Page last updated: 2024-11-05

desoxycorticosterone

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Description

Desoxycorticosterone: A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6166
CHEMBL ID1498
CHEBI ID16973
SCHEMBL ID4065
MeSH IDM0006087

Synonyms (123)

Synonym
MLS001076270 ,
BRD-K98521173-001-03-8
gtpl2871
CHEBI:16973 ,
4-pregnen-21-ol-3,20-dione
21-hydroxypregn-4-ene-3,20-dione
PRESTWICK2_000957
MLS000028537 ,
PRESTWICK3_000957
LMST02030087
desossicortone [dcit]
desoxicortona [inn-spanish]
desoxycortonum
einecs 200-596-4
desoxycortonum [inn-latin]
nsc 11319
1ca ,
kendall's desoxy compound b
desoxycorticosterone
reichstein's substance q
nsc-11319
11-dehydroxycorticosterone
21-hydroxyprogesterone
11-desoxycorticosterone
progesterone, 21-hydroxy-
deoxycortone
corticosterone, 11-deoxy-
NCGC00016292-01
cas-64-85-7
BSPBIO_000954
BPBIO1_001050
[4-14c]-11-deoxycorticosterone
desoxycorticosteronum
21-hydroxy-delta4-pregnane-3,20-dione
'reichstein q'
delta4-pregnene-21-ol-3,20-dione
desoxicortonum
1,2(3h)-deoxycorticosterone
21-hydroxy-3,20-dioxopregn-4-ene
cmc_13409
21-hydroxy-delta4-pregnene-3,20-dione
desossicortone
pregn-4-ene-3,20-dione, 21-hydroxy-
11-dcortic
AB00490029
desoxycortone
C03205
64-85-7
11-deoxycorticosterone ,
DOC ,
deoxycorticosterone
21-hydroxy-4-pregnene-3,20-dione
cortexone
21-hydroxyprogesterone, >=97% (hplc)
smr000058340
SPBIO_003103
PRESTWICK0_000957
PRESTWICK1_000957
NCGC00021304-03
21 hydroxy 4 pregnene 3,20 dione
11-deoxy-corticosterone
11-decorticosterone
11 decorticosterone
21 hydroxyprogesterone
BD5D7BC9-0CD8-404E-9BA0-F670962012F8
CHEMBL1498
BMSE000535
D07792
desoxycortone (inn)
AKOS005111365
HMS1570P16
(8s,9s,10r,13s,14s,17s)-17-(2-hydroxyacetyl)-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one
HMS2097P16
desoxycortone [inn:ban]
unii-40gp35yq49
40gp35yq49 ,
desoxicortona
dtxcid8025254
dtxsid0045254 ,
tox21_302402
NCGC00256184-01
tox21_110356
HMS2235G07
desoxycortone [inn]
21-hydroxy-pregn-4-ene-3,20-dione
21-hydroxy-.delta.4-pregnene-3,20-dione
desoxycortone [who-dd]
desoxycorticosterone [vandf]
desoxycortone [mart.]
deoxycorticosterone [mi]
CCG-220957
bdbm8582
(1s,2r,10s,11s,14s,15s)-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0;{2,7}.0;{11,15}]heptadec-6-en-5-one
SCHEMBL4065
NCGC00021304-05
tox21_110356_1
hydroxy-4-pregnene-3,20-dione
4-pregnene-3,20-dione-21-ol
W-104814
doca (salt/mix)
21-hydroxypregn-4-ene-3,20-dione #
11-deoxy corticosterone
OPERA_ID_581
SR-01000003106-2
sr-01000003106
desoxycorticosteron
HMS3714P16
21-hydroxy-d4-pregnene-3,20-dione
d4-pregnene-21-ol-3,20-dione
21-hydroxy-progesterone
21-hydroxy-d4-pregnane-3,20-dione
(14beta)-21-hydroxypregn-4-ene-3,20-dione
4-pregnen-21-ol-3,20-dione; doc; 21-hydroxyprogesterone
(8s,10r,13s,17s)-17-(2-hydroxy-acetyl)-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanthren-3-one
Q948846
CS-0059402
HY-113414
AS-77189
acatate de dasoxycortone
desoxycortonum (inn-latin)
desoxicortona (inn-spanish)
h02aa02
desoxycortone (mart.)

Research Excerpts

Overview

Desoxycorticosterone pivalate is a suggested alternative treatment in these and all other cases of hypoadrenocorticism.

ExcerptReferenceRelevance
"Desoxycorticosterone pivalate is a suggested alternative treatment in these and all other cases of hypoadrenocorticism."( Desoxycorticosterone pivalate in the management of canine primary hypoadrenocorticism.
Hyman, WB; Van Zyl, M, 1994
)
2.45

Treatment

Rats treated with desoxycorticosterone acetate and sodium chloride (DOCA/NaCl) developed a time-dependent increase in blood pressure. This was associated with a reduced in vitro beta- and an elevated alpha-adrenergic responsiveness.

