Page last updated: 2024-12-10

17-(dimethylaminoethylamino)-17-demethoxygeldanamycin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

17-(dimethylaminoethylamino)-17-demethoxygeldanamycin, also known as **17-DMAG**, is a synthetic analog of the natural product **geldanamycin**. It is a potent inhibitor of the **heat shock protein 90 (Hsp90)**, a molecular chaperone that plays a critical role in the folding and stability of many proteins involved in cell signaling and survival.

**Why is 17-DMAG important for research?**

* **Cancer research:** Hsp90 is overexpressed in many cancer cells and is essential for their survival. 17-DMAG has shown promising preclinical activity against a variety of cancers, including leukemia, lymphoma, breast cancer, and prostate cancer. It works by inhibiting Hsp90, leading to the degradation of client proteins that are essential for cancer cell growth and survival.
* **Mechanism of action:** 17-DMAG serves as a valuable tool for understanding the role of Hsp90 in various cellular processes. By studying its effects on different cell types, researchers can gain insights into the mechanisms underlying its anticancer activity and potential off-target effects.
* **Drug development:** 17-DMAG has been investigated in clinical trials as a potential anticancer drug. While it has shown some efficacy, further research is needed to optimize its therapeutic potential and address potential side effects.

**Key features of 17-DMAG:**

* **Potent Hsp90 inhibitor:** It binds tightly to Hsp90, blocking its chaperone activity and leading to the degradation of its client proteins.
* **Synthetic analog:** It is a synthetic derivative of geldanamycin, designed to improve its pharmacological properties, such as bioavailability and toxicity.
* **Preclinical efficacy:** It has demonstrated significant anti-cancer activity in preclinical studies.
* **Clinical trials:** It has been evaluated in clinical trials for various cancers, but further research is needed to optimize its therapeutic potential.

**Overall, 17-DMAG is an important research tool that has the potential to lead to new cancer therapies. Its ability to target Hsp90 makes it a valuable agent for studying cancer cell survival and developing new anticancer drugs.**

17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

alvespimycin : A 19-membered macrocyle that is geldanamycin in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group. [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]

Cross-References

ID SourceID
PubMed CID5288674
CHEBI ID65324
CHEBI ID94772
SCHEMBL ID5449716
MeSH IDM0479533

Synonyms (45)

Synonym
HY-10389
(4e,6z,10e,12s,13r,16r)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
17-desmethoxy-17-n,n-dimethylaminoethylamino-geldanamycin
nsc707545
nsc-707545
nsc 707545
kos 1022
17-(dimethylaminoethylamino)-17-demethoxy-geldanamycin
17-dimethylaminoethylamino-17-demethoxy-geldanamycin
alvespimycin
((4e,6z,8s,9s,10e,12s,13r,14s,16r)-19-(2-dimethylaminoethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo(16.3.1)docosa-4,6,10,18,21-pentaen-9-yl) carbamate
kos1022
17-(dimethylaminoethylamino)-17-demethoxygeldanamycin
chebi:65324 ,
dmag
467214-20-6
alvespimycin [inn]
001l2fe0m3 ,
unii-001l2fe0m3
17-dimethylaminoethylamino-17-demethoxygeldanamycin
CS-0912
(4e,6z,8s,9s,10e,12s,13r,14s,16r)-19-{[2-(dimethylamino)ethyl]amino}-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
150270-08-9
alvespimycin [who-dd]
geldanamycin, 17-demethoxy-17-((2-(dimethylamino)ethyl)amino)-
(4e,6z,8s,9s,10e,12s,13r,14s,16r)-19-((2-(dimethylamino)ethyl)amino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo(16.3.1)docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
BRD-K83988098-003-01-8
M03709
SCHEMBL5449716
bdbm50005781
AC-33174
EX-A1103
17-demethoxy-17-[[2-(dimethylamino)ethyl]amino]geldanamycin
CHEBI:94772
gtpl9828
[(3r,5s,6r,7s,8e,10s,11s,12z,14e)-21-[2-(dimethylamino)ethylamino]-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate
DB12442
Q4552287
KUFRQPKVAWMTJO-LMZWQJSESA-N
BRD-K83988098-001-02-0
DTXSID00963646
[(4e,6z,8s,9s,10e,12s,13r,14s,16r)-19-[2-(dimethylamino)ethylamino]-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl] carbamate
17-(dimethylaminoethylamino)-17-demethoxygeldanamycin hcl
A1-50459
dimethylaminoethylamino-17-demethoxygeldanamycin, 17-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" All adverse effects were fully reversible in surviving animals after treatment was complete."( Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance.
Brown, AP; Covey, JM; Egorin, MJ; Eiseman, JL; Glaze, ER; Holleran, JL; Johnson, WD; Lambert, AL; Levine, BS; McCormick, DL; Page, JG; Sausville, EA; Smith, AC; Tomaszewski, JE, 2005
)
0.59
" In this study, we tested the hypothesis that the low lysosomal pH of normal cells plays an important role in protecting normal tissues from the toxic effects of lysosomotropic anticancer drugs."( The role of lysosomes in limiting drug toxicity in mice.
Forrest, ML; Krise, JP; Ndolo, RA, 2010
)
0.36
" Because of its adverse effects on liver, its less toxic derivatives 17-(allylamino)-17-demethoxygeldanamycin (17-AAG) and 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG) are currently being evaluated for the treatment of cancer."( Reactive oxygen species mediate hepatotoxicity induced by the Hsp90 inhibitor geldanamycin and its analogs.
Goldstein, S; Hyodo, F; Ishii, H; Krishna, MC; Mitchell, JB; Samuni, U; Samuni, Y, 2010
)
0.57
" 17-DMAG has the possibility to be a safe and effective anti-ototoxic drug."( 17-DMAG induces Hsp70 and protects the auditory hair cells from kanamycin ototoxicity in vitro.
Bing, D; Chen, J; Chen, Q; Chu, H; Cui, Y; Liu, Y; Pan, C; Sun, Y; Wang, S; Yu, Y; Zhou, L, 2015
)
0.42

