Rhein is a naturally occurring anthraquinone derivative found in plants such as rhubarb and senna. It has been studied for its potential medicinal properties, including its effects on the digestive system and its anti-inflammatory and antioxidant activities. Rhein is thought to exert its effects by modulating the activity of various enzymes and signaling pathways. It has been shown to inhibit the growth of certain cancer cells in vitro and to possess antimicrobial activity against bacteria and fungi. However, further research is needed to fully understand the mechanisms of action and potential clinical applications of rhein.'
| ID Source | ID |
|---|---|
| PubMed CID | 10168 |
| CHEMBL ID | 418068 |
| CHEBI ID | 8825 |
| SCHEMBL ID | 25253 |
| MeSH ID | M0074242 |
| Synonym |
|---|
| REGID855879 |
| BRD-K27335680-001-01-9 |
| rhubarb yellow |
| chrysazin-3-carboxylic acid |
| 4,5-dihydroxy-2-anthraquinonecarboxylic acid |
| 4,5-dihydroxyanthraquinone-2-carboxylic acid |
| nsc-38629 |
| 2-anthracenecarboxylic acid,10-dihydro-4,5-dihydroxy-9,10-dioxo- |
| monorhein |
| 1,8-dihydroxyanthraquinone-3-carboxylic acid |
| rheic acid |
| nsc38629 |
| cassic acid |
| 2-anthroic acid,10-dihydro-4,5-dihydroxy-9,10-dioxo- |
| 9,10-dihydro-4,5-dihydroxy-9,10-dioxo-2-anthracenecarboxylic acid |
| einecs 207-521-4 |
| 2-anthracenecarboxylic acid, 9,10-dihydro-4,5-dihydroxy-9,10-dioxo- |
| c15h8o6 |
| dipropionyl rhein |
| ccris 5129 |
| nsc 38629 |
| 9,10-dihydro-4,5-dihydroxy-9,10-dioxoanthracene-2-carboxylic acid |
| 2-anthroic acid, 9,10-dihydro-4,5-dihydroxy-9,10-dioxo- |
| brn 2222155 |
| MEGXP0_001866 |
| ACON1_000217 |
| 9,10-dihydro-4,5-dihydroxy-9,10-dioxo-2-anthracene carboxylic acid |
| 4,5-dihydroxy-9,10-dioxo-anthracene-2-carboxylic acid |
| 4,5-dioh-anthraquinone-2-cooh |
| rhein (1,8-dihydroxy-3-carboxyl anthraquinone) |
| NCGC00023342-03 |
| 478-43-3 |
| rhein |
| rhein, technical grade |
| MLS000069639 , |
| smr000058210 |
| 1,8-dihydroxy-3-carboxyl anthraquinone |
| 4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid |
| NCGC00023342-04 |
| NCGC00018199-01 |
| 1,8-dihydroxy-3-carboxyl-9,10-anthraquinone |
| LMPK13040015 |
| CHEMBL418068 |
| chebi:8825 , |
| 4,5-dihydroxy-9,10-dioxoanthracene-2-carboxylic acid |
| AKOS005259272 |
| NCGC00018199-03 |
| NCGC00018199-06 |
| NCGC00018199-04 |
| NCGC00018199-07 |
| NCGC00018199-02 |
| NCGC00018199-05 |
| RHN , |
| ST057726 |
| 4-10-00-04088 (beilstein handbook reference) |
| ym64c2p6ux , |
| unii-ym64c2p6ux |
| 1,8-dihydroxy-3-carboxyanthraquinone |
| NCGC00258650-01 |
| tox21_201098 |
| cas-478-43-3 |
| dtxsid4026000 , |
| dtxcid606000 |
| A827360 |
| D3986 |
| BBL009695 |
| RHEIN - MONORHEIN |
| rheinic acid |
| STL141046 |
| RHEIN(MONORHEIN) , |
| FT-0645050 |
| 4IE7 |
| S2400 |
| AM807834 |
| SCHEMBL25253 |
| rhein [inci] |
| parietic acid |
| rhein [mi] |
| dihydroxy-3-carboxylanthraquinone, 1,8- |
| CS-5239 |
| HY-N0105 |
| MLS006011744 |
| bdbm32021 |
| 4,5-dihydroxy-9,10-diketo-anthracene-2-carboxylic acid |
| 4,5-dihydroxy-9,10-dioxo-2-anthracenecarboxylic acid |
| 4,5-bis(oxidanyl)-9,10-bis(oxidanylidene)anthracene-2-carboxylic acid |
| cid_10168 |
| us9238626, rhein |
| Q-100512 |
| 9,10-dihydro-4,5-dihydroxy-9,10-dioxo-2-anthroic acid |
| 4,5-dihydroxy-9,10-dioxo-9,10-dihydro-2-anthracenecarboxylic acid # |
| 2-anthraquinonecarboxylic acid, 4,5-dihydroxy- |
| mfcd00009618 |
| AC-7978 |
| rhein, analytical standard |
| 4,5-dihydroxy-9,10-dioxoanthracene-2-carboxylicacid |
| 9,10-dihydro-4,5-dihydroxy-9,10-dioxo-2-anthracenecarboxylic acid, 9ci |
| 4, 5-dihydroxyanthraquinone-2-carboxylic acid |
| DB13174 |
| 4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylicacid |
| rhein; rhubarb yellow |
| SY051290 |
| FT-0674401 |
| rhein,(s) |
| AS-11635 |
| BCP28202 |
| Q720356 |
| EN300-303248 |
| 4,5-dihydroxy-9,10-dioxo-9,10-dihydro-2-anthracenecarboxylic acid |
Rhein is an anthraquinone found in Rheum palmatum, used in Chinese medicine. Rhein (RH) is a monomer extracted from Chinese herbs that has been reported to show anti-tumor effects in a variety of tumors.
