General Information of Drug (ID: DMPF2N1)

Drug Name
paxilline Drug Info
Synonyms
4b-Hydroxy-2-(1-hydroxy-1-methylethyl)-12b,12c-dimethyl-5,6,6a,7,12,12b,12c,13,14,14a-decahydro-2H-chromeno[5',6':6,7]indeno[1,2-b]indol-3(4bH)-one; paxillin; AC1L1IR1; GTPL2309; BDBM86263; CTK7H1286; ACNHBCIZLNNLRS-UHFFFAOYSA-N; NCGC00168476-01; CAS_57186-25-1; hydroxy-(1-hydroxy-1-methyl-ethyl)-dimethyl-[ ]one; 4b-Hydroxy-2-(1-hydroxy-1-methylethyl)-12b,12c-dimethyl-5,6,6a,7,12,12b,12c,13,14,14a-decahydro-2H-chromeno[5',6':6,7]indeno[1,2-b]indol-3(4bh)-one #
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
105008
ChEBI ID
CHEBI:34907
CAS Number
CAS 57186-25-1
TTD Drug ID
DMPF2N1

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Patented Agent(s)
Investigative Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
US9073931, E2 DMK9FJG N. A. N. A. Patented [5]
BDBM50177019 DMEL28G N. A. N. A. Patented [6]
US9006244, E2b DMP0TBO N. A. N. A. Patented [7]
US9073931, E1 DM2Z43I N. A. N. A. Patented [5]
US9006244, E1 DMBF1C0 N. A. N. A. Patented [7]
BDBM50177012 DM52IQF N. A. N. A. Patented [6]
US9006244, E2a DMPDF9B N. A. N. A. Patented [7]
67S DMJL1MB N. A. N. A. Patented [6]
US9073931, E3 DMCYM8P N. A. N. A. Patented [5]
desmosterol DMV8SUM Discovery agent N.A. Investigative [8]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BMS-223131 DMJUV6C Erectile dysfunction HA01.1 Phase 2 [9]
NS-1619 DMES0OT Asthma CA23 Terminated [10]
CNS-1237 DMP3QAZ Cerebrovascular ischaemia 8B1Z Terminated [11]
[14C]TEA DM6SFYH Discovery agent N.A. Investigative [12]
iberiotoxin DMRIG3O Discovery agent N.A. Investigative [12]
slotoxin DMBD6TC Discovery agent N.A. Investigative [13]
⏷ Show the Full List of 6 Drug(s)
Drug(s) Affected By Stearoyl-CoA desaturase (SCD)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Clavulanate DM2FGRT Bacteremia 1A73 Approved [14]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [15]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
Quercetin DM3NC4M Obesity 5B81 Approved [17]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [18]
Fluoxetine DM3PD2C Bipolar depression Approved [15]
Fructose DM43AN2 Vomiting MD90 Approved [19]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [20]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [21]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [22]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [23]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [24]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [14]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [25]
Quercetin DM3NC4M Obesity 5B81 Approved [17]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [26]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [27]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [28]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [29]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [30]
Panobinostat DM58WKG Chronic graft versus host disease Approved [31]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [32]
Leflunomide DMR8ONJ Arthritis FA20 Approved [33]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [34]
Clorgyline DMCEUJD Parkinson disease 8A00.0 Approved [35]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [36]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [37]
Teniposide DMLW57T Acute lymphoblastic leukaemia 2A85 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Fatty acid synthase (FASN)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [39]
Selenium DM25CGV N. A. N. A. Approved [40]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [41]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [42]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [43]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [26]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [45]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [46]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [47]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Calcipotriol DM03CP7 Psoriasis EA90 Approved [48]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [49]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [50]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [14]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [49]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [51]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [52]
Quercetin DM3NC4M Obesity 5B81 Approved [17]
Fluoxetine DM3PD2C Bipolar depression Approved [49]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [53]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [36]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [54]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [55]
Decitabine DMQL8XJ Acute myelogenous leukaemia 2A41 Approved [56]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [57]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [58]
Triclosan DMZUR4N Malaria 1F40-1F45 Approved [59]
Urethane DM7NSI0 N. A. N. A. Phase 4 [60]
SNDX-275 DMH7W9X Breast cancer 2C60-2C65 Phase 3 [31]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Charybdotoxin receptor beta-4 (BKbeta4) TT1AQ50 KCMB4_HUMAN Blocker (channel blocker) [2]
Oxysterols receptor LXR-alpha (NR1H3) TTECBXN NR1H3_HUMAN Agonist [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Carbohydrate-responsive element-binding protein (MLXIPL) OTR9MLLW MLXPL_HUMAN Gene/Protein Processing [4]
Fatty acid synthase (FASN) OTFII9KG FAS_HUMAN Gene/Protein Processing [4]
Nuclear receptor subfamily 0 group B member 2 (NR0B2) OT7UVICX NR0B2_HUMAN Gene/Protein Processing [4]
Nuclear receptor-interacting protein 1 (NRIP1) OTIZOJQV NRIP1_HUMAN Gene/Protein Processing [4]
Stearoyl-CoA desaturase (SCD) OTB1073G SCD_HUMAN Gene/Protein Processing [4]
Sterol regulatory element-binding protein 1 (SREBF1) OTWBRPAI SRBP1_HUMAN Gene/Protein Processing [4]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2309).
