as induction of autophagy activity by measuring MDC positive cells at 5 uM after 6 hrs by MDC-fluorescence based flow cytometric analysis relative to control	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID1357994	Inhibition of BRD2 BD2 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1409608	AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).	2020	Nature, 07, Volume: 583, Issue:7816 ISSN: 1476-4687	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1462228	Inhibition of human BRD4 bromodomain2 by Alphascreen assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 ISSN: 1464-3405	Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID1882324	Inhibition of BRD4 (unknown origin)	2022	European journal of medicinal chemistry, Feb-15, Volume: 230ISSN: 1768-3254	Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.
AID1513805	Displacement of BI-BODIPY from BRD4 C-terminal bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID1513795	Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coli	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID1549006	Binding affinity to human BRD4 BD1 by isothermal calorimetry analysis	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of
AID1368372	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID1357999	Inhibition of CBP (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1606741	Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID1606743	Binding affinity to recombinant BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752935	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1318697	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254	Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.
AID1594404	Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain1 (unknown origin) measured after 60 mins by AlphaScreen assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1477999	Induction of autophagy in GFP/mRFP treated human MDA-MB-231 cells assessed as induction of LC3 puncta at 150 uM by fluorescence microscopic analysis	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID1368369	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID752950	Drug metabolism in Yucatan minipig liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1357998	Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1821725	Binding affinity human BRD4 BD2 incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1478046	Induction of autophagy in human MDA-MB-231 cells assessed as downregulation of p62/SQSTM1 expression at 150 uM by Western blot analysis	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID1606740	Binding affinity to recombinant BRD4 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID1357991	Inhibition of BRD4 BD1 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1409607	IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).	2020	Nature, 07, Volume: 583, Issue:7816 ISSN: 1476-4687	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID752953	Drug metabolism in human liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1280136	Binding affinity to human BRD2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1547248	Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1821732	Binding affinity CBP (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1594416	Antifibrotic activity against human HLF1 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1591809	Inhibition of BRD4 bromodomain 2 (unknown origin) incubated for 30 mins by ELISA	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
AID752980	Drug metabolism in New Zealand White rabbit liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1280138	Binding affinity to human BRD4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1827531	Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 ISSN: 1520-4804	CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
AID1280135	Binding affinity to human BRD2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 ISSN: 1520-4804	New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
AID1358023	Anti-inflammatory activity in poly(I:C)-induced airway inflammation C57BL/6 mouse model assessed as reduction in mIL6 expression in lung at 10 mg/kg, ip administered 1 day prior to poly(I:C) stimulation and redosed on day 2 followed by poly(I:C) stimulati	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1606746	Binding affinity to recombinant BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752941	Drug metabolism in New Zealand White rabbit liver microsomes assessed per mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752975	Drug metabolism in calf liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1821728	Binding affinity BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1462214	Inhibition of human BRD4 bromo domain 2	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 ISSN: 1464-3405	Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID752963	Drug metabolism in Sprague-Dawley rat liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1606745	Binding affinity to recombinant BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752970	Activity at human recombinant glucuronyl transferase at 100 uM after 1 to 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1594414	Induction of apoptosis in human A375 cells at 10 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based fluorescence microscopic analysis	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1559435	Inhibition of LPS-induced NO overproduction in mouse RAW264.7 cells at 1 uM incubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by Griess reagent based assay relative to control	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID752926	Drug metabolism in calf liver microsomes assessed per 4 mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1478045	Induction of autophagy in human MCF7 cells assessed as downregulation of p62/SQSTM1 expression at 150 uM by Western blot analysis	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID1821727	Binding affinity BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID752962	Drug metabolism in Sprague-Dawley rat liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1460671	Inhibition of recombinant human His6-tagged BRD2 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells	2017	Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 ISSN: 1520-4804	Drug Discovery Targeting Bromodomain-Containing Protein 4.
AID752948	Drug metabolism in New Zealand White rabbit liver microsomes assessed per 4 mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1375120	Chromatographic hydrophobicity index, log D of the compound at pH 7.4 by HPLC method	2018	Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804	Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
AID1594411	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID752943	Drug metabolism in New Zealand White rabbit liver microsomes assessed per 4 mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752930	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per mg/ml of protein at 0.5 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1357988	Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID1859897	Binding affinity to human BRD4 BD2 assessed as dissociation constant by ITC analysis	2022	European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254	Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
AID752946	Drug metabolism in New Zealand White rabbit liver microsomes assessed per mg/ml of protein at 2 mM after 24 hrs by LC-MS/MS analysis in presence of 5 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1409611	AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.	2020	Nature, 07, Volume: 583, Issue:7816 ISSN: 1476-4687	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1547247	Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	2020	Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 ISSN: 1520-4804	Discovery of Thieno[2,3-
AID1534669	Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay	2019	European journal of medicinal chemistry, Feb-01, Volume: 163ISSN: 1768-3254	Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
AID1375118	Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assay	2018	Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804	Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
AID1594422	Inhibition of BRD4 in human HLF1 cells assessed as reduction in collagen-1 mRNA expression at 10 uM measured after 24 hrs by RT-PCR analysis	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1606739	Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible IL-6 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID1477945	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	2017	Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 ISSN: 1520-4804	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.
AID1606737	Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible IL-6 gene expression at 10 uM pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis relative to control	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
AID752968	Drug metabolism in Beagle dog liver S9 fraction assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1600708	Inhibition of human recombinant N-terminal 6his-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3) using using H4 peptide as substrate by alphascreen assay	2019	Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 ISSN: 1464-3405	Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.
AID1591813	Antihyperlipidemic activity in po dosed Sprague-Dawley rat assessed as increase in HDL-C level administered twice daily for 1 week measured 2 hrs post-last dose by HPLC analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
AID752971	Drug metabolism in Yucatan minipig liver microsomes assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752929	Drug metabolism in New Zealand White rabbit liver S9 fraction assessed per mg/ml of protein at 0.2 mM after 24 hrs by LC-MS/MS analysis in presence of 25 mM UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1821721	Antiinflammatory activity in human SAEC assessed as inhibition of Poly(I:C) induced CIG5 expression pretreated for 24 hrs followed by Poly(I:C) addition for 4 hrs by qRT-PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804	Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
AID1594406	Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain2 (unknown origin) measured after 60 mins by AlphaScreen assay	2019	Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 ISSN: 1464-3391	Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
AID1513831	Inhibition of BRD4 bromodomain 2 in human A549 cells assessed as reduction in TNFalpha-induced NFkappaB transcription at 10 uM after 8 hrs by bright-glo luciferase reporter gene assay relative to control	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID1549010	Selectivity index, ratio of Kd for human BRD4 BD1 to Kd for human BRD4 BD2	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of
AID752958	Drug metabolism in ICR/CD1 mouse liver S9 fraction assessed as M4 metabolite level at 100 uM after 24 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID752960	Drug metabolism in ICR/CD1 mouse liver S9 fraction assessed as M4 metabolite level at 100 uM after 1 hr by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1513788	Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
AID1409613	Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.	2020	Nature, 07, Volume: 583, Issue:7816 ISSN: 1476-4687	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1368368	Cytotoxicity against human NALM16 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 ISSN: 1464-3391	Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
AID1559489	Displacement of tetra-acetylated histone H4 peptide from recombinant human N-terminal His-tagged BRD4 BD1 incubated for 2 hrs by TR-FRET assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 ISSN: 1520-4804	Discovery of Benzo[
AID1549007	Binding affinity to human BRD4 BD2 by isothermal calorimetry analysis	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 ISSN: 1520-4804	Discovery of
AID1881999	Binding affinity to BRD4 BD2 (unknown origin) by isothermal titration calorimetry	2022	European journal of medicinal chemistry, Jan-05, Volume: 227ISSN: 1768-3254
AID1357997	Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assay	2018	European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254	Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
AID752990	Drug metabolism in cynomolgus monkey liver microsomes assessed as M4 metabolite level at 100 uM after 6 hrs by LC-MS/MS analysis in presence of UDPGA	2013	European journal of medicinal chemistry, Jun, Volume: 64ISSN: 1768-3254	In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208).
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 ISSN: 1091-6490	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 ISSN: 1091-6490	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508612	NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling	2017	Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 ISSN: 1464-3391	Highly predictive and interpretable models for PAMPA permeability.
AID1508591	NCATS Rat Liver Microsome Stability Profiling	2020	Scientific reports, 11-26, Volume: 10, Issue:1 ISSN: 2045-2322	Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1645848	NCATS Kinetic Aqueous Solubility Profiling	2019	Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 ISSN: 1464-3391	Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID977611	Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB	2013	Proceedings of the National Academy of Sciences of the United States of America, Dec-03, Volume: 110, Issue:49 ISSN: 1091-6490	RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
AID1346122	Human bromodomain containing 3 (Bromodomain kinase (BRDK) family)	2013	PloS one, , Volume: 8, Issue:12 ISSN: 1932-6203	RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
AID1345665	Human bromodomain containing 4 (Bromodomain kinase (BRDK) family)	2013	PloS one, , Volume: 8, Issue:12 ISSN: 1932-6203	RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
AID1345662	Human bromodomain containing 2 (Bromodomain kinase (BRDK) family)	2013	PloS one, , Volume: 8, Issue:12 ISSN: 1932-6203	RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
AID1346122	Human bromodomain containing 3 (Bromodomain kinase (BRDK) family)	2013	Proceedings of the National Academy of Sciences of the United States of America, Dec-03, Volume: 110, Issue:49 ISSN: 1091-6490	RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	55 (59.78)	24.3611
2020's	37 (40.22)	2.80

Publication Type	This drug (%)	All Drugs (%)
Trials	13 (14.13%)	5.53%
Reviews	15 (16.30%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	64 (69.57%)	84.16%