ExcerptReferenceRelevance
"Rats treated with desoxycorticosterone acetate and sodium chloride (DOCA/NaCl) developed a time-dependent increase in blood pressure which was associated with a reduced in vitro beta- and an elevated alpha-adrenergic responsiveness. "( Time course alterations in vascular adrenergic responsiveness in the DOCA/NaCl-treated rat.
Field, FP; Iloeje, E; Katovich, MJ; Soltis, EE, 1984
)
0.6
"Treatment with desoxycorticosterone acetate (DOCA) and methyl prednisolone acetate also increased the number of animals surviving after adrenalectomy."( Effects of adrenalectomy on reproduction in the mouse.
Emmens, CW; Gidley-Baird, AA; White, BM, 1980
)
0.6
"Treatment with desoxycorticosterone alone produced intense staining in the organum vasculosum of the laminal terminalis and some staining in the median preoptic nucleus."( Increased sodium appetite stimulates c-fos expression in the organum vasculosum of the lamina terminalis.
Fitzsimons, JT; Herbert, J; Lane, JM, 1997
)
0.64
"Treatment with desoxycorticosterone acetate (DOCA) and 1 per cent saline as drinking water for 21 days caused a significant and similar increase in blood pressure in haired mice, with a normal thymus function, as in nude mice with genetical aplasia of the thymus. "( Evidence for an initial, thymus independent and a chronic, thymus dependent phase of DOCA and salt hypertension in mice.
Svendsen, UG, 1976
)
0.61
"Treatment with desoxycorticosterone resulted in an increased GFR but with impaired urine concentrating capacity."( Effects of triamcinolone and of desoxycorticosterone on renal function in sheep.
Gans, JH, 1975
)
0.88

Toxicity

ExcerptReferenceRelevance
" In DCA-saline pretreated rats the LD50 of isoproterenol was determined to be 14."( Potentiation of isoproterenol cardiotoxicity by corticoids.
Green, M; Guideri, G; Lehr, D, 1978
)
0.26
"This study tested the hypothesis that the adverse effects of cyclosporine (Cy) are accelerated in animals with induced hypertension."( Cyclosporine-induced nephrotoxicity in deoxycorticosterone-NaCl treated rats.
Abrahamson, DR; Mozaffari, MS; St John, PL; Wyss, JM, 1993
)
0.29

Pharmacokinetics

ExcerptReferenceRelevance
" administration, the pharmacokinetic and pharmacodynamic parameters of bumetanide did not vary significantly between SHRs and the control Wistar rats."( Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to spontaneously hypertensive rats and DOCA-salt induced hypertensive rats.
Han, KS; Kim, ND; Lee, MG; Lee, SH, 1993
)
0.29
" However, the increase in the two aforementioned pharmacokinetic parameters in the case of M4 were possibly due solely to the increased amount of aldo-keto reductase in the liver."( Pharmacokinetics of DA-125, a new anthracycline, after intravenous administration to spontaneously hypertensive rats and DOCA-salt-induced hypertensive rats.
Kim, WB; Lee, JJ; Lee, MG; Lee, SD; Shim, HJ; Yang, J; Yoon, EJ, 1997
)
0.3
" The above pharmacokinetic parameter changes in 16-week-old SHRs were due to both hereditary characteristic of SHRs and the hypertensive status itself."( Pharmacokinetics of a new proton pump inhibitor, YJA-20379-8, after intravenous and oral administration to spontaneously hypertensive rats and DOCA-salt-induced hypertensive rats.
Chang, MS; Chung, YK; Han, KS; Kim, HJ; Kim, YG; Lee, MG, 2000
)
0.31
" The pharmacokinetic and pharmacodynamic profile was determined in rodents in vivo."( Pharmacokinetic and pharmacodynamic properties of SOL1: a novel dual inhibitor of neutral endopeptidase and endothelin converting enzyme.
Bassissi, F; Bindl, M; De Mey, JG; Janssen, BJ; Jasserand, D; Lemkens, P; Nelissen, J; Sann, H, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
"On a model of transplantable albeolar-mucous RS cancer it is shown that hydrocortisone, desoxycorticosteonre-acetate (DOCA), cyanocobalamine used in combination with folic and nicotinic acids does not lower the cytostatic activity of thiophosphamide and in a number cases even potentiates its action."( [Effect of corticosteroids, vitamins and their combination with thiophosphamide on the indicators of carbohydrate and electrolyte metabolism of animals with experimental tumors].
Butov, VI; Dunaev, VV,
)
0.13
"The paper presents data on the content of corticosteroids in adrenals of rats exposed to 46, 53- and 60-day hypokinesia as well as to 60-day hypokinesia combined with graded exercises."( [Rat adrenal corticosteroid concentration during hypokinesia combined with measured physical exertion].
Zagorskaia, EA,
)
0.13