Rhein has a comprehensive pharmacological function in reducing inflammation and can play a neuroprotective role in many neurological diseases. Rhein lysinate has a good prospect to be an adjuvant chemotherapeutic drug.
Rhein has been shown to inhibit the growth and proliferation of human nasopharyngeal carcinoma (NPC) cells. Rhein lysinate has a good prospect to be an adjuvant chemotherapeutic drug.
Rhein can inhibit the hypertrophy of renal proximal tubular epithelial cells induced by high glucose and Angiotensin II in rats. Rhein could inhibit angiogenesis, which may play a role in antitumor and anti-inflammatory actions.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Rhein inhibited the increase of phenol red flux and the decrease of TEER, as well as recovered the expression and distribution of ZO-1 and weakened MLC phosphorylation, MLCK expression and NF-κB activation. " | ( Rhein protects against barrier disruption and inhibits inflammation in intestinal epithelial cells. Liu, P; Liu, Z; Zhong, J; Zhong, Y; Zhou, Q; Zhuang, S, 2019) | 3.4 |
| "Rhein can enhance the expression of ZO-1 and occludin, repair damaged tight junctions, and protect the intestinal barrier." | ( Effects of rhein on intestinal epithelial tight junction in IgA nephropathy. Chen, XW; Fu, AX; Peng, SN; Zeng, HH; Zhu, QX, 2013) | 2.22 |
| "Rhein could enhance cell viability and suppresse the release of MCP-1 and IL-8 in LPS-stimulated HK-2 cells Furthermore, rhein down regulated the expression of phosphorylated NF-κB p65, IκBα and IKKβ stimulated by LPS both in vivo and in vitro." | ( Rhein prevents endotoxin-induced acute kidney injury by inhibiting NF-κB activities. Fan, HY; Li, P; Qi, D; Sun, JF; Yu, C, 2015) | 2.58 |
| "Rhein plays its role by inducing cell cycle arrest via downregulation of oncogene c-Myc and apoptosis through the caspase-dependent pathway." | ( Rhein induces apoptosis and cell cycle arrest in human hepatocellular carcinoma BEL-7402 cells. Chen, G; Huang, Z; Shi, P, 2008) | 2.51 |
| "Rhein can inhibit the genetic transcription and the translation of AQP4 gene in LoVo cells, which demonstrates that the change of AQP4 expression regulated by rhein may be related to the cathartic effect of rhubarb." | ( [Regulative effects of aquaporin 4 expression by rhein in rhubarb to intestinal epithelial cell line LoVo]. Bao, JQ; Li, F; Li, JC; Shang, GW; Wang, CH; Wang, SC; Zhang, WS, 2008) | 2.04 |
| "Rhein can inhibit the hypertrophy of renal proximal tubular epithelial cells induced by high glucose and Angiotensin II in rats." | ( [Effects of Rhein on the hypertrophy of renal proximal tubular epithelial cells induced by high glucose and angiotensin II in rats]. Gao, Y; Liu, XH; Yu, DQ, 2010) | 2.18 |
| "Rhein could inhibit angiogenesis, which may play a role in antitumor and anti-inflammatory actions." | ( Anti-angiogenic effect and mechanism of rhein from Rhizoma Rhei. But, PP; Ge, W; He, MF; He, ZH; Lau, CB; Yue, GG; Zhou, R, 2011) | 2.08 |
| "Rhein is shown to inhibit 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cell transformation and activator protein-1 (AP-1) activation in a dose-dependent manner." | ( Rhein inhibits TPA-induced activator protein-1 activation and cell transformation by blocking the JNK-dependent pathway. Fujii, M; Hou, DX; Li, JJ; Lin, S, 2003) | 2.48 |
| "The rhein-evoked increase in Isc was reduced by serosal addition of 50 mumol/l bumetanide, 1 mumol/l tetrodotoxin, 1 mumol/l atropine and 10 mumol/l piroxicam but not 100 mumol/l hexamethonium, 1 mumol/l ICS 205 930 or 10 mumol/l cimetidine." | ( Rhein stimulates electrogenic chloride secretion by activation of submucosal neurons in guinea pig colon. Frieling, T; Rupprecht, C; Schemann, M, 1993) | 2.21 |
| "Rhein could inhibit 2-DG uptake of MCGT1(560 +/- 64) dpm.microgram prot-1 vs (741 +/- 60.5) dpm.microgram prot-1, (P < 0.05) in a dose-dependent manner, and reverse the cell hypertrophy of MCGT 1." | ( [Inhibition of glucose transporter 1 overexpression in mesangial cells by rhein]. Li, Y; Liu, Z; Zhu, J, 2001) | 1.26 |
| "Rhein can inhibit cell hypertrophy and ECM accumulation in LLC-PK1 cells induced by TGFbeta1, which may partly account for the role of rhein in preventing and retarding the progression of diabetic nephropathy." | ( Rhein inhibits renal tubular epithelial cell hypertrophy and extracellular matrix accumulation induced by transforming growth factor beta1. Dai, CS; Guo, XH; Li, H; Li, LS; Liu, D; Liu, ZH, 2001) | 3.2 |
Rhein treatment dose-dependently ameliorated neurological deficits, reduced infarct volume, and attenuated blood-brain barrier (BBB) disruption in the MCAO model. Rhein pretreatment markedly inhibited the levels of serum diamine oxidase (DAO), D-lactate (D-lac) and intestinal histological damage.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Rhein treatment dose-dependently ameliorated neurological deficits, reduced infarct volume, and attenuated blood-brain barrier (BBB) disruption in the MCAO model." | ( Rhein attenuates cerebral ischemia-reperfusion injury via inhibition of ferroptosis through NRF2/SLC7A11/GPX4 pathway. Hu, Y; Huang, SR; Liu, H; Sun, J; Zhang, TA; Zhang, WY, 2023) | 3.07 |