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic and metabolite data generated should prove relevant to the design of additional preclinical studies as well as to contemplated clinical trials of 17DMAG and could be useful in their interpretation."( Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats.
Covey, JM; Egorin, MJ; Eiseman, JL; Hamburger, DR; Lagattuta, TF; Musser, SM; White, KD, 2002
)
0.56
"We have used a semimechanistic pharmacodynamic model to characterize concentration-effect relationships of ATO and HSP90 inhibitors on constitutive STAT3 activity, HSP70 expression, and cell death in a cell line model."( Synergism between arsenic trioxide and heat shock protein 90 inhibitors on signal transducer and activator of transcription protein 3 activity--pharmacodynamic drug-drug interaction modeling.
Brady, MT; Earp, JC; Jusko, WJ; Keng, MK; Wetzler, M, 2007
)
0.34
" Hsp70 induction in tumor and liver tissue was used as a pharmacodynamic measure of Hsp90 inhibition and stress response induction."( Stage 1 testing and pharmacodynamic evaluation of the HSP90 inhibitor alvespimycin (17-DMAG, KOS-1022) by the pediatric preclinical testing program.
Carol, H; Houghton, PJ; Keir, ST; Kolb, EA; Lock, R; Maris, JM; Morton, CL; Phelps, DA; Reynolds, CP; Smith, MA; Wu, J, 2008
)
0.35
" 17DMAG half-life was 24 +/- 15 hours."( Phase I pharmacokinetic and pharmacodynamic study of 17-dimethylaminoethylamino-17-demethoxygeldanamycin, an inhibitor of heat-shock protein 90, in patients with advanced solid tumors.
Belani, CP; Egorin, MJ; Erlichman, C; Holleran, JL; Ivy, SP; Naret, C; Ramalingam, SS; Ramanathan, RK; Remick, SC; TenEyck, CJ, 2010
)
0.36
"To identify sources of exposure variability for the tumor growth inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) using a population pharmacokinetic analysis."( Population pharmacokinetic analysis of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) in adult patients with solid tumors.
Aregbe, AO; Belani, CP; Bies, RR; Egorin, MJ; Ivy, PS; Ramalingam, S; Ramanathan, RK; Scher, HI; Sherer, EA; Solit, DB, 2012
)
0.38
" Population pharmacokinetic analysis of the 17-DMAG plasma concentration with time was performed using nonlinear mixed effect modeling to evaluate the effects of covariates, inter-individual variability, and between-occasion variability on model parameters using a stepwise forward addition then backward elimination modeling approach."( Population pharmacokinetic analysis of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) in adult patients with solid tumors.
Aregbe, AO; Belani, CP; Bies, RR; Egorin, MJ; Ivy, PS; Ramalingam, S; Ramanathan, RK; Scher, HI; Sherer, EA; Solit, DB, 2012
)
0.38
"Population pharmacokinetic analysis of 17-DMAG found no significant covariate effects and considerable inter-individual variability; this implies a wide range of exposures in the population and which may affect treatment outcome."( Population pharmacokinetic analysis of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) in adult patients with solid tumors.
Aregbe, AO; Belani, CP; Bies, RR; Egorin, MJ; Ivy, PS; Ramalingam, S; Ramanathan, RK; Scher, HI; Sherer, EA; Solit, DB, 2012
)
0.38
" Pharmacokinetic models of alvespimycin would help in the understanding of drug disposition, predicting drug exposure and interpreting dose-response relationship."( A physiologically based pharmacokinetic model of alvespimycin in mice and extrapolation to rats and humans.
Hu, ZY; Lu, J; Zhao, Y, 2014
)
0.4
"A literature search was performed to collect pharmacokinetic data for alvespimycin."( A physiologically based pharmacokinetic model of alvespimycin in mice and extrapolation to rats and humans.
Hu, ZY; Lu, J; Zhao, Y, 2014
)
0.4

Bioavailability

Hsp90 inhibitors which are derivates of the natural compound geldanamycin are currently being tested in clinical trials and small molecule inhibitors are in development. 17-DMAG is an orally bioavailable Hsp90 inhibitor.

ExcerptReferenceRelevance
" The oral bioavailability of 17-DMAG might be of advantage in investigating the potential of this compound in clinical trials with antiangiogenic as well as antiproliferative endpoints."( Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator.
Belotti, D; Borsotti, P; Burger, AM; Fisher-Nielson, K; Giavazzi, R; Hollingshead, M; Kaur, G; Riccardi, E; Sausville, EA; Thillainathan, J, 2004
)
0.61
" Therefore, we have investigated the effects of the orally bioavailable Hsp90 inhibitor 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG) on the radiosensitivity of human tumor cells in vitro and grown as tumor xenografts."( Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin.
Brady, KJ; Bull, EE; Burgan, WE; Camphausen, K; Carter, DJ; Cerra, MA; Dote, H; Hollingshead, MG; Oswald, KA; Tofilon, PJ, 2004
)
0.76
" Evidence of oral bioavailability of 17-DMAG in a saline-based formulation prompted more detailed examination of its antitumor efficacy in vivo."( In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative.
Alley, M; Borgel, S; Burger, AM; Fiebig, HH; Hollingshead, M; Pacula-Cox, C; Sausville, EA, 2005
)
0.33
" Hsp90 inhibitors which are derivates of the natural compound geldanamycin, such as the orally bioavailable 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), are currently being tested in clinical trials and small molecule inhibitors are in development."( Efficacy of Hsp90 inhibition for induction of apoptosis and inhibition of growth in cervical carcinoma cells in vitro and in vivo.
Cao, MP; Hedley, DW; Pham, NA; Schwock, J, 2008
)
0.56
" Optimization of a screening hit using structure-based design and modification of log D and chemical structural features led to the identification of a class of orally bioavailable non-quinone-containing Hsp90 inhibitors."( Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.
Davies, JF; Digits, JA; Elleraas, J; Gajiwala, KS; Gehring, MR; Hickey, MJ; Huang, B; Kung, PP; Mehta, P; Neul, D; Rodgers, C; Skaptason, J; Wang, J; Yamazaki, S; Yin, MJ; Zhang, G; Zhou, JZ; Zientek, M, 2010
)
0.36