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	2010's	post-2020
b 844-39	1	diarylmethane		2017	2017	7.0	low	1	0
pk 11195	3	aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes	antineoplastic agent	2017	2020	5.3	low	3	0
jtv519	3			2017	2020	5.3	high	3	0
alprazolam	3	organochlorine compound; triazolobenzodiazepine	anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic	2017	2020	5.3	low	3	0
dan 2163	3	aromatic amide; aromatic amine; benzamides; pyrrolidines; sulfone	environmental contaminant; second generation antipsychotic; xenobiotic	2017	2020	5.3	low	3	0
amlexanox	3	monocarboxylic acid; pyridochromene	anti-allergic agent; anti-ulcer drug; non-steroidal anti-inflammatory drug	2017	2020	5.3	low	3	0
astemizole	4	benzimidazoles; piperidines	anti-allergic agent; anticoronaviral agent; H1-receptor antagonist	2017	2020	5.0	low	4	0
benzbromarone	3	1-benzofurans; aromatic ketone	uricosuric drug	2017	2020	5.3	low	3	0
bisindolylmaleimide i	3			2017	2020	5.3	low	3	0
bufexamac	3	aromatic ether; hydroxamic acid	antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug	2017	2020	5.3	low	3	0
cadralazine	3	organic molecular entity		2017	2020	5.3	low	3	0
verapamil	1	aromatic ether; nitrile; polyether; tertiary amino compound		2020	2020	4.0	low	1	0
camostat	1	benzoate ester; carboxylic ester; diester; guanidines; tertiary carboxamide	anti-inflammatory agent; anticoronaviral agent; antifibrinolytic drug; antihypertensive agent; antineoplastic agent; antiviral agent; serine protease inhibitor	2020	2020	4.0	low	1	0
carbetapentane	1	benzenes		2020	2020	4.0	low	1	0
carvedilol	2	carbazoles; secondary alcohol; secondary amino compound	alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent	2019	2020	4.5	low	2	0
cetirizine	2	ether; monocarboxylic acid; monochlorobenzenes; piperazines	anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic	2019	2020	4.5	low	2	0
chlorcyclizine	3	diarylmethane		2017	2020	5.3	low	3	0
chloroquine	1	aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug	2020	2020	4.0	low	1	0
ci 994	3	acetamides; benzamides; substituted aniline	antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor	2017	2020	5.3	low	3	0
clofibrate	1	aromatic ether; ethyl ester; monochlorobenzenes	anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist	2019	2019	5.0	low	1	0
cloperastine	1	diarylmethane		2020	2020	4.0	low	1	0
cyclosporine	2			2017	2020	5.5	high	2	0
valproic acid	1	branched-chain fatty acid; branched-chain saturated fatty acid	anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent	2020	2020	4.0	low	1	0
fenbendazole	3	aryl sulfide; benzimidazoles; carbamate ester	antinematodal drug	2017	2020	5.3	low	3	0
berotek	1	resorcinols; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; sympathomimetic agent; tocolytic agent	2017	2017	7.0	low	1	0
gemfibrozil	1	aromatic ether	antilipemic drug	2019	2019	5.0	low	1	0
go 6976	3	indolocarbazole; organic heterohexacyclic compound	EC 2.7.11.13 (protein kinase C) inhibitor	2017	2020	5.3	low	3	0
haloperidol	4	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist	2017	2020	5.0	low	4	0
homochlorocyclizine	3	diarylmethane		2017	2020	5.3	low	3	0
hydroxychloroquine	1	aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug	2020	2020	4.0	low	1	0
hydroxyzine	3	hydroxyether; monochlorobenzenes; N-alkylpiperazine	anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist	2017	2020	5.3	low	3	0
ifenprodil	4	piperidines		2017	2020	5.0	low	4	0
indomethacin	1	aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole	analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic	2020	2020	4.0	low	1	0
1-(2-naphthalenyl)-3-[(phenylmethyl)-propan-2-ylamino]-1-propanone	3	naphthalenes		2017	2020	5.3	medium	3	0
ketamine	3	cyclohexanones; monochlorobenzenes; secondary amino compound	analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic	2017	2020	5.3	low	3	0
ketoprofen	3	benzophenones; oxo monocarboxylic acid	antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic	2017	2020	5.3	low	3	0
loratadine	1	benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide	anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist	2020	2020	4.0	low	1	0
4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide	1	benzamides; hydroxamic acid; secondary carboxamide; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor	2021	2021	3.0	low	0	1
mebendazole	3	aromatic ketone; benzimidazoles; carbamate ester	antinematodal drug; microtubule-destabilising agent; tubulin modulator	2017	2020	5.3	low	3	0
mephenesin	3	aromatic ether; glycerol ether		2017	2020	5.3	low	3	0
metformin	1	guanidines	environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic	2020	2020	4.0	low	1	0
minoxidil	1	dialkylarylamine; tertiary amino compound		2020	2020	4.0	low	1	0
nafamostat	1	benzoic acids; guanidines		2020	2020	4.0	low	1	0
niclosamide	3	benzamides; C-nitro compound; monochlorobenzenes; salicylanilides; secondary carboxamide	anthelminthic drug; anticoronaviral agent; antiparasitic agent; apoptosis inducer; molluscicide; piscicide; STAT3 inhibitor	2017	2020	5.3	low	3	0
oxibendazole	3	benzimidazoles; carbamate ester		2017	2020	5.3	low	3	0
4-(2'-methoxyphenyl)-1-(2'-(n-(2''-pyridinyl)-4-iodobenzamido)ethyl)piperazine	3			2017	2020	5.3	low	3	0
perphenazine	3	N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines	antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug	2017	2020	5.3	low	3	0
pimobendan	3	benzimidazoles; pyridazinone	cardiotonic drug; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent	2017	2020	5.3	low	3	0
pioglitazone	1	aromatic ether; pyridines; thiazolidinediones	antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic	2020	2020	4.0	low	1	0
ag 1879	3	aromatic amine; monochlorobenzenes; pyrazolopyrimidine	beta-adrenergic antagonist; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; geroprotector	2017	2020	5.3	low	3	0
3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1H-indol-2-one	2	indoles		2017	2020	5.5	medium	2	0
ro 31-8220	3	imidothiocarbamic ester; indoles; maleimides	EC 2.7.11.13 (protein kinase C) inhibitor	2017	2020	5.3	low	3	0
ropinirole	3	indolones; tertiary amine	antidyskinesia agent; antiparkinson drug; central nervous system drug; dopamine agonist	2017	2020	5.3	low	3	0
sb 202190	1	imidazoles; organofluorine compound; phenols; pyridines	apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor	2017	2017	7.0	low	1	0
vorinostat	6	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor	2017	2021	5.0	low	5	1
thalidomide	1	phthalimides; piperidones		2015	2015	9.0	low	1	0
2-[4-(4-chloro-1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanamine	2	stilbenoid		2017	2020	5.5	high	2	0
trifluperidol	1	aromatic ketone		2017	2017	7.0	low	1	0
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole	3	aromatic primary alcohol; furans; indazoles	antineoplastic agent; apoptosis inducer; platelet aggregation inhibitor; soluble guanylate cyclase activator; vasodilator agent	2017	2020	5.3	low	3	0
zotepine	3	dibenzothiepine; tertiary amino compound	alpha-adrenergic drug; second generation antipsychotic; serotonergic drug	2017	2020	5.3	low	3	0
chloramphenicol	1	C-nitro compound; carboxamide; diol; organochlorine compound	antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor	2020	2020	4.0	low	1	0
colchicine	3	alkaloid; colchicine	anti-inflammatory agent; gout suppressant; mutagen	2017	2020	5.3	low	3	0
benziodarone	3	aromatic ketone		2017	2020	5.3	low	3	0
cyclizine	1	N-alkylpiperazine	antiemetic; central nervous system depressant; cholinergic antagonist; H1-receptor antagonist; local anaesthetic	2019	2019	5.0	low	1	0
trehalose	3	trehalose	Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2017	2020	5.3	low	3	0
triclocarban	3	dichlorobenzene; monochlorobenzenes; phenylureas	antimicrobial agent; antiseptic drug; disinfectant; environmental contaminant; xenobiotic	2017	2020	5.3	low	3	0
4-tert-octylphenol	3	alkylbenzene		2017	2020	5.3	low	3	0
ethamivan	3	methoxybenzenes; phenols		2017	2020	5.3	low	3	0
azacitidine	1	N-glycosyl-1,3,5-triazine; nucleoside analogue	antineoplastic agent	2021	2021	3.0	low	0	1
methysergide	3	ergoline alkaloid		2017	2020	5.3	low	3	0
emetine	3	isoquinoline alkaloid; pyridoisoquinoline	antiamoebic agent; anticoronaviral agent; antiinfective agent; antimalarial; antineoplastic agent; antiprotozoal drug; antiviral agent; autophagy inhibitor; emetic; expectorant; plant metabolite; protein synthesis inhibitor	2017	2020	5.3	low	3	0
podophyllotoxin	3	furonaphthodioxole; lignan; organic heterotetracyclic compound	antimitotic; antineoplastic agent; keratolytic drug; microtubule-destabilising agent; plant metabolite; tubulin modulator	2017	2020	5.3	low	3	0
ferrocin c	1			2016	2016	8.0	low	1	0
etonitazene	3			2017	2020	5.3	low	3	0
clothiapine	3	dibenzothiazepine		2017	2020	5.3	low	3	0
pimozide	1	benzimidazoles; heteroarylpiperidine; organofluorine compound	antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist	2020	2020	4.0	low	1	0
benperidol	3	aromatic ketone		2017	2020	5.3	low	3	0
7-hydroxychlorpromazine	3	phenothiazines		2017	2020	5.3	medium	3	0
nitroxoline	1	C-nitro compound; monohydroxyquinoline	antifungal agent; antiinfective agent; antimicrobial agent; renal agent	2019	2019	5.0	low	1	0
camptothecin	3	delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite	2017	2020	5.3	low	3	0
clemastine	1	monochlorobenzenes; N-alkylpyrrolidine	anti-allergic agent; antipruritic drug; H1-receptor antagonist; muscarinic antagonist	2020	2020	4.0	low	1	0
thenalidine	3	dialkylarylamine; tertiary amino compound		2017	2020	5.3	medium	3	0
1-deoxynojirimycin	1	2-(hydroxymethyl)piperidine-3,4,5-triol; piperidine alkaloid	anti-HIV agent; anti-obesity agent; bacterial metabolite; EC 3.2.1.20 (alpha-glucosidase) inhibitor; hepatoprotective agent; hypoglycemic agent; plant metabolite	2020	2020	4.0	low	1	0
daunorubicin	1	aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones	antineoplastic agent; bacterial metabolite	2020	2020	4.0	low	1	0
bromocriptine	3	indole alkaloid	antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist	2017	2020	5.3	low	3	0
dexchlorpheniramine	3	chlorphenamine		2017	2020	5.3	low	3	0
dv 1006	3			2017	2020	5.3	medium	3	0
ribavirin	1	1-ribosyltriazole; aromatic amide; monocarboxylic acid amide; primary carboxamide	anticoronaviral agent; antiinfective agent; antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor	2020	2020	4.0	low	1	0
climbazole	3	aromatic ether; hemiaminal ether; imidazoles; ketone; monochlorobenzenes		2017	2020	5.3	low	3	0
triadimenol	3	aromatic ether; conazole fungicide; hemiaminal ether; monochlorobenzenes; secondary alcohol; triazole fungicide	antifungal agrochemical; EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor; xenobiotic metabolite	2017	2020	5.3	medium	3	0
nitazoxanide	1	benzamides; carboxylic ester		2020	2020	4.0	low	1	0
captopril	1	alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor	2020	2020	4.0	low	1	0
amonafide	3	isoquinolines		2017	2020	5.3	low	3	0
lovastatin	1	delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring)	anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug	2020	2020	4.0	low	1	0
flupirtine	3	aminopyridine		2017	2020	5.3	low	3	0
chaetochromin	3			2017	2020	5.3	medium	3	0
rimcazole	1	carbazoles		2020	2020	4.0	low	1	0
enoximone	3	aromatic ketone		2017	2020	5.3	low	3	0
aripiprazole	3	aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone	drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist	2017	2020	5.3	low	3	0