| "Rhein treatment did not alter the phosphorylated MAPKs activation including p-38, JNK and NF-κB, transcription unit whereas rhein significantly inhibited ERK1/2 activation in F98 glioma cells." | ( Rhein induces apoptosis and autophagy in human and rat glioma cells and mediates cell differentiation by ERK inhibition. Chang, J; Cheng, HL; Lu, HC; Rao, J; Shi, JX; Tang, N; Zhuang, Z, 2017) | 2.62 |
| "Rhein treatment in rats up-regulated nuclear factor erythroid 2-related factor 2 (Nrf2), B-cell lymphoma-2 (Bcl-2), heme oxygenase 1 (HO-1) and glutamate-cysteine ligase catalytic subunit (GCLC), and down-regulated Bcl-2 associated x (Bax) in mRNA and protein levels." | ( Hepatoprotective effect of rhein against methotrexate-induced liver toxicity. Bu, T; Huo, X; Liu, K; Liu, Z; Ma, X; Meng, Q; Sun, H; Sun, P; Wang, C; Zheng, S, 2018) | 1.5 |
| "Rhein pretreatment markedly inhibited the levels of serum diamine oxidase (DAO), D-lactate (D-lac) and intestinal histological damage, significantly recovered the levels of intestinal DAO, ZO-1 and occludin. " | ( Rhein ameliorates lipopolysaccharide-induced intestinal barrier injury via modulation of Nrf2 and MAPKs. Bian, Y; Chen, Q; Fan, Y; Liu, P; Liu, Z; Zhong, J; Zhuang, S, 2019) | 3.4 |
| "The Rhein-treated group was given rhein from week 7 until the rats were sacrificed." | ( Effects of rhein on intestinal epithelial tight junction in IgA nephropathy. Chen, XW; Fu, AX; Peng, SN; Zeng, HH; Zhu, QX, 2013) | 1.26 |
| "Rhein treatment significantly improved glucose tolerance, restored the first-phase insulin secretion and protected the islets function." | ( [Effect of rhein treatment on first-phase insulin secretory function in db/db mice]. Du, H; Gu, P; Liu, Z; Lu, B; Shao, J; Wang, J, 2010) | 2.19 |
| "Rhein treatment also reduced liver triglyceride levels, reversed hepatic steatosis, and normalized alanine aminotransferase (ALT) levels in these mice." | ( Rhein ameliorates fatty liver disease through negative energy balance, hepatic lipogenic regulation, and immunomodulation in diet-induced obese mice. Lu, M; Sheng, H; Sheng, X; Wang, M; Xi, B; Zang, YQ, 2011) | 2.53 |
| "Rhein treatment significantly improved glucose- dependent and independent insulin secretion by preservation of β cell mass and inhibition of β cell apoptosis in db/db mice. " | ( Improvement of glucose tolerance by rhein with restored early-phase insulin secretion in db/db mice. Du, H; Gu, P; Liu, Z; Lu, B; Shao, J; Ye, X, 2012) | 2.1 |
| "Rhein treatment decreased all these features of MCGT1 cells but did not exert a direct effect on GFAT enzymatic activity." | ( Rhein reverses the diabetic phenotype of mesangial cells over-expressing the glucose transporter (GLUT1) by inhibiting the hexosamine pathway. Li, LS; Liu, ZH; Zheng, JM; Zhu, JM, 2008) | 2.51 |
| "Treatment with rhein inhibited the survival and suppressed glycolysis in MiaPaCa-2 and PANC-1 cells exposed to hypoxia." | ( Inhibition of hypoxia-induced HIF-1α-mediated autophagy enhances the in vitro antitumor activity of rhein in pancreatic cancer cells. Wang, F; Yao, C, 2022) | 1.28 |
| "Treatment with rhein also partly blocked these responses." | ( Rhein alleviates renal interstitial fibrosis by inhibiting tubular cell apoptosis in rats. Chen, Y; Fu, S; Li, S; Mu, L; Xing, L, 2019) | 2.3 |
| "Treatment with rhein increased accumulation of DOX in SMMC-7721/DOX cells, inhibited mitochondrial energy metabolism, decreased cellular ATP, and ADP levels, and altered the ratio of ATP to ADP." | ( Rhein reverses doxorubicin resistance in SMMC-7721 liver cancer cells by inhibiting energy metabolism and inducing mitochondrial permeability transition pore opening. Cao, K; Chen, Z; Li, W; Liu, X; Ni, Z; Wang, S; Wu, L, 2019) | 2.3 |
| "Pretreatment with rhein for 7 days increased the total blood concentration of clozapine, but significantly reduced the unbound clozapine concentrations in the mPFC by approximately 3-fold." | ( The Drug-Drug Effects of Rhein on the Pharmacokinetics and Pharmacodynamics of Clozapine in Rat Brain Extracellular Fluid by In Vivo Microdialysis. Hou, ML; Lin, CH; Lin, LC; Tsai, TH, 2015) | 1.04 |
| "The treatment of rhein markedly reduced the ALT activity, HA and PC-III concentrations, and liver MDA level in CCl4/ethanol-injured rats (P<0.01). " | ( Rhein inhibits liver fibrosis induced by carbon tetrachloride in rats. Guo, MZ; Li, XS; Mei, ZC; Shen, W; Xu, HR; Ye, XF, 2002) | 2.1 |
The pharmacokinetic parameters of rhein in the DCQD group, including peak concentration (C(max), area under the plasma concentration-time curve (AUC), distribution phase half-life (t(1/2alpha) and elimination rate constant (K(10) were significantly different to those in theDCQD plus ranitidine group. The aim of the study was to develop rhein.
The drug-drug effects of rhein on extracellular neurotransmitter efflux in the rat medial prefrontal cortex (mPFC) produced by clozapine were assayed by high-performance liquid chromatography-electrochemical detection.
