Page last updated: 2024-08-02 20:03:46

nutlin-3a

Description

nutlin 3: an MDM2 antagonist; structure in first source [MeSH]

4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazol-1-yl]-oxomethyl]-2-piperazinone : no description available [CHeBI]

Cross-References

ID Source	ID
PubMed CID	11433190
CHEMBL ID	191334
SCHEMBL ID	1155752
CHEBI ID	95096
MeSH ID	M0510642

Synonyms (71)

Synonym
HY-10029
nutlin-3
nutlin 3
nutlin-3a ,
(4s,5r)-nutlin-3
4-((4s,5r)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
(rac)-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl)(piperazin-1-yl)methanone
bdbm50229787
rac-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
4-[(4s,5r)-4,5-bis-(4-chloro-phenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
nsc-732664
CHEMBL191334 ,
nsc 732664
53ia0v845c ,
unii-53ia0v845c
BCP9001003
675576-98-4
(+)-nutlin-3
4HG7
4J3E
CS-0296
(-)-nutlin 3
4-(((4s,5r)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl)carbonyl)piperazin-2-one
rebemadlin
sml-0580
rebemadlin [inn]
S8059
nutlin 3a
l7c92ioe65 ,
2-piperazinone, 4-(((4s,5r)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1h-imidazol-1-yl)carbonyl)-
unii-l7c92ioe65
SCHEMBL1155752
2-piperazinone, 4-(((4r,5s)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1h-imidazol-1-yl)carbonyl)-, rel-
4-[[(4s,5r)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1h-imidazol-1-yl]carbonyl]-2-piperazinone
nutlin-3, (-)-
BDUHCSBCVGXTJM-WUFINQPMSA-N
4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4, 5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
HMS3649P17
4-[(4s,5r)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
nutlin 3b
nutlin (3a)
EX-A1359
AKOS027422740
CHEBI:95096
nutlin-3a chiral
(-)-nutlin-3
(?)-nutlin-3
4-[(4s,5r)-4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1h-imidazole-1-carbonyl]piperazin-2-one
AS-75148
nutlin-3a, >=98% (hplc)
AC-35379
NCGC00344347-05
nutlin3a
Q27166862
(+/-)-4-[4,5-bis-(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
548472-68-0 (4r5s, and 4s5r)
mfcd14636430
SR-01000946691-1
sr-01000946691
4-[cis-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl]piperazin-2-one
675576-98-4 (4s5r)
nsc763443
nsc-763443
nsc-756875
nsc-756876
nsc756876
nsc756875
(-)-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
DTXSID801317967
4-[(4s,5r)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
Z2037279564

Drug Classes (1)

Class	Description
stilbenoid	Any olefinic compound characterised by a 1,2-diphenylethylene backbone.

Protein Targets (15)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	0.3379	AID1645841
cytochrome P450 2D6	Homo sapiens (human)	Potency	13.4504	AID1645840
Cellular tumor antigen p53	Homo sapiens (human)	Potency	0.3000	AID243263
E3 ubiquitin-protein ligase Mdm2	Homo sapiens (human)	Potency	0.3000	AID243263

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Protein Mdm4	Homo sapiens (human)	IC50	4.6273	AID1238675; AID1285801; AID1908071; AID453615
Protein Mdm4	Homo sapiens (human)	Ki	5.8600	AID707317
Cellular tumor antigen p53	Homo sapiens (human)	IC50	3.4349	AID1238620; AID1239847; AID1285800; AID1285801; AID1285802; AID1285803; AID1300245; AID1387289; AID1632470; AID1720556; AID1872997; AID1908070; AID1908071; AID438431; AID438435; AID658338; AID706601; AID706602; AID706603; AID721248
Cellular tumor antigen p53	Homo sapiens (human)	Ki	1.2860	AID626520; AID707317; AID707326; AID749326; AID749491
Apoptosis regulator Bcl-2	Homo sapiens (human)	Ki	10.0000	AID1296598
E3 ubiquitin-protein ligase Mdm2	Mus musculus (house mouse)	Ki	0.0199	AID1238646
Cytochrome P450 2C19	Homo sapiens (human)	IC50	0.0700	AID1300245
Death-associated protein kinase 1	Homo sapiens (human)	IC50	25.0000	AID1285802
E3 ubiquitin-protein ligase Mdm2	Canis lupus familiaris (dog)	Ki	0.0105	AID1238645
E3 ubiquitin-protein ligase Mdm2	Homo sapiens (human)	IC50	1.4548	AID1125680; AID1195730; AID1238620; AID1239847; AID1252240; AID1285800; AID1300245; AID1387289; AID1420852; AID1421138; AID1555409; AID1632470; AID1656006; AID1659344; AID1720556; AID1872997; AID1908070; AID265956; AID318566; AID417066; AID453614; AID587349; AID587948; AID658338; AID691697; AID700922; AID706601; AID706602; AID721248; AID738689; AID739072; AID739073; AID746383; AID748501
E3 ubiquitin-protein ligase Mdm2	Homo sapiens (human)	Ki	0.0860	AID1143657; AID1152866; AID1238644; AID1296599; AID1361628; AID1415891; AID1656007; AID1908077; AID265955; AID267242; AID626520; AID684825; AID707326; AID749326; AID749491
Induced myeloid leukemia cell differentiation protein Mcl-1	Homo sapiens (human)	Ki	10.0000	AID1296597
Peptidyl-prolyl cis-trans isomerase D	Homo sapiens (human)	IC50	25.0000	AID1285803
Histone deacetylase 1	Homo sapiens (human)	IC50	100.0000	AID1361627

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Apoptosis regulator Bcl-2	Homo sapiens (human)	Kd	15.0000	AID1296639
Delta-type opioid receptor	Mus musculus (house mouse)	Kd	0.5000	AID362382
E3 ubiquitin-protein ligase Mdm2	Homo sapiens (human)	Kd	0.6050	AID1296640; AID362378; AID362381; AID362382; AID362383; AID362384; AID362385
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	Kd	0.5000	AID362385

Bioassays (378)