benzylaminopurine	1	6-aminopurines	cytokinin; plant metabolite	2015	2015	9.0	low	1	0
aloxistatin	1	epoxide; ethyl ester; L-leucine derivative; monocarboxylic acid amide	anticoronaviral agent; cathepsin B inhibitor	2019	2019	5.0	low	1	0
indocate	3			2017	2020	5.3	medium	3	0
N(4)-acetylsulfathiazole	3	1,3-thiazoles; acetamides; sulfonamide	marine xenobiotic metabolite	2017	2020	5.3	high	3	0
cyclizine hydrochloride	2			2017	2020	5.5	medium	2	0
2,3-trimethylene-4-quinazolone	3	quinazolines		2017	2020	5.3	medium	3	0
1,3-dimethyluric acid	3	oxopurine	metabolite	2017	2020	5.3	low	3	0
danofloxacin	3	quinolines		2017	2020	5.3	low	3	0
nitrefazole	3	imidazoles		2017	2020	5.3	medium	3	0
methotrimeprazine	3	phenothiazines; tertiary amine	anticoronaviral agent; cholinergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; non-narcotic analgesic; phenothiazine antipsychotic drug; serotonergic antagonist	2017	2020	5.3	low	3	0
honokiol	3	biphenyls		2017	2020	5.3	low	3	0
9-methoxyellipticine	3			2017	2020	5.3	low	3	0
3-aminophenoxazone	3	phenoxazine		2017	2020	5.3	low	3	0
3-deazaneplanocin	3			2017	2020	5.3	low	3	0
tryptanthrine	3	alkaloid antibiotic; organic heterotetracyclic compound; organonitrogen heterocyclic compound		2017	2020	5.3	low	3	0
2-chlorodiazepam	3			2017	2020	5.3	medium	3	0
Polycartine B	3	phenazines		2017	2020	5.3	high	3	0
aminoquinuride dihydrochloride	3			2017	2020	5.3	high	3	0
thioproperazine mesylate	3	phenothiazines		2017	2020	5.3	medium	3	0
n(6)-(delta(2)-isopentenyl)adenine	3	6-isopentenylaminopurine	cytokinin	2017	2020	5.3	low	3	0
lekoptin	1	2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile		2020	2020	4.0	low	1	0
4-methyl-N-(phenylmethyl)benzenesulfonamide	3	sulfonamide		2017	2020	5.3	medium	3	0
zpck	2			2019	2020	4.5	low	2	0
sr141716	3	amidopiperidine; carbohydrazide; dichlorobenzene; monochlorobenzenes; pyrazoles	anti-obesity agent; appetite depressant; CB1 receptor antagonist	2017	2020	5.3	low	3	0
indolactam v	1	indoles		2021	2021	3.0	low	0	1
(6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide	2	aromatic ketone		2017	2020	5.5	high	2	0
fingolimod	3	aminodiol; primary amino compound	antineoplastic agent; CB1 receptor antagonist; immunosuppressive agent; prodrug; sphingosine-1-phosphate receptor agonist	2017	2020	5.3	low	3	0
tesmilifene	3	diarylmethane		2017	2020	5.3	low	3	0
sr 27897	3	indolyl carboxylic acid		2017	2020	5.3	low	3	0
n-(n-(3-carboxyoxirane-2-carbonyl)leucyl)isoamylamine	3	leucine derivative		2017	2020	5.3	low	3	0
norketamine	3	organochlorine compound		2017	2020	5.3	low	3	0
indatraline	2	indanes		2019	2020	4.5	low	2	0
bd 1008	1	primary amine		2020	2020	4.0	low	1	0
methotrexate	3	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent	2017	2020	5.3	low	3	0
salvinorin a	1	organic heterotricyclic compound; organooxygen compound	metabolite; oneirogen	2019	2019	5.0	low	1	0
4-diethoxyphosphorylmethyl-n-(4-bromo-2-cyanophenyl)benzamide	3			2017	2020	5.3	low	3	0
n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide	3	phenylindole		2017	2020	5.3	low	3	0
l 741626	3	piperidines		2017	2020	5.3	low	3	0
dx 8951	3	pyranoindolizinoquinoline		2017	2020	5.3	low	3	0
vx 497	1			2020	2020	4.0	low	1	0
tipifarnib	3	imidazoles; monochlorobenzenes; primary amino compound; quinolone	antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor	2017	2020	5.3	low	3	0
cyc 202	3	2,6-diaminopurines	antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor	2017	2020	5.3	low	3	0
avasimibe	3	monoterpenoid		2017	2020	5.3	low	3	0
sb 203580	1	imidazoles; monofluorobenzenes; pyridines; sulfoxide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent	2018	2018	6.0	low	1	0
l 163191	3			2017	2020	5.3	low	3	0
dizocilpine	3	secondary amino compound; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist	2017	2020	5.3	low	3	0
s-benzylcysteine	3	S-aryl-L-cysteine zwitterion		2017	2020	5.3	high	3	0
chelidonine	3	alkaloid antibiotic; alkaloid fundamental parent; benzophenanthridine alkaloid		2017	2020	5.3	low	3	0
lapatinib	3	furans; organochlorine compound; organofluorine compound; quinazolines	antineoplastic agent; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
roxindole	3	indoles	alpha-adrenergic antagonist; serotonergic drug	2017	2020	5.3	low	3	0
conidendrin	3			2017	2020	5.3	high	3	0
Porfiromycine	3	mitomycin		2017	2020	5.3	high	3	0
nsc 95397	3	1,4-naphthoquinones		2017	2020	5.3	low	3	0
4-methyl-2-quinazolinamine	3			2017	2020	5.3	high	3	0
2-glycineamide-5-chlorophenyl-2-pyrryl ketone	3			2017	2020	5.3	high	3	0
niguldipine hydrochloride	2			2019	2020	4.5	medium	2	0
2,5-bis(5-hydroxymethyl-2-thienyl)furan	3	thiophenes		2017	2020	5.3	low	3	0
ritonavir	3	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic	2017	2020	5.3	low	3	0
bardoxolone methyl	1	cyclohexenones		2019	2019	5.0	low	1	0
Destruxin B	3	cyclodepsipeptide		2017	2020	5.3	high	3	0
tosylphenylalanyl chloromethyl ketone	3	alpha-chloroketone; sulfonamide	alkylating agent; serine proteinase inhibitor	2017	2020	5.3	low	3	0
trichostatin a	2	antibiotic antifungal agent; hydroxamic acid; trichostatin	bacterial metabolite; EC 3.5.1.98 (histone deacetylase) inhibitor; geroprotector	2019	2021	4.0	low	1	1
mycophenolic acid	1	2-benzofurans; gamma-lactone; monocarboxylic acid; phenols	anticoronaviral agent; antimicrobial agent; antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; environmental contaminant; immunosuppressive agent; mycotoxin; Penicillium metabolite; xenobiotic	2020	2020	4.0	low	1	0
brivudine	1			2020	2020	4.0	low	1	0
zithromax	1	macrolide antibiotic	antibacterial drug; environmental contaminant; xenobiotic	2020	2020	4.0	low	1	0
zeatin	1	zeatin	plant metabolite	2015	2015	9.0	low	1	0
h 89	1	N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide		2020	2020	4.0	low	1	0
12-deoxyphorbol 13-acetate	1	phorbol ester	metabolite	2021	2021	3.0	low	0	1
sitafloxacin	1	fluoroquinolone antibiotic; quinolines; quinolone antibiotic		2019	2019	5.0	low	1	0
2'-c-methylcytidine	3			2017	2020	5.3	low	3	0
jp-1302	3			2017	2020	5.3	medium	3	0
7-chloro-5,10-dihydrothieno[3,4-b][1,5]benzodiazepin-4-one	3	benzodiazepine		2017	2020	5.3	high	3	0
tenatoprazole	3	imidazopyridine		2017	2020	5.3	low	3	0
s 1033	3	(trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
5-[(2-fluoroanilino)methyl]-8-quinolinol	3	hydroxyquinoline		2017	2020	5.3	high	3	0
benidipine hydrochloride	2			2017	2020	5.5	low	2	0
benidipine	1			2019	2019	5.0	low	1	0
2-(1,3-benzoxazol-2-ylamino)-5-spiro[1,6,7,8-tetrahydroquinazoline-4,1'-cyclopentane]one	3	quinazolines		2017	2020	5.3	high	3	0
chlorprothixene	3	chlorprothixene		2017	2020	5.3	medium	3	0
jrf 12	4			2017	2020	5.0	medium	4	0
5-amino-3-(4-methoxyphenyl)-4-oxo-1-thieno[3,4-d]pyridazinecarboxylic acid ethyl ester	3	methoxybenzenes; substituted aniline		2017	2020	5.3	high	3	0
3-hydroxypyridine, sodium salt	3			2017	2020	5.3	high	3	0
N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide	3	naphthalenecarboxamide		2017	2020	5.3	medium	3	0
(2'-(4-aminophenyl)-(2,5'-bi-1h-benzimidazol)-5-amine)	1	benzimidazoles		2019	2019	5.0	low	1	0
5-[(2-bromoanilino)methyl]-8-quinolinol	4	hydroxyquinoline		2017	2020	5.2	high	4	0
3-amino-n-(4-methoxybenzyl)-4,6-dimethylthieno(2,3-b)pyridine-2-carboxamide	3			2017	2020	5.3	medium	3	0
N-[(2-methoxyphenyl)methyl]-4-(1-piperidinyl)aniline	3	aromatic amine		2017	2020	5.3	high	3	0
1-[4-(4-bromophenyl)-2-thiazolyl]-4-piperidinecarboxamide	3	piperidinecarboxamide		2017	2020	5.3	high	3	0
5-[[2-(trifluoromethyl)anilino]methyl]-8-quinolinol	3	hydroxyquinoline		2017	2020	5.3	high	3	0
N-[3-[2-[(4-methyl-2-pyridinyl)amino]-4-thiazolyl]phenyl]acetamide	3	acetamides; anilide		2017	2020	5.3	high	3	0
5-bromo-N-(5-cyclohexyl-1,3,4-thiadiazol-2-yl)-2-thiophenecarboxamide	3	aromatic amide; thiophenes		2017	2020	5.3	high	3	0
6-amino-1-[2-(3,4-dimethoxyphenyl)ethyl]-2-sulfanylidene-4-pyrimidinone	3	dimethoxybenzene		2017	2020	5.3	high	3	0
N-[4-[(3,4-dimethyl-5-isoxazolyl)sulfamoyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide	3	aromatic amide		2017	2020	5.3	high	3	0
N-[5-[(4-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-5-methyl-3-phenyl-4-isoxazolecarboxamide	3	aromatic ether		2017	2020	5.3	high	3	0
3-chloro-1-(2,5-dimethoxyphenyl)-4-(1-piperidinyl)pyrrole-2,5-dione	3	maleimides		2017	2020	5.3	high	3	0
Src Inhibitor-1	3	aromatic ether; polyether; quinazolines; secondary amino compound	EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor	2017	2020	5.3	high	3	0
1-[2-(3,4-dimethoxyphenyl)ethyl]-6-propyl-2-sulfanylidene-7,8-dihydro-5H-pyrimido[4,5-d]pyrimidin-4-one	3	dimethoxybenzene		2017	2020	5.3	high	3	0
2-phenyl-N-[4-(2-thiazolylsulfamoyl)phenyl]-4-quinolinecarboxamide	3	quinolines		2017	2020	5.3	high	3	0
4E2RCat	1	organic molecular entity		2020	2020	4.0	medium	1	0
3-(2,5-dimethyl-1-phenyl-3-pyrrolyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine	3	pyrroles		2017	2020	5.3	high	3	0
digoxin	1	cardenolide glycoside; steroid saponin	anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope	2016	2016	8.0	low	1	0
bi-78d3	3	aryl sulfide		2017	2020	5.3	medium	3	0
kartogenin	3			2017	2020	5.3	low	3	0
toremifene	1	aromatic ether; organochlorine compound; tertiary amine	antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator	2019	2019	5.0	low	1	0
vx-745	3	aryl sulfide; dichlorobenzene; difluorobenzene; pyrimidopyridazine	anti-inflammatory drug; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor	2017	2020	5.3	low	3	0
dasatinib	3	1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
ha 1100	1			2022	2022	2.0	low	0	1
zd 6474	3	aromatic ether; organobromine compound; organofluorine compound; piperidines; quinazolines; secondary amine	antineoplastic agent; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	2	indoles		2019	2020	4.5	high	2	0
nih-12848	3			2017	2020	5.3	high	3	0
2,4-dioxo-3-pentyl-N-[3-(1-piperidinyl)propyl]-1H-quinazoline-7-carboxamide	3	quinazolines		2017	2020	5.3	high	3	0
[1-(3-methylphenyl)-5-benzimidazolyl]-(1-piperidinyl)methanone	3	benzimidazoles		2017	2020	5.3	high	3	0
2-[[(6-bromo-1H-imidazo[4,5-b]pyridin-2-yl)thio]methyl]benzonitrile	3	imidazopyridine		2017	2020	5.3	high	3	0
3-[(3-fluorophenyl)methyl]-8-[4-(4-fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one	3	aromatic ketone		2017	2020	5.3	high	3	0
4-[[7-[(4-fluorophenyl)methyl]-1,3-dimethyl-2,6-dioxo-8-purinyl]methyl]-1-piperazinecarboxylic acid ethyl ester	3	oxopurine		2017	2020	5.3	high	3	0
N,N-dimethylcarbamodithioic acid (1-acetamido-2,2,2-trichloroethyl) ester	3	organonitrogen compound; organosulfur compound		2017	2020	5.3	high	3	0
6-bromo-2-(4-methylphenyl)-N-[(1-methyl-4-pyrazolyl)methyl]-4-quinolinecarboxamide	3	quinolines		2017	2020	5.3	high	3	0
LSM-1924	3	organic heterotricyclic compound; organooxygen compound		2017	2020	5.3	high	3	0
ferrostatin-1	3	ethyl ester; primary arylamine; substituted aniline	antifungal agent; antioxidant; ferroptosis inhibitor; neuroprotective agent; radiation protective agent; radical scavenger	2017	2020	5.3	low	3	0
6-(2-methyl-1-piperidinyl)-5-nitro-4-pyrimidinamine	3	C-nitro compound		2017	2020	5.3	high	3	0
rabeprazole(1-)	2	organic nitrogen anion		2019	2020	4.5	high	2	0
ncgc00099374	3			2017	2020	5.3	high	3	0
2-nitro-4-[(6-nitro-4-quinolinyl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide	3	benzamides		2017	2020	5.3	high	3	0