The low oral bioavailability of rhein has limited its utility as a potential treatment of osteoarthritis (OA), a chronic inflammatory disease. morphine caused nearly all radioactive compound to be retained in the colon. Rhein significantly facilitated the transfer of marker from colon through mucosal barrier to blood.
The aim of the study was to develop a physiologically based pharmacokinetic (PBPK) model of rhein to predict human pharmacokinetics before dosing. Rhein concentration time courses showed highest levels of 150-160 ng/ml.
| Class | Description |
|---|---|
| dihydroxyanthraquinone | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 25.2027 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 0.5012 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 79.4328 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 22.3342 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 12.5893 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 12.5893 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 56.2341 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 21.1546 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 64.5271 | 0.1259 | 19.1169 | 125.8920 | AID2549; AID2708 |
| interleukin 8 | Homo sapiens (human) | Potency | 74.9780 | 0.0473 | 49.4806 | 74.9780 | AID651758 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 12.5893 | 0.0126 | 10.6917 | 88.5700 | AID887 |
| WRN | Homo sapiens (human) | Potency | 26.6795 | 0.1683 | 31.2583 | 100.0000 | AID651768 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 56.2341 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 35.6943 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 16.9168 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 39.8107 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
| GLS protein | Homo sapiens (human) | Potency | 22.3872 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 16.9168 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
| TDP1 protein | Homo sapiens (human) | Potency | 23.7246 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 28.1133 | 0.0007 | 14.5928 | 83.7951 | AID1259369 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 21.0880 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
| AR protein | Homo sapiens (human) | Potency | 6.7698 | 0.0002 | 21.2231 | 8,912.5098 | AID743036; AID743053 |
| Smad3 | Homo sapiens (human) | Potency | 15.8489 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 28.1838 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 33.9972 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 12.5893 | 0.0013 | 7.7625 | 44.6684 | AID914; AID915 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 15.8489 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 100.0000 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 34.0429 | 0.0013 | 10.1577 | 42.8575 | AID1259255 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 50.1187 | 0.0002 | 14.3764 | 60.0339 | AID588533 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 11.2875 | 0.0008 | 17.5051 | 59.3239 | AID1159527 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 42.6929 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1259401 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 19.7020 | 0.3758 | 27.4851 | 61.6524 | AID588526; AID588527 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 28.1133 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 14.8117 | 0.0002 | 29.3054 | 16,493.5996 | AID588514; AID743069; AID743075; AID743079 |
| 67.9K protein | Vaccinia virus | Potency | 15.1861 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 50.1187 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 14.1406 | 0.0010 | 24.5048 | 61.6448 | AID588534; AID588535 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 27.3102 | 0.0010 | 19.4141 | 70.9645 | AID588536; AID743094; AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 18.8918 | 0.0237 | 23.2282 | 63.5986 | AID588541; AID743222 |
| IDH1 | Homo sapiens (human) | Potency | 25.9290 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 39.8107 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 20.0724 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 14.0882 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 58.3665 | 0.0391 | 47.5451 | 146.8240 | AID1224845 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 0.5406 | 17.6392 | 96.1227 | AID2528 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 15.8489 | 1.0000 | 12.2326 | 31.6228 | AID1452 |
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 0.0018 | 15.6638 | 39.8107 | AID894 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 28.1838 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 28.1838 | 0.0100 | 39.5371 | 1,122.0200 | AID1479 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 14.1254 | 0.7943 | 21.2757 | 50.1187 | AID624246 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 14.0900 | 0.0376 | 17.0823 | 61.1927 | AID1259364; AID1259388 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 11.2202 | 0.0224 | 21.0102 | 89.1251 | AID485314 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 27.1874 | 0.1337 | 25.4129 | 89.1251 | AID588795; AID720498 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 21.1923 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 24.2125 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID743202; AID743219 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 15.8489 | 0.4256 | 12.0591 | 28.1838 | AID504891 |
| tumor susceptibility gene 101 protein | Homo sapiens (human) | Potency | 43.3533 | 0.1298 | 10.8331 | 32.6090 | AID493005; AID651600 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 62.9025 | 0.1000 | 28.9256 | 213.3130 | AID588591; AID720502 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 53.4132 | 0.0501 | 27.0736 | 89.1251 | AID588590; AID720496 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 12.5893 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 12.5893 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 12.5893 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 31.8326 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
| geminin | Homo sapiens (human) | Potency | 29.0929 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 32.7855 | 0.0316 | 22.3146 | 100.0000 | AID588579; AID720501 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 2.8184 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 10.0000 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 2.5119 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
| caspase-1 isoform alpha precursor | Homo sapiens (human) | Potency | 35.7168 | 0.0003 | 11.4484 | 31.6228 | AID896; AID900 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 12.5893 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 25.1189 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 19.9027 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Caspase-1 | Homo sapiens (human) | Potency | 22.0289 | 1.1220 | 9.5843 | 25.1189 | AID888; AID929; AID996 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 25.1189 | 0.0063 | 8.2350 | 39.8107 | AID881 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 37.5780 | 0.0266 | 22.4482 | 66.8242 | AID651802 |