Assay ID	Title	Year	Journal	Article
AID756930	Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 3 uM after 24 to 72 hrs by annexin V-FITC/propidium iodide staining based FACS flow cytometry (Rvb = 4 %)	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1125680	Binding affinity to HDM2 (unknown origin) by fluorescence polarization peptide displacement assay	2014	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3405	Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
AID1908076	Displacement of 5-FAM labeled PDI peptide from MDM4 C17S mutant (14 to 111 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant incubated for 1.5 hrs by fluorescence polarization competition assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID756946	Cytotoxicity against human HGF cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID748499	Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID706602	Inhibition of human MDM2-p53 interaction after 18 hrs by HTRF assay in presence of 15% human serum	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 ISSN: 1520-4804	Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID1238620	Inhibition of MDM2/p53 interaction (unknown origin) using biotinylated MDM2 and Cy5-p53 (18 to 26 amino acids) by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1285810	Upregulation of p53 in human MCF7 cells after 24 hrs by Western blot analysis	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID621852	Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay	2011	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 ISSN: 1464-3405	MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1125677	Permeability of the compound in human Caco2 cells	2014	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3405	Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
AID1908032	Upregulation of p53 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1300940	Decrease in procaspase-3 expression level in human p53-null HCT116 -/- cells at 10 uM after 24 hrs by western blot analysis	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID739072	Inhibition of human recombinant GST-thrombin-MDM2 (1 to 188) expressed in Escherichia coli assessed as reduction of MDM2-p53 interaction incubated for 20 mins followed by p53 addition measured after 60 mins by HTRF assay in presence of 15% serum	2013	Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 ISSN: 1520-4804	Rational design and binding mode duality of MDM2-p53 inhibitors.
AID541422	Inhibition of human recombinant p53-MDM2 interaction assessed as p53 release by NMR spectroscopy relative to untreated control	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 ISSN: 1520-4804	Identification of the spiro(oxindole-3,3'-thiazolidine)-based derivatives as potential p53 activity modulators.
AID1296620	Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at G1 phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 28%)	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID626520	Inhibition of Mdm2-p53 protein interaction preincubated for 30 mins by fluorescence polarization assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 ISSN: 1768-3254	Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction.
AID756944	Inhibition of p53-MDM2 interaction (unknown origin) at 5 uM after 1 hr by ELISA	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1212290	Drug uptake in C57BL/6 mouse plasma at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1366819	Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID503026	Antiproliferative activity against human MCF7 cells at 4 uM after 14 days by coomassie staining	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1908081	Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1155057	Antiproliferative activity against human SK-UT-1 cells expressing p53 mutant protein by cell Titer-Glo assay	2014	ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 ISSN: 1948-5875	Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
AID756938	Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 3 uM after 24 to 72 hrs by propidium iodide staining-based FACS analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1361647	Induction of apoptosis in human A549 cells assessed as viable cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 93.01%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID503032	Induction of cell cycle arrest in human MCF7 cells 53BP1-targeting iRNA-based shRNA assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID749326	Inhibition of p53-MDM2 (unknown origin) interaction expressed in Escherichia coli BL-21 (DE3) after 1 hr by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1296639	Binding affinity to 15N-labeled Bcl-2 (unknown origin) by 2D 1H-15N HSQC NMR spectroscopic method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1143658	Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID738689	Inhibition of MDM2 (unknown origin) assessed as activation of p53	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID415699	Inhibition of interaction between human DMX(1-555) and p53 at upto 30 uM	2009	Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 ISSN: 1464-3391	Beta-peptides with improved affinity for hDM2 and hDMX.
AID1296597	Displacement of FAM-Bid peptide from N-terminal 8x His-tagged MCl-1 (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1908031	Upregulation of MDM2 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID739073	Inhibition of human recombinant GST-thrombin-MDM2 (1 to 188) expressed in Escherichia coli assessed as reduction of MDM2-p53 interaction incubated for 20 mins followed by p53 addition measured after 60 mins by HTRF assay	2013	Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 ISSN: 1520-4804	Rational design and binding mode duality of MDM2-p53 inhibitors.
AID1212300	Drug uptake in C57BL/6 mouse liver at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID362381	Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration	2008	Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 ISSN: 1520-4804	NMR screening for lead compounds using tryptophan-mutated proteins.
AID707326	Inhibition of p53-MDM2 interaction after 1 hr by fluorescence polarization assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID265955	Displacement of PMDM6-F from human recombinant MDM2	2006	Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 ISSN: 0022-2623	Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
AID438432	Induction of p21 mRNA in human HCT116 cells by RT-PCR	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID738714	Antiproliferative activity against human RKO cells expressing wild type p53 after 5 days by MTS assay	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID587349	Inhibition of human GST-tagged Mdm2 expressed in Escherichia coli harboring integrated p53-Mmd2 protein assessed as blockade of enzyme-p53 interaction by ELISA assay	2011	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 ISSN: 1464-3405	Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
AID1300910	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1361650	Induction of apoptosis in human A549 cells assessed as necrotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 0.52%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1249875	Activation of p53 in human U2OS cells assessed as increase of MDM2 expression at 2.5 uM after 12 hrs by Western blotting	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8 ISSN: 1948-5875	Discovery of Novel Isatin-Based p53 Inducers.
AID1212292	Drug uptake in C57BL/6 mouse adrenal gland at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID749490	Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID621851	Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay	2011	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 ISSN: 1464-3405	MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1674908	Inhibition of P-gp-mediated Rhodamine-123 efflux in human p53 +/+ H1299 cells assessed as Rhodamine-123 accumulation measured after 40 mins by spectrofluorimetry	2020	Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18 ISSN: 1464-3405	Mdm2 inhibitors as a platform for the design of P-glycoprotein inhibitors.
AID362385	Binding affinity to human recombinant Mdm2 F55W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration	2008	Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 ISSN: 1520-4804	NMR screening for lead compounds using tryptophan-mutated proteins.
AID1908078	Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1361624	Growth inhibition of Saccharomyces cerevisiae expressing p53 at 10 uM after 42 hrs by Yeast-based assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-3254	Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID749488	Inhibition of p53/MDM2 (1 to 118) (unknown origin) interaction at 10 uM after 1 hr by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID1285800	Inhibition of Flag-tagged p53/GST-tagged Mdm2 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1300908	Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1361627	Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1361653	Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.37%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1195733	Cytotoxicity against human RKO cells	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 ISSN: 1520-4804	Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID749491	Inhibition of p53/MDM2 (1 to 118) (unknown origin) interaction after 1 hr by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID503037	Induction of p53 accumulation in human MCF7 cells after 18 hrs by Western blot analysis in presence of 2.5 mM caffeine	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1296633	Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID749324	Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1361625	Growth inhibition of Saccharomyces cerevisiae expressing MDM2 at 10 uM after 42 hrs by Yeast-based assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-3254	Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID1285803	Inhibition of Flag-tagged p53/GST-tagged PPID (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID756857	Inhibition of MDM2-P53 interaction in human SJSA1 cells assessed as p53-mediated decrease in full length PARP level at 24 hrs by Western blot analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID1212304	Drug uptake in C57BL/6 mouse lung at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1659344	Inhibition of MDM2 (unknown origin) by HTRF assay	2020	Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 ISSN: 1520-4804	Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.
AID1296640	Binding affinity to 15N-labeled MDM2 (unknown origin) by 2D 1H-15N HSQC NMR spectroscopic method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID736743	Inhibition of human p53 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell cycle arrest at 10 uM after 42 hrs	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1285816	Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as decrease in tumor growth at 150 mg/kg/day, po administered every other day until day 38 and measured on day 40	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1720556	Inhibition of human MDM2-p53 interaction	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13 ISSN: 1464-3391	A critical update on the strategies towards modulators targeting androgen receptors.
AID1908070	Inhibition of GST-tagged MDM2/Biotin-tagged p53 interaction (unknown origin) incubated for 40 mins by TR-FRET assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1060451	Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay	2014	Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 ISSN: 1464-3391	Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1155058	Ratio of IC50 for human SK-UT-1 cells expressing p53 mutant protein to IC50 for human SJSA1 cells expressing wild type p53 protein	2014	ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5 ISSN: 1948-5875	Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
AID1057111	Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 ISSN: 1464-3391	Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID503033	Induction of p53 expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1296632	Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1143671	Induction of apoptosis in human HCT116 cells assessed as accumulation at G2 phase at 20 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1361637	Inhibition of MDM2/P53 interaction in human A549 cells assessed as increase in MDM2 expression after 24 hrs by Western blot analysis	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID691697	Inhibition of MDM2 binding to p53	2012	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 ISSN: 1464-3405	Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships.
AID1632470	Inhibition of C-terminal biotin-tagged streptavidin labelled human MDM2 ( 2 to 188 residues)/Cy5-labelled p53 (18 to 26 residues)(unknown origin) interaction after 15 mins by TR-FRET assay	2016	Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 ISSN: 1464-3405	Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.
AID1387292	Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID588009	Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of MDM2 protein at 1 to 10 uM after 6 hrs by Western blot analysis	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1296626	Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 35%)	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID756926	Induction of apoptosis in human MCF7 cells assessed as increase in p21 expression level at 3 uM after 24 to 72 hrs by Western blotting analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1361648	Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.10%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1361626	Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1212302	Drug uptake in C57BL/6 mouse plasma at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1238647	Inhibition of rat MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1361643	Cell cycle arrest in human A549 cells assessed as accumulation of cells at G2 phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 19.81%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID748501	Inhibition of N-terminal human recombinant MDM2 assessed as inhibition of protein interaction with p53 by HTRF assay	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID738727	Antiproliferative activity against human MDA-MB-435S cells harboring p53 mutant at 10 uM after 5 days by MTS assay	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID1060449	Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay	2014	Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 ISSN: 1464-3391	Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1296634	Inhibition of Mcl-1/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID748504	Apparent half life in mouse at 100 mg/kg, po	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID1212283	Ratio of drug level in blood to plasma in C57BL/6 mouse after 30 mins	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1238675	Inhibition of human MDM4 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID503024	Induction of cell cycle arrest in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID442457	Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation at 10 uM by Western blot	2009	Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 ISSN: 1520-4804	Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.
AID621853	Growth inhibition of human A2780 cells expressing MDM2 by SRB assay	2011	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 ISSN: 1464-3405	MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1392508	Cytotoxicity against human U2OS cells harboring p53-dependent EGFP reporter gene assessed as reduction in cell viability at 30 uM after 48 hrs	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 ISSN: 1464-3391	Design, in silico prioritization and biological profiling of apoptosis-inducing lactams amenable by the Castagnoli-Cushman reaction.
AID503034	Induction of p53 expression in human MCF7 cells by Western blot analysis	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID425673	Inhibition of GST-tagged MDM2 (1-150) / full-length His6-tagged p53 interaction expressed in Escherichia coli by alphascreen assay	2009	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 ISSN: 1464-3405	Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.
AID1361646	Cell cycle arrest in human A549 cells assessed as accumulation of cells at G2 phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 19.81%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID756948	Cytotoxicity against human Calu cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID626522	Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 ISSN: 1768-3254	Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction.
AID1908079	Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1656003	Solubility of compound in PBS	2020	ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 ISSN: 1948-5875	HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
AID707325	Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1361631	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1212285	Fraction unbound in C57BL/6 mouse plasma at 300 uM up to 24 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1285814	Increase in p53 expression in human MCF7 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1908093	Induction of PARP cleavage in human RKO cells at 0.3125 to 2.5 uM incubated for 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1361644	Cell cycle arrest in human A549 cells assessed as accumulation of cells at G1 phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 49.01%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1143670	Induction of apoptosis in human HCT116 cells assessed as accumulation at S phase at 20 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1908055	Upregulation of p53 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1565005	Induction of apoptosis in human HCT116 cells expressing wild type p53 assessed as live cells at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 83.7 %)	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1908092	Downregulation of MDM4 expression in human RKO cells at 0.3125 to 2.5 uM incubated for 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1060450	Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay	2014	Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 ISSN: 1464-3391	Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID588013	Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID587948	Inhibition of Mdm2 -p53 protein interaction by ELISA	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1212294	Drug uptake in C57BL/6 mouse muscle at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1296607	Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p53 expression after 12 hrs by immunoblotting method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID438434	Induction of apoptosis in human SJSA1 cells assessed as caspase 3/7 activity after 48 hrs	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID746383	Antagonist activity at human GST-tagged MDM2 assessed as inhibition of binding to full length p53	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 ISSN: 1464-3405	Inhibitors of the p53/hdm2 protein-protein interaction-path to the clinic.
AID1125681	Antiproliferative activity against human SJSA1 cells	2014	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3405	Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
AID1212296	Drug uptake in C57BL/6 mouse brain at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1143669	Induction of apoptosis in human HCT116 cells assessed as accumulation at G1 phase at 20 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID588016	Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1908058	Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1239847	Inhibition of p53-MDM2 interaction (unknown origin) by TR-FRET assay	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 ISSN: 1464-3405	Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.
AID1285811	Upregulation of p21 in human MCF7 cells after 24 hrs by Western blot analysis	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID453614	Binding to HDM2 expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy competition method	2009	Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 ISSN: 1464-3391	N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.
AID1908028	Upregulation of p53 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1565006	Induction of apoptosis in human HCT116 cells expressing wild type p53 assessed as early apoptotic cells expressing wild type p53 at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 8.8 %)	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1296623	Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 42%)	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1296624	Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 31%)	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1057102	Ratio of IC50 for human H1299 cells to IC50 for human HCT116 cells	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 ISSN: 1464-3391	Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID707311	Induction of apoptosis in human A549 cells expressing wild type p53 at 20 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1908077	Displacement of 5-FAM labeled PDI peptide from MDM2 (1 to 118 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant incubated for 1.5 hrs by fluorescence polarization competition assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID700922	Inhibition of HDM2 binding to p53	2012	Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 ISSN: 1464-3391	Chemical modulators working at pharmacological interface of target proteins.
AID503039	Induction of apoptosis in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1361641	Cell cycle arrest in human A549 cells assessed as accumulation of cells at G1 phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 49.01%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID438435	Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID1060441	Inhibition of p53-MDM2 (unknown origin) interaction expressed in p53-deficient human HCT116 cells at 50 uM after 24 hrs by BiFC-based FACS flow cytometric analysis	2014	Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 ISSN: 1464-3391	Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1143674	Induction of apoptosis in human HCT116 cells assessed as accumulation at G2 phase at 50 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 12.7%)	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1361623	Growth inhibition of Saccharomyces cerevisiae expressing empty vector at 10 uM after 42 hrs by Yeast-based assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-3254	Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID1192743	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 ISSN: 1464-3391	Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID1060447	Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay	2014	Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 ISSN: 1464-3391	Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1212301	Drug uptake in C57BL/6 mouse spleen at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1212297	Drug uptake in C57BL/6 mouse bone marrow at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID621854	Growth inhibition of human A2780/CP70 cells expressing isogenically paired p53 mutant by SRB assay	2011	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 ISSN: 1464-3405	MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1908053	Upregulation of p21 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1361654	Induction of apoptosis in human A549 cells assessed as necrotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 0.52%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID318566	Binding affinity to human HDM2 assessed as inhibition of HDM2-p53 interaction	2007	Nature, Dec-13, Volume: 450, Issue:7172 ISSN: 1476-4687	Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.
AID503025	Induction of cell cycle arrest in human MCF7 cells transfected hnRNPK-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1212295	Drug uptake in C57BL/6 mouse retina at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1908027	Upregulation of p21 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1565008	Induction of apoptosis in human HCT116 cells expressing wild type p53 assessed as necrotic cells at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 0.7 %)	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1238650	Selectivity index, ratio of Ki for rat MDM2 to Ki for human MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1872997	Inhibition of recombinant human MDM2/p53 interaction by Biacore's surface plasmon resonance analysis	2022	European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254	Small-molecule MDM2 inhibitors in clinical trials for cancer therapy.
AID1296625	Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at S phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 36%)	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1300246	Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3 ISSN: 1948-5875	Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
AID1656006	Inhibition of 6xHis-taged MDM2 (unknown origin) expressed in Escherichia coli Gold (DE3)	2020	ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 ISSN: 1948-5875	HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
AID1195731	Cytotoxicity against human SJSA1 cells	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 ISSN: 1520-4804	Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID1654661	Inhibition of mdm2 in human ARN8 cells assessed as induction of DNA damage by measuring increase in p53 phosphorylation at Ser15 at 2 uM incubated for 24 hrs by Western blot analysis	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 ISSN: 1520-4804	Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
AID1633977	Inhibition of MDM2/P53 interaction in human RKO cells assessed as ratio of p53 to GAPDH level at 20 uM after 24 hrs by Western blot analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID587354	Induction of p53-dependent luciferase activity in human U2OS cells at 5 uM relative to control	2011	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 ISSN: 1464-3405	Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
AID1195732	Cytotoxicity against human HCT116 cells	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 ISSN: 1520-4804	Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID1143668	Induction of apoptosis in human HCT116 cells assessed as accumulation at G2 phase at 10 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID362383	Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration	2008	Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 ISSN: 1520-4804	NMR screening for lead compounds using tryptophan-mutated proteins.
AID1300941	Decrease in procaspase-9 expression level in human p53-null HCT116 -/- cells at 10 uM after 24 hrs by western blot analysis	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1361628	Inhibition of MDM2 (unknown origin) preincubated for 30 mins by fluorescence polarization assay	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1212293	Drug uptake in C57BL/6 mouse lung at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1555409	Inhibition of p53 protein binding to MDM2 (unknown origin)	2019	European journal of medicinal chemistry, Aug-15, Volume: 176ISSN: 1768-3254	The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy.
AID1420852	Inhibition of recombinant p53 protein binding to recombinant human MDM2 by surface plasmon resonance method	2018	European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254	Role of p53 circuitry in tumorigenesis: A brief review.
AID1366814	Inhibition of MDM2/p53 interaction in human U2OS cells assessed as p53 activation by measuring EGFP-positive cells at 10 uM after 24 hrs by Hoechst 33258 staining based fluorescence microscopic analysis relative to control	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID738716	Antiproliferative activity against human HCT116 cells expressing wild type p53 after 5 days by MTS assay	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID588014	Cytotoxicity against human LS cells after 72 hrs by sulforhodamine B assay	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1387289	Inhibition of human MDM2 (1 to 125 residues) and p53 (unknown origin) interaction pre-incubated for 20 mins before peptide-2-biot addition and measured after 3 hrs by HTRF assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID1296635	Inhibition of Mcl-1/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1252240	Inhibition of human MDM2 (17 to 125 residues) assessed as reduction in MDM2 interaction with FAM-LTFEHYWAQLTS-CONH2 peptide incubated for 30 mins by fluorescence polarisation assay	2015	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21 ISSN: 1464-3405	Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin.
AID1152866	Binding affinity to MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by fluorescence polarization binding assay	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12 ISSN: 1464-3405	Discovery of 1-arylpyrrolidone derivatives as potent p53-MDM2 inhibitors based on molecule fusing strategy.
AID1654653	Inhibition of mdm2 in human ARN8 cells assessed as increase in p53 level at 2 uM incubated for 24 hrs by Western blot analysis	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 ISSN: 1520-4804	Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
AID1633983	Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 80 uM after 24 hrs by Western blot analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID1212284	Fraction unbound in C57BL/6 mouse plasma at 0.1 uM up to 24 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID748498	Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID1361619	Inhibition of human MDM2-p53 interaction in Saccharomyces cerevisiae assessed as p53 induced cell growth arrest at 10 uM after 42 hrs by Yeast-based assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-3254	Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID756940	Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reduction in p53 level bound to MDM2 after 24 hrs by immunoprecipitation assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1908080	Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID503036	Induction of p53 expression in human MCF7 cells assessed as increase in p21CIP1 level after 18 hrs by Western blot method in presence of 2.5 mM caffeine	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1143657	Binding affinity to MDM2 (1 to 118) (unknown origin) after 30 mins by fluorescence polarization assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1366812	Induction of apoptosis in human U2OS cells at 10 uM after 24 hrs by Annexin V-FITC/propidium iodide based FACS analysis (Rvb= 0.1%)	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID756860	Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation after 24 hrs by Western blot analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID1212308	Drug uptake in C57BL/6 mouse bone marrow at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1366818	Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID438433	Inhibition of human HCT116 cell proliferation after 16 hrs by BrdU assay	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID756953	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID658338	Inhibition of p53 (18 to 26)-MDM2 (2 to 188) interaction using fluorescent dye Cy5 by TR-FRET assay	2012	Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 ISSN: 1464-3405	The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.