Bioavailability

ExcerptReferenceRelevance
" The low oral bioavailability of SK&F 104078 did not appear to be due to high first-pass oxidative metabolism, since pretreatment of SHR with the suicide substrate inhibitor of cytochrome P-450, 1-aminobenzotriazole (ABT), did not result in increased oral efficacy."( Cardiovascular effects of SK&F 104078, a novel alpha-adrenoceptor antagonist, in normotensive and hypertensive rats.
Gombar, CT; Gutzait, L; Hieble, JP; Sulpizio, AC, 1990
)
0.28
" Torasemide was practically fully absorbed by the gastrointestinal tract, its bioavailability by oral route ranged from 80 to 100%."( Pharmacological properties of the new potent diuretic torasemide in rats and dogs.
de Suray, JM; Delarge, J; Denef, J; Georges, A; Gerin, M; Ghys, A; Willems, J, 1985
)
0.27
" In additional experiments, similar procedures were followed with an alternate vehicle (1% Tween-80 instead of sesame oil) and a longer initial progestin-to-facilitation test interval (8 rather than 4 hours) in attempts to improve bioavailability of the steroids."( The relative effectiveness of progestins for facilitation and inhibition of sexual receptivity in hamsters.
DeBold, JF; Pleim, ET, 1984
)
0.27
" In animal studies, compound 6 (CCD 1042) is an orally active anticonvulsant, while the naturally occurring progesterone metabolites 1 and 2 are inactive when administered orally, suggesting that 3 beta-substitution slows metabolism of the 3-hydroxyl, resulting in orally bioavailable steroid modulators of the GABAA receptor."( Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Acosta-Burruel, M; Alauddin, M; Bolger, MB; Gee, KW; Hawkinson, JE; Hogenkamp, DJ; Kimbrough, CL; Lan, NC; Tahir, SH; Upasani, RB; Whittemore, ER; Woodward, RM, 1997
)
0.3
" Bioavailability of TA-606 was 11 times higher than that of 606A in Sprague-Dawley rats, with consistent hypotensive potencies in spontaneously hypertensive rats (SHRs)."( Pharmacologic profile of TA-606, a novel angiotensin II-receptor antagonist in the rat.
Hashimoto, Y; Hayashida, K; Kaji, H; Kurosawa, Y; Minami, K; Murata, S; Narita, H; Ohashi, R, 1998
)
0.3
" In control rats, the elimination half-life of pirfenidone following a single intravenous dose of 200 mg kg(-1) was 37 min while oral bioavailability at this dose was 25."( Attenuation of cardiac fibrosis by pirfenidone and amiloride in DOCA-salt hypertensive rats.
Brown, L; Fenning, A; Margolin, SB; Mirkovic, S; Seymour, AM; Strachan, A; Taylor, SM, 2002
)
0.31
" These data indicate that there is reduced purinergic input to mesenteric arteries of DOCA-salt rats because of decreased ATP bioavailability in sympathetic nerves."( Impaired purinergic neurotransmission to mesenteric arteries in deoxycorticosterone acetate-salt hypertensive rats.
Demel, SL; Galligan, JJ, 2008
)
0.35
" The mechanism may involve decreased production of nitric oxide via endothelial nitric oxide synthase (eNOS), impaired bioavailability of nitric oxide, and elevated plasma levels of asymmetric dimethylarginine (ADMA)."( Salt-induced hemodynamic regulation mediated by nitric oxide.
Arakawa, K; Toda, N, 2011
)
0.37
" Preincubation with sepiapterin (10 μmol/l for 30 min) failed to improve NO(·) bioavailability in hypertensive aortas while it augmented NO(·) production from control vessels, implicating a hypertension-associated deficiency in sepiapterin reductase (SPR), the rate-limiting enzyme for sepiapterin conversion to H(4)B."( Endothelium-specific sepiapterin reductase deficiency in DOCA-salt hypertension.
Blair, J; Cai, H; Harrison, DG; Laude, KM; McCann, LA; Oak, JH; Wang, T; Youn, JY, 2012
)
0.38
" The bioavailability of vasoactive peptides was modified by chronic treatment of the rats with the dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor SOL1."( Impaired flow-induced arterial remodeling in DOCA-salt hypertensive rats.
De Mey, JG; Debets, JJ; Fazzi, GE; Janssen, BJ; Janssen, GJ; Lemkens, P; Meens, MJ; Nelissen, J; Schiffers, PM, 2012
)
0.38
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" A satisfactory IVIVR was generated for cortisone, whereas testosterone and desoxycorticosterone showed higher bioavailability in vitro compared to in vivo."( Percutaneous absorption of steroids from finite doses: Predicting urinary excretion from in vitro skin permeation testing.
Anissimov, YG; Cheruvu, HS; Ghosh, P; Grice, JE; Liu, X; Ni, Z; Roberts, MS; Tsakalozou, E; van der Hoek, J, 2022
)
0.95

Dosage Studied

Desoxycorticosterone pivalate (DOCP) is a commonly used mineralocorticoid replacement for dogs with primary hypoadrenocorticism (HA) Manufacturer-recommended dosing protocols can be cost-prohibitive.