quercetin	1	7-hydroxyflavonol; pentahydroxyflavone	antibacterial agent; antineoplastic agent; antioxidant; Aurora kinase inhibitor; chelator; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; geroprotector; phytoestrogen; plant metabolite; protein kinase inhibitor; radical scavenger	2020	2020	4.0	low	1	0
luteolin	3	3'-hydroxyflavonoid; tetrahydroxyflavone	angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; c-Jun N-terminal kinase inhibitor; EC 2.3.1.85 (fatty acid synthase) inhibitor; immunomodulator; nephroprotective agent; plant metabolite; radical scavenger; vascular endothelial growth factor receptor antagonist	2017	2020	5.3	low	3	0
cyclosporine	1			2019	2019	5.0	low	1	0
kaempferol	3	7-hydroxyflavonol; flavonols; tetrahydroxyflavone	antibacterial agent; geroprotector; human blood serum metabolite; human urinary metabolite; human xenobiotic metabolite; plant metabolite	2017	2020	5.3	low	3	0
genistein	3	7-hydroxyisoflavones	antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; human urinary metabolite; phytoestrogen; plant metabolite; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
mycophenolate mofetil	3	carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound	anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug	2017	2020	5.3	medium	3	0
bruceantin	3	triterpenoid		2017	2020	5.3	low	3	0
chrysin	3	7-hydroxyflavonol; dihydroxyflavone	anti-inflammatory agent; antineoplastic agent; antioxidant; EC 2.7.11.18 (myosin-light-chain kinase) inhibitor; hepatoprotective agent; plant metabolite	2017	2020	5.3	low	3	0
daidzein	3	7-hydroxyisoflavones	antineoplastic agent; EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; phytoestrogen; plant metabolite	2017	2020	5.3	low	3	0
neticonazole	3	aromatic ether; benzenes; conazole antifungal drug; enamine; imidazole antifungal drug; imidazoles; methyl sulfide	antifungal drug; EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor	2017	2020	5.3	medium	3	0
N-(4Z,7Z,10Z,13Z,16Z,19Z)-docosahexaenoylethanolamine	3	endocannabinoid; N-acylethanolamine 22:6		2017	2020	5.3	medium	3	0
n-oleoylethanolamine	3	endocannabinoid; N-(long-chain-acyl)ethanolamine; N-acylethanolamine 18:1	EC 3.5.1.23 (ceramidase) inhibitor; geroprotector; PPARalpha agonist	2017	2020	5.3	low	3	0
sirolimus	1	antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol	antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor	2020	2020	4.0	low	1	0
alpha-zearalenol	3	macrolide		2017	2020	5.3	high	3	0
su 9516	3			2017	2020	5.3	low	3	0
N-(4-bromo-3-methylphenyl)-2,5-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine	3	triazolopyrimidines		2017	2020	5.3	high	3	0
sb 277011	3			2017	2020	5.3	low	3	0
sb 223412	3			2017	2020	5.3	low	3	0
sr 59230a	3	tetralins		2017	2020	5.3	high	3	0
3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide	3	pyrimidines		2017	2020	5.3	medium	3	0
kn 62	3	piperazines		2017	2020	5.3	low	3	0
MeJA	3	Jasmonate derivatives		2017	2020	5.3	high	3	0
1h-pyrrole-2,5-dione, 3-(1-methyl-1h-indol-3-yl)-4-(1-methyl-6-nitro-1h-indol-3-yl)-	3			2017	2020	5.3	high	3	0
pd 161570	3			2017	2020	5.3	medium	3	0
su 11248	1	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist	2017	2017	7.0	low	1	0
palbociclib	3	aminopyridine; aromatic ketone; cyclopentanes; piperidines; pyridopyrimidine; secondary amino compound; tertiary amino compound	antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor	2017	2020	5.3	low	3	0
jnj-7706621	3	sulfonamide		2017	2020	5.3	low	3	0
romidepsin	1	cyclodepsipeptide; heterocyclic antibiotic; organic disulfide	antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor	2017	2017	7.0	low	1	0
dextromethorphan	2	6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene	antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic	2020	2020	4.0	low	2	0
lisinopril	1	dipeptide	EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor	2020	2020	4.0	low	1	0
virginiamycin factor s1	3	cyclodepsipeptide; macrolide antibiotic	antibacterial drug; bacterial metabolite	2017	2020	5.3	high	3	0
pepstatin	1	pentapeptide; secondary carboxamide	bacterial metabolite; EC 3.4.23.* (aspartic endopeptidase) inhibitor	2020	2020	4.0	low	1	0
fenoterol	2	hydrobromide	beta-adrenergic agonist; bronchodilator agent; sympathomimetic agent	2019	2020	4.5	low	2	0
xib 4035	3			2017	2020	5.3	high	3	0
gw-5074	1			2019	2019	5.0	low	1	0
bafilomycin a1	1	cyclic hemiketal; macrolide antibiotic; oxanes	apoptosis inducer; autophagy inhibitor; bacterial metabolite; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor; ferroptosis inhibitor; fungicide; potassium ionophore; toxin	2020	2020	4.0	low	1	0
belotecan	3	pyranoindolizinoquinoline		2017	2020	5.3	low	3	0
norgestimate	3	ketoxime; steroid ester; terminal acetylenic compound	contraceptive drug; progestin; synthetic oral contraceptive	2017	2020	5.3	high	3	0
b 43	3	aromatic amine; aromatic ether; cyclopentanes; primary amino compound; pyrrolopyrimidine	EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; geroprotector	2017	2020	5.3	medium	3	0
4-(2' methoxyphenyl)-1-(2'-(n-(2''-pyridinyl)-4-fluorobenzamido)ethyl)piperazine	3			2017	2020	5.3	medium	3	0
methiazole	3	benzimidazoles; carbamate ester		2017	2020	5.3	high	3	0
sb 218795	3	quinolines		2017	2020	5.3	medium	3	0
bvt.948	3			2017	2020	5.3	high	3	0
fk 866	1	benzamides; N-acylpiperidine		2019	2019	5.0	low	1	0
a 38503	3			2017	2020	5.3	medium	3	0
(3S,6S,9S,12R)-3-[(2S)-Butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone	1	oligopeptide		2020	2020	4.0	low	1	0
belinostat	2	hydroxamic acid; olefinic compound; sulfonamide	antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor	2017	2021	5.0	low	1	1
panobinostat	2	cinnamamides; hydroxamic acid; methylindole; secondary amino compound	angiogenesis modulating agent; antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor	2017	2021	5.0	low	1	1
parthenolide	2	sesquiterpene lactone	drug allergen; inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug	2017	2019	6.0	medium	2	0
krn 633	3			2017	2020	5.3	medium	3	0
5-amino-4-oxo-3-phenyl-1-thieno[3,4-d]pyridazinecarboxylic acid	3	organonitrogen heterocyclic compound; organosulfur heterocyclic compound		2017	2020	5.3	high	3	0
n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide	1			2021	2021	3.0	low	0	1
gw 501516	3	1,3-thiazoles; aromatic ether; aryl sulfide; monocarboxylic acid; organofluorine compound	carcinogenic agent; PPARbeta/delta agonist	2017	2020	5.3	low	3	0
dolastatin 10	3	1,3-thiazoles; tetrapeptide	animal metabolite; antineoplastic agent; apoptosis inducer; marine metabolite; microtubule-destabilising agent	2017	2020	5.3	low	3	0
pd 144418	1			2020	2020	4.0	medium	1	0
spc-839	3			2017	2020	5.3	low	3	0
midostaurin	4	benzamides; gamma-lactam; indolocarbazole; organic heterooctacyclic compound	antineoplastic agent; EC 2.7.11.13 (protein kinase C) inhibitor	2017	2020	5.0	low	4	0
lu 28-179	1			2020	2020	4.0	low	1	0
valnemulin	2			2019	2020	4.5	medium	2	0
nu 7026	3	organic heterotricyclic compound; organooxygen compound		2017	2020	5.3	low	3	0
osi 930	3	aromatic amide		2017	2020	5.3	medium	3	0
ticagrelor	3	aryl sulfide; hydroxyether; organofluorine compound; secondary amino compound; triazolopyrimidines	P2Y12 receptor antagonist; platelet aggregation inhibitor	2017	2020	5.3	low	3	0
l 692585	3	peptide		2017	2020	5.3	high	3	0
pi103	3	aromatic amine; morpholines; organic heterotricyclic compound; phenols; tertiary amino compound	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor	2017	2020	5.3	low	3	0
nnc 26-9100	3	aminopyridine		2017	2020	5.3	medium	3	0
2-(3-chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine	3			2017	2020	5.3	high	3	0
tivozanib	3	aromatic ether		2017	2020	5.3	low	3	0
hki 272	1	nitrile; quinolines	antineoplastic agent; tyrosine kinase inhibitor	2019	2019	5.0	low	1	0
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide	3			2017	2020	5.3	medium	3	0
tae226	3	morpholines		2017	2020	5.3	low	3	0
gw0742	3	monocarboxylic acid		2017	2020	5.3	low	3	0
6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)-	5	organonitrogen heterocyclic compound; organosulfur heterocyclic compound		2016	2022	4.8	low	3	2
u 18666a	3	hydrochloride	antiviral agent; EC 1.3.1.72 (Delta(24)-sterol reductase) inhibitor; Hedgehog signaling pathway inhibitor; nicotinic antagonist; sterol biosynthesis inhibitor	2017	2020	5.3	low	3	0
sb 525334	3	quinoxaline derivative		2017	2020	5.3	low	3	0
bx795	3	ureas		2017	2020	5.3	low	3	0
pazopanib	1	aminopyrimidine; indazoles; sulfonamide	angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist	2020	2020	4.0	low	1	0
azd 6244	3	benzimidazoles; bromobenzenes; hydroxamic acid ester; monochlorobenzenes; organofluorine compound; secondary amino compound	anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor	2017	2020	5.3	low	3	0
1-(2-(1-adamantyl)ethyl)-1-pentyl-3-(3-(4-pyridyl)propyl)urea	3			2017	2020	5.3	medium	3	0
cl 075	1			2021	2021	3.0	low	0	1
bay 61-3606	3	pyrimidines		2017	2020	5.3	medium	3	0
sd-208	3			2017	2020	5.3	low	3	0
vx 702	1	phenylpyridine		2018	2018	6.0	low	1	0
crenolanib	3	aminopiperidine; aromatic ether; benzimidazoles; oxetanes; quinolines; tertiary amino compound	angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor	2017	2020	5.3	low	3	0
cj 033466	3			2017	2020	5.3	high	3	0
cc 401	3	pyrazoles; ring assembly		2017	2020	5.3	medium	3	0
PB28	4	aromatic ether; piperazines; tetralins	anticoronaviral agent; antineoplastic agent; apoptosis inducer; sigma-2 receptor agonist	2017	2020	5.0	medium	4	0
arterolane	3			2017	2020	5.3	low	3	0
cariprazine	3			2017	2020	5.3	low	3	0
krp-203	3			2017	2020	5.3	high	3	0
regorafenib	3	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; monofluorobenzenes; phenylureas; pyridinecarboxamide	antineoplastic agent; hepatotoxic agent; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
at 7867	3	monochlorobenzenes; piperidines; pyrazoles	antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor	2017	2020	5.3	high	3	0
acetic acid 2-[4-methyl-8-(4-morpholinylsulfonyl)-1,3-dioxo-2-pyrrolo[3,4-c]quinolinyl]ethyl ester	3	pyrroloquinoline		2017	2020	5.3	high	3	0
ptc 124	3	oxadiazole; ring assembly		2017	2020	5.3	low	3	0
degrasyn	2			2019	2020	4.5	low	2	0
bi 2536	6			2017	2021	5.3	low	5	1
azd 1152	3	anilide; monoalkyl phosphate; monofluorobenzenes; pyrazoles; quinazolines; secondary amino compound; secondary carboxamide; tertiary amino compound	antineoplastic agent; Aurora kinase inhibitor; prodrug	2017	2020	5.3	medium	3	0
carfilzomib	3	epoxide; morpholines; tetrapeptide	antineoplastic agent; proteasome inhibitor	2017	2020	5.3	low	3	0
idelalisib	3	aromatic amine; organofluorine compound; purines; quinazolines; secondary amino compound	antineoplastic agent; apoptosis inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor	2017	2020	5.3	low	3	0
motesanib	3	pyridinecarboxamide		2017	2020	5.3	medium	3	0
pf-562,271	3	indoles		2017	2020	5.3	medium	3	0
gliocladin c	3			2017	2020	5.3	high	3	0
sb 706504	3			2017	2020	5.3	high	3	0
at 13387	1	benzamides; isoindoles; N-alkylpiperazine; resorcinols; tertiary carboxamide	antineoplastic agent; Hsp90 inhibitor	2020	2020	4.0	low	1	0
ku-0060648	3	dibenzothiophenes		2017	2020	5.3	medium	3	0
bgt226	3	aromatic ether; imidazoquinoline; N-arylpiperazine; organofluorine compound; pyridines	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor	2017	2020	5.3	medium	3	0
n-desmethyldanofloxacin	3			2017	2020	5.3	high	3	0
rabeprazole sodium	1	organic sodium salt		2017	2017	7.0	low	1	0