AID1372140	Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay	2018	Bioorganic & medicinal chemistry, 03-15, Volume: 26, Issue:6 ISSN: 1464-3391	Unique arginine array improves cytosolic localization of hydrocarbon-stapled peptides.
AID736737	Inhibition of human MDM2-p53 interaction expressed in Saccharomyces cerevisiae CG379 assessed as reversal of MDM2-dependent inhibition of p53-induced S-phase cell cycle arrest at 10 uM after 42 hrs by Sytox Green-based flow cytometric analysis	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1238649	Selectivity index, ratio of Ki for mouse MDM2 to Ki for human MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID588017	Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID756858	Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as accumulation of p21 after 24 hrs by Western blot analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID1175611	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	2015	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 ISSN: 1464-3405	Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors.
AID1654654	Inhibition of mdm2 in human ARN8 cells assessed as increase in p53 level at 2 uM incubated for 24 hrs in presence of 100 uM de novo pyrimidine ribonucleotide synthesis pathway inhibitor, uridine by Western blot analysis	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 ISSN: 1520-4804	Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
AID503028	Antiproliferative activity against human MCF7 cells transfected with p53-targeting iRNA-based shRNA assessed as effect on cellular morphology at 4 uM after 14 days by coomassie staining	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1564997	Displacement of 5'FAM-LTFEHYWAQLTS from human recombinant N-terminal domain of MDM2 (1 to 118 residues) expressed in Escherichia coli BL21 (DE3) cells measured after 15 mins by fluorescence polarization assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1192744	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 ISSN: 1464-3391	Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID706604	Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 ISSN: 1520-4804	Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID756951	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1908060	Upregulation of p21 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1285813	Increase in p53 expression in human IMR32 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1361651	Induction of apoptosis in human A549 cells assessed as viable cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 93.01%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1565010	Inhibition of MDM2-p53 interaction in human SJSA1 cells expressing wild-type p53 assessed as upregulation of p21 expression at 5 uM measured after 24 hrs by Western blot analysis	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID453615	Binding to GST-tagged HDMX expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy competition method	2009	Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 ISSN: 1464-3391	N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.
AID1296609	Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of MDM2 expression after 12 hrs by immunoblotting method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1296599	Displacement of FAM-p53TAD peptide from N-terminal 8x His-tagged human MDM2 (25 to 108 residues) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1908071	Inhibition of GST-tagged MDM4/Biotin-tagged p53 interaction (unknown origin) incubated for 40 mins by TR-FRET assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID503042	Induction of apoptosis in human MCF7 cells co-transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1633982	Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 40 uM after 24 hrs by Western blot analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID1908083	Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID756952	Cytotoxicity against human U937 cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID267242	Binding affinity to MDM2	2006	Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 ISSN: 0022-2623	Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
AID1361649	Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.37%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID707324	Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1908090	Upregulation of p21 expression in human RKO cells incubated for 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID684828	Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56ISSN: 1768-3254	Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID1908082	Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1908089	Upregulation of p53 expression in human RKO cells incubated for 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID362384	Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay	2008	Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 ISSN: 1520-4804	NMR screening for lead compounds using tryptophan-mutated proteins.
AID1212310	Drug uptake in C57BL/6 mouse adipose tissue at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1366813	Inhibition of MDM2/p53 interaction in human U2OS cells assessed as p53 activation by measuring EGFP-positive cells after 24 hrs by Hoechst 33258 staining based fluorescence microscopic analysis	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID707310	Induction of apoptosis in human A549 cells expressing wild type p53 after 48 hrs using annexin V-FITC staining by flow cytometry assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID749325	Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1212305	Drug uptake in C57BL/6 mouse muscle at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1633968	Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 20 uM after 24 hrs by Western blot analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID1057110	Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 ISSN: 1464-3391	Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID415698	Inhibition of interaction between human DM2(1-549) and p53	2009	Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 ISSN: 1464-3391	Beta-peptides with improved affinity for hDM2 and hDMX.
AID1366815	Inhibition of MDM2/p53 interaction in human U2OS cells by assessed as p53 activation measuring EGFP-positive cells at 5 uM after 24 hrs by Hoechst 33258 staining based fluorescence microscopic analysis relative to control	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID1057105	Induction of p53 translocation in human HCT116 cells assessed as protein nuclear to cytosolic ratio at 3.3 uM after 20 hrs by immunofluorescence analysis	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 ISSN: 1464-3391	Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID1212306	Drug uptake in C57BL/6 mouse retina at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID707312	Induction of apoptosis in human A549 cells expressing wild type p53 at 10 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1212307	Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID438431	Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID1192746	Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 ISSN: 1464-3391	Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID503029	Antiproliferative activity against human A549 cells transfected with 53BP1-targeting iRNA-based shRNA assessed as effect on cellular morphology at 4 uM after 14 days by coomassie staining	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1361659	Antitumor activity against human A549 cells xenografted in BALB/C nude mouse assessed as inhibition of tumor growth at 100 mg/kg, po administered once daily for 21 days starting day 11 after tumor cells implantation	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1565009	Inhibition of MDM2-p53 interaction in human SJSA1 cells expressing wild-type p53 assessed as upregulation of MDM2 expression at 5 uM measured after 24 hrs by Western blot analysis	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1296608	Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1565011	Inhibition of MDM2-p53 interaction in human U2OS cells expressing wild-type p53 assessed as upregulation of MDM2 expression at 5 uM measured after 24 hrs by Western blot analysis	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID755375	Antitumor activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 200 mg/kg/day, po bid administered on day 21 to 24 and day 27 to 30 measured on day 31 relative to control	2013	Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 ISSN: 1464-3391	Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.
AID756920	Induction of apoptosis in human MCF7 cells assessed as accumulation of caspase-3 cleavage product at 50 nM after 24 to 72 hrs by Western blotting analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1366820	Inhibition of MDM2/p53 (unknown origin) complex at 10 uM by ELISA	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 ISSN: 1464-3405	Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID1238646	Inhibition of mouse MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1503133	Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay	2017	European journal of medicinal chemistry, Nov-10, Volume: 140ISSN: 1768-3254
AID1421138	Inhibition of Cy5-labeled p53 derived TFSDLWKLL peptide binding to C-terminal biotin-labelled human MDM2 (2 to 188 residues) by TR-FRET assay	2018	Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 ISSN: 1464-3405	In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.
AID438437	Inhibition of human p21 deficient HCT116 cell proliferation after 16 hrs by BrdU assay	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID756933	Induction of apoptosis in human MCF7 cells assessed as accumulation at subG1 phase at 3 uM by propidium iodide staining-based FACS analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID684826	Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56ISSN: 1768-3254	Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID756922	Induction of apoptosis in human MCF7 cells assessed as increase in Bcl-xS expression level at 3 uM after 24 to 72 hrs by Western blotting analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID588015	Cytotoxicity against human NGP cells after 72 hrs by sulforhodamine B assay	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1212299	Drug uptake in C57BL/6 mouse intestine at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID503027	Antiproliferative activity against human MCF7 cells assessed as appearance of flattened phenotype at 4 uM after 14 days by coomassie staining	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1908026	Upregulation of MDM2 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1212303	Drug uptake in C57BL/6 mouse adrenal gland at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID425674	Inhibition of GST-tagged MDM2/His6-tagged p53 interaction by surface plasmon resonance study	2009	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 ISSN: 1464-3405	Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.
AID755374	Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as body weight loss at 200 mg/kg/day, po bid administered on day 21 to 24 and day 27 to 30 measured every 2 days during compound administration relative to control	2013	Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 ISSN: 1464-3391	Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.
AID1387293	Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID707323	Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID748502	AUClast in mouse at 100 mg/kg, po	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID706601	Inhibition of human MDM2-p53 interaction after 18 hrs by HTRF assay	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 ISSN: 1520-4804	Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID1285802	Inhibition of Flag-tagged p53/GST-tagged DAPK1 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID707317	Inhibition of p53-MDMX interaction after 1 hr by fluorescence polarization assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID684829	Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56ISSN: 1768-3254	Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID1908049	Downregulation of MDM4 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1143672	Induction of apoptosis in human HCT116 cells assessed as accumulation at G1 phase at 50 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 62.5%)	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1503134	Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay	2017	European journal of medicinal chemistry, Nov-10, Volume: 140ISSN: 1768-3254
AID749489	Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID1238648	Selectivity index, ratio of Ki for dog MDM2 to Ki for human MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1361636	Inhibition of MDM2/P53 interaction in human A549 cells assessed as increase in p53 expression after 24 hrs by Western blot analysis	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID621850	Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay	2011	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 ISSN: 1464-3405	MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1212289	Drug uptake in C57BL/6 mouse spleen at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1249873	Stabilization of p53 in human U2OS cells assessed as intracellular p53 level at 2.5 uM after 12 hrs by Western blotting	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8 ISSN: 1948-5875	Discovery of Novel Isatin-Based p53 Inducers.
AID1633969	Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 10 uM after 24 hrs by Western blot analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID756949	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1143673	Induction of apoptosis in human HCT116 cells assessed as accumulation at S phase at 50 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 24.8%)	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1285812	Upregulation of Mdm2 in human MCF7 cells after 24 hrs by Western blot analysis	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1238645	Inhibition of dog MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1300245	Inhibition of human recombinant His-tagged MDM2 (1 to 118 residues) interaction with FAM-tagged p53-based peptide (unknown origin) incubated for 15 mins by fluorescence polarization assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3 ISSN: 1948-5875	Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
AID1212287	Drug uptake in C57BL/6 mouse intestine at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1143660	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID756925	Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl-xL expression level at 3 uM after 24 to 72 hrs by Western blotting analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1143661	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID438436	Inhibition of human p53 deficient HCT116 cell proliferation after 16 hrs by BrdU assay	2009	Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 ISSN: 1520-4804	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID1212298	Drug uptake in C57BL/6 mouse vitreous humor at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1195730	Binding affinity to MDM2 (unknown origin)	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 ISSN: 1520-4804	Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID503038	Induction of p21CIP1 expression in irradiated human BJ cells at 3 uM by Western blot analysis	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1212309	Drug uptake in C57BL/6 mouse vitreous humor at 10 mg/kg, iv as single dose measured at 24 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID503031	Induction of cell cycle arrest in human MCF7 cells p53-targeting iRNA-based shRNA assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID626521	Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 ISSN: 1768-3254	Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction.
AID1908047	Effect on MDM4 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID707327	Induction of apoptosis in human A549 cells expressing wild type p53 at 5 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID684827	Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56ISSN: 1768-3254	Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID736742	Inhibition of human MDM2 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell cycle arrest after 42 hrs	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID417066	Binding affinity to MDM2	2008	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405	Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.
AID1565007	Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells expressing wild type p53 at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 6.8 %)	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID684825	Inhibition of MDM2 binding domain assessed as inhibition of p53 binding to MDM2 after 1 hr by fluorescence polarization assay	2012	European journal of medicinal chemistry, Oct, Volume: 56ISSN: 1768-3254	Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID707322	Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 ISSN: 1520-4804	Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1143665	Induction of apoptosis in human HCT116 cells after 48 hrs by propidium iodide staining-based flow cytometry	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1212286	Cytotoxicity against doxorubicin-resistant human UKF-NB-3 cells after 96 hrs by MTT assay	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID588008	Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p21 protein at 1 to 10 uM after 6 hrs by Western blot analysis	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID756859	Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as MDM2 accumulation after 24 hrs by Western blot analysis	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID503035	Induction of CDKN1A gene expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID243263	Potency against MDM2 (murine double minute-2 gene) binding to p53; Range =100-300 nM	2005	Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14 ISSN: 0022-2623	p53 Activation by small molecules: application in oncology.
AID1908039	Effect on MDM4 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID503041	Induction of cell cycle arrest in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1415891	Inhibition of 5'-FAM-LTFEHYWAQLTS binding to N-terminal domain of recombinant human MDM2 expressed in Escherichia coli BL21(DE3) after 15 mins by fluorescence polarization assay	2017	MedChemComm, May-01, Volume: 8, Issue:5 ISSN: 2040-2503	Scaffold hopping via ANCHOR.QUERY: β-lactams as potent p53-MDM2 antagonists
AID1296598	Displacement of FAM-Bid peptide from N-terminal 8x His-tagged Bcl-2 (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID736744	Inhibition of human p53 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell growth at 10 uM after 42 hrs	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1908091	Upregulation of MDM2 expression in human RKO cells incubated for 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID706603	Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 ISSN: 1520-4804	Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID748500	Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID738713	Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 5 days by MTS assay	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID503030	Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID588007	Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p53 protein at 1 to 10 uM after 6 hrs by Western blot analysis	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID587350	Inhibition of human GST-tagged MDMX expressed in Escherichia coli harboring integrated p53-Hmd2 protein assessed as blockade of enzyme-p53 interaction by ELISA assay	2011	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 ISSN: 1464-3405	Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
AID1212291	Drug uptake in C57BL/6 mouse adipose tissue at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID721248	Inhibition of human p53/MDM2 interaction	2013	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 ISSN: 1464-3405	Lead optimization of novel p53-MDM2 interaction inhibitors possessing dihydroimidazothiazole scaffold.
AID1300911	Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID756947	Cytotoxicity against human C643 cells after 24 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 ISSN: 1520-4804	Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1387291	Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID738979	Antiproliferative activity against human HeLa cells harboring p53 mutant at 10 uM after 5 days by MTS assay	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID1296621	Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1143659	Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1361652	Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.10%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1656007	Binding affinity to 6xHis-taged MDM2 (unknown origin) expressed in Escherichia coli Gold (DE3) assessed as inhibition constant	2020	ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 ISSN: 1948-5875	HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
AID1192745	Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 ISSN: 1464-3391	Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID1361629	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1238644	Inhibition of human MDM2 by TR-FRET assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 ISSN: 1520-4804	Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1908059	Upregulation of MDM2 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 ISSN: 1520-4804
AID1387290	Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 ISSN: 1520-4804	Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID588018	Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay	2011	Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 ISSN: 1520-4804	Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID503040	Antiproliferative activity against human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA assessed as effect on cellular morphology at 4 uM after 14 days by coomassie staining	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1296610	Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p21 expression after 12 hrs by immunoblotting method	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1361645	Cell cycle arrest in human A549 cells assessed as accumulation of cells at S phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 31.18%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1195734	Antitumor activity against human SJSA1 cells xenografted in mouse assessed as tumor growth inhibition at 200 mg/kg, po bid administered for 20 days	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 ISSN: 1520-4804	Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID1296622	Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 26%)	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 ISSN: 1520-4804	Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID736738	Inhibition of human MDM2-p53 interaction expressed in Saccharomyces cerevisiae CG379 assessed as reversal of MDM2-dependent inhibition of p53-induced growth inhibition at 10 uM after 42 hrs	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1633978	Inhibition of MDM2/P53 interaction in human RKO cells assessed as ratio of p53 to GAPDH level at 10 uM after 24 hrs by Western blot analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 ISSN: 1464-3405	2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID362378	Binding affinity to human wild type Mdm2 by isothermal titration calorimetry	2008	Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 ISSN: 1520-4804	NMR screening for lead compounds using tryptophan-mutated proteins.
AID1378961	Inhibition of V1-p53/MDM2-V2 (unknown origin) interaction expressed in human HCT116 p53-/- cells at 10 uM after 20 hrs by biomolecular fluorescence complementation-based flow cytometric analysis	2017	European journal of medicinal chemistry, Oct-20, Volume: 139ISSN: 1768-3254	In vitro targeting of colon cancer cells using spiropyrazoline oxindoles.
AID1300912	Inhibition of HIF-1 (unknown origin) expressed in human MCF7 cells co-transfected with hypoxia reporter plasmid p(HRE)3-Luc at 20 uM measured under hypoxia condition after 24 hrs by dual-luciferase reporter assay	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1580651	Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay	2019	Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 ISSN: 1520-4804	Enhancing the Cell Permeability of Stapled Peptides with a Cyclic Cell-Penetrating Peptide.
AID1392511	Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 ISSN: 1464-3391	Design, in silico prioritization and biological profiling of apoptosis-inducing lactams amenable by the Castagnoli-Cushman reaction.
AID1361630	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID265956	Antiproliferative activity against human LnCAP cell line with wild type p53	2006	Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 ISSN: 0022-2623	Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
AID738725	Antiproliferative activity against human SW480 cells harboring p53 mutant at 10 uM after 5 days by MTS assay	2013	Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3391	Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID503043	Induction of p21 expression in irradiated human BJ cells at 3 uM by Western blot analysis	2006	Nature chemical biology, Apr, Volume: 2, Issue:4 ISSN: 1552-4450	An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1285801	Inhibition of Flag-tagged p53/GST-tagged Mdmx (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 ISSN: 1464-3391	Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1057104	Induction of p53 translocation in human HCT116 cells assessed as protein nuclear to cytosolic ratio at 10 uM after 20 hrs by immunofluorescence analysis	2013	Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 ISSN: 1464-3391	Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID1361642	Cell cycle arrest in human A549 cells assessed as accumulation of cells at S phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 31.18%)	2018	Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 ISSN: 1520-4804	Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID736735	Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reversal of MDM2-dependent inhibition of p53-induced transcriptional activity at 10 uM after 16 hrs by dual-luciferase reporter gene assay	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1212288	Drug uptake in C57BL/6 mouse liver at 50 to 200 mg/kg, po as single dose measured at 2 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 ISSN: 1521-009X	Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1143667	Induction of apoptosis in human HCT116 cells assessed as accumulation at S phase at 10 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1392512	Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	2018	Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 ISSN: 1464-3391	Design, in silico prioritization and biological profiling of apoptosis-inducing lactams amenable by the Castagnoli-Cushman reaction.
AID1143666	Induction of apoptosis in human HCT116 cells assessed as accumulation at G1 phase at 10 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control	2014	European journal of medicinal chemistry, Jun-23, Volume: 81ISSN: 1768-3254	Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1300909	Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 ISSN: 1464-3405	Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID748503	Cmax in mouse at 100 mg/kg, po	2013	ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 ISSN: 1948-5875	Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID362382	Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay	2008	Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 ISSN: 1520-4804	NMR screening for lead compounds using tryptophan-mutated proteins.
AID736736	Inhibition of human MDM2-p53 interaction expressed in Saccharomyces cerevisiae CG379 assessed as reversal of MDM2-dependent inhibition of p53-induced transcriptional activity at 10 uM after 16 hrs by dual-luciferase reporter gene assay	2013	Journal of natural products, Apr-26, Volume: 76, Issue:4 ISSN: 1520-6025	Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1564998	Displacement of 5'FAM-LTFEHYWAQLTS from human recombinant MDMX (18 to 111 residues) expressed in Escherichia coli BL21 (DE3) cells measured after 30 mins by fluorescence polarization assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID749323	Selectivity ratio of IC50 for human p53-null PC3 cells to IC50 for human A549 cells expressing wild type p53	2013	Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 ISSN: 1464-3391	Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1565012	Inhibition of MDM2-p53 interaction in human U2OS cells expressing wild-type p53 assessed as upregulation of p21 expression at 5 uM measured after 24 hrs by Western blot analysis	2019	European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254	Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
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.
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.
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.
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.
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.
AID977608	Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB	2013	Acta crystallographica. Section D, Biological crystallography, Aug, Volume: 69, Issue:Pt 8 ISSN: 1399-0047	The structure of an MDM2-Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant.