ExcerptRelevanceReference
"Young, unilaterally nephrectomized, female Sprague-Dawley rats were given daily sc injections of 19-nor-deoxycorticosterone acetate (19-nor-DOCA) in oil at a dosage of 100 micrograms/day for 21 days and twice that amount for a further 11 days."( Influence of 19-nor-deoxycorticosterone on blood pressure, saline consumption, and serum electrolytes, corticosterone, and renin activity.
Gomez-Sanchez, CE; Hall, CE; Holland, OB; Nasseth, D, 1979
)
0.26
" The catecholamine depletion occurred in all the peripheral tissues examined but in the brain was restricted to certain regions, these being the hind-brain on single dosing and the hind-brain, hypothalamus and mid-brain on repeated dosing."( BRL 13776: a novel antihypertensive agent with interesting monoamine depleting properties.
Melrose, J; Palfreyman, MG; Poyser, RH; Whiting, RL, 1977
)
0.26
" There also was a shift to the left in the dose-response curves."( Whole body vascular reactivity during the development of deoxycorticosterone acetate hypertension in the pig.
Berecek, KH; Bohr, DF, 1978
)
0.26
" Slight hypertension did develop at 3 weeks in salt-loaded rats on the lowest dose, but this was neither increased by higher dosage or longer treatment, nor reflected by increased heart or kidney weight."( Experimental hypertension and other responses to 18-hydroxy-deoxycorticosterone treatment in the rat.
Gomez-Sanchez, CE; Hall, CE; Hall, O; Holland, OB; Nasseth, D, 1978
)
0.26
" In response to intra-arterial injections of norepinephrine, hypertensive pigs (n = 8) demonstrated shifts in the dose-response curves to the left and lower vasoconstrictor thresholds than controls (n = 10)."( Structural and functional changes in vascular resistance and reactivity in the deoxycorticosterone acetate (DOCA)-hypertensive pig.
Berecek, KH; Bohr, DF, 1977
)
0.26
" After the strips had been contracted by 3x10-6M phenylephrine, a concentration which was able to produce an about 90% maximal contraction, dose-response curves to the relaxant effect of isoprenaline were determined in the absence and in the presence of U-0521 (10-4M)."( Relation between the amount of smooth muscle of venous tissue and the degree of supersensitivity to isoprenaline caused by inhibition of catechol-O-methyl transferase.
Azevedo, I; Cardoso, W; Guimarães, S; Oliveira, MC, 1975
)
0.25
" The dose-response curves to all three vasoconstrictor agents obtained from hypertensive animals exhibited a steeper slope, and higher maximum without any significant change in the threshold dose suggesting that adaptive/structural changes in the blood vessels had taken place."( An increased reactivity in hypertensive rats unaffected by prolonged antihypertensive therapy.
Finch, L, 1975
)
0.25
" The glucocorticoid effect on motoneuron outlasts the dosing period, suggesting an underlying alteration in the neuron."( Glucocorticoids and mammalian motor nerve excitability.
Baker, T; Okamoto, M; Riker, WF, 1975
)
0.25
" The experiments have indicated that 11-desoxycorticosterone acetate (DOCA) injected intramuscularly in the dosage of 30-45 and 80-90 mg/Kg daily during 6-8 days (terms of observation-14-16 days since the moment of tumor transplantation) lessens the antiblastic effect of prospidine (injected intraperitoneally in the same dosage and regimen), especially in an impaired mineral metabolism, caused by adrenalectomy."( [The effect of 11-deoxycortiocosterone acetate on the antitumor activity of prospidin].
Chernov, VA; Kravchenko, AI, 1975
)
0.52
"In previously untreated rats, pretreatment with enalaprilat shifted the dose-response curve for the hypotensive effect of doxazosin to the left, indicating synergism."( A study of the interaction between the hypotensive actions of doxazosin and enalaprilat in anaesthetized rats.
Marwood, JF; Stokes, GS; Tierney, G, 1992
)
0.28
"8 mM) in the bath significantly depressed the dose-response curve to noradrenaline in aorta with endothelium."( [In vitro study of the role of endothelium on the vasorelaxant effect of magnesium on the aorta from DOCA-salt hypertensive rats].
Berthelot, A; Laurant, P, 1992
)
0.28
"The aim of this double blind placebo-controlled cross-over study was to evaluate the effects of fadrozole, a new oral nonsteroidal aromatase inhibitor, on basal and stimulated cortisol and aldosterone secretion at a daily dosage of 4 mg given for 14 days to eight healthy men."( The effects of fadrozole hydrochloride on aldosterone secretion in healthy male subjects.
Aupetit, B; Bhatnagar, AS; Ezzet, F; Girard, F; Menard, J; Mueller, P; Trunet, PF; Zognbi, F, 1992
)
0.28
" Tolerance of the antihypertensive effect of TC-81 in long-term daily dosing and the rebound phenomenon after discontinuance of the treatment were not observed in hypertensive rats."( Antihypertensive effect of the new calcium antagonist (+-)-3-(benzylmethylamino)-2,2-dimethylpropyl-methyl-4-(2-fluoro-5- nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate hydrochloride in rats.
Aoki, K; Kishimoto, T; Naruchi, T; Okamiya, Y; Sunakawa, K; Takeshita, T; Tanabe, H, 1992
)
0.28
" Compared to WKY, the dose-response curve for the inhibition of dopamine release by quinpirole was shifted to the left in SHR and the maximal inhibition in response to the highest dose was significantly greater."( Effect of the dopamine D2 receptor agonist quinpirole on the in vivo release of dopamine in the caudate nucleus of hypertensive rats.
De Jong, W; De Lang, H; Linthorst, AC; Versteeg, DH, 1991
)
0.28
" bolus dosing with 125I-labelled ANF 99-126."( Neutral metalloendopeptidase inhibitors as ANF potentiators: sites and mechanisms of action.
Chiu, PJ; Sybertz, EJ; Vemulapalli, S; Watkins, RW, 1991
)
0.28
"Behavioral performances of six baboons were tested during chronic oral dosing with diuretic (hydrochlorothiazide/triamterene), a calcium channel blocker (verapamil), and a combination of the two drugs."( Behavioral effects of chronic, orally administered diuretic and verapamil in baboons.
Hienz, RD; Turkkan, JS, 1991
)
0.28
" Most of this compounds showed significant diuretic activity at the dosage of 3-24 mg/kg."( Diuretic and hypotensive activities of 4-anilino derivatives of 2-methylthiopyrido[2,3-d]pyrimidines.
Artigas, P; Bellver, C; Fernandez, FJ; Martinez-Merino, V; Monge, A; Ochoa, MC; Sanmartin, C, 1990