Dosage Studied

ExcerptRelevanceReference
" In summary, these results suggest that dosage will be a critical factor in the treatment of tumor patients with HSP90 inhibitors."( Induction of the hypoxia-inducible factor system by low levels of heat shock protein 90 inhibitors.
Franke, C; Hahn, T; Ibrahim, NO; Katschinski, DM; Stiehl, DP; Wenger, RH; Wirthner, R, 2005
)
0.33
" Furthermore, efficacy experiments performed in a NCI-N87 mouse xenograft model demonstrated tumor regression in some dosing regimens."( Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.
Aay, N; Anand, NK; Arcalas, A; Baik, T; Blazey, CM; Bowles, OJ; Buhr, CA; Bussenius, J; Costanzo, S; Curtis, JK; DeFina, SC; Dubenko, L; Heuer, TS; Huang, P; Jaeger, C; Joshi, A; Kennedy, AR; Kim, AI; Lara, K; Lee, J; Li, J; Lougheed, JC; Ma, S; Malek, S; Manalo, JC; Martini, JF; McGrath, G; Nicoll, M; Nuss, JM; Pack, M; Peto, CJ; Rice, KD; Tsang, TH; Wang, L; Womble, SW; Yakes, M; Zhang, W, 2012
)
0.38
" Pharmacokinetic models of alvespimycin would help in the understanding of drug disposition, predicting drug exposure and interpreting dose-response relationship."( A physiologically based pharmacokinetic model of alvespimycin in mice and extrapolation to rats and humans.
Hu, ZY; Lu, J; Zhao, Y, 2014
)
0.4
" A refined PBPK model would benefit the understanding of dose-response relationships and optimization of dosing regimens."( A physiologically based pharmacokinetic model of alvespimycin in mice and extrapolation to rats and humans.
Hu, ZY; Lu, J; Zhao, Y, 2014
)
0.4
" Based on the dose-response study, synergistic interactions between the two regimens were evaluated using clonogenic assay and combination index values."( Synergistic Antitumor Effects of Combined Treatment with HSP90 Inhibitor and PI3K/mTOR Dual Inhibitor in Cisplatin-Resistant Human Bladder Cancer Cells.
Cho, NH; Choi, YD; Gong, MK; Kang, J; Kim, HJ; Rha, SY; Yoon, CY; Yun, M, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
Hsp90 inhibitorAn EC 3.6.4.10 (non-chaperonin molecular chaperone ATPase) inhibitor that blocks the action of heat shock protein 90.
[role 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]

Drug Classes (5)

ClassDescription
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
ansamycinA class of macrocyclic lactams that consist of an aromatic (phenyl or naphthyl) or quinonoid (benzoquinone or naphthoquinone) moiety that is bridged by an aliphatic chain.
1,4-benzoquinonesAny member of the class of benzoquinones that is 1,4-benzoquinone or its C-substituted derivatives.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[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 Targets (27)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Lysine-specific demethylase 6BHomo sapiens (human)IC50 (µMol)0.40000.01601.66726.9000AID1885317
Lysine-specific demethylase 4BHomo sapiens (human)IC50 (µMol)0.70000.20001.22003.8000AID1885314
Heat shock protein HSP 90-alphaHomo sapiens (human)IC50 (µMol)0.16990.00040.695010.0000AID1625290; AID1632347; AID344853; AID344854; AID344856; AID444595; AID596787
Heat shock protein HSP 90-alphaHomo sapiens (human)Ki0.68000.00020.54152.7000AID596788
Heat shock protein HSP 90-betaHomo sapiens (human)IC50 (µMol)0.27240.00100.683610.0000AID1076813; AID1127396; AID1127397; AID1625290; AID344853; AID344854; AID344856; AID395892; AID444595; AID596787
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.00360.00031.38338.4000AID327961
Lysine-specific demethylase 5AHomo sapiens (human)IC50 (µMol)0.13000.13002.374710.0000AID1885316
Hypoxia-inducible factor 1-alphaHomo sapiens (human)IC50 (µMol)5.03580.00072.46529.2100AID291914; AID291915; AID327961; AID422511; AID422513; AID485530
Endothelial PAS domain-containing protein 1Homo sapiens (human)IC50 (µMol)7.52510.00302.60028.5100AID291914; AID291915; AID327961; AID422513
Lysine-specific demethylase 4CHomo sapiens (human)IC50 (µMol)0.70000.16002.11489.4000AID1885315
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Heat shock protein HSP 90-alphaHomo sapiens (human)EC50 (µMol)0.02360.00400.13311.2000AID266546; AID266550; AID266551; AID266552; AID266553; AID344858
Heat shock protein HSP 90-alphaHomo sapiens (human)Kd0.36230.00030.94889.8000AID254267; AID394598; AID394599
Heat shock protein HSP 90-betaHomo sapiens (human)EC50 (µMol)0.02360.00400.23851.7000AID266546; AID266550; AID266551; AID266552; AID266553; AID344858
Heat shock protein HSP 90-betaHomo sapiens (human)Kd0.50000.00031.33309.8000AID350568
Cholesteryl ester transfer proteinHomo sapiens (human)Kd0.08700.08700.12350.1600AID394599
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.73677.0000AID266551
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.00011.46937.0000AID266551
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
EndoplasminCanis lupus familiaris (dog)EC50 (µMol)0.06500.04800.07900.1240AID266547
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01902.149910.0000AID266551
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.73677.0000AID266551
GABA theta subunitRattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)EC50 (µMol)0.04600.01901.70547.0000AID266551
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (192)