Research

Studies (696)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	135 (19.40)	29.6817
2010's	501 (71.98)	24.3611
2020's	60 (8.62)	2.80

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (0.14%)	5.53%
Reviews	28 (4.01%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	669 (95.85%)	84.16%

Substance	Classes	Roles	Relationship Strength
diethylstilbestrol	stilbenoid		low
hexestrol	stilbenoid		low
3,3',4,5'-tetrahydroxystilbene	stilbenoid		low
sarpogrelate	hemisuccinate; stilbenoid		low
2-[4-(1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanamine	stilbenoid		low
2-[4-(4-chloro-1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanamine	stilbenoid		low
triphenylethylene	stilbenoid		low
ethamoxytriphetol	stilbenoid		low
triparanol	stilbenoid	anticoronaviral agent	low
iodoalphionic acid	stilbenoid		low
norpropoxyphene	stilbenoid		low
2,3,3-triphenylacrylonitrile	stilbenoid		low
remacemide	stilbenoid		low
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol	stilbenoid		low
hexestrol bis(diethylaminoethyl ether)	stilbenoid		low
tetraphenylcyclopentadienone	stilbenoid		low
1-(4-hydroxyphenyl)-2-phenylethan-1-one	stilbenoid		low
o-desmethylangolensin	stilbenoid		low
4,5-diphenyl-1,5-dihydroimidazol-2-one	stilbenoid		low
3,3'-Dihydroxyhexestrol	stilbenoid		low
lunularic acid	stilbenoid		low
lunularin	stilbenoid		low
diphenidine	stilbenoid		low
nutlin 3	stilbenoid		low
1-(2,4-Dihydroxyphenyl)-2-(4-methoxyphenyl)ethanone	stilbenoid		low
sc 57666	stilbenoid		low
lephetamine	stilbenoid		low
pallidol	carbopolycyclic compound; polyphenol; stilbenoid	antifungal agent; antioxidant; plant metabolite	low
1-(4-bromophenyl)-2-phenylethan-1-one	stilbenoid		low
vedelianin	cyclic ether; organic heterotricyclic compound; resorcinols; stilbenoid	antineoplastic agent; plant metabolite	low
2-(2-chloro-6-fluorophenyl)-1-(2,4-dihydroxyphenyl)ethanone	stilbenoid		low
2-(3,4-dimethoxyphenyl)-1-(2,4,6-trihydroxyphenyl)ethanone	stilbenoid		low
1-(3,4-dimethoxy-2-methylphenyl)-2-(3,4-dimethoxyphenyl)ethanone	stilbenoid		low
zuclomiphene	stilbenoid		low
2-(4-bromophenyl)-1-(2,4-dihydroxyphenyl)ethanone	stilbenoid		low
5-[2-(4-ethoxy-2-hydroxyphenyl)-2-oxoethyl]-2-benzofurancarboxylic acid	stilbenoid		low
tamoxifen	stilbenoid; tertiary amino compound	angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator	low
ly 288513	stilbenoid		low
2-[(4,7-dimethyl-2-quinazolinyl)thio]-1,2-diphenylethanone	stilbenoid		low
dimethylstilbestrol	stilbenoid		low
toremifene citrate	stilbenoid	anticoronaviral agent	low
droloxifene	stilbenoid		low
1-(4-hydroxyphenyl)-1,2-diphenyl-1-butene	stilbenoid		low
idoxifene	stilbenoid		low
n-desmethyltoremifene	stilbenoid		low
desdimethyltamoxifen	stilbenoid		low
alpha-hydroxytamoxifen	stilbenoid		low
2-chloro-N-(1,2-diphenylethyl)acetamide	stilbenoid		low
resveratrol-4'-o-glucuronide	glycoside; stilbenoid		low
astringin	beta-D-glucoside; monosaccharide derivative; polyphenol; stilbenoid	antineoplastic agent; antioxidant; metabolite	low
isorhapontin	glycoside; stilbenoid		low
trans-2,3',4,5'-tetrahydroxystilbene	stilbenoid		low
polydatin	beta-D-glucoside; monosaccharide derivative; polyphenol; stilbenoid	anti-arrhythmia drug; antioxidant; geroprotector; hepatoprotective agent; metabolite; nephroprotective agent; potassium channel modulator	low
Pinosylvin methyl ether	stilbenoid		low
epsilon-viniferin	1-benzofurans; polyphenol; stilbenoid	metabolite	low
salvianolic acid a	stilbenoid		low
4-acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid	stilbenoid		low
(+)-trans-epsilon-viniferin	1-benzofurans; polyphenol; stilbenoid		low
desoxyrhaponticin	glycoside; stilbenoid		low
3,5-dimethoxy-trans-stilbene	stilbenoid		low
quadrangularin a	indanes; polyphenol; stilbenoid	antioxidant; plant metabolite	low
isorhapontigenin	stilbenoid		low
rhapontigenin	stilbenoid		low
(E)-2,3,5,4'-tetrahydroxystilbene-2-O-beta-D-glucoside	beta-D-glucoside; resorcinols; stilbenoid	anti-inflammatory agent; antioxidant; apoptosis inhibitor; cardioprotective agent; cyclooxygenase 2 inhibitor; platelet aggregation inhibitor	low
fosbretabulin	stilbenoid		low
n-desmethyltamoxifen	stilbenoid		low
mulberroside a	glycoside; stilbenoid		low
cajanine	stilbenoid		low
metaflumizone	semicarbazone; stilbenoid		low
bms453	benzoic acids; dihydronaphthalenes; stilbenoid	retinoic acid receptor alpha antagonist; retinoic acid receptor beta agonist; retinoic acid receptor gamma antagonist; teratogenic agent	low
gw 4064	stilbenoid		low
bms 204493	acetylenic compound; benzoic acids; dihydronaphthalenes; stilbenoid	retinoic acid receptor antagonist	low
4-hydroxy-n-desmethyltamoxifen	stilbenoid		low
delta-viniferin	1-benzofurans; polyphenol; stilbenoid		low
palovarotene	stilbenoid		low
aiphanol	aromatic ether; benzodioxine; lignan; stilbenoid	EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor	low
batatasin-iii	stilbenoid		low
n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide	stilbenoid		low
bay94 9172	(18)F radiopharmaceutical; aromatic ether; polyether; secondary amino compound; stilbenoid; substituted aniline	radioactive imaging agent	low
3-[[(3R,4S)-2-(4-bromophenyl)-5-(3-chlorophenyl)-4-(2-methoxyphenyl)-3,4-dihydropyrazol-3-yl]-oxomethyl]-2-oxazolidinone	stilbenoid		low
schweinfurthin g	cyclic ether; organic heterotricyclic compound; resorcinols; stilbenoid	antineoplastic agent; metabolite	low
schweinfurthin f	cyclic ether; organic heterotricyclic compound; resorcinols; stilbenoid	metabolite	low
amorfrutin a	stilbenoid		low
3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid	stilbenoid		low

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	2000's	2010's	post-2020
ci 994	1	acetamides; benzamides; substituted aniline	antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor	2018	2018	6.0	low	0	1	0
gossypol	1			2016	2016	8.0	low	0	1	0
vorinostat	1	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor	2018	2018	6.0	low	0	1	0
paclitaxel	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent	2016	2016	8.0	low	0	1	0
etoposide	1	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor	2020	2020	4.0	low	0	1	0
staurosporine	1	indolocarbazole alkaloid; organic heterooctacyclic compound	apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector	2020	2020	4.0	low	0	1	0
brequinar	1	biphenyls; monocarboxylic acid; monofluorobenzenes; quinolinemonocarboxylic acid	anticoronaviral agent; antimetabolite; antineoplastic agent; antiviral agent; EC 1.3.5.2 [dihydroorotate dehydrogenase (quinone)] inhibitor; immunosuppressive agent; pyrimidine synthesis inhibitor	2020	2020	4.0	low	0	1	0
irinotecan	2	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug	2009	2012	13.5	low	1	1	0
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol	1	stilbenoid		2015	2015	9.0	low	0	1	0
docetaxel anhydrous	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent	2016	2016	8.0	low	0	1	0
tariquidar	1	benzamides		2020	2020	4.0	low	0	1	0
cyc 202	1	2,6-diaminopurines	antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor	2008	2008	16.0	low	1	0	0
nutlin 3	4	stilbenoid		2006	2019	13.2	high	2	2	0
nsc 23766	1	aminopyrimidine; aminoquinoline; primary amino compound; secondary amino compound; tertiary amino compound	antiviral agent; apoptosis inducer; EC 3.6.5.2 (small monomeric GTPase) inhibitor; muscarinic antagonist	2007	2007	17.0	low	1	0	0
nbd 556	1			2007	2007	17.0	low	1	0	0
epi 001	1	diether; organochlorine compound	androgen antagonist	2020	2020	4.0	low	0	1	0
butein	1	chalcones; polyphenol	antineoplastic agent; antioxidant; EC 1.1.1.21 (aldehyde reductase) inhibitor; geroprotector; hypoglycemic agent; plant metabolite; radiosensitizing agent; tyrosine kinase inhibitor	2008	2008	16.0	low	1	0	0
mangostin	1	aromatic ether; phenols; xanthones	antimicrobial agent; antineoplastic agent; antioxidant; plant metabolite	2013	2013	11.0	low	0	1	0
ro26-4550	1			2012	2012	12.0	medium	0	1	0
N(2)-carbamimidoyl-N-{2-[4-(3-{4-[(5-carboxyfuran-2-yl)methoxy]-2,3-dichlorophenyl}-1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxoethyl}-D-leucinamide	2	D-leucine derivative; dichlorobenzene; furoic acid; glycine derivative; guanidines; pyrazolylpiperidine		2007	2012	14.5	high	1	1	0
nutlin 2	4			2005	2015	12.8	high	1	3	0
spd-304	1			2007	2007	17.0	low	1	0	0
flavokawain a	1	chalcones		2018	2018	6.0	low	0	1	0
gambogic acid	1	pyranoxanthones	metabolite	2013	2013	11.0	low	0	1	0
nutlin 1	2			2013	2018	8.5	low	0	2	0
abt-737	2	aromatic amine; aryl sulfide; biphenyls; C-nitro compound; monochlorobenzenes; N-arylpiperazine; N-sulfonylcarboxamide; secondary amino compound; tertiary amino compound	anti-allergic agent; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; B-cell lymphoma 2 inhibitor	2007	2016	12.5	low	1	1	0
MI-63	4	azaspiro compound; monochlorobenzenes; monofluorobenzenes; morpholines; oxindoles; pyrrolidines; secondary carboxamide	apoptosis inducer	2006	2012	14.5	high	2	2	0
mdv 3100	1	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent	2020	2020	4.0	low	0	1	0
nutlin-3b	1	Nutlin; piperazinone	anticoronaviral agent	2012	2012	12.0	low	0	1	0
2,3,4,10-tetrahydro-7,10-dimethyl-2,4-dioxobenzo(g)pteridine	1	flavin		2012	2012	12.0	medium	0	1	0
pb 12	1			2015	2015	9.0	high	0	1	0
nvp-cgm097	2			2015	2019	7.0	medium	0	2	0
sar405838	4			2013	2018	8.0	medium	0	4	0
(1S,2R)-2-[[(1S)-1-[(1,3-dioxo-2-isoindolyl)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-oxomethyl]-1-cyclohexanecarboxylic acid	1	phthalimides		2020	2020	4.0	low	0	1	0
rg7112	3			2013	2022	5.7	low	0	2	1
amg 232	3			2018	2022	4.0	high	0	2	1