)
0.28
" ACH dose-response curves for dexamethasone (DM)- and corticosterone (B)-treated but not deoxycorticosterone (DOC)-treated BSM were significantly shifted to the right; this provides evidence that glucocorticoid treatment reduced the sensitivity of BSM to ACH."( Effect of acetylcholine and morphine on bronchial smooth muscle contraction and its modulation by steroid hormones.
Kadir, BA; Khalid, BA; Morat, PB; Nabishah, BM, 1990
)
0.28
" The hypotensive action in spontaneously hypertensive rats was reproducible after repeated dosing twice a day for 29 days."( Antihypertensive and diuretic effects of NZ-105, a novel dihydropyridine derivative.
Arakawa, C; Hibi, M; Kasuya, Y; Masuda, Y; Sakai, T; Shigenobu, K; Takeguchi, M; Tanaka, S,
)
0.13
" By the end of pregnancy with increasing body mass of the female rats, the hormonal dosage dropped."( [Morphofunctional characteristics of the skin of newborn rat pups with prenatal exposure to desoxycorticosterone acetate].
Pavlova, IG, 1987
)
0.49
" Although maximal reduction in systolic blood pressure at single oral dosing of TF-80 (50, 100 mg/kg) and FA (15, 30 mg/kg) was approximately the same extent, respectively, the antihypertensive action of TF-80 was longer-lasting than that of FA."( [Antihypertensive action of dl-alpha-tocopherol 5-n-butyl-2-pyridinecarboxylate (TF-80)].
Nagura, J; Nakajima, A; Nishikibe, M; Shioya, M, 1986
)
0.27
" These effects were mitigated at a lower dosage especially by the addition of cefoxitin and deoxycortone."( An attempt to develop a model to study the effects of intrathecal steroids.
Rosen, M; Swai, EA, 1986
)
0.27
" Dose-response curves to NE were generated in normal (5."( Sodium pump activity and norepinephrine responsiveness of femoral arterial smooth muscle from DOCA-salt rats.
Field, FP; Soltis, EE, 1987
)
0.27
" The acetylcholine dose-response curves for steroid pretreated ileum but not duodenum were significantly shifted to the right; evidence that pretreated ileum required higher dose of acetylcholine than normal to cause 50% maximal contraction."( The effect of corticosteroid pretreatment in vivo on the contraction of guinea-pig ileum and duodenum.
Alias, AK; Idid, SZ; Khalid, BA; Merican, Z; Morat, P, 1987
)
0.27
" Dose-response curves in low Ca2+ (0."( Extracellular calcium and altered vascular responsiveness in the deoxycorticosterone acetate-salt rat.
Field, FP; Soltis, EE, 1986
)
0.27
" Pargyline and tranylcypromine shifted the dose-response curves for tyramine and beta-phenylethylamine, but not serotonin, to the left, indicating inhibition of type B MAO."( Some cardiovascular effects of monoamine oxidase inhibitors in unanaesthetized rats.
Huston, V; Marwood, JF; Wall, KT,
)
0.13
" In each of three repeated measures, females given an intermediate dosage (800 micrograms/animal/injection) showed substantially higher levels of receptivity than those given vehicle injections or other dosages."( Facilitation of sexual receptivity in female mice through blockade of adrenal 11 beta-hydroxylase.
de Catanzaro, D; Kerr, TH; Lee, PC, 1985
)
0.27
"The hypertensogenic effect of 18-oxocortisol, an aldosterone analogue possessing both mineralocorticoid and glucocorticoid properties, was studied at the same dosage but under different experimental conditions in two experiments."( Hypertensive potency of 18-oxocortisol in the rat.
Gomez-Sanchez, CE; Hall, CE, 1986
)
0.27
" Dose-response curves to arachidonate (10(-10) to 10(-4) g/ml) in arteries from DOCA and 2K-1C hypertensive rats were shifted to the left compared to those in arteries from control rats."( Vascular responses to sodium arachidonate in experimental hypertension.
Lockette, WE; Webb, RC, 1985
)
0.27
" To eliminate ACTH-dependent steroid synthesis, the experiments were performed in subjects receiving constant dosage of dexamethasone."( Site of stimulation of aldosterone biosynthesis by angiotensin and potassium.
Brown, RD; Liddle, GW; Strott, CA, 1972
)
0.25
" The best dose-response curves indicated that DOC was nearly 5 times more potent than hydrocortisone at comparable dosages."( Effects of desoxycorticosterone and hydrocortisone singly and in various combinations on in vitro maturation of oocytes of the catfish, Heteropneustes fossilis (Bloch).
Goswami, SV; Sundararaj, BI, 1971
)
0.64
"2-200 mug/d) concurrently suppressed plasma ir-ACTH and ir-betaEP, with a near maximal effect at 20 mug, and a half-maximal effect between 2 and 6 mug; similar dose-response characteristics were found for thymolysis."( Glucocorticoid and mineralocorticoid effects on adrenocorticotropin and beta-endorphin in the adrenalectomized rat.
Clements, J; Funder, JW; Khalid, BA; Lim, AT, 1982
)
0.26
"6 to 2,000 mug) of concentrations of DM administered daily for 7 d, the dose-response curve of DM for induction of pulmonary ACE mirrored that for thymolysis; for both, half-maximal effects were seen at approximately 6 mug DM/d, and plateau levels at 60 mug/d."( Induction by glucocorticoids of angiotensin converting enzyme production from bovine endothelial cells in culture and rat lung in vivo.
Funder, JW; Kachel, C; Lloyd, CJ; Mendelsohn, FA, 1982
)
0.26
" These results as well as the time-course and dose-response data imply that the response is mediated by the glucocorticoid receptor pathway."( Glucocorticoid stimulation of Na-K-ATPase in superfused distal segments of kidney tubules in vitro.
Edelman, IS; Rayson, BM, 1982
)
0.26
" The mesenteric arteries from all three types of hypertensive rats showed an increased reactivity to noradrenaline as characterized by a steeper dose-response curve and elevated maximal vasoconstriction when compared with normotensive controls."( Vascular reactivity of rats after prevention of hypertension by central administration of 6-hydroxydopamine.
Haeusler, G, 1984
)
0.27
" Cumulative dose-response curves to NE or KC1 were similar for strips from controls and hypertensive animals in both forms of hypertension."( Contractile responses of vasa deferentia from rats with genetic and experimental hypertension.
Daniel, EE; Kwan, CY; Sakai, Y, 1984
)
0.27
"In DOCA-pretreated men during hypotonic polyuria Dopamine (DA) infusion in a subpressor dosage (0."( [Sulpiride (stereoisomers, racemic) and dopamine: actions and interactions on tubular reabsorption].