Processvia Protein(s)Taxonomy
inflammatory response to antigenic stimulusLysine-specific demethylase 6BHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 6BHomo sapiens (human)
response to activityLysine-specific demethylase 6BHomo sapiens (human)
hippocampus developmentLysine-specific demethylase 6BHomo sapiens (human)
cell fate commitmentLysine-specific demethylase 6BHomo sapiens (human)
endothelial cell differentiationLysine-specific demethylase 6BHomo sapiens (human)
positive regulation of transcription by RNA polymerase IILysine-specific demethylase 6BHomo sapiens (human)
mesodermal cell differentiationLysine-specific demethylase 6BHomo sapiens (human)
cardiac muscle cell differentiationLysine-specific demethylase 6BHomo sapiens (human)
response to fungicideLysine-specific demethylase 6BHomo sapiens (human)
cellular response to hydrogen peroxideLysine-specific demethylase 6BHomo sapiens (human)
positive regulation of cold-induced thermogenesisLysine-specific demethylase 6BHomo sapiens (human)
heart developmentLysine-specific demethylase 6BHomo sapiens (human)
regulation of gene expressionLysine-specific demethylase 6BHomo sapiens (human)
brain developmentLysine-specific demethylase 4BHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 4BHomo sapiens (human)
regulation of gene expressionLysine-specific demethylase 4BHomo sapiens (human)
telomere maintenance via telomeraseHeat shock protein HSP 90-alphaHomo sapiens (human)
neuron migrationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein phosphorylationHeat shock protein HSP 90-alphaHomo sapiens (human)
activation of innate immune responseHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of defense response to virus by hostHeat shock protein HSP 90-alphaHomo sapiens (human)
skeletal muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrial transportHeat shock protein HSP 90-alphaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-alphaHomo sapiens (human)
response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
response to coldHeat shock protein HSP 90-alphaHomo sapiens (human)
response to xenobiotic stimulusHeat shock protein HSP 90-alphaHomo sapiens (human)
response to salt stressHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of lamellipodium assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cardiac muscle cell apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein polymerizationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of interferon-beta productionHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-alphaHomo sapiens (human)
protein refoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to cocaineHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein import into nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein-containing complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
protein unfoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to estrogenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein insertion into mitochondrial outer membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein catabolic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cell sizeHeat shock protein HSP 90-alphaHomo sapiens (human)
response to antibioticHeat shock protein HSP 90-alphaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cardiac muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated autophagyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to virusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levelsHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of tau-protein kinase activityHeat shock protein HSP 90-alphaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-alphaHomo sapiens (human)
telomere maintenance via telomeraseHeat shock protein HSP 90-betaHomo sapiens (human)
placenta developmentHeat shock protein HSP 90-betaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-betaHomo sapiens (human)
virion attachment to host cellHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of transforming growth factor beta receptor signaling pathwayHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal ubiquitin-dependent protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of apoptotic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of cell differentiationHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of cell cycleHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to interleukin-4Heat shock protein HSP 90-betaHomo sapiens (human)
supramolecular fiber organizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of protein localization to cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-betaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-betaHomo sapiens (human)
triglyceride metabolic processCholesteryl ester transfer proteinHomo sapiens (human)
lipid transportCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol metabolic processCholesteryl ester transfer proteinHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationCholesteryl ester transfer proteinHomo sapiens (human)
regulation of cholesterol effluxCholesteryl ester transfer proteinHomo sapiens (human)
phospholipid transportCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol transportCholesteryl ester transfer proteinHomo sapiens (human)
positive regulation of cholesterol transportCholesteryl ester transfer proteinHomo sapiens (human)
triglyceride transportCholesteryl ester transfer proteinHomo sapiens (human)
very-low-density lipoprotein particle remodelingCholesteryl ester transfer proteinHomo sapiens (human)
low-density lipoprotein particle remodelingCholesteryl ester transfer proteinHomo sapiens (human)
high-density lipoprotein particle remodelingCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
reverse cholesterol transportCholesteryl ester transfer proteinHomo sapiens (human)
phosphatidylcholine metabolic processCholesteryl ester transfer proteinHomo sapiens (human)
lipid homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
phospholipid homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
triglyceride homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
positive regulation of phospholipid transportCholesteryl ester transfer proteinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific demethylase 5AHomo sapiens (human)
circadian regulation of gene expressionLysine-specific demethylase 5AHomo sapiens (human)
positive regulation of DNA-templated transcriptionLysine-specific demethylase 5AHomo sapiens (human)
regulation of DNA-binding transcription factor activityLysine-specific demethylase 5AHomo sapiens (human)
facultative heterochromatin formationLysine-specific demethylase 5AHomo sapiens (human)
regulation of DNA-templated transcriptionLysine-specific demethylase 5AHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 5AHomo sapiens (human)
ERAD pathwayEndoplasminCanis lupus familiaris (dog)
positive regulation of chemokine-mediated signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of signaling receptor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to reactive oxygen speciesHypoxia-inducible factor 1-alphaHomo sapiens (human)
angiogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular glucose homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
neural crest cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
epithelial to mesenchymal transitionHypoxia-inducible factor 1-alphaHomo sapiens (human)
embryonic placenta developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
B-1 B cell homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of endothelial cell proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
heart loopingHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of neuroblast proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
chondrocyte differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
glandular epithelial cell maturationHypoxia-inducible factor 1-alphaHomo sapiens (human)
connective tissue replacement involved in inflammatory response wound healingHypoxia-inducible factor 1-alphaHomo sapiens (human)
outflow tract morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
cardiac ventricle morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
lactate metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of glycolytic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular iron ion homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
signal transductionHypoxia-inducible factor 1-alphaHomo sapiens (human)
neuroblast proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
lactationHypoxia-inducible factor 1-alphaHomo sapiens (human)
visual learningHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to iron ionHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
vascular endothelial growth factor productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of epithelial cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to muscle activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
axonal transport of mitochondrionHypoxia-inducible factor 1-alphaHomo sapiens (human)
neural fold elevation formationHypoxia-inducible factor 1-alphaHomo sapiens (human)
cerebral cortex developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
bone mineralizationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of bone mineralizationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
TOR signalingHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of TOR signalingHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular oxygen homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of chemokine productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of transforming growth factor beta2 productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
collagen metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to oxidative stressHypoxia-inducible factor 1-alphaHomo sapiens (human)
embryonic hemopoiesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
insulin secretion involved in cellular response to glucose stimulusHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusHypoxia-inducible factor 1-alphaHomo sapiens (human)
hemoglobin biosynthetic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of erythrocyte differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of angiogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of growthHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
muscle cell cellular homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of hormone biosynthetic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
digestive tract morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of nitric-oxide synthase activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
neuron apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
elastin metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
intestinal epithelial cell maturationHypoxia-inducible factor 1-alphaHomo sapiens (human)
epithelial cell differentiation involved in mammary gland alveolus developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
iris morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
retina vasculature development in camera-type eyeHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of thymocyte apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to interleukin-1Hypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
dopaminergic neuron differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
mesenchymal cell apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
hypoxia-inducible factor-1alpha signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to virusHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of mitophagyHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of miRNA transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of miRNA transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of aerobic respirationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of protein neddylationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of mesenchymal cell apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaEndothelial PAS domain-containing protein 1Homo sapiens (human)
angiogenesisEndothelial PAS domain-containing protein 1Homo sapiens (human)
embryonic placenta developmentEndothelial PAS domain-containing protein 1Homo sapiens (human)
blood vessel remodelingEndothelial PAS domain-containing protein 1Homo sapiens (human)
regulation of heart rateEndothelial PAS domain-containing protein 1Homo sapiens (human)
epithelial cell maturationEndothelial PAS domain-containing protein 1Homo sapiens (human)
response to oxidative stressEndothelial PAS domain-containing protein 1Homo sapiens (human)
mitochondrion organizationEndothelial PAS domain-containing protein 1Homo sapiens (human)
signal transductionEndothelial PAS domain-containing protein 1Homo sapiens (human)
visual perceptionEndothelial PAS domain-containing protein 1Homo sapiens (human)
erythrocyte differentiationEndothelial PAS domain-containing protein 1Homo sapiens (human)
lung developmentEndothelial PAS domain-containing protein 1Homo sapiens (human)
norepinephrine metabolic processEndothelial PAS domain-containing protein 1Homo sapiens (human)
mRNA transcription by RNA polymerase IIEndothelial PAS domain-containing protein 1Homo sapiens (human)
surfactant homeostasisEndothelial PAS domain-containing protein 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIEndothelial PAS domain-containing protein 1Homo sapiens (human)
myoblast fate commitmentEndothelial PAS domain-containing protein 1Homo sapiens (human)
multicellular organismal-level iron ion homeostasisEndothelial PAS domain-containing protein 1Homo sapiens (human)
cellular response to hypoxiaEndothelial PAS domain-containing protein 1Homo sapiens (human)
positive regulation of cold-induced thermogenesisEndothelial PAS domain-containing protein 1Homo sapiens (human)
regulation of protein neddylationEndothelial PAS domain-containing protein 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIEndothelial PAS domain-containing protein 1Homo sapiens (human)
blastocyst formationLysine-specific demethylase 4CHomo sapiens (human)
positive regulation of cell population proliferationLysine-specific demethylase 4CHomo sapiens (human)
stem cell population maintenanceLysine-specific demethylase 4CHomo sapiens (human)
androgen receptor signaling pathwayLysine-specific demethylase 4CHomo sapiens (human)
positive regulation of transcription by RNA polymerase IILysine-specific demethylase 4CHomo sapiens (human)
regulation of androgen receptor signaling pathwayLysine-specific demethylase 4CHomo sapiens (human)
regulation of stem cell differentiationLysine-specific demethylase 4CHomo sapiens (human)
regulation of gene expressionLysine-specific demethylase 4CHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 4CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (84)