| Caspase-7 | Homo sapiens (human) | Potency | 25.1189 | 3.9811 | 18.5856 | 31.6228 | AID889 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Type 1 InsP3 receptor isoform S2 | Sus scrofa (pig) | Potency | 15.8489 | 2.5119 | 13.8154 | 25.1189 | AID929 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 90-kda heat shock protein beta HSP90 beta, partial | Homo sapiens (human) | IC50 (µMol) | 3.3393 | 0.1736 | 9.8032 | 29.2701 | AID712 |
| plectin 1 | Homo sapiens (human) | IC50 (µMol) | 129.3066 | 1.5180 | 6.4106 | 15.6610 | AID1817; AID2127; AID2141 |
| heat shock protein HSP 90-alpha isoform 2 | Homo sapiens (human) | IC50 (µMol) | 3.3393 | 0.1736 | 9.8032 | 29.2701 | AID712 |
| tyrosine-protein phosphatase non-receptor type 7 isoform 2 | Homo sapiens (human) | IC50 (µMol) | 19.6200 | 0.1000 | 12.7265 | 63.0000 | AID521 |
| Thioredoxin reductase 1, cytoplasmic | Rattus norvegicus (Norway rat) | IC50 (µMol) | 84.0000 | 0.2720 | 1.8260 | 6.0000 | AID551520 |
| Transthyretin | Homo sapiens (human) | IC50 (µMol) | 12.0000 | 0.1600 | 4.2921 | 10.0000 | AID1755162 |
| Cholinesterase | Homo sapiens (human) | IC50 (µMol) | 17.0000 | 0.0000 | 1.5599 | 10.0000 | AID1128623 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.9332 | 10.0000 | AID1128622 |
| Tissue alpha-L-fucosidase | Bos taurus (cattle) | IC50 (µMol) | 32.0000 | 0.0050 | 0.0575 | 0.1100 | AID1688689 |
| Sialidase-2 | Homo sapiens (human) | IC50 (µMol) | 130.0000 | 3.9000 | 6.7333 | 7.8000 | AID466938 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| POsterior Segregation | Caenorhabditis elegans | EC50 (µMol) | 29.1760 | 2.2010 | 47.1808 | 186.6810 | AID1964 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | EC50 (µMol) | 21.5690 | 0.0820 | 31.0243 | 168.9080 | AID1960 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 9.6000 | 0.0070 | 1.5179 | 10.4870 | AID1801002 |
| Zinc finger protein mex-5 | Caenorhabditis elegans | EC50 (µMol) | 21.5690 | 0.0820 | 33.5679 | 168.9080 | AID1960 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| NAD-dependent protein deacylase sirtuin-5, mitochondrial | Homo sapiens (human) | AC50 | 30.0000 | 4.1900 | 12.0150 | 18.1100 | AID720591 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC 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 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID720501 | qHTS for Inhibitors of Polymerase Kappa: Confirmatory Assay for Cherry-picked Compounds | 2012 | PloS one, , Volume: 7, Issue:10 | A comprehensive strategy to discover inhibitors of the translesion synthesis DNA polymerase κ. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID260055 | Antifungal activity against Phytopthora infestans at 0.5 mg/ml | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. |
| AID1098599 | Larvicidal activity against Spodoptera litura fed on compound-treated castor leaf assessed as mortality at 250 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1128622 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID466939 | Selectivity for Trypanosoma cruzi trans-sialidase mutant over human Neu2 | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4 | Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase. |
| AID675631 | Tmax in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1238296 | Inhibition of scavenger receptor A (unknown origin) in mouse B3Z cells assessed as anti-CD3/CD28 antibody-induced T cell activation by measuring transcription of il2 gene after 5 hrs by beta-galactosidase assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID675634 | MRT (0 to 9 hrs) in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1128627 | Inhibition of human recombinant AChE-mediated amyloid beta-40 aggregation assessed as amyloid fibril formation at 100 uM after 24 hrs by thioflavin T fluorescence method | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID1064220 | Cytotoxicity against human HCT116 cells | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID1330880 | Inhibition of RANKL/M-CSF-induced osteoclastogenesis in C57/BL6 mouse primary BMDM assessed as reduction in TRAP activity using pNPP as substrate after 2 days by colorimetric assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and biological evaluation of rhein amides as inhibitors of osteoclast differentiation and bone resorption. |
| AID755275 | Antidiabetic nephropathic activity in rat HBZY-1 cells assessed as inhibition of high concentration glucose-induced IL-6 production at 35 uM treated 1 hr before glucose challenge measured after 24 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Anthraquinone derivatives from Rumex plants and endophytic Aspergillus fumigatus and their effects on diabetic nephropathy. |
| AID1855718 | Acute toxicity in female ICR mouse assessed as changes in ALT level in liver at 25 mg/kg | |||
| AID1509318 | Induction of paraptosis in human SMMC7721 cells assessed as increase in GRP78 expression by Western blot analysis | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Novel Anthraquinone Compounds Induce Cancer Cell Death through Paraptosis. |
| AID1128629 | Permeability of the compound by PAMPA assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID1238294 | Inhibition of scavenger receptor A in wild type C57BL/6 mouse BMDC assessed as OVA257-264 peptide-induced T cell activation by measuring IL2 production at 30 uM after 56 hrs by ELISA | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID1064222 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID1128635 | Inhibition of aggregation of amyloid beta-42 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as amyloid fibril formation at 10 uM after 24 hrs by thioflavin S fluorescence method | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID551520 | Inhibition of rat liver cytosolic TrxR1 by spectrophotometry | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Hypericins and thioredoxin reductase: Biochemical and docking studies disclose the molecular basis for effective inhibition by naphthodianthrones. |
| AID52630 | Inhibitory activity against Chymotrypsinogen at 86 uM concentration | 1992 | Journal of medicinal chemistry, May-01, Volume: 35, Issue:9 | Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G. |
| AID736936 | Inhibition of AChE in rat cortex using acetylthiocholine iodide as substrate at 100 ug/ml preincubated with enzyme for 10 mins prior to substrate addition by Ellman's colorimetric method | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | Synthesis, biological evaluation and molecular modeling of aloe-emodin derivatives as new acetylcholinesterase inhibitors. |
| AID1855714 | Acute toxicity in female ICR mouse assessed as pathological changes in intestine at 25 mg/kg measured by H and E staining method | |||