azd 1152-hqpa	2	anilide; monofluorobenzenes; primary alcohol; pyrazoles; quinazolines; secondary amino compound; secondary carboxamide; tertiary amino compound	antineoplastic agent; Aurora kinase inhibitor	2019	2020	4.5	low	2	0
CDN1163	3	aromatic ether; quinolines; secondary carboxamide	SERCA activator	2017	2020	5.3	medium	3	0
gsk 269962a	3			2017	2020	5.3	medium	3	0
pha 848125	3			2017	2020	5.3	medium	3	0
tg101209	1	N-alkylpiperazine; N-arylpiperazine; pyrimidines; secondary amino compound; sulfonamide	antineoplastic agent; apoptosis inducer; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor	2017	2017	7.0	low	1	0
nvp-bhg712	3	benzamides		2017	2020	5.3	medium	3	0
pf 04217903	3	quinolines		2017	2020	5.3	medium	3	0
5-[[4-(4-acetylphenyl)-1-piperazinyl]sulfonyl]-1,3-dihydroindol-2-one	3	aromatic ketone		2017	2020	5.3	high	3	0
ph 797804	3	aromatic ether; benzamides; organobromine compound; organofluorine compound; pyridone	anti-inflammatory agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor	2017	2020	5.3	low	3	0
olaparib	1	cyclopropanes; monofluorobenzenes; N-acylpiperazine; phthalazines	antineoplastic agent; apoptosis inducer; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor	2022	2022	2.0	low	0	1
srt1720	3			2017	2020	5.3	low	3	0
cx 4945	1			2020	2020	4.0	low	1	0
purfalcamine	3			2017	2020	5.3	high	3	0
bms 754807	3	pyrazoles; pyridines; pyrrolidines; pyrrolotriazine	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor	2017	2020	5.3	low	3	0
ponatinib	4	(trifluoromethyl)benzenes; acetylenic compound; benzamides; imidazopyridazine; N-methylpiperazine	antineoplastic agent; tyrosine kinase inhibitor	2017	2020	5.0	low	4	0
quizartinib	3	benzoimidazothiazole; isoxazoles; morpholines; phenylureas	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; necroptosis inhibitor	2017	2020	5.3	low	3	0
PP121	3	aromatic amine; cyclopentanes; pyrazolopyrimidine; pyrrolopyridine	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; tyrosine kinase inhibitor	2017	2020	5.3	medium	3	0
az 505	1			2021	2021	3.0	low	0	1
navitoclax	3	aryl sulfide; monochlorobenzenes; morpholines; N-sulfonylcarboxamide; organofluorine compound; piperazines; secondary amino compound; sulfone; tertiary amino compound	antineoplastic agent; apoptosis inducer; B-cell lymphoma 2 inhibitor	2017	2020	5.3	low	3	0
gsk 650394	3	phenylpyridine		2017	2020	5.3	medium	3	0
dcc-2036	3	organofluorine compound; phenylureas; pyrazoles; pyridinecarboxamide; quinolines	tyrosine kinase inhibitor	2017	2020	5.3	medium	3	0
cabozantinib	3	aromatic ether; dicarboxylic acid diamide; organofluorine compound; quinolines	antineoplastic agent; tyrosine kinase inhibitor	2017	2020	5.3	low	3	0
incb-018424	1	nitrile; pyrazoles; pyrrolopyrimidine	antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor	2020	2020	4.0	low	1	0
bix 01294	1	piperidines		2021	2021	3.0	low	0	1
TAK-580	3	1,3-thiazolecarboxamide; aminopyrimidine; chloropyridine; organofluorine compound; pyrimidinecarboxamide; secondary carboxamide	antineoplastic agent; apoptosis inducer; B-Raf inhibitor	2017	2020	5.3	medium	3	0
8-(4-aminophenyl)-2-(4-morpholinyl)-1-benzopyran-4-one	3	chromones		2017	2020	5.3	high	3	0
pf 3758309	3	organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound		2017	2020	5.3	low	3	0
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol	2	benzyl alcohols; morpholines; pyridopyrimidine; tertiary amino compound	antineoplastic agent; apoptosis inducer; mTOR inhibitor	2019	2020	4.5	low	2	0
5-(2-benzofuranyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidine	3	aryl sulfide; thienopyrimidine		2017	2020	5.3	high	3	0
5-(3-methylsulfonylphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidine	3	aryl sulfide; thienopyrimidine		2017	2020	5.3	high	3	0
5-bromo-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidine	3	aryl sulfide; thienopyrimidine		2017	2020	5.3	high	3	0
baricitinib	3	azetidines; nitrile; pyrazoles; pyrrolopyrimidine; sulfonamide	anti-inflammatory agent; antirheumatic drug; antiviral agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; immunosuppressive agent	2017	2020	5.3	low	3	0
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-ylmethyl)-4-quinazolinamine	3	quinazolines		2017	2020	5.3	high	3	0
6-[(3-aminophenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinone	3	organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound		2017	2020	5.3	medium	3	0
e-52862	1			2020	2020	4.0	low	1	0
N-[(5-bromo-8-hydroxy-7-quinolinyl)-thiophen-2-ylmethyl]acetamide	3	hydroxyquinoline		2017	2020	5.3	high	3	0
p505-15	3			2017	2020	5.3	high	3	0
mrt67307	3	aromatic amine		2017	2020	5.3	medium	3	0
au-1	1			2016	2016	8.0	medium	1	0
N-[3-[[5-chloro-2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide	3	piperazines		2017	2020	5.3	high	3	0
ribociclib	3			2017	2020	5.3	low	3	0
1-[3-[4-[(1-methyl-5-tetrazolyl)thio]-5-thieno[2,3-d]pyrimidinyl]phenyl]ethanone	3	aromatic ketone; thienopyrimidine		2017	2020	5.3	high	3	0
5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine	1	benzoxazole		2020	2020	4.0	low	1	0
pha 793887	3	piperidinecarboxamide		2017	2020	5.3	high	3	0
gsk 2334470	1	indazoles		2019	2019	5.0	low	1	0
unc 0638	1	quinazolines		2021	2021	3.0	low	0	1
ml228 probe	3	1,2,4-triazines; biphenyls; pyridines; secondary amino compound	hypoxia-inducible factor pathway activator	2017	2020	5.3	high	3	0
pf-03882845	3			2017	2020	5.3	high	3	0
jq1 compound	22	carboxylic ester; organochlorine compound; tert-butyl ester; thienotriazolodiazepine	angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; bromodomain-containing protein 4 inhibitor; cardioprotective agent; ferroptosis inducer	2015	2022	5.5	high	19	3
pf-04620110	3			2017	2020	5.3	medium	3	0
gsk525762a	8	benzodiazepine		2016	2020	6.4	low	8	0
ML240	1	aromatic amine; aromatic ether; benzimidazoles; primary amino compound; quinazolines; secondary amino compound	antineoplastic agent	2020	2020	4.0	low	1	0
birinapant	1	dipeptide		2019	2019	5.0	low	1	0
torin 1	3	N-acylpiperazine; N-arylpiperazine; organofluorine compound; pyridoquinoline; quinolines	antineoplastic agent; mTOR inhibitor	2017	2020	5.3	medium	3	0
abt-199	3	aromatic ether; C-nitro compound; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; N-sulfonylcarboxamide; oxanes; pyrrolopyridine	antineoplastic agent; apoptosis inducer; B-cell lymphoma 2 inhibitor	2017	2020	5.3	low	3	0
1-[4-fluoro-3-(trifluoromethyl)phenyl]-3-(5-pyridin-4-yl-1,3,4-thiadiazol-2-yl)urea	3	ureas		2017	2020	5.3	medium	3	0
N-(4-methyl-2-pyridinyl)-4-[3-(trifluoromethyl)anilino]-1-piperidinecarbothioamide	3	(trifluoromethyl)benzenes		2017	2020	5.3	high	3	0
LSM-6732	1	organonitrogen heterocyclic compound; organosulfur heterocyclic compound; tert-butyl ester		2017	2017	7.0	medium	1	0
ncgc00242364	3	quinazolines		2017	2020	5.3	high	3	0
gsk1210151a	6	imidazoquinoline		2015	2020	6.7	low	6	0
i-bet726	3			2017	2018	6.3	high	3	0
hs-173	3			2017	2020	5.3	high	3	0
sr1664	3	indolecarboxamide		2017	2020	5.3	high	3	0
4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-n-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide	3			2017	2020	5.3	high	3	0
N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide	2	benzamides; N-acylpiperidine		2017	2020	5.5	high	2	0
N-[4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide	2	aminoquinoline		2017	2020	5.5	high	2	0
cudc-907	3			2017	2020	5.3	low	3	0
methacycline	1			2019	2019	5.0	low	1	0
methacycline monohydrochloride	2			2017	2020	5.5	low	2	0
2-[[[4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]-oxomethyl]amino]acetic acid	3	quinolines		2017	2020	5.3	high	3	0
agi-5198	3			2017	2020	5.3	low	3	0
cep-32496	3			2017	2020	5.3	medium	3	0
epz004777	3	N-glycosyl compound		2017	2020	5.3	low	3	0
3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid	3	organonitrogen heterocyclic compound		2017	2020	5.3	medium	3	0
entecavir	3	benzamides; N-acylpiperidine		2017	2020	5.3	medium	3	0
pelabresib	3	monochlorobenzenes; organic heterotricyclic compound; primary carboxamide	antineoplastic agent; bromodomain-containing protein 4 inhibitor	2019	2022	3.7	medium	2	1
gkt137831	3			2017	2020	5.3	low	3	0
vx-509	3			2017	2020	5.3	high	3	0
vx-970	3	sulfonamide		2017	2020	5.3	low	3	0
gs-9973	3			2017	2020	5.3	high	3	0
amg 925	3			2017	2020	5.3	high	3	0
epz-6438	1			2021	2021	3.0	low	0	1
sf 1126	1			2019	2019	5.0	low	1	0
gne-618	3			2017	2020	5.3	high	3	0
g007-lk	3			2017	2020	5.3	medium	3	0
volitinib	3			2017	2020	5.3	high	3	0
ML355	3	benzothiazoles; monomethoxybenzene; phenols; secondary amino compound; substituted aniline; sulfonamide	EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor; platelet aggregation inhibitor	2017	2020	5.3	high	3	0
acp-196	3	aromatic amine; benzamides; imidazopyrazine; pyridines; pyrrolidinecarboxamide; secondary carboxamide; tertiary carboxamide; ynone	antineoplastic agent; apoptosis inducer; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor	2017	2020	5.3	low	3	0
gsk343	4	aminopyridine; indazoles; N-alkylpiperazine; N-arylpiperazine; pyridone; secondary carboxamide	antineoplastic agent; apoptosis inducer; EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor	2017	2021	4.8	low	3	1
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide	3	quinazolines		2016	2021	5.3	medium	2	1
agi-6780	3			2017	2020	5.3	medium	3	0
khs101	3			2017	2020	5.3	medium	3	0
cb-839	3			2017	2020	5.3	low	3	0
gsk-j4	3	organonitrogen heterocyclic compound		2017	2020	5.3	low	3	0
pf-06424439	3			2017	2020	5.3	high	3	0
etp-46464	3			2017	2020	5.3	high	3	0
onc201	3			2017	2020	5.3	low	3	0
kai407	3			2017	2020	5.3	high	3	0
pf-06687252	1	azabicycloalkane; enone; phenols; pyridines		2016	2016	8.0	low	1	0
6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine	3			2017	2020	5.3	high	3	0
PF-06446846	1	benzamides; monochloropyridine; piperidines; tertiary carboxamide; triazolopyridine	antilipemic drug; EC 3.4.21.61 (kexin) inhibitor	2020	2020	4.0	medium	1	0
enasidenib	3	1,3,5-triazines; aminopyridine; aromatic amine; organofluorine compound; secondary amino compound; tertiary alcohol	antineoplastic agent; EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor	2017	2020	5.3	low	3	0
oicr-9429	3			2017	2020	5.3	medium	3	0
lly-507	3			2017	2020	5.3	medium	3	0
dBET6	1	organic molecular entity		2020	2020	4.0	medium	1	0
MZ1	1	organic molecular entity		2020	2020	4.0	medium	1	0
AZ3451	1	benzimidazoles; benzodioxoles; nitrile; organobromine compound; secondary carboxamide	anti-inflammatory agent; autophagy inducer; PAR2 negative allosteric modulator	2020	2020	4.0	medium	1	0
at 9283	3			2017	2020	5.3	medium	3	0
hypoxanthine	3	nucleobase analogue; oxopurine; purine nucleobase	fundamental metabolite	2017	2020	5.3	low	3	0
clozapine	3	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic	2017	2020	5.3	low	3	0
olanzapine	1	benzodiazepine; N-arylpiperazine; N-methylpiperazine	antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor	2020	2020	4.0	low	1	0
1-hydroxyphenazine	3	phenazines		2017	2020	5.3	low	3	0
ro 24-7429	3	benzodiazepine		2017	2020	5.3	medium	3	0
nintedanib	3			2017	2020	5.3	low	3	0
n'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthahydrazide	3	catechols; hydrazide; hydrazone; naphthols	EC 3.6.5.5 (dynamin GTPase) inhibitor	2017	2020	5.3	high	3	0
ver 52296	4	aromatic amide; isoxazoles; monocarboxylic acid amide; morpholines; resorcinols	angiogenesis inhibitor; antineoplastic agent; Hsp90 inhibitor	2017	2020	5.0	low	4	0
bmn 673	3			2017	2020	5.3	low	3	0