Processvia Protein(s)Taxonomy
protein bindingLysine-specific demethylase 6BHomo sapiens (human)
beta-catenin bindingLysine-specific demethylase 6BHomo sapiens (human)
histone demethylase activityLysine-specific demethylase 6BHomo sapiens (human)
metal ion bindingLysine-specific demethylase 6BHomo sapiens (human)
histone H3K27me2/H3K27me3 demethylase activityLysine-specific demethylase 6BHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingLysine-specific demethylase 6BHomo sapiens (human)
chromatin DNA bindingLysine-specific demethylase 6BHomo sapiens (human)
histone demethylase activityLysine-specific demethylase 4BHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific demethylase 4BHomo sapiens (human)
metal ion bindingLysine-specific demethylase 4BHomo sapiens (human)
histone H3K36 demethylase activityLysine-specific demethylase 4BHomo sapiens (human)
histone H3K9me2/H3K9me3 demethylase activityLysine-specific demethylase 4BHomo sapiens (human)
UTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
CTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
RNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
mRNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-alphaHomo sapiens (human)
sulfonylurea receptor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein phosphatase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-alphaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
dATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-alphaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
transmembrane transporter bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTPase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
Rho GDP-dissociation inhibitor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
scaffold protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-alphaHomo sapiens (human)
protein tyrosine kinase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
double-stranded RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-betaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-betaHomo sapiens (human)
heat shock protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
peptide bindingHeat shock protein HSP 90-betaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
cadherin bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein dimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
receptor ligand inhibitor activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone methyltransferase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
phospholipid transporter activityCholesteryl ester transfer proteinHomo sapiens (human)
lipid bindingCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol bindingCholesteryl ester transfer proteinHomo sapiens (human)
triglyceride bindingCholesteryl ester transfer proteinHomo sapiens (human)
phosphatidylcholine bindingCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol transfer activityCholesteryl ester transfer proteinHomo sapiens (human)
transcription cis-regulatory region bindingLysine-specific demethylase 5AHomo sapiens (human)
DNA bindingLysine-specific demethylase 5AHomo sapiens (human)
transcription coactivator activityLysine-specific demethylase 5AHomo sapiens (human)
enzyme inhibitor activityLysine-specific demethylase 5AHomo sapiens (human)
protein bindingLysine-specific demethylase 5AHomo sapiens (human)
zinc ion bindingLysine-specific demethylase 5AHomo sapiens (human)
chromatin DNA bindingLysine-specific demethylase 5AHomo sapiens (human)
histone demethylase activityLysine-specific demethylase 5AHomo sapiens (human)
histone H3K4me/H3K4me2/H3K4me3 demethylase activityLysine-specific demethylase 5AHomo sapiens (human)
methylated histone bindingLysine-specific demethylase 5AHomo sapiens (human)
histone bindingLysine-specific demethylase 5AHomo sapiens (human)
ATP bindingEndoplasminCanis lupus familiaris (dog)
ATP hydrolysis activityEndoplasminCanis lupus familiaris (dog)
ATP-dependent protein folding chaperoneEndoplasminCanis lupus familiaris (dog)
DNA-binding transcription factor activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
cis-regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription activator activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription repressor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
transcription coactivator bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
p53 bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription factor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear receptor bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
enzyme bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein kinase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein domain specific bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
histone deacetylase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein heterodimerization activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
Hsp90 protein bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
E-box bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
transcription regulator activator activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
sequence-specific DNA bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEndothelial PAS domain-containing protein 1Homo sapiens (human)
transcription coactivator bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEndothelial PAS domain-containing protein 1Homo sapiens (human)
protein bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
protein heterodimerization activityEndothelial PAS domain-containing protein 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
histone H3K9me2/H3K9me3 demethylase activityLysine-specific demethylase 4CHomo sapiens (human)
zinc ion bindingLysine-specific demethylase 4CHomo sapiens (human)
enzyme bindingLysine-specific demethylase 4CHomo sapiens (human)
nuclear receptor coactivator activityLysine-specific demethylase 4CHomo sapiens (human)
histone demethylase activityLysine-specific demethylase 4CHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific demethylase 4CHomo sapiens (human)
nuclear androgen receptor bindingLysine-specific demethylase 4CHomo sapiens (human)
histone H3K36 demethylase activityLysine-specific demethylase 4CHomo sapiens (human)
H3K9me3 modified histone bindingLysine-specific demethylase 4CHomo sapiens (human)
histone H3K9me2/H3K9me3 demethylase activityLysine-specific demethylase 4CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (47)