Agnoli, GC; Andreone, P; Cacciari, M; Garutti, C; Ikonomu, E; Lenzi, P, 1984
)
0.27
" Captopril was infused intravenously in graded dosage from 10 to 3,000 microgram/kg, and renal blood flow measured with an electromagnetic flowmeter."( Specificity of renal vasodilation with captopril: saralasin prevents the response in the DOCA-treated, salt-loaded rabbit.
Hollenberg, NK; Passan, DR, 1982
)
0.26
" Pressor reponses to angiotensin II were increased, dose-response curve (d."( Effect of sodium, deoxycorticosterone and duration of hypertension on pressor responses in rats.
Bing, RF; Russell, GI; Swales, JD; Thurston, H, 1982
)
0.26
" A dose-response curve constructed by counting the number of cells on day 16, or at regular intervals, showed that glucocorticoids (hydrocortisone and cortisone) and mineralocorticoids (aldosterone and deoxycorticosterone) caused an increase in cell density when added at physiological concentrations or higher."( Effects of various steroids on in vitro lifespan and cell growth of human fetal lung fibroblasts (WI-38).
Kasuga, H; Kondo, H; Noumura, T,
)
0.13
" Complete vasopressin/blood pressure dose-response curves were constructed from circulating plasma vasopressin concentrations measured at the end of each infusion."( Effect of acute vasopressin infusion on blood pressure and plasma angiotensin II in normotensive and DOCA-salt hypertensive rats.
Garcia del Rio, C; Hughes, MJ; Morton, JJ, 1982
)
0.26
" Both NNT and EDP did not affect blood pressure in normotensive animals but significantly reduced blood pressure in SHR and DOCA/salt hypertensive animals in the acute studies with single dosing of 1 to 10 mg/kg (p."( Antihypertensive actions of isoprenoids.
Igarashi, T; Mori, N; Nakajima, Y; Saeki, T, 1982
)
0.26
" Intraarterial injections of norepinephrine produced a dose-response curve for precapillary vessels in the hypertensive group that was asymmetrically shifted to the left (increased slope) and exhibited a significant decrease in vasoconstrictor threshold."( Pre- and postcapillary vascular responses to sympathetic nerve stimulation in DOCA-hypertensive dogs.
Brock, TA; Diana, JN; Fleming, BP,
)
0.13
" In isolated perfused hindlimb preparations from rats which had received DOCA for 7 days, the dose-response curve to noradrenaline but not that to KCl was shifted to the left."( Plasma catecholamines, noradrenaline metabolism and vascular response in desoxycorticosterone acetate hypertension of rats.
Dietz, R; Gross, F; Rascher, W; Schömig, A; Weber, J, 1981
)
0.49
" Dose-response curves for NE and ADH showed parallel leftward shifts and decreased threshold doses."( Significance of sodium, sympathetic innervation, and central adrenergic structures on renal vascular responsiveness in DOCA-treated rats.
Berecek, KH; Gross, F; Murray, RD, 1980
)
0.26
" After treatment with DOCA/salt for 1, 3 and 4 weeks, aortic and portal vein strips were prepared from control and treated rats for studies of cumulative dose-response relationships to noradrenaline (NA) in Krebs' solutions containing normal (2."( Contractile responses of aortic and portal vein strips during the development of DOCA/salt hypertension.
Pang, CC; Sutter, MC, 1980
)
0.26
" After 3 weeks of treatment with hydralazine, cumulative dose-response relationships to NA were studied using aortic and portal vein strips from hydralazine-treated and control rats."( Hydralazine prevents changes in the contractile response of aortic but not portal vein strips in hypertensive rats.
Pang, CC; Sutter, MC, 1980
)
0.26
" Height SD score for age (HtSDS(ca)), HtSDS for bone age (HtSDS(ba)), BMI and steroid dosage in early childhood (3."( Adult height in women with early-treated congenital adrenal hyperplasia (21-hydroxylase type): relation to body mass index in earlier childhood.
Grant, DB; Yu, AC, 1995
)
0.29
" These results suggested that AJ-2615 has potential as a long-acting (once daily dosage regimen) antihypertensive drug without causing a steep blood pressure fall and tachycardia."( Antihypertensive effects of AJ-2615, a new calcium antagonist with alpha 1-adrenergic blocking activity in experimental hypertensive animals.
Fukuya, F; Hosoki, K; Ikeno, A; Karasawa, T; Minato, H; Nose, I; Takeyama, K, 1993
)
0.29
" In genetic and renal hypertensive rats, the antihypertensive effect induced after acute dosing of SR 47436 was similar to that observed after losartan and enalapril."( Efficacy of SR 47436 (BMS-186295), a non-peptide angiotensin AT1 receptor antagonist in hypertensive rat models.
Canals, F; Cazaubon, C; Galindo, G; Lacour, C; Nisato, D; Segondy, D, 1994
)
0.29
" All C21-deoxysteroids, except 11,19-oxidoprogesterone, exhibited parabolic log dose-response functions, indicating an effect that opposes renal sodium retention at high doses."( Sodium-retaining activity of some natural and synthetic 21-deoxysteroids.
Brachet-Cota, AL; Burton, G; Damasco, MC; De Lavallaz, S; Galigniana, M; Ghini, AA; Lantos, CP; Sproviero, EM, 1995
)
0.29
" 18-E-DOC inhibited the stimulated secretion of aldosterone and 18-hydroxycorticosterone in a similar dose-response and time fashion."( 18-Ethynyl-deoxycorticosterone inhibition of steroid production is different in freshly isolated compared to cultured calf zona glomerulosa cells.
Chiou, S; Gomez-Sanchez, CE; Yamakita, N, 1993
)
0.29
"The carfentamil-xylazine combination at the dosage used induced hypoxemia, pronounced arterial hypertension, and significant increase in plasma norepinephrine and decrease in plasma 3,4-dihydroxyphenylacetic acid concentrations in bongo antelopes."( Effects of a carfentanil-xylazine combination on cardiopulmonary function and plasma catecholamine concentrations in female bongo antelopes.
Citino, SB; Dawson, R; Schumacher, J, 1997
)
0.3
" Neither bicuculline nor GABA altered the dose-response of steroids in the [3H]GHB assay, suggesting that there was no GABAA component involved in the steroid-inhibition of [3H]GHB binding."( Steroid-inhibition of [3H]gamma-hydroxybutyric acid (GHB) binding in thalamic relay nuclei increases during absence seizures.
Banerjee, PK; Liu, CC; Snead, OC, 1998
)
0.3
" Cumulative dose-response curves to bradykinin induced an important vasodilation in NTRs, with a maximal response that remained unaffected in the presence of either NNLA (30 pmol/I), indomethacin (10 pmol/l) or the two combined."( Altered coronary dilation in deoxycorticosterone acetate-salt hypertension.