| AID285172 | Effect on Streptococcus mutans LMG 14558 assessed as inhibition of biofilm formation in modified Robbin's device at 5 ug/ml relative to BHIS control | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | In vitro inhibition of Streptococcus mutans biofilm formation on hydroxyapatite by subinhibitory concentrations of anthraquinones. |
| AID1098610 | Antifeedant activity against pre-starved fourth-instar larva of Helicoverpa armigera fed on compound-treated cotton leaf assessed as antifeedant index at 1000 ppm after 24 hr by leaf disk no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID363329 | Cytotoxicity against MDR1 Pgp overexpressing human HepG2 cells after 24 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Comparison of the cytotoxic activities of naturally occurring hydroxyanthraquinones and hydroxynaphthoquinones. |
| AID1855690 | Selectivity index, ratio IC50 for antiproliferative activity against human WI-38 cells over IC50 for antiproliferative activity against human A549 cells | |||
| AID102410 | Compound was tested for enhancement of proliferation of MCF-7 cell line at a concentration 10 uM | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14 | Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity. |
| AID675639 | Half life in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID260053 | Antifungal activity against Fusarium oxysporum at 0.5 mg/ml | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. |
| AID1098607 | Antifeedant activity against pre-starved fourth-instar larva of Spodoptera litura fed on compound-treated castor leaf assessed as antifeedant index at 500 ppm after 24 hr by leaf disc no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1688687 | Inhibition of Saccharomyces cerevisiae alpha-glucosidase using PNPG as substrate incubated for 10 mins by spectrophotometric method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes. |
| AID1098596 | Larvicidal activity against Spodoptera litura fed on compound-treated castor leaf assessed as mortality after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1098609 | Antifeedant activity against pre-starved fourth instar larva of Spodoptera litura fed on compound-treated castor leaf assessed as antifeedant index at 125 ppm after 24 hr by leaf disc no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID260051 | Antiproliferative activity against human epidermal carcinoma A431 cell line at 20 uM by MTT method | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. |
| AID1098604 | Larvicidal activity against Helicoverpa armigera fed on compound-treated cotton leaf assessed as mortality at 250 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1064210 | Binding affinity to calf thymus DNA assessed as change in melting temperature by FRET assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID675648 | AUC (0 to infinity) in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1064219 | Cytotoxicity against human CNE cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID1876801 | Cytotoxicity against human NOMO-1 cells assessed as reduction in cell viability incubated for 72 hrs by alamarblue assay | |||
| AID675638 | Tmax in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1330889 | Induction of C57/BL6 mouse primary BMDM proliferation assessed at 5 uM after 2 days by MTT assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and biological evaluation of rhein amides as inhibitors of osteoclast differentiation and bone resorption. |
| AID1855713 | Acute toxicity in female ICR mouse assessed as pathological changes in kidney at 25 mg/kg measured by H and E staining method | |||
| AID719444 | n-Octanol-phosphate buffer partition coefficient, log P of the compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and pharmacokinetic profile of rhein- boswellic acid conjugate. |
| AID1336378 | Antagonist activity at SRA in RM1-OVA tumor bearing wild type C57BL/6 mouse derived CD11bpositiveLy6ChighLy6Gnegative myeloid-derived suppressive cells co-cultured with splenocytes assessed as reduction in protein-mediated inhibition of anti CD3/CD28 anti | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1 | Design, synthesis, and characterization of rhein analogs as novel inhibitors of scavenger receptor A. |
| AID338266 | Inhibition of Ca2+ ATPase activity in human red blood cells at 1600 uM by spectrophotometry | 1994 | Journal of natural products, Dec, Volume: 57, Issue:12 | Novel Ca(2+)-ATPase inhibitors from the dried root tubers of Polygonum Multiflorum. |
| AID1855720 | Acute toxicity in female ICR mouse assessed as changes in creatine kinase (CK) level in heart at 25 mg/kg | |||
| AID1855689 | Antiproliferative activity against human WI-38 cells measured after 48 hrs by MTT assay | |||
| AID285171 | Activity against planktonic Streptococcus mutans LMG 14558 | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | In vitro inhibition of Streptococcus mutans biofilm formation on hydroxyapatite by subinhibitory concentrations of anthraquinones. |
| AID1688684 | Inhibition of Saccharomyces cerevisiae alpha-glucosidase using maltose as substrate preincubated for 5 mins followed by substrate addition and measured after 15 mins by LC-TQ-MS/MS analysis | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes. |
| AID335924 | Antiplatelet activity in rat platelet rich plasma assessed as drug level causing inhibition of collagen-stimulated platelet aggregation pretreated 2 mins before collagen challenge | |||
| AID1098608 | Antifeedant activity against pre-starved fourth-instar larva of Spodoptera litura fed on compound-treated castor leaf assessed as antifeedant index at 250 ppm after 24 hr by leaf disc no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1509319 | Induction of paraptosis in human SMMC7721 cells assessed as increase in LC3-II/LC3-I expression ratio by Western blot analysis | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Novel Anthraquinone Compounds Induce Cancer Cell Death through Paraptosis. |
| AID1098597 | Larvicidal activity against Spodoptera litura fed on compound-treated castor leaf assessed as mortality at 1000 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1238292 | Inhibition of scavenger receptor A in wild type C57BL/6 mouse BMDC assessed as gp100 (25 to 33) peptide-induced T cell activation by measuring IL2 production at 20 uM after 56 hrs by ELISA | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID1238295 | Inhibition of OVA257-264 peptide-induced T cell activation in SRA-deficient C57BL/6 mouse BMDC assessed as IL2 production at 10 to 30 uM after 56 hrs by ELISA | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID1185253 | Antitumor activity against human HeLa cells after 3 days by SRB assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Natural product-based design, synthesis and biological evaluation of anthra[2,1-d]thiazole-6,11-dione derivatives from rhein as novel antitumour agents. |
| AID1072539 | Inhibition of bovine xanthine oxidase using xanthine as substrate measured for 6 mins at 50 uM at 25 degC by spectrophotometry | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis and molecular modeling of aloe-emodin derivatives as potent xanthine oxidase inhibitors. |