2 Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology. 1996;35(7):963-8.
3 A natural product ligand of the oxysterol receptor, liver X receptor. J Pharmacol Exp Ther. 2003 Oct;307(1):291-6.
4 Combinations of LXR and RXR agonists induce triglyceride accumulation in human HepaRG cells in a synergistic manner. Arch Toxicol. 2020 Apr;94(4):1303-1320. doi: 10.1007/s00204-020-02685-7. Epub 2020 Mar 2.
5 Liver X receptor modulators. US9073931.
6 Piperazine derivatives as liver X receptor modulators. US10144715.
7 Liver X receptor modulators. US9006244.
8 Sterol intermediates from cholesterol biosynthetic pathway as liver X receptor ligands. J Biol Chem. 2006 Sep 22;281(38):27816-26.
9 Effect of 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), a novel opener of large conductance ... J Pharmacol Exp Ther. 2005 May;313(2):840-7.
10 BK channel activation by NS-1619 is partially mediated by intracellular Ca2+ release in smooth muscle cells of porcine coronary artery
11 Effects of Ca2+ and Na+ channel inhibitors in vitro and in global cerebral ischaemia in vivo. Eur J Pharmacol. 1997 Aug 6;332(2):121-31.
12 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 380).
13 Slotoxin, alphaKTx1.11, a new scorpion peptide blocker of MaxiK channels that differentiates between alpha and alpha+beta (beta1 or beta4) complexes. FEBS Lett. 2001 Sep 21;505(3):369-73.
14 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
15 Antidepressant drugs activate SREBP and up-regulate cholesterol and fatty acid biosynthesis in human glial cells. Neurosci Lett. 2006 Mar 13;395(3):185-90. doi: 10.1016/j.neulet.2005.10.096. Epub 2005 Dec 1.
16 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
17 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
18 Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
19 Effects of four-week high-fructose diet on gene expression in skeletal muscle of healthy men. Diabetes Metab. 2008 Feb;34(1):82-5. doi: 10.1016/j.diabet.2007.08.004. Epub 2007 Dec 11.
20 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
21 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
22 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
23 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
24 Poly(ADP-Ribose) Polymerase Inhibitor PJ34 Attenuated Hepatic Triglyceride Accumulation in Alcoholic Fatty Liver Disease in Mice. J Pharmacol Exp Ther. 2018 Mar;364(3):452-461. doi: 10.1124/jpet.117.243105. Epub 2018 Jan 9.
25 Delta5 desaturase mRNA levels are increased by simvastatin via SREBP-1 at early stages, not via PPARalpha, in THP-1 cells. Eur J Pharmacol. 2007 Oct 1;571(2-3):97-105.
26 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
27 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
28 Inhibition of liver x receptor/retinoid X receptor-mediated transcription contributes to the proatherogenic effects of arsenic in macrophages in vitro. Arterioscler Thromb Vasc Biol. 2010 Jun;30(6):1228-36. doi: 10.1161/ATVBAHA.110.205500. Epub 2010 Mar 25.