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	Trials	2000's	2010's	post-2020
phosphoserine	1	non-proteinogenic alpha-amino acid; O-phosphoamino acid; serine derivative	human metabolite	2014	2014	10.0	low	0	0	1	0
adenine	2	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2016	2020	6.0	low	0	0	2	0
carbamates	2	amino-acid anion		2009	2009	15.0	low	0	2	0	0
coumarin	1	coumarins	fluorescent dye; human metabolite; plant metabolite	2011	2011	13.0	low	0	0	1	0
cytosine	1	aminopyrimidine; pyrimidine nucleobase; pyrimidone	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2020	2020	4.0	low	0	0	1	0
lactic acid	2	2-hydroxy monocarboxylic acid	algal metabolite; Daphnia magna metabolite	2012	2015	10.5	low	0	0	2	0
dimethyl sulfoxide	1	sulfoxide; volatile organic compound	alkylating agent; antidote; Escherichia coli metabolite; geroprotector; MRI contrast agent; non-narcotic analgesic; polar aprotic solvent; radical scavenger	2013	2013	11.0	low	0	0	1	0
glycine	2	alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid	EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical	2014	2020	7.0	low	0	0	2	0
niacinamide	3	pyridine alkaloid; pyridinecarboxamide; vitamin B3	anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor	2012	2013	11.7	low	1	0	3	0
phosphorylcholine	1	phosphocholines	allergen; epitope; hapten; human metabolite; mouse metabolite	2010	2010	14.0	low	0	1	0	0
pteridines	1	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; pteridines		2009	2009	15.0	low	0	1	0	0
thymine	1	pyrimidine nucleobase; pyrimidone	Escherichia coli metabolite; human metabolite; mouse metabolite	2017	2017	7.0	low	0	0	1	0
toluene	12	methylbenzene; toluenes; volatile organic compound	cholinergic antagonist; fuel additive; neurotoxin; non-polar solvent	2010	2020	10.0	low	0	2	10	0
urea	3	isourea; monocarboxylic acid amide; one-carbon compound	Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2008	2018	10.0	low	0	1	2	0
1,5-dihydroxyisoquinoline	1	isoquinolinol	EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor	2014	2014	10.0	low	0	0	1	0
acetaminophen	1	acetamides; phenols	antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic	2017	2017	7.0	low	0	0	1	0
pimagedine	1	guanidines; one-carbon compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor; EC 1.4.3.4 (monoamine oxidase) inhibitor	2008	2008	16.0	low	0	1	0	0
aspirin	2	benzoic acids; phenyl acetates; salicylates	anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent	2018	2021	4.5	low	0	0	1	1
bepridil	2	pyrrolidines; tertiary amine	anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent	2012	2019	8.5	low	0	0	2	0
berberine	1	alkaloid antibiotic; berberine alkaloid; botanical anti-fungal agent; organic heteropentacyclic compound	antilipemic drug; antineoplastic agent; antioxidant; EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor; EC 1.21.3.3 (reticuline oxidase) inhibitor; EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor; EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor; EC 2.7.11.10 (IkappaB kinase) inhibitor; EC 3.1.1.4 (phospholipase A2) inhibitor; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; hypoglycemic agent; metabolite; potassium channel blocker	2022	2022	2.0	low	0	0	0	1
caffeine	1	purine alkaloid; trimethylxanthine	adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic	2010	2010	14.0	low	0	1	0	0
verapamil	1	aromatic ether; nitrile; polyether; tertiary amino compound		2014	2014	10.0	low	0	0	1	0
chlorambucil	2	aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound	alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent	2008	2010	15.0	low	0	2	0	0
chloroquine	1	aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug	2015	2015	9.0	low	0	0	1	0
ciprofloxacin	1	aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion	antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic	2018	2018	6.0	low	0	0	1	0
clofazimine	1	monochlorobenzenes; phenazines	dye; leprostatic drug; non-steroidal anti-inflammatory drug	2013	2013	11.0	low	0	0	1	0
deferoxamine	1	acyclic desferrioxamine	bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore	2020	2020	4.0	low	0	0	1	0
3,3'-diindolylmethane	1	indoles	antineoplastic agent; P450 inhibitor	2020	2020	4.0	low	0	0	1	0
disulfiram	1	organic disulfide; organosulfur acaricide	angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor	2016	2016	8.0	low	0	0	1	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	2012	2012	12.0	low	0	0	1	0
ellipticine	1	indole alkaloid; organic heterotetracyclic compound; organonitrogen heterocyclic compound; polycyclic heteroarene	antineoplastic agent; plant metabolite	2010	2010	14.0	low	0	1	0	0
fluorouracil	6	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic	2010	2021	9.5	low	0	1	4	1
ifenprodil	1	piperidines		2013	2013	11.0	low	0	0	1	0
staurosporine aglycone	1			2014	2014	10.0	low	0	0	1	0
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one	1	chromones; morpholines; organochlorine compound	autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector	2008	2008	16.0	low	0	1	0	0
mebendazole	1	aromatic ketone; benzimidazoles; carbamate ester	antinematodal drug; microtubule-destabilising agent; tubulin modulator	2015	2015	9.0	low	0	0	1	0
vitamin k 3	1	1,4-naphthoquinones; vitamin K	angiogenesis inhibitor; antineoplastic agent; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; human urinary metabolite; nutraceutical	2012	2012	12.0	low	0	0	1	0
metformin	2	guanidines	environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic	2011	2017	10.0	low	0	0	2	0
nocodazole	4	aromatic ketone; benzimidazoles; carbamate ester; thiophenes	antimitotic; antineoplastic agent; microtubule-destabilising agent; tubulin modulator	2011	2013	12.5	low	0	0	4	0
mitoxantrone	2	dihydroxyanthraquinone	analgesic; antineoplastic agent	2010	2011	13.5	low	0	1	1	0
entinostat	2	benzamides; carbamate ester; primary amino compound; pyridines; substituted aniline	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor	2012	2020	8.0	low	0	0	2	0
pd 98059	1	aromatic amine; monomethoxyflavone	EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector	2007	2007	17.0	low	0	1	0	0
pifithrin	12	aromatic ketone		2010	2020	10.0	low	0	2	10	0
4-aminobenzoic acid	6	aminobenzoate; aromatic amino-acid anion	Escherichia coli metabolite; plant metabolite; Saccharomyces cerevisiae metabolite	2014	2018	7.5	low	0	0	6	0
vorinostat	2	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor	2012	2016	10.0	low	0	0	2	0
temozolomide	4	imidazotetrazine; monocarboxylic acid amide; triazene derivative	alkylating agent; antineoplastic agent; prodrug	2011	2019	9.2	low	0	0	4	0
diethylnitrosamine	1	nitrosamine	carcinogenic agent; hepatotoxic agent; mutagen	2017	2017	7.0	low	0	0	1	0
serine	9	L-alpha-amino acid; proteinogenic amino acid; serine family amino acid; serine zwitterion; serine	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2004	2018	11.9	low	0	3	6	0
lysine	1	aspartate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; lysine; organic molecular entity; proteinogenic amino acid	algal metabolite; anticonvulsant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite	2016	2016	8.0	low	0	0	1	0
9,10-dimethyl-1,2-benzanthracene	1	ortho-fused polycyclic arene; tetraphenes	carcinogenic agent	2010	2010	14.0	low	0	1	0	0
bromodeoxyuridine	1	pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent	2014	2014	10.0	low	0	0	1	0
tyrosine	2	amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; proteinogenic amino acid; tyrosine	EC 1.3.1.43 (arogenate dehydrogenase) inhibitor; fundamental metabolite; micronutrient; nutraceutical	2005	2013	15.0	low	0	1	1	0
cycloheximide	1	antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol	anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor	2008	2008	16.0	low	0	1	0	0
cytarabine	3	beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside	antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent	2012	2021	9.0	low	0	0	2	1
caramiphen	1	benzenes		2013	2013	11.0	low	0	0	1	0
dichloroacetic acid	2	monocarboxylic acid; organochlorine compound	astringent; marine metabolite	2014	2020	7.0	low	0	0	2	0
isatin	2	indoledione	EC 1.4.3.4 (monoamine oxidase) inhibitor; plant metabolite	2018	2020	5.0	low	0	0	2	0
1,3-dichloro-2-propanol	1	organochlorine compound; secondary alcohol	cross-linking reagent; protic solvent	2018	2018	6.0	low	0	0	1	0
alpha-chlorohydrin	1	chloropropane-1,2-diol		2018	2018	6.0	low	0	0	1	0
quinuclidines	1	quinuclidines; saturated organic heterobicyclic parent		2011	2011	13.0	low	0	0	1	0
pyrroles	4	pyrrole; secondary amine		2013	2020	8.5	low	0	0	4	0
thiophenes	4	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent	2016	2018	6.5	low	0	0	4	0
pyrazolanthrone	1	anthrapyrazole; aromatic ketone; cyclic ketone	antineoplastic agent; c-Jun N-terminal kinase inhibitor; geroprotector	2016	2016	8.0	low	0	0	1	0
2-naphthol	1	naphthol	antinematodal drug; genotoxin; human urinary metabolite; human xenobiotic metabolite; mouse metabolite; radical scavenger	2012	2012	12.0	low	0	0	1	0
quinazolines	4	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines		2013	2014	10.5	low	0	0	4	0
benzoxazoles	1	1,3-benzoxazoles; mancude organic heterobicyclic parent		2015	2015	9.0	low	0	0	1	0
cyclopentane	2	cycloalkane; cyclopentanes; volatile organic compound	non-polar solvent	2013	2020	7.5	low	0	0	2	0
thiazoles	5	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene		2011	2016	10.4	low	0	0	5	0
pyrazines	6	diazine; pyrazines	Daphnia magna metabolite	2009	2018	11.2	low	0	3	3	0
hydrazine	1	azane; hydrazines	EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor	2018	2018	6.0	low	0	0	1	0
azacitidine	1	N-glycosyl-1,3,5-triazine; nucleoside analogue	antineoplastic agent	2014	2014	10.0	low	0	0	1	0
thymidine monophosphate	1	thymidine 5'-monophosphate	fundamental metabolite	2015	2015	9.0	low	0	0	1	0
alpha-aminopyridine	5			2016	2018	7.6	low	0	0	5	0
aminoacetonitrile	1			2011	2011	13.0	low	0	0	1	0
acetylcysteine	1	acetylcysteine; L-cysteine derivative; N-acetyl-L-amino acid	antidote to paracetamol poisoning; antiinfective agent; antioxidant; antiviral drug; ferroptosis inhibitor; geroprotector; human metabolite; mucolytic; radical scavenger; vulnerary	2013	2013	11.0	low	0	0	1	0
2-piperidone	1	delta-lactam; piperidones	EC 1.2.1.88 (L-glutamate gamma-semialdehyde dehydrogenase) inhibitor	2018	2018	6.0	low	0	0	1	0
deoxycytidine	6	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2006	2016	11.7	low	0	2	4	0
deoxyuridine	1	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2010	2010	14.0	low	0	1	0	0
arsenic trioxide	1			2014	2014	10.0	low	0	0	1	0
vidarabine	5	beta-D-arabinoside; purine nucleoside	antineoplastic agent; bacterial metabolite; nucleoside antibiotic	2006	2015	13.4	low	0	2	3	0
camptothecin	6	delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite	2007	2018	12.5	low	0	3	3	0
tetradecanoylphorbol acetate	1	acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester	antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator	2016	2016	8.0	low	0	0	1	0
phenyl acetate	2	benzenes; phenyl acetates		2015	2018	7.5	low	0	0	2	0
azoxymethane	2			2006	2012	15.0	low	0	1	1	0
flubendazole	1	aromatic ketone; benzimidazoles; carbamate ester; organofluorine compound	antinematodal drug; teratogenic agent	2015	2015	9.0	low	0	0	1	0
paclitaxel	7	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent	2005	2021	10.6	low	0	2	4	1
etoposide	15	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor	2004	2019	13.4	low	0	9	6	0
simvastatin	1	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug	2017	2017	7.0	low	0	0	1	0
topotecan	5	pyranoindolizinoquinoline	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor	2007	2016	13.2	low	0	3	2	0
gemcitabine	6	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic	2006	2016	11.7	low	0	2	4	0
irinotecan	4	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug	2019	2020	4.5	low	0	0	4	0
adenosine	1	adenosines; purines D-ribonucleoside	analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent	2018	2018	6.0	low	0	0	1	0
vanadates	1	trivalent inorganic anion; vanadium oxoanion	EC 3.1.3.1 (alkaline phosphatase) inhibitor; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor	2021	2021	3.0	low	0	0	0	1
thiazolyl blue	1	organic bromide salt	colorimetric reagent; dye	2012	2012	12.0	low	0	0	1	0
5-chloro-2'-deoxyuridine	1			2010	2010	14.0	low	0	1	0	0
st 679	1	N-acyl-amino acid		2014	2014	10.0	low	0	0	1	0
telmisartan	1	benzimidazoles; biphenyls; carboxybiphenyl	angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic	2014	2014	10.0	low	0	0	1	0
triazoles	2	1,2,3-triazole		2013	2018	8.5	low	0	0	2	0
3-deazaneplanocin	1			2018	2018	6.0	low	0	0	1	0
glucuronic acid	1	D-glucuronic acid	algal metabolite	2011	2011	13.0	low	0	0	1	0
triptolide	1	diterpenoid; epoxide; gamma-lactam; organic heteroheptacyclic compound	antispermatogenic agent; plant metabolite	2008	2008	16.0	low	0	1	0	0
parthenolide	1	germacranolide		2009	2009	15.0	low	0	1	0	0
ecteinascidin 743	1	acetate ester; azaspiro compound; bridged compound; hemiaminal; isoquinoline alkaloid; lactone; organic heteropolycyclic compound; organic sulfide; oxaspiro compound; polyphenol; tertiary amino compound	alkylating agent; angiogenesis modulating agent; anti-inflammatory agent; antineoplastic agent; marine metabolite	2015	2015	9.0	low	0	0	1	0