de Champlain, J; Lamontagne, D; Millette, E, 2000
)
0.31
" In dose-response studies, DOC suppressed MMT seizures with an ED(50) of about 5 mg/kg (sc)."( Dose-, time-, age-, and sex-response profiles for the anticonvulsant effects of deoxycorticosterone in 15-day-old rats.
Burnham, WM; Edwards, HE; Vimal, S, 2002
)
0.31
" Angiotensin II dose-response curves were studied in rat perfused pressurized small-diameter arteries in the presence of losartan (AT1R antagonist)."( High-salt diet inhibits expression of angiotensin type 2 receptor in resistance arteries.
Castillo, F; Galleguillos, L; Gonzalez, M; Lobos, L; Lopez, NC; Michea, L, 2005
)
0.33
" The GABA dose-response properties of alpha(1)-beta(3)-alpha(1)/beta(3)-delta and beta(3)-alpha(1)-delta/alpha(1)-beta(3) match most closely the properties of non-concatenated alpha(1)beta(3)delta receptors."( Unanticipated structural and functional properties of delta-subunit-containing GABAA receptors.
Baur, R; Kaur, KH; Sigel, E, 2009
)
0.35
" Desoxycorticosterone acetate (DCA) and NaCl, in the dosage employed in normal rats, caused renal and cardiac hypertrophy, characteristic changes in the renal tubular epithelium, atrophic changes in the subcapsular zone of the adrenal cortex, and serum electrolyte changes characterized by a rise in sodium and fall in potassium."( DESOXYCORTICOSTERONE ACETATE : THE POTENTIATION OF ITS ACTIVITY BY SODIUM CHLORIDE.
Knowlton, AI; Loeb, EN; Seegal, BC; Stoerk, HC, 1947
)
2.58
" For this purpose, we measured plasma concentrations of adrenal steroids in rats dosed with ketoconazole, a known inhibitor of adrenal steroidogenesis, and examined its relationship with the changes in histopathology and mRNA expression of steroidogenic enzymes in the adrenal gland."( Changes in plasma concentrations of corticosterone and its precursors after ketoconazole administration in rats: An application of simultaneous measurement of multiple steroids using LC-MS/MS.
Fujii, Y; Funabashi, H; Kouchi, M; Matsumoto, I; Miyawaki, I; Tochitani, T; Yamada, T; Yamashita, A,
)
0.13
"Clinicians alter dosing for desoxycorticosterone pivalate (DOCP) to mitigate costs, but this practice has not been critically evaluated in a prospective clinical trial."( Desoxycorticosterone Pivalate Duration of Action and Individualized Dosing Intervals in Dogs with Primary Hypoadrenocorticism.
Cannon, AB; DeClue, AE; Jaffey, JA; Nurre, P, 2017
)
2.19
" Overall, the final DOCP dosing interval for all dogs that completed phase II (n = 36) ranged from 38 days to 90 days (median, 58 days; CI, 53, 61)."( Desoxycorticosterone Pivalate Duration of Action and Individualized Dosing Intervals in Dogs with Primary Hypoadrenocorticism.
Cannon, AB; DeClue, AE; Jaffey, JA; Nurre, P, 2017
)
1.9
" Plasma concentrations of corticosterone and its precursors were examined in rats dosed with compounds that affect adrenal steroidogenesis via different modes of action as well as the relationships of the changes with blood chemistry and adrenal histopathology."( Usefulness of Simultaneous Measurement of Plasma Steroids, Including Precursors, for the Evaluation of Drug Effects on Adrenal Steroidogenesis in Rats.
Bando, K; Fujii, Y; Kouchi, M; Matsumoto, I; Miyawaki, I; Tochitani, T; Yamada, T; Yamashita, A, 2017
)
0.46
" The DOCP dosage was adjusted to obtain an injection interval of 28-30 days and to keep serum electrolyte concentrations within the reference interval."( Evaluation of a low-dose desoxycorticosterone pivalate treatment protocol for long-term management of dogs with primary hypoadrenocorticism.
Boretti, FS; Hofer-Inteeworn, N; Hofmann-Lehmann, R; Kuemmerle-Fraune, C; Müller, C; Reusch, CE; Sieber-Ruckstuhl, NS, 2019
)
0.82
"To verify simultaneous measurement of blood levels of adrenal steroids as a tool to evaluate drug effects on adrenal steroidogenesis, dose- and time-dependent changes in blood levels of corticosterone and its precursors (pregnenolone, progesterone and deoxycorticosterone), as well as their relationship with the pathological changes in the adrenal gland, were examined in rats dosed with ketoconazole (KET)."( Dose- and time-dependent changes in blood and adrenal levels of multiple steroids in rats after administration of ketoconazole with or without ACTH.
Fujii, Y; Kouchi, M; Matsumoto, I; Miyawaki, I; Tochitani, T; Yamashita, A, 2019
)
0.51
"05), with a nonlinear dose-response trend, but the association between 11-deoxycorticosterone and T2DM was no statistical significance after adjustment."( Mineralocorticoids, glucose homeostasis and type 2 diabetes mellitus: The Henan Rural Cohort study.
Fan, M; Hou, J; Huo, W; Jiang, J; Li, L; Li, R; Liu, X; Mao, Z; Qiao, D; Tu, R; Wang, C; Wang, Y; Wei, D; Yang, X; Yu, S; Zhang, J, 2020
)
0.56
"Desoxycorticosterone pivalate (DOCP) is a commonly used mineralocorticoid replacement for dogs with primary hypoadrenocorticism (HA), but manufacturer-recommended dosing protocols can be cost-prohibitive."( Low-dose desoxycorticosterone pivalate treatment of hypoadrenocorticism in dogs: A randomized controlled clinical trial.
Berghoff, N; Brudvig, JM; Langlois, DK; Okonkowski, LK; Olivier, NB; Refsal, KR; Vincent, AM, 2021
)
2.48
" In vivo models were derived by convolution of a skin absorption input function for finite dosing with that for in vivo disposition PK."( Percutaneous absorption of steroids from finite doses: Predicting urinary excretion from in vitro skin permeation testing.
Anissimov, YG; Cheruvu, HS; Ghosh, P; Grice, JE; Liu, X; Ni, Z; Roberts, MS; Tsakalozou, E; van der Hoek, J, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[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
mineralocorticoidMineralocorticoids are a class of steroid hormones that regulate water and electrolyte metabolism.
3-oxo-Delta(4) steroidA 3-oxo steroid conjugated to a C=C double bond at the alpha,beta position.
20-oxo steroidAn oxo steroid carrying an oxo group at position 20.
21-hydroxy steroid
primary alpha-hydroxy ketoneAn alpha-hydroxy ketone in which the carbonyl group and the hydroxy group are linked by a -CH2 (methylene) group.
[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]