29 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
30 Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.
31 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
32 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
33 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
34 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
35 Anti-oncogenic and pro-differentiation effects of clorgyline, a monoamine oxidase A inhibitor, on high grade prostate cancer cells. BMC Med Genomics. 2009 Aug 20;2:55. doi: 10.1186/1755-8794-2-55.
36 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
37 PPARgamma controls CD1d expression by turning on retinoic acid synthesis in developing human dendritic cells. J Exp Med. 2006 Oct 2;203(10):2351-62.
38 Regulation of Hepatic Cholesteryl Ester Transfer Protein Expression and Reverse Cholesterol Transport by Inhibition of DNA Topoisomerase II. J Biol Chem. 2015 Jun 5;290(23):14418-29. doi: 10.1074/jbc.M115.643015. Epub 2015 Apr 25.
39 Organochloride pesticides induced hepatic ABCG5/G8 expression and lipogenesis in Chinese patients with gallstone disease. Oncotarget. 2016 Jun 7;7(23):33689-702. doi: 10.18632/oncotarget.9399.
40 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
41 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
42 Drug-induced hepatic steatosis in absence of severe mitochondrial dysfunction in HepaRG cells: proof of multiple mechanism-based toxicity. Cell Biol Toxicol. 2021 Apr;37(2):151-175. doi: 10.1007/s10565-020-09537-1. Epub 2020 Jun 14.
43 Effect of atorvastatin, simvastatin, and lovastatin on the metabolism of cholesterol and triacylglycerides in HepG2 cells. Biochem Pharmacol. 2001 Dec 1;62(11):1545-55. doi: 10.1016/s0006-2952(01)00790-0.
44 Hypoxia-inducible factor-1 (HIF-1) pathway activation by quercetin in human lens epithelial cells. Exp Eye Res. 2009 Dec;89(6):995-1002. doi: 10.1016/j.exer.2009.08.011. Epub 2009 Sep 1.
45 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
46 Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitro. J Invest Dermatol. 2005 Jul;125(1):143-53.
47 Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes. Toxicol Appl Pharmacol. 2013 Oct 1;272(1):245-55.
48 Adaptive homeostasis of the vitamin D-vitamin D nuclear receptor axis in 8-methoxypsoralen-induced hepatotoxicity. Toxicol Appl Pharmacol. 2019 Jan 1;362:150-158. doi: 10.1016/j.taap.2018.11.002. Epub 2018 Nov 10.
49 A toxicogenomic approach to drug-induced phospholipidosis: analysis of its induction mechanism and establishment of a novel in vitro screening system. Toxicol Sci. 2005 Feb;83(2):282-92.
50 Time series analysis of oxidative stress response patterns in HepG2: a toxicogenomics approach. Toxicology. 2013 Apr 5;306:24-34.
51 Determination of phospholipidosis potential based on gene expression analysis in HepG2 cells. Toxicol Sci. 2007 Mar;96(1):101-14.
52 Farnesoid X receptor induces murine scavenger receptor Class B type I via intron binding. PLoS One. 2012;7(4):e35895. doi: 10.1371/journal.pone.0035895. Epub 2012 Apr 23.
53 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
54 Identification of mechanisms of action of bisphenol a-induced human preadipocyte differentiation by transcriptional profiling. Obesity (Silver Spring). 2014 Nov;22(11):2333-43.
55 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
56 Acute hypersensitivity of pluripotent testicular cancer-derived embryonal carcinoma to low-dose 5-aza deoxycytidine is associated with global DNA Damage-associated p53 activation, anti-pluripotency and DNA demethylation. PLoS One. 2012;7(12):e53003. doi: 10.1371/journal.pone.0053003. Epub 2012 Dec 27.
57 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
58 Blood transcript immune signatures distinguish a subset of people with elevated serum ALT from others given acetaminophen. Clin Pharmacol Ther. 2016 Apr;99(4):432-41.
59 Primary Human Hepatocyte Spheroids as Tools to Study the Hepatotoxic Potential of Non-Pharmaceutical Chemicals. Int J Mol Sci. 2021 Oct 12;22(20):11005. doi: 10.3390/ijms222011005.
60 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.