deoxyglucose	1			2016	2016	8.0	low	0	0	1	0
tanshinone	1	abietane diterpenoid	anticoronaviral agent	2017	2017	7.0	low	0	0	1	0
imatinib mesylate	4	methanesulfonate salt	anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor	2010	2017	10.5	low	0	1	3	0
gefitinib	1	aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound	antineoplastic agent; epidermal growth factor receptor antagonist	2014	2014	10.0	low	0	0	1	0
27-hydroxycholesterol	1	26-hydroxycholesterol	apoptosis inducer; human metabolite; mouse metabolite; neuroprotective agent	2015	2015	9.0	low	0	0	1	0
docetaxel anhydrous	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent	2010	2010	14.0	low	0	1	0	0
perifosine	1	ammonium betaine; phospholipid	EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor	2010	2010	14.0	low	0	1	0	0
tariquidar	2	benzamides		2020	2021	3.5	low	0	0	1	1
cyc 202	5	2,6-diaminopurines	antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor	2006	2020	12.6	low	0	3	2	0
tanshinone ii a	1	abietane diterpenoid		2019	2019	5.0	low	0	0	1	0
biotin	1	biotins; vitamin B7	coenzyme; cofactor; Escherichia coli metabolite; fundamental metabolite; human metabolite; mouse metabolite; nutraceutical; prosthetic group; Saccharomyces cerevisiae metabolite	2019	2019	5.0	low	0	0	1	0
erlotinib hydrochloride	2	hydrochloride; terminal acetylenic compound	antineoplastic agent; protein kinase inhibitor	2014	2020	7.0	low	0	0	2	0
lapatinib	3	furans; organochlorine compound; organofluorine compound; quinazolines	antineoplastic agent; tyrosine kinase inhibitor	2013	2020	8.3	low	0	0	3	0
sorafenib	4	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor	2012	2020	9.8	low	1	0	4	0
anisomycin	1	monohydroxypyrrolidine; organonitrogen heterocyclic antibiotic	anticoronaviral agent; antimicrobial agent; antineoplastic agent; antiparasitic agent; bacterial metabolite; DNA synthesis inhibitor; protein synthesis inhibitor	2005	2005	19.0	low	0	1	0	0
benzofurans	1			2019	2019	5.0	low	0	0	1	0
2,2-bis(hydroxymethyl)-1-azabicyclo(2,2,2,)octan-3-one	1	cyclic ketone; quinuclidines		2014	2014	10.0	low	0	0	1	0
pifithrin mu	1	benzenes		2010	2010	14.0	low	0	1	0	0
2,5-bis(5-hydroxymethyl-2-thienyl)furan	12	thiophenes		2009	2020	10.5	high	0	2	10	0
bortezomib	7	amino acid amide; L-phenylalanine derivative; pyrazines	antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor	2009	2017	11.0	low	0	3	4	0
nsc 146109	1			2011	2011	13.0	high	0	0	1	0
leupeptins	3			2008	2010	15.3	low	0	3	0	0
carboplatin	3			2007	2015	12.0	low	0	1	2	0
leptomycin b	3			2007	2013	13.3	low	0	1	2	0
indican	1	beta-D-glucoside; exopolysaccharide; indolyl carbohydrate		2013	2013	11.0	low	0	0	1	0
trichostatin a	2	antibiotic antifungal agent; hydroxamic acid; trichostatin	bacterial metabolite; EC 3.5.1.98 (histone deacetylase) inhibitor; geroprotector	2010	2013	12.5	low	0	1	1	0
resveratrol	1	resveratrol	antioxidant; phytoalexin; plant metabolite; quorum sensing inhibitor; radical scavenger	2013	2013	11.0	low	0	0	1	0
zithromax	1	macrolide antibiotic	antibacterial drug; environmental contaminant; xenobiotic	2022	2022	2.0	low	0	0	0	1
afimoxifene	1	phenols; tertiary amino compound	antineoplastic agent; estrogen receptor antagonist; metabolite	2006	2006	18.0	low	0	1	0	0
dactinomycin	12	actinomycin	mutagen	2007	2020	11.0	low	0	4	8	0
melphalan	1	L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound	alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent	2005	2005	19.0	low	0	1	0	0
benzyloxycarbonylleucyl-leucyl-leucine aldehyde	3	amino aldehyde; carbamate ester; tripeptide	proteasome inhibitor	2008	2010	15.3	low	0	3	0	0
chalcone	1	chalcone	EC 3.2.1.1 (alpha-amylase) inhibitor	2005	2005	19.0	low	0	1	0	0
stilbenes	1	stilbene		2013	2013	11.0	low	0	0	1	0
s 1033	2	(trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor	2015	2020	6.5	low	0	0	2	0
isopropyl thiogalactoside	2	S-glycosyl compound		2011	2011	13.0	low	0	0	2	0
fludarabine	5	purine nucleoside		2006	2015	13.4	low	0	2	3	0
sesquiterpenes	1			2009	2009	15.0	low	0	1	0	0
curcumin	1	aromatic ether; beta-diketone; diarylheptanoid; enone; polyphenol	anti-inflammatory agent; antifungal agent; antineoplastic agent; biological pigment; contraceptive drug; dye; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; flavouring agent; food colouring; geroprotector; hepatoprotective agent; immunomodulator; iron chelator; ligand; lipoxygenase inhibitor; metabolite; neuroprotective agent; nutraceutical; radical scavenger	2012	2012	12.0	low	0	0	1	0
tenovin-1	1	thioureas		2015	2015	9.0	low	0	0	1	0
5-(4-ethylbenzylidene)-2-thioxothiazolidin-4-one	1			2016	2016	8.0	low	0	0	1	0
sj 172550	1			2015	2015	9.0	medium	0	0	1	0
thiourea	2	one-carbon compound; thioureas; ureas	antioxidant; chromophore	2011	2015	11.0	low	0	0	2	0
tempo	1	aminoxyls; piperidines	catalyst; ferroptosis inhibitor; radical scavenger	2013	2013	11.0	low	0	0	1	0
2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide	1			2008	2008	16.0	low	0	1	0	0
tamoxifen	2	stilbenoid; tertiary amino compound	angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator	2006	2019	11.5	low	0	1	1	0
p5091	1			2018	2018	6.0	low	0	0	1	0
sirtinol	1	aldimine; benzamides; naphthols	anti-inflammatory agent; EC 3.5.1.98 (histone deacetylase) inhibitor; Sir2 inhibitor	2012	2012	12.0	low	0	0	1	0
u 0126	2	aryl sulfide; dinitrile; enamine; substituted aniline	antineoplastic agent; antioxidant; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; osteogenesis regulator; vasoconstrictor agent	2012	2013	11.5	low	0	0	2	0
rtki cpd	1			2013	2013	11.0	low	0	0	1	0
dasatinib	1	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	2011	2011	13.0	low	0	0	1	0
naphthoquinones	1			2016	2016	8.0	low	0	0	1	0
osteoprotegerin	1	long-chain fatty acid		2008	2008	16.0	low	0	1	0	0
rhodamine 123	1	organic cation; xanthene dye	fluorochrome	2009	2009	15.0	low	0	1	0	0
ku 55933	3			2012	2020	8.3	low	0	0	3	0
calcitriol	2	D3 vitamins; hydroxycalciol; triol	antineoplastic agent; antipsoriatic; bone density conservation agent; calcium channel agonist; calcium channel modulator; hormone; human metabolite; immunomodulator; metabolite; mouse metabolite; nutraceutical	2010	2012	13.0	low	0	1	1	0
genistein	1	7-hydroxyisoflavones	antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; human urinary metabolite; phytoestrogen; plant metabolite; tyrosine kinase inhibitor	2009	2009	15.0	low	0	1	0	0
garcinol	1			2011	2011	13.0	low	0	0	1	0
zearalenone	1	macrolide; resorcinols	fungal metabolite; mycoestrogen	2020	2020	4.0	low	0	0	1	0
myricetin	1	7-hydroxyflavonol; hexahydroxyflavone	antineoplastic agent; antioxidant; cyclooxygenase 1 inhibitor; food component; geroprotector; hypoglycemic agent; plant metabolite	2019	2019	5.0	low	0	0	1	0
sirolimus	7	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	2010	2018	11.7	low	0	2	5	0
kn 93	1	monochlorobenzenes; monomethoxybenzene; primary alcohol; sulfonamide; tertiary amino compound	EC 2.7.11.17 (Ca(2+)/calmodulin-dependent protein kinase) inhibitor; geroprotector	2014	2014	10.0	low	0	0	1	0
casein kinase ii	1			2010	2010	14.0	low	0	1	0	0
semaxinib	1	olefinic compound; oxindoles; pyrroles	angiogenesis modulating agent; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; vascular endothelial growth factor receptor antagonist	2013	2013	11.0	low	0	0	1	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	2021	2021	3.0	low	0	0	0	1
jnj-7706621	1	sulfonamide		2013	2013	11.0	low	0	0	1	0
bay 11-7082	1	nitrile; sulfone	apoptosis inducer; EC 2.7.11.10 (IkappaB kinase) inhibitor; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor	2019	2019	5.0	low	0	0	1	0
arsenic	1	metalloid atom; pnictogen	micronutrient	2014	2014	10.0	low	0	0	1	0
geldanamycin	2			2007	2014	13.5	low	0	1	1	0
l 685458	1	carbamate ester; monocarboxylic acid amide; peptide; secondary alcohol	EC 3.4.23.46 (memapsin 2) inhibitor; peptidomimetic	2009	2009	15.0	low	0	1	0	0
vx680	4	N-arylpiperazine		2008	2014	13.5	low	0	3	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	2015	2015	9.0	low	0	0	1	0
axitinib	1	aryl sulfide; benzamides; indazoles; pyridines	antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist	2019	2019	5.0	low	0	0	1	0
tanespimycin	1	1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound; secondary amino compound	antineoplastic agent; apoptosis inducer; Hsp90 inhibitor	2011	2011	13.0	low	0	0	1	0
panobinostat	1	cinnamamides; hydroxamic acid; methylindole; secondary amino compound	angiogenesis modulating agent; antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor	2015	2015	9.0	low	0	0	1	0
staurosporine	2	ammonium ion derivative		2005	2010	16.5	low	0	2	0	0
sl 327	1			2011	2011	13.0	low	0	0	1	0
pi103	1	aromatic amine; morpholines; organic heterotricyclic compound; phenols; tertiary amino compound	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor	2008	2008	16.0	low	0	1	0	0
avn 944	1			2009	2009	15.0	low	0	1	0	0
motexafin gadolinium	1			2010	2010	14.0	low	0	1	0	0
bibr 1532	1			2021	2021	3.0	low	0	0	0	1
cp 31398	2			2011	2020	8.5	low	0	0	2	0
nutlin 1	4			2004	2012	17.5	medium	0	3	1	0
sepantronium	1	organic cation		2016	2016	8.0	low	0	0	1	0
azd 6244	1	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	2010	2010	14.0	low	0	1	0	0
ningalin b	1			2020	2020	4.0	low	0	0	1	0
abt-737	7	aromatic amine; aryl sulfide; biphenyls; C-nitro compound; monochlorobenzenes; N-arylpiperazine; N-sulfonylcarboxamide; secondary amino compound; tertiary amino compound	anti-allergic agent; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; B-cell lymphoma 2 inhibitor	2006	2019	11.6	low	0	2	5	0
px 478	1			2020	2020	4.0	low	0	0	1	0
fg-4592	1	aromatic ether; isoquinolines; N-acylglycine	EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor; EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor	2020	2020	4.0	low	0	0	1	0
bi 2536	1			2009	2009	15.0	low	0	1	0	0
fi-700	2			2010	2011	13.5	high	0	1	1	0
jnj 26854165	1			2017	2017	7.0	low	0	0	1	0
cytochrome c-t	2			2007	2014	13.5	low	0	1	1	0
hbx 41108	1			2018	2018	6.0	medium	0	0	1	0
kn 92	1			2014	2014	10.0	low	0	0	1	0
pevonedistat	1	cyclopentanols; indanes; pyrrolopyrimidine; secondary amino compound; sulfamidate	antineoplastic agent; apoptosis inducer	2020	2020	4.0	low	0	0	1	0
hoe 33342	1			2011	2011	13.0	low	0	0	1	0
olaparib	1	cyclopropanes; monofluorobenzenes; N-acylpiperazine; phthalazines	antineoplastic agent; apoptosis inducer; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor	2016	2016	8.0	low	0	0	1	0
thiostrepton	1			2014	2014	10.0	low	0	0	1	0
plx 4720	1	aromatic ketone; difluorobenzene; organochlorine compound; pyrrolopyridine; sulfonamide	antineoplastic agent; B-Raf inhibitor	2020	2020	4.0	low	0	0	1	0
mln 8237	3	benzazepine		2014	2017	8.7	low	0	0	3	0
tenovin-6	1	monocarboxylic acid amide; tertiary amino compound; thioureas	antineoplastic agent; p53 activator; Sir2 inhibitor	2012	2012	12.0	low	0	0	1	0
pci 32765	1	acrylamides; aromatic amine; aromatic ether; N-acylpiperidine; pyrazolopyrimidine; tertiary carboxamide	antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor	2016	2016	8.0	low	0	0	1	0
mk-1775	2	piperazines		2015	2018	7.5	low	0	0	2	0
mk 2206	1	organic heterotricyclic compound	EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor	2017	2017	7.0	low	0	0	1	0
navitoclax	1	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	2019	2019	5.0	low	0	0	1	0
plx4032	3	aromatic ketone; difluorobenzene; monochlorobenzenes; pyrrolopyridine; sulfonamide	antineoplastic agent; B-Raf inhibitor	2013	2015	10.3	low	0	0	3	0
piperidines	2			2013	2016	9.5	low	0	0	2	0
interleukin-8	2			2013	2014	10.5	low	0	0	2	0
dabrafenib	1	1,3-thiazoles; aminopyrimidine; organofluorine compound; sulfonamide	anticoronaviral agent; antineoplastic agent; B-Raf inhibitor	2020	2020	4.0	low	0	0	1	0
yk 4-279	1	aromatic ketone		2014	2014	10.0	low	0	0	1	0
gx 15-070	1			2015	2015	9.0	low	0	0	1	0
apr-246	1			2011	2011	13.0	low	0	0	1	0
rg7388	6			2014	2018	7.5	low	0	0	6	0
sar405838	3			2016	2018	7.3	medium	0	0	3	0
ascorbic acid	1	ascorbic acid; vitamin C	coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent	2010	2010	14.0	low	0	1	0	0
tetracycline	1			2012	2012	12.0	low	0	0	1	0
warfarin	1	benzenes; hydroxycoumarin; methyl ketone		2011	2011	13.0	low	0	0	1	0
transforming growth factor beta	1			2011	2011	13.0	low	0	0	1	0
rg7112	3			2015	2021	7.0	low	0	0	2	1
gsk2830371	5			2016	2018	7.6	high	0	0	5	0
selinexor	1			2018	2018	6.0	low	0	0	1	0
cyclin d1	5			2007	2016	12.2	low	0	2	3	0
benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone	2			2013	2014	10.5	low	0	0	2	0
nitrophenols	7			2006	2019	11.6	low	0	2	5	0
oridonin	1			2017	2017	7.0	low	0	0	1	0
apicidin	1			2012	2012	12.0	low	0	0	1	0
deoxyguanosine	1	purine 2'-deoxyribonucleoside; purines 2'-deoxy-D-ribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2017	2017	7.0	low	0	0	1	0
guanosine triphosphate	1	guanosine 5'-phosphate; purine ribonucleoside 5'-triphosphate	Escherichia coli metabolite; mouse metabolite; uncoupling protein inhibitor	2009	2009	15.0	low	0	1	0	0
folic acid	2	folic acids; N-acyl-amino acid	human metabolite; mouse metabolite; nutrient	2012	2013	11.5	low	0	0	2	0
dacarbazine	2	dacarbazine		2011	2012	12.5	low	0	0	2	0
8-hydroxy-2'-deoxyguanosine	1	guanosines	biomarker	2017	2017	7.0	low	0	0	1	0
mi-219	3			2012	2016	9.3	high	0	0	3	0
pyrimidinones	2			2015	2018	7.5	low	0	0	2	0
phenanthrenes	1			2008	2008	16.0	low	0	1	0	0