Processvia Protein(s)Taxonomy
nucleusLysine-specific demethylase 6BHomo sapiens (human)
nucleoplasmLysine-specific demethylase 6BHomo sapiens (human)
MLL3/4 complexLysine-specific demethylase 6BHomo sapiens (human)
nucleoplasmLysine-specific demethylase 4BHomo sapiens (human)
chromatinLysine-specific demethylase 4BHomo sapiens (human)
nucleusLysine-specific demethylase 4BHomo sapiens (human)
extracellular regionHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-alphaHomo sapiens (human)
membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
basolateral plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
apical plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
brush border membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
lysosomal lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
collagen-containing extracellular matrixHeat shock protein HSP 90-alphaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
endocytic vesicle lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm mitochondrial sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
myelin sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
COP9 signalosomeHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionHeat shock protein HSP 90-betaHomo sapiens (human)
nucleusHeat shock protein HSP 90-betaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
membraneHeat shock protein HSP 90-betaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-betaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-betaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-betaHomo sapiens (human)
dynein axonemal particleHeat shock protein HSP 90-betaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-betaHomo sapiens (human)
aryl hydrocarbon receptor complexHeat shock protein HSP 90-betaHomo sapiens (human)
HSP90-CDC37 chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionCholesteryl ester transfer proteinHomo sapiens (human)
extracellular spaceCholesteryl ester transfer proteinHomo sapiens (human)
vesicleCholesteryl ester transfer proteinHomo sapiens (human)
extracellular exosomeCholesteryl ester transfer proteinHomo sapiens (human)
high-density lipoprotein particleCholesteryl ester transfer proteinHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleusLysine-specific demethylase 5AHomo sapiens (human)
nucleoplasmLysine-specific demethylase 5AHomo sapiens (human)
nucleolusLysine-specific demethylase 5AHomo sapiens (human)
nucleusLysine-specific demethylase 5AHomo sapiens (human)
chromatinLysine-specific demethylase 5AHomo sapiens (human)
sarcoplasmic reticulum lumenEndoplasminCanis lupus familiaris (dog)
melanosomeEndoplasminCanis lupus familiaris (dog)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
nucleusHypoxia-inducible factor 1-alphaHomo sapiens (human)
nucleoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
cytoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
cytosolHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear bodyHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear speckHypoxia-inducible factor 1-alphaHomo sapiens (human)
motile ciliumHypoxia-inducible factor 1-alphaHomo sapiens (human)
axon cytoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
chromatinHypoxia-inducible factor 1-alphaHomo sapiens (human)
euchromatinHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein-containing complexHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexHypoxia-inducible factor 1-alphaHomo sapiens (human)
nucleoplasmEndothelial PAS domain-containing protein 1Homo sapiens (human)
cytosolEndothelial PAS domain-containing protein 1Homo sapiens (human)
nuclear speckEndothelial PAS domain-containing protein 1Homo sapiens (human)
chromatinEndothelial PAS domain-containing protein 1Homo sapiens (human)
transcription regulator complexEndothelial PAS domain-containing protein 1Homo sapiens (human)
nucleoplasmLysine-specific demethylase 4CHomo sapiens (human)
chromatinLysine-specific demethylase 4CHomo sapiens (human)
pericentric heterochromatinLysine-specific demethylase 4CHomo sapiens (human)
nucleusLysine-specific demethylase 4CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (120)