| AID1098603 | Larvicidal activity against Helicoverpa armigera fed on compound-treated cotton leaf assessed as mortality at 500 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1128628 | Inhibition of amyloid beta-42 (unknown origin) aggregation assessed as amyloid fibril formation at 10 uM after 24 hrs by thioflavin T fluorescence method | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID675647 | Binding affinity to bone mineral hydroxyapatite after 30 mins by RP-HPLC analysis | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1353613 | Anti-inflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, ig administered once daily for 7 days relative to control | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Recent progress in the structural modification and pharmacological activities of ligustrazine derivatives. |
| AID1330879 | Cytotoxicity against C57/BL6 mouse primary BMDM assessed as cell viability at 5 uM after 2 days in presence of M-CSF by MTT assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and biological evaluation of rhein amides as inhibitors of osteoclast differentiation and bone resorption. |
| AID1238298 | Inhibition of scavenger receptor A in mouse DC1.2 cells assessed as decrease in poly(I:C)-induced activation of STAT1 pretreated for 2 hrs before poly(I:C) stimulation measured after 3 hrs by immunoblotting | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID1098602 | Larvicidal activity against Helicoverpa armigera fed on compound-treated cotton leaf assessed as mortality at 1000 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1083211 | Bactericidal activity against Erwinia amylovora 295/93 assessed as growth inhibition in King's B full medium measured at pH 7.2 after overnight incubation by suspension culture assay | 2012 | Journal of agricultural and food chemistry, Dec-12, Volume: 60, Issue:49 | Potent and specific bactericidal effect of juglone (5-hydroxy-1,4-naphthoquinone) on the fire blight pathogen Erwinia amylovora. |
| AID1238293 | Inhibition of scavenger receptor A in wild type C57BL/6 mouse BMDC assessed as OVA257-264 peptide-induced T cell activation by measuring IL2 production at 10 uM after 56 hrs by ELISA | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID1688689 | Inhibition of bovine kidney alpha-fucosidase using PNPG as substrate incubated for 10 mins by spectrophotometric method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes. |
| AID335922 | Antiplatelet activity in rat platelet rich plasma assessed as drug level causing inhibition of arachidonic acid-stimulated platelet aggregation pretreated 2 mins before arachidonic acid challenge | |||
| AID260049 | Inhibitory activity on PDGF-induced ERK phosphorylation in NIH3T3 cells at 20 uM | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. |
| AID67656 | Inhibitory activity against Porcine Pancreatic Elastase (PPE) at 86 uM concentration; NI = no inhibition | 1992 | Journal of medicinal chemistry, May-01, Volume: 35, Issue:9 | Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G. |
| AID551521 | Inhibition of rat liver mitochondrial TrxR2 by spectrophotometry | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Hypericins and thioredoxin reductase: Biochemical and docking studies disclose the molecular basis for effective inhibition by naphthodianthrones. |
| AID1855719 | Acute toxicity in female ICR mouse assessed as changes in AST level in liver at 25 mg/kg | |||
| AID1509320 | Decrease in p62 expression level in human SMMC7721 cells by Western blot analysis | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Novel Anthraquinone Compounds Induce Cancer Cell Death through Paraptosis. |
| AID1855709 | Acute toxicity in female ICR mouse assessed as pathological changes in heart at 25 mg/kg measured by H and E staining method | |||
| AID1185252 | Antitumor activity against human A549 cells after 3 days by SRB assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Natural product-based design, synthesis and biological evaluation of anthra[2,1-d]thiazole-6,11-dione derivatives from rhein as novel antitumour agents. |
| AID1855712 | Acute toxicity in female ICR mouse assessed as pathological changes in lung at 25 mg/kg measured by H and E staining method | |||
| AID1855710 | Acute toxicity in female ICR mouse assessed as pathological changes in liver at 25 mg/kg measured by H and E staining method | |||
| AID1330882 | Inhibition of RANKL/M-CSF-induced osteoclastogenesis in C57/BL6 mouse primary BMDM assessed reduction in TRAP-positive multinucleated cells at 5 uM after 5 days | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and biological evaluation of rhein amides as inhibitors of osteoclast differentiation and bone resorption. |
| AID675636 | AUC (0 to 9 hrs) in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID675637 | Cmax in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1855688 | Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay | |||
| AID1098613 | Antifeedant activity against pre-starved fourth-instar larva of Helicoverpa armigera fed on compound-treated cotton leaf assessed as antifeedant index at 125 ppm after 24 hr by leaf disk no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1688692 | Inhibition of jack bean alpha-mannosidase at 1 mM using PNPG as substrate incubated for 10 mins by spectrophotometric method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes. |
| AID102411 | Compound was tested for enhancement of proliferation of MCF-7 cell line at a concentration 3 uM | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14 | Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity. |
| AID1064218 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID1098601 | Larvicidal activity against Helicoverpa armigera fed on compound-treated cotton leaf assessed as mortality after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID675649 | MRT (0 to 9 hrs) in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID67324 | Inhibitory activity against Human Leukocyte Elastase (HLE) at 86 uM concentration; NI = no inhibition | 1992 | Journal of medicinal chemistry, May-01, Volume: 35, Issue:9 | Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G. |
| AID675633 | Half life in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID675630 | Cmax in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1128624 | Inhibition of human recombinant BACE1 using methoxycoumarin-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys-dinitrophenyl as substrate preincubated for 1 hr by FRET assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID1128623 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID260054 | Antifungal activity against Gibberella zeae at 0.5 mg/ml | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. |