Condition	Studies	First Year	Last Year	Average Age	Relationship Strength	Trials	2000's	2010's	post-2020
17p11.2 Monosomy	1	2012	2012	12.0	low	0	0	1	0
Abnormalities, Autosome	1	2008	2008	16.0	low	0	1	0	0
Abnormalities, Congenital, Nervous System	1	2020	2020	4.0	low	0	0	1	0
Acute Confusional Senile Dementia	1	2016	2016	8.0	low	0	0	1	0
Acute Disease	5	2007	2019	13.2	low	0	4	1	0
Acute Kidney Failure	1	2012	2012	12.0	low	0	0	1	0
Acute Kidney Injury	1	2012	2012	12.0	low	0	0	1	0
Acute Liver Injury, Drug-Induced	1	2017	2017	7.0	low	0	0	1	0
Acute Lung Injury	1	2009	2009	15.0	low	0	1	0	0
Acute Lymphoid Leukemia	5	2008	2021	8.8	low	0	1	3	1
Acute Myelogenous Leukemia	21	2005	2021	12.7	low	1	10	10	1
Adenocarcinoma	4	2012	2020	7.8	low	0	0	4	0
Adenocarcinoma Of Kidney	4	2010	2021	9.5	low	0	1	2	1
Adenocarcinoma of Lung	2	2017	2018	6.5	low	0	0	2	0
Adenocarcinoma, Basal Cell	4	2012	2020	7.8	low	0	0	4	0
Adenocarcinoma, Mucinous	1	2013	2013	11.0	low	0	0	1	0
Adjuvant Arthritis	1	2016	2016	8.0	low	0	0	1	0
Adrenocortical Carcinoma	1	2018	2018	6.0	low	0	0	1	0
African Lymphoma	3	2009	2010	14.7	low	0	3	0	0
Age-Related Macular Degeneration	2	2013	2022	6.5	low	0	0	1	1
Aging	1	2012	2012	12.0	low	0	0	1	0
Alcohol Drinking	1	2017	2017	7.0	low	0	0	1	0
Alloxan Diabetes	2	2013	2016	9.5	low	0	0	2	0
Alzheimer Disease	1	2016	2016	8.0	low	0	0	1	0
Anaplastic Ependymoma	1	2016	2016	8.0	low	0	0	1	0
Anaplastic Large-Cell Lymphoma	1	2009	2009	15.0	low	0	1	0	0
Anemia, Congenital Hypoplastic, Of Blackfan And Diamond	1	2011	2011	13.0	low	0	0	1	0
Anemia, Diamond-Blackfan	1	2011	2011	13.0	low	0	0	1	0
Anemia, Macrocytic	1	2011	2011	13.0	low	0	0	1	0
Aneuploid	2	2010	2015	11.5	low	0	1	1	0
Angiogenesis, Pathologic	4	2007	2014	13.0	low	0	1	3	0
Anoxemia	6	2005	2023	12.2	low	0	3	2	1
Arachnoidal Cerebellar Sarcoma, Circumscribed	3	2012	2016	10.7	low	0	0	3	0
Arthritis, Rheumatoid	1	2016	2016	8.0	low	0	0	1	0
Astrocytoma, Grade IV	7	2011	2020	8.4	low	0	0	7	0
ATLL	1	2009	2009	15.0	low	0	1	0	0
Atypical Lipomatous Tumor	6	2007	2023	10.5	low	0	2	3	1
Autoimmune Diabetes	2	2018	2020	5.0	low	0	0	2	0
Autoimmune Diseases of the Nervous System	1	2020	2020	4.0	low	0	0	1	0
B Virus Infection	2	2007	2017	12.0	low	0	1	1	0
B-Cell Chronic Lymphocytic Leukemia	26	2006	2016	13.4	low	0	13	13	0
B-Cell Lymphoma	2	2006	2012	15.0	low	0	1	1	0
B16 Melanoma	5	2010	2017	10.6	low	0	1	4	0
Bacterial Disease	1	2012	2012	12.0	low	0	0	1	0
Bacterial Infections	1	2012	2012	12.0	low	0	0	1	0
Benign Cerebellar Neoplasms	1	2012	2012	12.0	low	0	0	1	0
Benign Neoplasms	57	2005	2023	11.5	low	0	20	35	2
Benign Neoplasms, Brain	6	2012	2020	8.3	low	0	0	6	0
Bile Duct Cancer	1	2010	2010	14.0	low	0	1	0	0
Bile Duct Neoplasms	1	2010	2010	14.0	low	0	1	0	0
Blast Crisis	3	2008	2015	13.0	low	0	2	1	0
Blast Phase	3	2008	2015	13.0	low	0	2	1	0
Bone Cancer	11	2008	2023	10.4	low	0	3	7	1
Bone Neoplasms	11	2008	2023	10.4	low	0	3	7	1
Brain Neoplasms	6	2012	2020	8.3	low	0	0	6	0
Breast Cancer	29	2005	2020	10.3	low	0	6	23	0
Breast Neoplasms	29	2005	2020	10.3	low	0	6	23	0
Bright Disease	2	2013	2016	9.5	low	0	0	2	0
Brill-Symmers Disease	1	2010	2010	14.0	low	0	1	0	0
Burkitt Lymphoma	3	2009	2010	14.7	low	0	3	0	0
Cancer of Colon	12	2005	2020	13.7	low	0	7	5	0
Cancer of Endometrium	2	2013	2014	10.5	low	0	0	2	0
Cancer of Esophagus	3	2018	2023	3.0	low	0	0	1	2
Cancer of Eye	2	2007	2013	14.0	low	0	1	1	0
Cancer of Gastrointestinal Tract	1	2012	2012	12.0	low	0	0	1	0
Cancer of Head	1	2011	2011	13.0	low	0	0	1	0
Cancer of Intestines	1	2018	2018	6.0	low	0	0	1	0
Cancer of Kidney	5	2009	2021	10.0	low	0	1	3	1
Cancer of Larynx	1	2010	2010	14.0	low	0	1	0	0
Cancer of Liver	10	2009	2022	10.0	low	0	2	7	1
Cancer of Lung	22	2006	2020	9.2	low	0	4	18	0
Cancer of Nasopharynx	2	2015	2018	7.5	low	0	0	2	0
Cancer of Ovary	6	2012	2016	9.8	low	0	0	6	0
Cancer of Pancreas	4	2013	2022	7.0	low	0	0	3	1
Cancer of Prostate	9	2007	2020	10.3	low	0	3	6	0
Cancer of Skin	10	2010	2020	9.9	low	0	1	9	0
Cancer of Stomach	3	2011	2021	7.3	low	0	0	2	1
Cancer of Testis	2	2010	2011	13.5	low	0	1	1	0
Cancer of the Retina	4	2006	2016	13.5	low	0	2	2	0
Cancer of the Uterus	2	2011	2012	12.5	low	0	0	2	0
Cancer, Radiation-Induced	1	2013	2013	11.0	low	0	0	1	0
Carcinogenesis	6	2014	2021	7.3	low	0	0	5	1
Carcinoma	6	2006	2018	12.8	low	0	3	3	0
Carcinoma, Anaplastic	6	2006	2018	12.8	low	0	3	3	0
Carcinoma, Colloid	1	2013	2013	11.0	low	0	0	1	0
Carcinoma, Ductal, Breast	1	2016	2016	8.0	low	0	0	1	0
Carcinoma, Ductal, Pancreatic	1	2019	2019	5.0	low	0	0	1	0
Carcinoma, Embryonal	1	2010	2010	14.0	low	0	1	0	0
Carcinoma, Epidermoid	3	2010	2018	11.0	low	0	1	2	0
Carcinoma, Hepatocellular	11	2009	2022	9.7	low	0	2	8	1
Carcinoma, Mucoepidermoid	1	2018	2018	6.0	low	0	0	1	0
Carcinoma, Non-Small Cell Lung	4	2012	2019	8.0	low	0	0	4	0
Carcinoma, Non-Small-Cell Lung	4	2012	2019	8.0	low	0	0	4	0
Carcinoma, Pancreatic Ductal	1	2019	2019	5.0	low	0	0	1	0
Carcinoma, Renal Cell	4	2010	2021	9.5	low	0	1	2	1
Carcinoma, Squamous Cell	3	2010	2018	11.0	low	0	1	2	0
Cardiac Diseases	1	2017	2017	7.0	low	0	0	1	0
Cardiovascular Stroke	1	2017	2017	7.0	low	0	0	1	0
Cat Diseases	1	2012	2012	12.0	low	0	0	1	0
Cell Transformation, Neoplastic	9	2006	2018	11.6	low	0	3	6	0
Cell Transformation, Viral	2	2007	2009	16.0	low	0	2	0	0
Chemical and Drug Induced Liver Injury	1	2017	2017	7.0	low	0	0	1	0
Chlamydia Infections	1	2022	2022	2.0	low	0	0	0	1
Cholangiocarcinoma	1	2010	2010	14.0	low	0	1	0	0
Cholangiocellular Carcinoma	1	2010	2010	14.0	low	0	1	0	0
Chromosomal Translocation	1	2011	2011	13.0	low	0	0	1	0
Chromosome Deletion	3	2011	2012	12.3	low	0	0	3	0
Cirrhosis	3	2016	2018	7.0	low	0	0	3	0
Cognition Disorders	1	2016	2016	8.0	low	0	0	1	0
Cognitive Decline	1	2022	2022	2.0	low	0	0	0	1
Cognitive Dysfunction	1	2022	2022	2.0	low	0	0	0	1
Collodion Baby Syndrome	1	2014	2014	10.0	low	0	0	1	0
Colonic Neoplasms	12	2005	2020	13.7	low	0	7	5	0
Colorectal Cancer	6	2008	2020	9.0	low	0	1	5	0
Colorectal Neoplasms	6	2008	2020	9.0	low	0	1	5	0
Congenital Zika Syndrome	1	2020	2020	4.0	low	0	0	1	0
Coronary Artery Stenosis	1	2019	2019	5.0	low	0	0	1	0
Coronary Stenosis	1	2019	2019	5.0	low	0	0	1	0
Cutaneous T-Cell Lymphoma	1	2012	2012	12.0	low	0	0	1	0
Cyst	1	2016	2016	8.0	low	0	0	1	0
Cystadenocarcinoma, Serous	1	2013	2013	11.0	low	0	0	1	0
Cystic Kidney Diseases	1	2016	2016	8.0	low	0	0	1	0
Degenerative Diseases, Central Nervous System	1	2012	2012	12.0	low	0	0	1	0
Diabetes Mellitus, Type 1	2	2018	2020	5.0	low	0	0	2	0
Diabetic Glomerulosclerosis	1	2017	2017	7.0	low	0	0	1	0
Diabetic Nephropathies	1	2017	2017	7.0	low	0	0	1	0
Diathesis	1	2012	2012	12.0	low	0	0	1	0
Diffuse Large B-Cell Lymphoma	1	2011	2011	13.0	low	0	0	1	0
Diffuse Lymphocytic Lymphoma, Poorly-Differentiated	4	2009	2016	13.0	low	0	3	1	0
Disease Exacerbation	5	2007	2018	11.4	low	0	2	3	0
Disease Models, Animal	25	2009	2022	8.9	low	0	2	22	1
Diseases of Immune System	1	2012	2012	12.0	low	0	0	1	0
Dysmyelopoietic Syndromes	1	2011	2011	13.0	low	0	0	1	0
Dysplastic Nevus Syndrome, Hereditary	2	2018	2020	5.0	low	0	0	2	0
Ectopic Ossification	1	2011	2011	13.0	low	0	0	1	0
Endometrial Neoplasms	2	2013	2014	10.5	low	0	0	2	0
Ependymoma	1	2016	2016	8.0	low	0	0	1	0
Eperythrozoonosis	1	2018	2018	6.0	low	0	0	1	0
Epithelial Neoplasms	1	2009	2009	15.0	low	0	1	0	0
ER-Negative PR-Negative HER2-Negative Breast Cancer	1	2015	2015	9.0	low	0	0	1	0
Erythremia	2	2012	2012	12.0	low	0	0	2	0
Erythroderma, Sezary	1	2012	2012	12.0	low	0	0	1	0
Esophageal Neoplasms	3	2018	2023	3.0	low	0	0	1	2
Esophageal Squamous Cell Carcinoma	2	2022	2023	1.5	low	0	0	0	2
Ewing Sarcoma	4	2011	2014	12.0	low	0	0	4	0
Experimental Hepatoma	1	2017	2017	7.0	low	0	0	1	0
Experimental Neoplasms	4	2004	2016	12.5	low	0	1	3	0
Eye Cancer, Retinoblastoma	9	2006	2016	14.7	low	0	5	4	0
Eye Diseases	1	2018	2018	6.0	low	0	0	1	0
Eye Disorders	1	2018	2018	6.0	low	0	0	1	0
Female Genital Neoplasms	1	2010	2010	14.0	low	0	1	0	0
Fibroid	2	2011	2012	12.5	low	0	0	2	0
Fibrosarcoma	1	2007	2007	17.0	low	0	1	0	0
Fibrosis	3	2016	2018	7.0	low	0	0	3	0
Fra(X) Syndrome	2	2016	2022	5.0	low	0	0	1	1
Fragile X Syndrome	2	2016	2022	5.0	low	0	0	1	1
Gastrointestinal Stromal Neoplasm	1	2012	2012	12.0	low	0	0	1	0
Gastrointestinal Stromal Tumors	1	2012	2012	12.0	low	0	0	1	0
Genital Neoplasms, Female	1	2010	2010	14.0	low	0	1	0	0
Germinoblastoma	6	2007	2016	12.5	low	0	2	4	0
Glial Cell Tumors	2	2010	2020	9.0	low	0	1	1	0
Glioblastoma	7	2011	2020	8.4	low	0	0	7	0
Glioma	2	2010	2020	9.0	low	0	1	1	0
Glomerulonephritis	2	2013	2016	9.5	low	0	0	2	0
Glomerulonephritis, Lupus	1	2011	2011	13.0	low	0	0	1	0
Granulocytic Leukemia	4	2007	2012	14.2	low	0	3	1	0
Granulocytic Leukemia, Chronic	1	2015	2015	9.0	low	0	0	1	0
Granuloma, Hodgkin	2	2007	2007	17.0	low	0	2	0	0
Head and Neck Neoplasms	1	2011	2011	13.0	low	0	0	1	0
Heart Diseases	1	2017	2017	7.0	low	0	0	1	0
Hematologic Malignancies	3	2008	2014	13.3	low	0	2	1	0
Hematologic Neoplasms	3	2008	2014	13.3	low	0	2	1	0
Hepatocellular Carcinoma	11	2009	2022	9.7	low	0	2	8	1
Hodgkin Disease	2	2007	2007	17.0	low	0	2	0	0
Hyperplasia	1	2011	2011	13.0	low	0	0	1	0
Hypertension, Pulmonary	1	2013	2013	11.0	low	0	0	1	0
Hypoxia	6	2005	2023	12.2	low	0	3	2	1
Ichthyosis, Lamellar	1	2014	2014	10.0	low	0	0	1	0
Immune System Diseases	1	2012	2012	12.0	low	0	0	1	0
Infections, Chlamydia	1	2022	2022	2.0	low	0	0	0	1
Infections, Plasmodium	1	2015	2015	9.0	low	0	0	1	0
Inflammation	4	2011	2018	9.5	low	0	0	4	0
Injury, Ischemia-Reperfusion	1	2012	2012	12.0	low	0	0	1	0
Innate Inflammatory Response	4	2011	2018	9.5	low	0	0	4	0
Intestinal Neoplasms	1	2018	2018	6.0	low	0	0	1	0
Intraocular Pressure	1	2011	2011	13.0	low	0	0	1	0
Invasiveness, Neoplasm	3	2010	2016	10.3	low	0	1	2	0
Ischemia	1	2013	2013	11.0	low	0	0	1	0
Kahler Disease	6	2005	2016	13.7	low	0	4	2	0
Kaposi Sarcoma	3	2007	2015	12.7	low	0	1	2	0
Keratoderma Blennorrhagicum	1	2014	2014	10.0	low	0	0	1	0
Keratosis	1	2014	2014	10.0	low	0	0	1	0
Kidney Diseases	1	2018	2018	6.0	low	0	0	1	0
Kidney Diseases, Cystic	1	2016	2016	8.0	low	0	0	1	0
Kidney Neoplasms	5	2009	2021	10.0	low	0	1	3	1
Laryngeal Neoplasms	1	2010	2010	14.0	low	0	1	0	0
Leiomyoma	2	2011	2012	12.5	low	0	0	2	0
Leucocythaemia	5	2010	2019	10.4	low	0	1	4	0
Leukemia	5	2010	2019	10.4	low	0	1	4	0
Leukemia-Lymphoma, Adult T-Cell	1	2009	2009	15.0	low	0	1	0	0
Leukemia, Lymphocytic	1	2008	2008	16.0	low	0	1	0	0
Leukemia, Lymphocytic, Chronic, B-Cell	26	2006	2016	13.4	low	0	13	13	0
Leukemia, Lymphoid	1	2008	2008	16.0	low	0	1	0	0
Leukemia, Myelogenous, Chronic, BCR-ABL Positive	1	2015	2015	9.0	low	0	0	1	0
Leukemia, Myeloid	4	2007	2012	14.2	low	0	3	1	0
Leukemia, Myeloid, Acute	21	2005	2021	12.7	low	1	10	10	1
Leukemia, Pre-B-Cell	1	2012	2012	12.0	low	0	0	1	0
Libman-Sacks Disease	1	2011	2011	13.0	low	0	0	1	0
Liposarcoma	6	2007	2023	10.5	low	0	2	3	1
Liver Neoplasms	10	2009	2022	10.0	low	0	2	7	1
Local Neoplasm Recurrence	1	2016	2016	8.0	low	0	0	1	0
Lung Adenocarcinoma	2	2017	2018	6.5	low	0	0	2	0
Lung Injury, Acute	1	2009	2009	15.0	low	0	1	0	0
Lung Neoplasms	22	2006	2020	9.2	low	0	4	18	0
Lupus Erythematosus, Systemic	1	2011	2011	13.0	low	0	0	1	0
Lupus Nephritis	1	2011	2011	13.0	low	0	0	1	0
Lymphoma	6	2007	2016	12.5	low	0	2	4	0
Lymphoma, B-Cell	2	2006	2012	15.0	low	0	1	1	0
Lymphoma, Follicular	1	2010	2010	14.0	low	0	1	0	0
Lymphoma, Large B-Cell, Diffuse	1	2011	2011	13.0	low	0	0	1	0
Lymphoma, Large-Cell, Anaplastic	1	2009	2009	15.0	low	0	1	0	0
Lymphoma, Mantle-Cell	4	2009	2016	13.0	low	0	3	1	0
Lymphoma, Primary Effusion	3	2013	2015	10.3	low	0	0	3	0
Lymphoma, T-Cell, Cutaneous	1	2012	2012	12.0	low	0	0	1	0
Macular Degeneration	2	2013	2022	6.5	low	0	0	1	1
Malaria	1	2015	2015	9.0	low	0	0	1	0
Malaria, Falciparum	1	2015	2015	9.0	low	0	0	1	0
Malignant Melanoma	17	2010	2020	9.1	low	0	2	15	0
Malignant Mesothelioma	3	2014	2017	8.0	low	0	0	3	0
Medulloblastoma	3	2012	2016	10.7	low	0	0	3	0
Melanoma	17	2010	2020	9.1	low	0	2	15	0
Mesothelioma	5	2014	2021	6.2	low	0	0	4	1
Metastase	3	2011	2015	11.0	low	0	0	3	0
Mole, Skin	1	2010	2010	14.0	low	0	1	0	0
Molluscum Contagiosum	1	2014	2014	10.0	low	0	0	1	0
Multiple Myeloma	6	2005	2016	13.7	low	0	4	2	0
Muscle Tissue Neoplasms	1	2009	2009	15.0	low	0	1	0	0
Myelodysplastic Syndromes	1	2011	2011	13.0	low	0	0	1	0
Myocardial Infarction	1	2017	2017	7.0	low	0	0	1	0
Nasopharyngeal Carcinoma	2	2015	2018	7.5	low	0	0	2	0
Nasopharyngeal Neoplasms	2	2015	2018	7.5	low	0	0	2	0
Necrosis	2	2011	2012	12.5	low	0	0	2	0
Neointima	1	2011	2011	13.0	low	0	0	1	0
Neoplasm Metastasis	3	2011	2015	11.0	low	0	0	3	0
Neoplasms	57	2005	2023	11.5	low	0	20	35	2
Neoplasms, Pleural	2	2014	2017	8.5	low	0	0	2	0
Neurilemmoma	1	2018	2018	6.0	low	0	0	1	0
Neurilemoma	1	2018	2018	6.0	low	0	0	1	0
Neuroblastoma	24	2006	2022	11.8	low	0	9	13	2
Neurodegenerative Diseases	1	2012	2012	12.0	low	0	0	1	0
Neuroendocrine Tumors	1	2018	2018	6.0	low	0	0	1	0
Osteogenic Sarcoma	19	2007	2023	10.5	low	0	5	13	1
Osteosarcoma	19	2007	2023	10.5	low	0	5	13	1
Ovarian Neoplasms	6	2012	2016	9.8	low	0	0	6	0
Pancreatic Neoplasms	4	2013	2022	7.0	low	0	0	3	1
Peritoneal Carcinomatosis	1	2013	2013	11.0	low	0	0	1	0
Peritoneal Neoplasms	1	2013	2013	11.0	low	0	0	1	0
Plasmodium falciparum Malaria	1	2015	2015	9.0	low	0	0	1	0
Polycythemia Vera	2	2012	2012	12.0	low	0	0	2	0
Polyploid	3	2008	2010	14.7	low	0	3	0	0
Precursor B-Cell Lymphoblastic Leukemia-Lymphoma	1	2012	2012	12.0	low	0	0	1	0
Precursor Cell Lymphoblastic Leukemia-Lymphoma	5	2008	2021	8.8	low	0	1	3	1
Pregnancy	1	2010	2010	14.0	low	0	1	0	0
Proliferative Vitreoretinopathy	1	2012	2012	12.0	low	0	0	1	0
Prostatic Neoplasms	9	2007	2020	10.3	low	0	3	6	0
Proteinuria	1	2013	2013	11.0	low	0	0	1	0
Pulmonary Arterial Hypertension	1	2021	2021	3.0	low	0	0	0	1
Pulmonary Hypertension	1	2013	2013	11.0	low	0	0	1	0
Reperfusion Injury	1	2012	2012	12.0	low	0	0	1	0
Retinal Detachment	1	2012	2012	12.0	low	0	0	1	0
Retinal Pigment Epithelial Detachment	1	2012	2012	12.0	low	0	0	1	0
Retinoblastoma	9	2006	2016	14.7	low	0	5	4	0
Rhabdomyosarcoma	1	2009	2009	15.0	low	0	1	0	0
Rhabdomyosarcoma 2	2	2009	2009	15.0	low	0	2	0	0
Rhabdomyosarcoma, Alveolar	2	2009	2009	15.0	low	0	2	0	0
Rhabdomyosarcoma, Embryonal	1	2009	2009	15.0	low	0	1	0	0
Rheumatoid Arthritis	1	2016	2016	8.0	low	0	0	1	0
Sarcoma	4	2013	2015	10.2	low	0	0	4	0
Sarcoma, Epithelioid	4	2013	2015	10.2	low	0	0	4	0
Sarcoma, Ewing	4	2011	2014	12.0	low	0	0	4	0
Sarcoma, Kaposi	3	2007	2015	12.7	low	0	1	2	0
Sarcoma, Synovial	1	2009	2009	15.0	low	0	1	0	0
Sensitivity and Specificity	3	2007	2013	13.0	low	0	1	2	0
Sezary Syndrome	1	2012	2012	12.0	low	0	0	1	0
Skin Neoplasms	10	2010	2020	9.9	low	0	1	9	0
Smith-Magenis Syndrome	1	2012	2012	12.0	low	0	0	1	0
Soft Tissue Neoplasms	1	2007	2007	17.0	low	0	1	0	0
Stomach Neoplasms	3	2011	2021	7.3	low	0	0	2	1
Synovioma	1	2009	2009	15.0	low	0	1	0	0
Testicular Neoplasms	2	2010	2011	13.5	low	0	1	1	0
Tetraploid	2	2010	2014	12.0	low	0	1	1	0
Thrombocytopenia	1	2016	2016	8.0	low	0	0	1	0
Thrombopenia	1	2016	2016	8.0	low	0	0	1	0
Triple Negative Breast Neoplasms	1	2015	2015	9.0	low	0	0	1	0
Ureteral Obstruction	1	2018	2018	6.0	low	0	0	1	0
Uterine Neoplasms	2	2011	2012	12.5	low	0	0	2	0
Uveal Neoplasms	1	2012	2012	12.0	low	0	0	1	0
Verruca	1	2014	2014	10.0	low	0	0	1	0
Viral Diseases	1	2012	2012	12.0	low	0	0	1	0
Virus Diseases	1	2012	2012	12.0	low	0	0	1	0
Vitreoretinopathy, Proliferative	1	2012	2012	12.0	low	0	0	1	0
Warts	1	2014	2014	10.0	low	0	0	1	0
Zika Virus Infection	1	2020	2020	4.0	low	0	0	1	0