Assay IDTitleYearJournalArticle
AID350571Cytotoxicity against human MCF7 cells after 72 hrs by celltiter-glo assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID395892Binding affinity to Hsp90 in human SKBR3 cells2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Discovery and development of heat shock protein 90 inhibitors.
AID266548Inhibition of human SKBR3 cell growth2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID394603Cytotoxicity against human MCF7 cells after 72 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID394598Binding affinity to human recombinant Hsp90alpha N-terminal domain by scintillation proximity assay2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID1212925Metabolic stability in human liver microsomes at 5 uM by liquid chromatography-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID444597Hepatic clearance in human liver microsomes measured per million cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.
AID327963Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.
AID465321Toxicity in iv dosed dog assessed as maximum tolerated dose2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID394604Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID344857Cytotoxicity against human A2058 cells by MTT assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
AID291918Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay2007Journal of natural products, Jul, Volume: 70, Issue:7
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.
AID1076811Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell viability after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold.
AID1076810Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold.
AID1127400Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID394605Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID1127401Antiproliferative activity against human A231 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID1885316Inhibition of KDM5A (unknown origin) measured by AlphaScreen assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Recent Advances with KDM4 Inhibitors and Potential Applications.
AID506585Inhibition of HSP90-mediated proliferation of human NCI-H526 cells at 1 uM after 96 hrs by sulforhodamine B assay2007Nature chemical biology, Aug, Volume: 3, Issue:8
Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1625290Inhibition of Hsp90 in human SKBR3 cells2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.
AID327961Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.
AID1212926Terminal half life in human2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID344856Inhibition of Hsp90 in human A2058 cells assessed as Akt degradation2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
AID715287Inhibition of Hsp90 in human COLO205 cells xenografted in mouse assessed as Her2 degradation at 100 mg/kg administered QD for 2 days measured 8 hrs post-last dose2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.
AID1212959Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-penta2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1212974Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-a2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID266550Degradation of Her2 in SKBR3 cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID1212960Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-92011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID394600Cytotoxicity against human SKBR3 cells after 72 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID1212969Drug metabolism assessed as human recombinant CYP2B6-mediated oxidative metabolism at 1 uM by liquid chromatography-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID266553Upregulation of Hsp70 in SKOV3 cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID465320Toxicity in iv dosed rat assessed as maximum tolerated dose2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID1212975Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1212961Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbam2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1625300Cytotoxicity against HGF-induced erlotinib-resistant human Ma1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.
AID485532Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA2010Journal of natural products, Jun-25, Volume: 73, Issue:6
An isoaurone and other constituents from Trichosanthes kirilowii seeds inhibit hypoxia-inducible factor-1 and nuclear factor-kappaB.
AID344858Inhibition of Hsp90 in human A2058 cells2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
AID1212956Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-8,13-dihydroxy-14-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate form2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1127395Inhibition of HSP90 (unknown origin)-mediated ATPase activity at 40 uM after 3 hrs by malachite green assay relative to control2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID1127397Displacement of FITC-geldanamycin from HSP90 (unknown origin) after 30 mins by fluorescence polarization assay2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID1212927Total clearance in human2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1076813Inhibition of full-length Hsp90-ATPase activity (unknown origin) assessed as inhibition of ATP hydrolysis by spectrophotometry2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold.
AID1632347Inhibition of 6x-His tagged human recombinant full length Hsp90alpha ATPase preincubated for 0.5 hrs followed by ATP addition measured after 30 mins by HTRF assay2016Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19
Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity.
AID350574Cytotoxicity against human CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID1212962Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbam2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID596788Displacement of [3H]-(R)-2-(5-chloro-2,4-dihydroxybenzoyl)-N-ethylisoindoline-1-carboxamide from human his(6)-tagged HSP90alpha after 30 mins by scintillation proximity assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl
AID394601Cytotoxicity against human SKOV3 cells after 72 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID266546Inhibition of BODIPY-AG binding to human HSP902006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID266547Inhibition of BODIPY-AG binding to dog Grp942006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID394602Cytotoxicity against human HCT116 cells after 72 hrs2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID1127396Inhibition of full-length HSP90 (unknown origin) expressed in Escherichia coli assessed as inhibition of ATPase activity after 3 hrs by spectrophotometric analysis2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID344855Cytotoxicity against human MDA-MB-231 cells by MTT assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
AID422512Inhibition of hypoxia-induced VEGF protein secretion in human Hep3B cells after 16 hrs by ELISA2009Journal of natural products, Jan, Volume: 72, Issue:1
Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.
AID1451199Cytotoxicity against mouse primary hepatocytes assessed as reduction in cell viability at 5 to 20 uM after 24 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID1451185Inhibition of HSP90 in human HeLa cells assessed as induction of Akt degradation at 10 uM after 6 hrs by Western blot method2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID1212937Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate form2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1212970Drug metabolism assessed as human recombinant CYP2C9-mediated oxidative metabolism at 1 uM by liquid chromatography-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID715289Inhibition of Hsp90 in human COLO205 cells xenografted in mouse assessed as Raf1 degradation at 100 mg/kg administered QD for 2 days measured 8 hrs post-last dose2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.
AID291914Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay2007Journal of natural products, Jul, Volume: 70, Issue:7
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.
AID1212928Drug metabolism in human liver microsomes assessed as stability after 2 hrs relative to control by liquid chromatography-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1212953Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carb2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID255773Cytotoxicity against SKBr3 cells2005Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
Structure-based design of 7-carbamate analogs of geldanamycin.
AID350567Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID1127398Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID1212957Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12R,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-12,16-bis(hydroxymethyl)-8,14-dimethoxy-4,10-dimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-p2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1212955Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13,14-dihydroxy-8-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate form2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID485530Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis2010Journal of natural products, Jun-25, Volume: 73, Issue:6