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery of
Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
Bioorganic & medicinal chemistry letters, , 08-15, Volume: 29, Issue:16, 2019

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.
Bioorganic & medicinal chemistry letters, , 08-15, Volume: 29, Issue:16, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Discovery of Thieno[2,3-
Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Discovery of
Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020

Discovery of Thieno[2,3-
Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020

Discovery of Benzo[
Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019

Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.
Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

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.
Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.
Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
Scientific reports, , 11-26, Volume: 10, Issue:1, 2020

Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
Bioorganic & medicinal chemistry, , 07-15, Volume: 27, Issue:14, 2019

Highly predictive and interpretable models for PAMPA permeability.
Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	Trials	2000's	2010's	post-2020
probucol	1	dithioketal; polyphenol	anti-inflammatory drug; anticholesteremic drug; antilipemic drug; antioxidant; cardiovascular drug	2011	2011	13.0	low	0	0	1	0
quinazolines	23	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines		2010	2017	10.6	low	5	2	21	0
phenyl acetate	1	benzenes; phenyl acetates		2011	2011	13.0	low	0	0	1	0
atorvastatin	1	aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic)	environmental contaminant; xenobiotic	2019	2019	5.0	low	1	0	1	0
triazoles	1	1,2,3-triazole		2014	2014	10.0	low	0	0	1	0
oxazolidin-2-one	1	carbamate ester; oxazolidinone	metabolite	2011	2011	13.0	low	0	0	1	0
varespladib	1	aromatic ether; benzenes; dicarboxylic acid monoamide; indoles; monocarboxylic acid; primary carboxamide	anti-inflammatory drug; antidote; EC 3.1.1.4 (phospholipase A2) inhibitor	2011	2011	13.0	low	0	0	1	0
succinobucol	1	benzoate ester; phenols		2011	2011	13.0	low	0	0	1	0
dalcetrapib	1	anilide		2011	2011	13.0	low	0	0	1	0
darapladib	1			2011	2011	13.0	low	0	0	1	0
anacetrapib	1			2011	2011	13.0	low	0	0	1	0
cardiovascular agents	3			2019	2021	3.7	low	1	0	1	2
gsk525762a	2	benzodiazepine		2014	2014	10.0	low	0	0	2	0
d-4f peptide	1			2011	2011	13.0	low	0	0	1	0