Safety/Toxicity (10)

Article	Year
An MDM2 inhibitor achieves synergistic cytotoxic effects with adenoviruses lacking E1B55kDa gene on mesothelioma with the wild-type p53 through augmenting NFI expression. Cell death & disease, , 07-02, Volume: 12, Issue:7	2021
The combination of Nutlin-3 and Tanshinone IIA promotes synergistic cytotoxicity in acute leukemic cells expressing wild-type p53 by co-regulating MDM2-P53 and the AKT/mTOR pathway. The international journal of biochemistry & cell biology, , Volume: 106	2019
Protective role of p53 in acetaminophen hepatotoxicity. Free radical biology & medicine, , Volume: 106	2017
Ibrutinib synergizes with MDM-2 inhibitors in promoting cytotoxicity in B chronic lymphocytic leukemia. Oncotarget, , Oct-25, Volume: 7, Issue:43	2016
Nutlin-3 treatment spares cisplatin-induced inhibition of bone healing while maintaining osteosarcoma toxicity. Journal of orthopaedic research : official publication of the Orthopaedic Research Society, , Volume: 34, Issue:10	2016
Mdm2 inhibition confers protection of p53-proficient cells from the cytotoxic effects of Wee1 inhibitors. Oncotarget, , Oct-20, Volume: 6, Issue:32	2015
Nutlin-3 sensitizes nasopharyngeal carcinoma cells to cisplatin-induced cytotoxicity. Oncology reports, , Volume: 34, Issue:4	2015
The sorafenib plus nutlin-3 combination promotes synergistic cytotoxicity in acute myeloid leukemic cells irrespectively of FLT3 and p53 status. Haematologica, , Volume: 97, Issue:11	2012
An evaluation of small-molecule p53 activators as chemoprotectants ameliorating adverse effects of anticancer drugs in normal cells. Cell cycle (Georgetown, Tex.), , May-01, Volume: 11, Issue:9	2012
Exposure of B cell chronic lymphocytic leukemia (B-CLL) cells to nutlin-3 induces a characteristic gene expression profile, which correlates with nutlin-3-mediated cytotoxicity. Current cancer drug targets, , Volume: 9, Issue:4	2009

Long-term Use (1)

Article	Year
Combination treatment in vitro with Nutlin, a small-molecule antagonist of MDM2, and pegylated interferon-α 2a specifically targets JAK2V617F-positive polycythemia vera cells. Blood, , Oct-11, Volume: 120, Issue:15	2012

Pharmacokinetics (3)

Article	Year
Effect of pharmacodynamical interaction between nutlin-3a and aspirin in the activation of p53. Journal of theoretical biology, , 08-07, Volume: 522	2021
Mdm2 and aurora kinase a inhibitors synergize to block melanoma growth by driving apoptosis and immune clearance of tumor cells. Cancer research, , Jan-01, Volume: 75, Issue:1	2015
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration. Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:1	2011

Bioavailability (8)

Article	Year
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5	2019
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors. ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3	2016
Mdm2 and aurora kinase a inhibitors synergize to block melanoma growth by driving apoptosis and immune clearance of tumor cells. Cancer research, , Jan-01, Volume: 75, Issue:1	2015
Nanoparticles loaded with Nutlin-3 display cytotoxicity towards p53(wild-type) JVM-2 but not towards p53(mutated) BJAB leukemic cells. Current medicinal chemistry, , Volume: 20, Issue:21	2013
Folate decorated dual drug loaded nanoparticle: role of curcumin in enhancing therapeutic potential of nutlin-3a by reversing multidrug resistance. PloS one, , Volume: 7, Issue:3	2012
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration. Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:1	2011
Epithelial cell adhesion molecule targeted nutlin-3a loaded immunonanoparticles for cancer therapy. Acta biomaterialia, , Volume: 7, Issue:1	2011
Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction. Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24	2009

Dosage (9)

Article	Year
Clearing Chlamydia abortus infection in epithelial cells and primary human macrophages by use of antibiotics and the MDM2-p53-inhibitor nutlin-3. Diagnostic microbiology and infectious disease, , Volume: 103, Issue:3	2022
Effect of pharmacodynamical interaction between nutlin-3a and aspirin in the activation of p53. Journal of theoretical biology, , 08-07, Volume: 522	2021
Surface plasmon resonance and cytotoxicity assays of drug efficacies predicted computationally to inhibit p53/MDM2 interaction. Analytical biochemistry, , 03-15, Volume: 569	2019
Synergistic effect of Nutlin-3 combined with MG-132 on schwannoma cells through restoration of merlin and p53 tumour suppressors. EBioMedicine, , Volume: 36	2018
On p53 revival using system oriented drug dosage design. Journal of theoretical biology, , 02-21, Volume: 415	2017
Potentiation of Carboplatin-Mediated DNA Damage by the Mdm2 Modulator Nutlin-3a in a Humanized Orthotopic Breast-to-Lung Metastatic Model. Molecular cancer therapeutics, , Volume: 14, Issue:12	2015
Rational design and binding mode duality of MDM2-p53 inhibitors. Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10	2013
Pharmacological inhibition of Mdm2 triggers growth arrest and promotes DNA breakage in mouse colon tumors and human colon cancer cells. Molecular carcinogenesis, , Volume: 51, Issue:5	2012
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration. Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:1	2011

Interactions (6)

Article	Year
MDM2 antagonist-loaded targeted micelles in combination with doxorubicin: effective synergism against human glioblastoma via p53 re-activation. Journal of drug targeting, , Volume: 27, Issue:5-6
Synergistic effect of Nutlin-3 combined with MG-132 on schwannoma cells through restoration of merlin and p53 tumour suppressors. EBioMedicine, , Volume: 36	2018
Metformin produces growth inhibitory effects in combination with nutlin-3a on malignant mesothelioma through a cross-talk between mTOR and p53 pathways. BMC cancer, , 05-02, Volume: 17, Issue:1	2017
Preliminary evaluation of prostate-targeted radiotherapy using (131) I-MIP-1095 in combination with radiosensitising chemotherapeutic drugs. The Journal of pharmacy and pharmacology, , Volume: 68, Issue:7	2016
Synergistic effects of p53 activation via MDM2 inhibition in combination with inhibition of Bcl-2 or Bcr-Abl in CD34+ proliferating and quiescent chronic myeloid leukemia blast crisis cells. Oncotarget, , Oct-13, Volume: 6, Issue:31	2015
Cyclin-dependent kinase inhibitors sensitize tumor cells to nutlin-induced apoptosis: a potent drug combination. Molecular cancer research : MCR, , Volume: 5, Issue:11	2007

Natural Sources (1)

Article	Year
Chemopreventive Agent 3,3'-Diindolylmethane Inhibits MDM2 in Colorectal Cancer Cells. International journal of molecular sciences, , Jun-30, Volume: 21, Issue:13	2020