An isoaurone and other constituents from Trichosanthes kirilowii seeds inhibit hypoxia-inducible factor-1 and nuclear factor-kappaB.
AID1451184Inhibition of HSP90 in human HeLa cells assessed as induction of chk1 degradation at 10 uM after 6 hrs by Western blot method2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID699452Inhibition of luciferase activity in human LN229-Lux cells at 2.5 to 10 uM incubated for 1 hr under normoxia followed by 24 hrs under hypoxia by reporter gene assay2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents.
AID266549Inhibition of human SKOV3 cell growth2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID422513Inhibition of hypoxia-induced HIF1 activation in human Hep3B cells by pGL3-HRE-luciferase reporter gene assay2009Journal of natural products, Jan, Volume: 72, Issue:1
Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.
AID1451187Inhibition of HSP90 in human PC3 cells assessed as induction of chk1 degradation at 10 uM after 6 hrs by Western blot method2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID596787Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl
AID1212973Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1127399Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, May-22, Volume: 79Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.
AID506584Binding affinity to HSP90 in human NCI-H526 cells at 1 uM after 24 hrs by fluorescence polarization assay2007Nature chemical biology, Aug, Volume: 3, Issue:8
Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID350575Cytotoxicity against human paclitaxel-resistant CCRF-CEM cells after 72 hrs by celltiter-96 aqueous one solution assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID1212963Drug metabolism assessed as human recombinant CYP3A5-mediated (4E,6Z,8S,9S,10E,12R,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-12,16-bis(hydroxymethyl)-8,14-dimethoxy-4,10-dimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,62011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID350572Cytotoxicity against human SKOV3 cells after 72 hrs by celltiter-glo assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID1212954Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl 2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1451186Inhibition of HSP90 in human HeLa cells assessed as induction of HSP70 protein expression at 10 uM after 6 hrs by Western blot method2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID1170900Reduction in oxygen consumption rate in human NCI-H1299 cells incubated for 12 hrs2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90.
AID1451189Inhibition of HSP90 in human PC3 cells assessed as induction of HSP70 protein expression at 10 uM after 6 hrs by Western blot method2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID580563Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034).
AID350568Binding affinity to human recombinant HSP902009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID266551Degradation of Her2 in SKOV3 cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID1212976Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-8,13-dihydroxy-14-methoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID444594Displacement of [3H]pGA from His-tagged Hsp90 by scintillation proximity assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.
AID394593Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID344853Inhibition of Hsp90 in human MDA-MB-231 cells assessed as Akt degradation2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
AID1076812Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold.
AID344854Inhibition of Hsp90 in human MDA-MB-231 cells assessed as her2 degradation2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
AID499473Binding affinity to Hsp90 N-terminal ATPase domain by isothermal titration calorimetry assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
AID1885314Inhibition of KDM4B (unknown origin) measured by AlphaScreen assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Recent Advances with KDM4 Inhibitors and Potential Applications.
AID1451188Inhibition of HSP90 in human PC3 cells assessed as induction of Akt degradation at 10 uM after 6 hrs by Western blot method2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID291915Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay2007Journal of natural products, Jul, Volume: 70, Issue:7
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.
AID465282Chemical stability assessed as half life2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Heat shock protein 90: inhibitors in clinical trials.
AID394592Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID327962Cytotoxicity against human AGS cells by MTT assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.
AID1625299Cytotoxicity against HGF-induced erlotinib-resistant human PC9 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.
AID394599Binding affinity to human recombinant Hsp90alpha N-terminal domain by isothermal titration calorimetry2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
AID1212977Drug metabolism in human liver microsomes assessed as 1 uM CYP3A inhibitor ketoconazole-mediated inhibition of (4E,6Z,8S,9S,10E,12R,13R,14S,16R)-19-(2-(dimethylamino)-1-hydroxyethylamino)-13-hydroxy-12,16-bis(hydroxymethyl)-8,14-dimethoxy-4,10-dimethyl-3,2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID266552Upregulation of Hsp70 in SKBR3 cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
AID596978Toxicity in human A2058 cells xenografted po dosed nu/nu athymic mouse2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl
AID1212971Drug metabolism assessed as human recombinant CYP2E1-mediated oxidative metabolism at 1 uM by liquid chromatography-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID580560Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034).
AID1212936Drug metabolism in human liver microsomes assessed as (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(2-(dimethylamino)ethylamino)-13-hydroxy-10-(hydroxymethyl)-8,14-dimethoxy-4,12,16-trimethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl 2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes.
AID1451198Cytotoxicity against human corneal cells assessed as reduction in cell viability at 5 to 20 uM after 24 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.
AID580561Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034).
AID1885315Inhibition of KDM4C (unknown origin) measured by AlphaScreen assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Recent Advances with KDM4 Inhibitors and Potential Applications.
AID291916Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay2007Journal of natural products, Jul, Volume: 70, Issue:7
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.
AID350573Cytotoxicity against human A549 cells after 72 hrs by celltiter-glo assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Potent cytotoxic C-11 modified geldanamycin analogues.
AID254267Binding affinity for human heat shock protein 90 in scintillation proximity assay2005Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
Structure-based design of 7-carbamate analogs of geldanamycin.
AID596793Intrinsic clearance in human liver microsomes at 1 uM after 45 mins by LC MS/MS analysis2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl
AID444595Inhibition of Hsp90 in human H1299 assessed as degradation of Hsp90 client protein Akt2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.
AID422511Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis2009Journal of natural products, Jan, Volume: 72, Issue:1
Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.
AID1885317Inhibition of KDM6B (unknown origin) measured by AlphaScreen assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Recent Advances with KDM4 Inhibitors and Potential Applications.
AID596980Antitumor activity against human A2058 cells xenografted in nu/nu athymic mouse model assessed as inhibition of tumor growth at 10 mg/kg, ip bid for 14 days2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difl
AID327964Cytotoxicity against human HeLa cells by MTT assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.
AID499474Cytotoxicity against human HCT116 cells by Alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (254)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's68 (26.77)29.6817
2010's164 (64.57)24.3611
2020's22 (8.66)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.32

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index14.32 (24.57)
Research Supply Index5.58 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (3.53%)5.53%
Reviews14 (5.49%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other232 (90.98%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]