| AID466937 | Inhibition of Trypanosoma cruzi trans-sialidase containing catalytic domain (N58F, R200K) and lectin-like domain (S495 K, V496G, E520K, D593G, I597D, H599R) mutation expressed in Escherichia coli JM109 assessed as MuNANA substrate hydrolysis in presence o | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4 | Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase. |
| AID335923 | Antiplatelet activity in rat platelet rich plasma assessed as drug level causing inhibition of ADP-stimulated platelet aggregation pretreated 2 mins before ADP challenge | |||
| AID675629 | AUC (0 to 9 hrs) in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1098611 | Antifeedant activity against pre-starved fourth-instar larva of Helicoverpa armigera fed on compound-treated cotton leaf assessed as antifeedant index at 500 ppm after 24 hr by leaf disk no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID48378 | Inhibitory activity against Cathepsin G (CatG) at 86 uM concentration | 1992 | Journal of medicinal chemistry, May-01, Volume: 35, Issue:9 | Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G. |
| AID363328 | Cytotoxicity against MDR1 Pgp under-expressing human HCT116 cells after 24 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Comparison of the cytotoxic activities of naturally occurring hydroxyanthraquinones and hydroxynaphthoquinones. |
| AID1098612 | Antifeedant activity against pre-starved fourth-instar larva of Helicoverpa armigera fed on compound-treated cotton leaf assessed as antifeedant index at 250 ppm after 24 hr by leaf disk no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID755274 | Antidiabetic nephropathic activity in rat HBZY-1 cells assessed as inhibition of high concentration glucose-induced IL-6 production at 88 uM treated 1 hr before glucose challenge measured after 24 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Anthraquinone derivatives from Rumex plants and endophytic Aspergillus fumigatus and their effects on diabetic nephropathy. |
| AID1098598 | Larvicidal activity against Spodoptera litura fed on compound-treated castor leaf assessed as mortality at 500 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1064216 | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID1098605 | Larvicidal activity against Helicoverpa armigera fed on compound-treated cotton leaf assessed as mortality at 125 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID19840 | Partition coefficient of compound in octanol and water by Fragmental method of Leo/Hansch | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4 | Determination of active components in rhubarb and study of their hydrophobicity by micellar electrokinetic chromatography. |
| AID1064217 | Cytotoxicity against human SPCA2 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID675632 | MRT (0 to infinity) in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1128636 | Inhibition of aggregation of tau protein (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as amyloid fibril formation at 10 uM after 24 hrs by thioflavin S fluorescence method | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents. |
| AID675635 | AUC (0 to infinity) in Sprague-Dawley rat assessed as rhein at 10 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1755162 | Inhibition of acid-mediated aggregation of TTR V30M mutant (unknown origin) expressed in Escherichia coli pretreated for 30 mins at pH 7 followed by protein dilution in acetate buffer and further incubated for 96 hrs at pH 4.6 by thioflavin-T fluorescence | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
| AID1098606 | Antifeedant activity against pre-starved fourth-instar larva of Spodoptera litura fed on compound-treated castor leaf assessed as antifeedant index at 1000 ppm after 24 hr by leaf disc no choice method | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID102409 | Compound was tested for enhancement of proliferation of MCF-7 cell line at a concentration 1 uM | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14 | Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity. |
| AID466938 | Inhibition of human Neu2 assessed as MuNANA substrate hydrolysis in presence of 0.1% Triton X-100 by discontinuous fluorimetric assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4 | Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase. |
| AID1098600 | Larvicidal activity against Spodoptera litura fed on compound-treated castor leaf assessed as mortality at 125 ppm after 96 hr relative to control | 2011 | Saudi journal of biological sciences, Apr, Volume: 18, Issue:2 | Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L. |
| AID1064221 | Cytotoxicity against human COLO320DM cells | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID1064215 | Cytotoxicity against human HUVEC after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and antitumor activities of novel rhein α-aminophosphonates conjugates. |
| AID260052 | Antiproliferative activity against prostate cancer PC3 cell line at 20 uM by MTT method | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. |
| AID1855711 | Acute toxicity in female ICR mouse assessed as pathological changes in spleen at 25 mg/kg measured by H and E staining method | |||
| AID675646 | Prodrug conversion at pH 1.2 assessed as hydrolysis up to 24 hrs by HPLC analysis | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1238297 | Inhibition of scavenger receptor A in mouse DC1.2 cells assessed as decrease in poly(I:C)-induced activation of IRF3 pretreated for 2 hrs before poly(I:C) stimulation measured after 3 hrs by immunoblotting | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Small molecule inhibits activity of scavenger receptor A: Lead identification and preliminary studies. |
| AID675650 | MRT (0 to infinity) in Sprague-Dawley rat at 5.26 mg/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies. |
| AID1801002 | Protein Kinase Assay from Article 10.1002/cbic.201402579: \\Tampering with cell division by using small-molecule inhibitors of CDK-CKS protein interactions.\\ | 2015 | Chembiochem : a European journal of chemical biology, Feb-09, Volume: 16, Issue:3 | Tampering with cell division by using small-molecule inhibitors of CDK-CKS protein interactions. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Structural basis for inhibition of the fat mass and obesity associated protein (FTO). |
| AID652178 | Confirmed Agonists of Novel Allosteric Modulators of the M1 Muscarinic Receptor | 2013 | Molecules (Basel, Switzerland), Jan-08, Volume: 18, Issue:1 | Benchmarking ligand-based virtual High-Throughput Screening with the PubChem database. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 48 (8.12) | 18.7374 |
| 1990's | 47 (7.95) | 18.2507 |
| 2000's | 110 (18.61) | 29.6817 |
| 2010's | 242 (40.95) | 24.3611 |
| 2020's | 144 (24.37) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (86.31) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 7 (1.13%) | 5.53% |
| Reviews | 16 (2.58%) | 6.00% |
| Case Studies | 1 (0.16%) | 4.05% |
| Observational | 1 (0.16%) | 0.25% |
| Other | 595 (95.97%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||