Condition	Indicated	Studies	First Year	Last Year	Average Age	Relationship Strength	Trials	2000's	2010's	post-2020
2019 Novel Coronavirus Disease	0	3	2020	2023	2.7	low	0	0	1	2
Acute Confusional Senile Dementia	0	1	2011	2011	13.0	low	0	0	1	0
Acute Coronary Syndrome	0	7	2011	2021	5.0	low	5	0	4	3
Acute Disease	0	1	2019	2019	5.0	low	0	0	1	0
Adjuvant Arthritis	0	1	2019	2019	5.0	low	0	0	1	0
alpha-Galactosidase A Deficiency	0	1	2022	2022	2.0	low	0	0	0	1
Alveolar Bone Atrophy	0	1	2023	2023	1.0	low	0	0	0	1
Alzheimer Disease	0	1	2011	2011	13.0	low	0	0	1	0
Angiitis	0	1	2019	2019	5.0	low	0	0	1	0
Aortic Diseases	0	1	2014	2014	10.0	low	0	0	1	0
Apoplexy	0	2	2019	2020	4.5	low	2	0	2	0
Arteriosclerosis, Coronary	0	6	2011	2019	10.7	low	4	0	6	0
Arthritis, Gouty	0	1	2019	2019	5.0	low	0	0	1	0
Atherogenesis	0	9	2011	2022	8.3	low	1	0	8	1
Atheroma	0	4	2012	2019	8.5	low	3	0	4	0
Atherosclerosis	0	9	2011	2022	8.3	low	1	0	8	1
Benign Neoplasms	0	1	2022	2022	2.0	low	0	0	0	1
Blood Poisoning	0	1	2022	2022	2.0	low	0	0	0	1
Breast Cancer	0	2	2017	2018	6.5	low	0	0	2	0
Breast Neoplasms	0	2	2017	2018	6.5	low	0	0	2	0
Cardiac Diseases	0	1	2021	2021	3.0	low	0	0	0	1
Cardiac Failure	0	3	2021	2021	3.0	low	2	0	0	3
Cardiovascular Diseases	0	22	2010	2023	5.5	medium	4	1	17	4
Cardiovascular Stroke	0	2	2019	2020	4.5	low	2	0	2	0
Chronic Kidney Diseases	0	4	2018	2021	4.5	low	3	0	3	1
Cognitive Decline	0	1	2021	2021	3.0	low	1	0	0	1
Cognitive Dysfunction	0	1	2021	2021	3.0	low	1	0	0	1
Colorectal Cancer	0	2	2018	2020	5.0	low	0	0	2	0
Colorectal Neoplasms	0	2	2018	2020	5.0	low	0	0	2	0
Complications of Diabetes Mellitus	0	1	2021	2021	3.0	low	1	0	0	1
Congenital Zika Syndrome	0	1	2020	2020	4.0	low	0	0	1	0
Coronary Artery Disease	0	6	2011	2019	10.7	low	4	0	6	0
Coronavirus Infections	0	1	2020	2020	4.0	low	0	0	1	0
Cytokine Release Syndrome	0	1	2023	2023	1.0	low	0	0	0	1
Diabetes Mellitus, Adult-Onset	0	10	2019	2023	3.2	low	5	0	5	5
Diabetes Mellitus, Type 2	0	10	2019	2023	3.2	low	5	0	5	5
Diabetic Angiopathies	0	1	2019	2019	5.0	low	1	0	1	0
Diabetic Glomerulosclerosis	0	1	2020	2020	4.0	low	0	0	1	0
Diabetic Nephropathies	0	1	2020	2020	4.0	low	0	0	1	0
Disease Exacerbation	0	1	2016	2016	8.0	low	1	0	1	0
Disease Models, Animal	0	4	2010	2020	6.8	low	1	1	3	0
Diseases, Metabolic	0	1	2015	2015	9.0	low	0	0	1	0
Dyslipidemia	0	2	2012	2015	10.5	low	0	0	2	0
Dyslipidemias	0	2	2012	2015	10.5	low	0	0	2	0
Endotoxemia	0	1	2020	2020	4.0	low	0	0	1	0
ER-Negative PR-Negative HER2-Negative Breast Cancer	0	1	2019	2019	5.0	low	0	0	1	0
Fabry Disease	1	1	2022	2022	2.0	low	0	0	0	1
Familial Primary Pulmonary Hypertension	0	1	2020	2020	4.0	low	0	0	1	0
Gouty Arthritis	0	1	2019	2019	5.0	low	0	0	1	0
Heart Diseases	0	1	2021	2021	3.0	low	0	0	0	1
Heart Failure	0	3	2021	2021	3.0	low	2	0	0	3
Heritable Pulmonary Arterial Hypertension	0	1	2020	2020	4.0	low	0	0	1	0
HIV Coinfection	0	2	2017	2021	5.0	low	0	0	1	1
HIV Infections	0	2	2017	2021	5.0	low	0	0	1	1
Hyperlipemia	0	1	2014	2014	10.0	low	0	0	1	0
Hyperlipidemias	0	1	2014	2014	10.0	low	0	0	1	0
Infections, Coronavirus	0	1	2020	2020	4.0	low	0	0	1	0
Inflammation	0	11	2014	2023	3.3	low	0	0	4	7
Innate Inflammatory Response	0	11	2014	2023	3.3	low	0	0	4	7
Invasiveness, Neoplasm	0	1	2018	2018	6.0	low	0	0	1	0
Kahler Disease	0	1	2019	2019	5.0	low	0	0	1	0
Leucocythaemia	0	4	2014	2019	7.0	low	0	0	4	0
Leukemia	0	4	2014	2019	7.0	low	0	0	4	0
Metabolic Diseases	0	1	2015	2015	9.0	low	0	0	1	0
Multiple Myeloma	0	1	2019	2019	5.0	low	0	0	1	0
Myocardial Infarction	0	2	2019	2020	4.5	low	2	0	2	0
Neoplasms	0	1	2022	2022	2.0	low	0	0	0	1
Obesity	0	2	2023	2023	1.0	low	0	0	0	2
Pericementitis	0	1	2023	2023	1.0	low	0	0	0	1
Periodontitis	0	1	2023	2023	1.0	low	0	0	0	1
Pneumonia, Viral	0	1	2020	2020	4.0	low	0	0	1	0
Prediabetes	0	1	2016	2016	8.0	low	1	0	1	0
Prediabetic State	0	1	2016	2016	8.0	low	1	0	1	0
Pulmonary Arterial Hypertension	0	3	2019	2020	4.3	low	0	0	3	0
Pulmonary Arterial Remodeling	0	1	2019	2019	5.0	low	0	0	1	0
Recrudescence	0	1	2021	2021	3.0	low	1	0	0	1
Renal Insufficiency, Chronic	1	4	2018	2021	4.5	low	3	0	3	1
Sepsis	0	1	2022	2022	2.0	low	0	0	0	1
Stroke	0	2	2019	2020	4.5	low	2	0	2	0
Triple Negative Breast Neoplasms	0	1	2019	2019	5.0	low	0	0	1	0
Vascular Calcification	0	1	2019	2019	5.0	low	0	0	1	0
Vasculitis	0	1	2019	2019	5.0	low	0	0	1	0
Zika Virus Infection	0	1	2020	2020	4.0	low	0	0	1	0

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

More Insights into the Association between RVX-208 and Pulmonary Arterial Hypertension.
American journal of respiratory and critical care medicine, , 02-01, Volume: 201, Issue:3, 2020

Reply to Ning
American journal of respiratory and critical care medicine, , 02-01, Volume: 201, Issue:3, 2020

Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension.
American journal of respiratory and critical care medicine, , 10-01, Volume: 200, Issue:7, 2019

Discovery of Benzo[
Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019

Rvx 208.
Drugs in R&D, , Volume: 11, Issue:2, 2011

Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy.
Pharmacology research & perspectives, , Volume: 10, Issue:3, 2022

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

BRCA1 deficiency sensitizes breast cancer cells to bromodomain and extra-terminal domain (BET) inhibition.
Oncogene, , Volume: 37, Issue:49, 2018

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.
Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017

Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis, , Volume: 364, 2023

Cognitive Effects of the BET Protein Inhibitor Apabetalone: A Prespecified Montreal Cognitive Assessment Analysis Nested in the BETonMACE Randomized Controlled Trial.
Journal of Alzheimer's disease : JAD, , Volume: 83, Issue:4, 2021

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Pharmacologic epigenetic modulators of alkaline phosphatase in chronic kidney disease.
Current opinion in nephrology and hypertension, , Volume: 29, Issue:1, 2020

Epigenetic Therapeutics for Cardiovascular Disease: Writing, Erasing, Reading, and Maybe Forgetting.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

BET Epigenetic Reader Proteins in Cardiovascular Transcriptional Programs.
Circulation research, , 04-24, Volume: 126, Issue:9, 2020

Apabetalone - BET protein inhibition in cardiovascular disease and Type 2 diabetes.
Future cardiology, , Volume: 16, Issue:5, 2020

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response
Cardiovascular therapeutics, , Volume: 2020, 2020

How Might Bromodomain and Extra-Terminal (BET) Inhibitors Operate in Cardiovascular Disease?
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 19, Issue:2, 2019

Apabetalone downregulates factors and pathways associated with vascular calcification.
Atherosclerosis, , Volume: 280, 2019

Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.
Clinical epigenetics, , 07-12, Volume: 11, Issue:1, 2019

Apabetalone lowers serum alkaline phosphatase and improves cardiovascular risk in patients with cardiovascular disease.
Atherosclerosis, , Volume: 290, 2019

Apabetalone Mediated Epigenetic Modulation is Associated with Favorable Kidney Function and Alkaline Phosphatase Profile in Patients with Chronic Kidney Disease.
Kidney & blood pressure research, , Volume: 43, Issue:2, 2018

Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208).
Journal of cardiovascular translational research, , Volume: 10, Issue:4, 2017

Evaluation of HDL-modulating interventions for cardiovascular risk reduction using a systems pharmacology approach.
Journal of lipid research, , Volume: 57, Issue:1, 2016

RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease.
Atherosclerosis, , Volume: 247, 2016

Emerging small molecule drugs.
Handbook of experimental pharmacology, , Volume: 224, 2015

Novel HDL-based therapeutic agents.
Pharmacology & therapeutics, , Volume: 135, Issue:1, 2012

RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases.
Current opinion in investigational drugs (London, England : 2000), , Volume: 11, Issue:3, 2010

The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 19, Issue:1, 2019

Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 16, Issue:1, 2016

ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies.
Cardiovascular drugs and therapy, , Volume: 26, Issue:2, 2012

Atherosclerosis: targeting endogenous apo A-I--a new approach for raising HDL.
Nature reviews. Cardiology, , Volume: 8, Issue:4, 2011

Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial.
Journal of the American College of Cardiology, , Mar-01, Volume: 57, Issue:9, 2011

Apolipoprotein A-I therapy promise, challenges, and disappointment.
Journal of the American College of Cardiology, , Mar-01, Volume: 57, Issue:9, 2011

Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis, , Volume: 364, 2023

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Relation of insulin treatment for type 2 diabetes to the risk of major adverse cardiovascular events after acute coronary syndrome: an analysis of the BETonMACE randomized clinical trial.
Cardiovascular diabetology, , 06-22, Volume: 20, Issue:1, 2021

Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study.
Cardiovascular diabetology, , 01-07, Volume: 20, Issue:1, 2021

Epigenetic Therapeutics for Cardiovascular Disease: Writing, Erasing, Reading, and Maybe Forgetting.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

Apabetalone - BET protein inhibition in cardiovascular disease and Type 2 diabetes.
Future cardiology, , Volume: 16, Issue:5, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Epigenetic Modifiers as Potential Therapeutic Targets in Diabetic Kidney Disease.
International journal of molecular sciences, , Jun-09, Volume: 21, Issue:11, 2020

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Cell, , 04-15, Volume: 184, Issue:8, 2021

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study.
Cardiovascular diabetology, , 01-07, Volume: 20, Issue:1, 2021

Epigenetic Therapies for Heart Failure: Current Insights and Future Potential.
Vascular health and risk management, , Volume: 17, 2021

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

Selective BET inhibitor RVX-208 ameliorates periodontal inflammation and bone loss.
Journal of clinical periodontology, , Volume: 50, Issue:12, 2023

Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis, , Volume: 364, 2023

Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation.
International immunopharmacology, , Volume: 117, 2023

Small Molecule BRD4 Inhibitors Apabetalone and JQ1 Rescues Endothelial Cells Dysfunction, Protects Monolayer Integrity and Reduces Midkine Expression.
Molecules (Basel, Switzerland), , Nov-02, Volume: 27, Issue:21, 2022

Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy.
Pharmacology research & perspectives, , Volume: 10, Issue:3, 2022

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Cell, , 04-15, Volume: 184, Issue:8, 2021

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension.
American journal of respiratory and critical care medicine, , 10-01, Volume: 200, Issue:7, 2019

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
European journal of medicinal chemistry, , May-10, Volume: 151, 2018

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019

Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.
Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Targeting the BET family for the treatment of leukemia.
Epigenomics, , Volume: 6, Issue:2, 2014

An evaluation of RVX-208 for the treatment of atherosclerosis.
Expert opinion on investigational drugs, , Volume: 24, Issue:10, 2015

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.
European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022

Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis, , Volume: 364, 2023

Selective BET inhibitor RVX-208 ameliorates periodontal inflammation and bone loss.
Journal of clinical periodontology, , Volume: 50, Issue:12, 2023

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Effects of the BET-inhibitor, RVX-208 on the HDL lipidome and glucose metabolism in individuals with prediabetes: A randomized controlled trial.
Metabolism: clinical and experimental, , Volume: 65, Issue:6, 2016

Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.
Clinical epigenetics, , 07-12, Volume: 11, Issue:1, 2019

Discovery of Thieno[2,3-
Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020

ABCA1 overexpression worsens colorectal cancer prognosis by facilitating tumour growth and caveolin-1-dependent invasiveness, and these effects can be ameliorated using the BET inhibitor apabetalone.
Molecular oncology, , Volume: 12, Issue:10, 2018

Discovery of Benzo[
Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019

HIV latency reversal agents: A potential path for functional cure?
European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021

BET inhibitors RVX-208 and PFI-1 reactivate HIV-1 from latency.
Scientific reports, , 11-30, Volume: 7, Issue:1, 2017

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022

Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response
Cardiovascular therapeutics, , Volume: 2020, 2020

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Emerging small molecule drugs.
Handbook of experimental pharmacology, , Volume: 224, 2015

Novel HDL-based therapeutic agents.
Pharmacology & therapeutics, , Volume: 135, Issue:1, 2012

Small Molecule BRD4 Inhibitors Apabetalone and JQ1 Rescues Endothelial Cells Dysfunction, Protects Monolayer Integrity and Reduces Midkine Expression.
Molecules (Basel, Switzerland), , Nov-02, Volume: 27, Issue:21, 2022

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 19, Issue:1, 2019

RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease.
Atherosclerosis, , Volume: 247, 2016

An evaluation of RVX-208 for the treatment of atherosclerosis.
Expert opinion on investigational drugs, , Volume: 24, Issue:10, 2015

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
PloS one, , Volume: 8, Issue:12, 2013

Rvx 208.
Drugs in R&D, , Volume: 11, Issue:2, 2011

[Novel therapy for atherosclerosis and inflammatory vascular disease].
Nihon rinsho. Japanese journal of clinical medicine, , Volume: 69, Issue:1, 2011

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Pharmacologic epigenetic modulators of alkaline phosphatase in chronic kidney disease.
Current opinion in nephrology and hypertension, , Volume: 29, Issue:1, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Apabetalone Mediated Epigenetic Modulation is Associated with Favorable Kidney Function and Alkaline Phosphatase Profile in Patients with Chronic Kidney Disease.
Kidney & blood pressure research, , Volume: 43, Issue:2, 2018

Relation of insulin treatment for type 2 diabetes to the risk of major adverse cardiovascular events after acute coronary syndrome: an analysis of the BETonMACE randomized clinical trial.
Cardiovascular diabetology, , 06-22, Volume: 20, Issue:1, 2021

Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study.
Cardiovascular diabetology, , 01-07, Volume: 20, Issue:1, 2021

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Epigenetic Therapeutics for Cardiovascular Disease: Writing, Erasing, Reading, and Maybe Forgetting.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Rvx 208.
Drugs in R&D, , Volume: 11, Issue:2, 2011

Cognitive Effects of the BET Protein Inhibitor Apabetalone: A Prespecified Montreal Cognitive Assessment Analysis Nested in the BETonMACE Randomized Controlled Trial.
Journal of Alzheimer's disease : JAD, , Volume: 83, Issue:4, 2021

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019

Reply to Ning
American journal of respiratory and critical care medicine, , 02-01, Volume: 201, Issue:3, 2020

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 16, Issue:1, 2016

Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.
European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Emerging small molecule drugs.
Handbook of experimental pharmacology, , Volume: 224, 2015

Novel HDL-based therapeutic agents.
Pharmacology & therapeutics, , Volume: 135, Issue:1, 2012

Small Molecule BRD4 Inhibitors Apabetalone and JQ1 Rescues Endothelial Cells Dysfunction, Protects Monolayer Integrity and Reduces Midkine Expression.
Molecules (Basel, Switzerland), , Nov-02, Volume: 27, Issue:21, 2022

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 19, Issue:1, 2019

RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease.
Atherosclerosis, , Volume: 247, 2016

An evaluation of RVX-208 for the treatment of atherosclerosis.
Expert opinion on investigational drugs, , Volume: 24, Issue:10, 2015

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
PloS one, , Volume: 8, Issue:12, 2013

[Novel therapy for atherosclerosis and inflammatory vascular disease].
Nihon rinsho. Japanese journal of clinical medicine, , Volume: 69, Issue:1, 2011

Rvx 208.
Drugs in R&D, , Volume: 11, Issue:2, 2011

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Pharmacologic epigenetic modulators of alkaline phosphatase in chronic kidney disease.
Current opinion in nephrology and hypertension, , Volume: 29, Issue:1, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Apabetalone Mediated Epigenetic Modulation is Associated with Favorable Kidney Function and Alkaline Phosphatase Profile in Patients with Chronic Kidney Disease.
Kidney & blood pressure research, , Volume: 43, Issue:2, 2018

The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 19, Issue:1, 2019

Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 16, Issue:1, 2016

An evaluation of RVX-208 for the treatment of atherosclerosis.
Expert opinion on investigational drugs, , Volume: 24, Issue:10, 2015

ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies.
Cardiovascular drugs and therapy, , Volume: 26, Issue:2, 2012

Cognitive Effects of the BET Protein Inhibitor Apabetalone: A Prespecified Montreal Cognitive Assessment Analysis Nested in the BETonMACE Randomized Controlled Trial.
Journal of Alzheimer's disease : JAD, , Volume: 83, Issue:4, 2021

Apabetalone downregulates factors and pathways associated with vascular calcification.
Atherosclerosis, , Volume: 280, 2019

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019

Reply to Ning
American journal of respiratory and critical care medicine, , 02-01, Volume: 201, Issue:3, 2020

Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension.
American journal of respiratory and critical care medicine, , 10-01, Volume: 200, Issue:7, 2019

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation.
International immunopharmacology, , Volume: 117, 2023

Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation.
International immunopharmacology, , Volume: 117, 2023

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Cell, , 04-15, Volume: 184, Issue:8, 2021

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Nature, , Volume: 583, Issue:7816, 2020

Rvx 208.
Drugs in R&D, , Volume: 11, Issue:2, 2011

Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy.
Pharmacology research & perspectives, , Volume: 10, Issue:3, 2022

Discovery of Benzo[
Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019

BRCA1 deficiency sensitizes breast cancer cells to bromodomain and extra-terminal domain (BET) inhibition.
Oncogene, , Volume: 37, Issue:49, 2018

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.
Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017

The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 19, Issue:1, 2019

Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial.
American journal of cardiovascular drugs : drugs, devices, and other interventions, , Volume: 16, Issue:1, 2016

ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies.
Cardiovascular drugs and therapy, , Volume: 26, Issue:2, 2012

Atherosclerosis: targeting endogenous apo A-I--a new approach for raising HDL.
Nature reviews. Cardiology, , Volume: 8, Issue:4, 2011

Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial.
Journal of the American College of Cardiology, , Mar-01, Volume: 57, Issue:9, 2011

Apolipoprotein A-I therapy promise, challenges, and disappointment.
Journal of the American College of Cardiology, , Mar-01, Volume: 57, Issue:9, 2011

Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis, , Volume: 364, 2023

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study.
Cardiovascular diabetology, , 01-07, Volume: 20, Issue:1, 2021

Relation of insulin treatment for type 2 diabetes to the risk of major adverse cardiovascular events after acute coronary syndrome: an analysis of the BETonMACE randomized clinical trial.
Cardiovascular diabetology, , 06-22, Volume: 20, Issue:1, 2021

Epigenetic Therapeutics for Cardiovascular Disease: Writing, Erasing, Reading, and Maybe Forgetting.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Apabetalone - BET protein inhibition in cardiovascular disease and Type 2 diabetes.
Future cardiology, , Volume: 16, Issue:5, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

Epigenetic Modifiers as Potential Therapeutic Targets in Diabetic Kidney Disease.
International journal of molecular sciences, , Jun-09, Volume: 21, Issue:11, 2020

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response
Cardiovascular therapeutics, , Volume: 2020, 2020

Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension.
American journal of respiratory and critical care medicine, , 10-01, Volume: 200, Issue:7, 2019

RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo.
Journal of the American College of Cardiology, , Jun-08, Volume: 55, Issue:23, 2010

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Cell, , 04-15, Volume: 184, Issue:8, 2021

Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome: Results from the BETonMACE Randomized Controlled Trial.
Clinical journal of the American Society of Nephrology : CJASN, , 05-08, Volume: 16, Issue:5, 2021

Epigenetic Therapies for Heart Failure: Current Insights and Future Potential.
Vascular health and risk management, , Volume: 17, 2021

Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study.
Cardiovascular diabetology, , 01-07, Volume: 20, Issue:1, 2021

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

Selective BET inhibitor RVX-208 ameliorates periodontal inflammation and bone loss.
Journal of clinical periodontology, , Volume: 50, Issue:12, 2023

Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation.
International immunopharmacology, , Volume: 117, 2023

Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells.
Atherosclerosis, , Volume: 364, 2023

Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy.
Pharmacology research & perspectives, , Volume: 10, Issue:3, 2022

Small Molecule BRD4 Inhibitors Apabetalone and JQ1 Rescues Endothelial Cells Dysfunction, Protects Monolayer Integrity and Reduces Midkine Expression.
Molecules (Basel, Switzerland), , Nov-02, Volume: 27, Issue:21, 2022

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection.
Cell, , 04-15, Volume: 184, Issue:8, 2021

BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes.
Clinical epigenetics, , 11-11, Volume: 12, Issue:1, 2020

Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension.
American journal of respiratory and critical care medicine, , 10-01, Volume: 200, Issue:7, 2019

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
European journal of medicinal chemistry, , May-10, Volume: 151, 2018

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Atherosclerosis, , Volume: 236, Issue:1, 2014

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019

Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.
Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.
Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016

Targeting the BET family for the treatment of leukemia.
Epigenomics, , Volume: 6, Issue:2, 2014

An evaluation of RVX-208 for the treatment of atherosclerosis.
Expert opinion on investigational drugs, , Volume: 24, Issue:10, 2015

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.
JAMA, , 04-28, Volume: 323, Issue:16, 2020

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial.
American heart journal, , Volume: 217, 2019

ABCA1 overexpression worsens colorectal cancer prognosis by facilitating tumour growth and caveolin-1-dependent invasiveness, and these effects can be ameliorated using the BET inhibitor apabetalone.
Molecular oncology, , Volume: 12, Issue:10, 2018

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.
European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022

Selective BET inhibitor RVX-208 ameliorates periodontal inflammation and bone loss.
Journal of clinical periodontology, , Volume: 50, Issue:12, 2023

Effects of the BET-inhibitor, RVX-208 on the HDL lipidome and glucose metabolism in individuals with prediabetes: A randomized controlled trial.
Metabolism: clinical and experimental, , Volume: 65, Issue:6, 2016

Relation of insulin treatment for type 2 diabetes to the risk of major adverse cardiovascular events after acute coronary syndrome: an analysis of the BETonMACE randomized clinical trial.
Cardiovascular diabetology, , 06-22, Volume: 20, Issue:1, 2021

Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.
Clinical epigenetics, , 07-12, Volume: 11, Issue:1, 2019

Discovery of Thieno[2,3-
Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020

ABCA1 overexpression worsens colorectal cancer prognosis by facilitating tumour growth and caveolin-1-dependent invasiveness, and these effects can be ameliorated using the BET inhibitor apabetalone.
Molecular oncology, , Volume: 12, Issue:10, 2018

Discovery of Benzo[
Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019

HIV latency reversal agents: A potential path for functional cure?
European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021

BET inhibitors RVX-208 and PFI-1 reactivate HIV-1 from latency.
Scientific reports, , 11-30, Volume: 7, Issue:1, 2017

Selective BET inhibitor RVX-208 ameliorates periodontal inflammation and bone loss.
Journal of clinical periodontology, , Volume: 50, Issue:12, 2023

rvx 208

Description

Cross-References

Synonyms (63)

Protein Targets (11)

Potency Measurements

Inhibition Measurements

Activation Measurements

Bioassays (254)

Research

Studies (92)

Study Types

Safety/Toxicity (1)

Bioavailability (4)

Dosage (2)

Article	Year
A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis, , Volume: 236, Issue:1	2014
RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases. Current opinion in investigational drugs (London, England : 2000), , Volume: 11, Issue:3	2010

rvx 208

Description

Cross-References

Synonyms (63)

Protein Targets (11)

Potency Measurements

Inhibition Measurements

Activation Measurements

Bioassays (254)

Research

Studies (92)

Study Types

Related Drugs (458)

Drugs Involved in Assays Together (445)

Drugs Researched Together (14)

Related Conditions (83)

Safety/Toxicity (1)

Bioavailability (4)

Dosage (2)