Pathways (32)

PathwayProteinsCompounds
Metabolism14961108
Metabolism of lipids500463
Metabolism of steroids111135
Metabolism of steroid hormones2537
Mineralocorticoid biosynthesis616
Biological oxidations150276
Phase I - Functionalization of compounds69175
Cytochrome P450 - arranged by substrate type30110
Endogenous sterols1838
Steroidogenesis1142
Adrenal Hyperplasia Type 3 or Congenital Adrenal Hyperplasia Due to 21-Hydroxylase Deficiency1142
Congenital Lipoid Adrenal Hyperplasia (CLAH) or Lipoid CAH1142
Adrenal Hyperplasia Type 5 or Congenital Adrenal Hyperplasia Due to 17 alpha-Hydroxylase Deficiency1142
17-alpha-Hydroxylase Deficiency (CYP17)1142
11-beta-Hydroxylase Deficiency (CYP11B1)1142
21-Hydroxylase Deficiency (CYP21)1142
Corticosterone Methyl Oxidase I Deficiency (CMO I)1142
Corticosterone Methyl Oxidase II Deficiency (CMO II)1142
Apparent Mineralocorticoid Excess Syndrome1142
3-beta-Hydroxysteroid Dehydrogenase Deficiency1142
Disease1278231
Diseases of metabolism69121
Metabolic disorders of biological oxidation enzymes647
Defective CYP11B2 causes CMO-1 deficiency06
Renin-angiotensin-aldosterone system (RAAS)011
Aldosterone from Steroidogenesis816
Steroid hormone precursor biosynthesis015
Mineralocorticoid biosynthesis08
Biosynthesis of aldosterone and cortisol010
Biochemical pathways: part I0466
Serotonin and anxiety04
Classical pathway of steroidogenesis with glucocorticoid and mineralocorticoid metabolism325
ACE inhibitor pathway09

Protein Targets (48)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
phosphopantetheinyl transferaseBacillus subtilisPotency79.43280.141337.9142100.0000AID1490
RAR-related orphan receptor gammaMus musculus (house mouse)Potency28.08720.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency21.87240.173734.304761.8120AID1346859; AID1346924
USP1 protein, partialHomo sapiens (human)Potency44.66840.031637.5844354.8130AID743255
GALC proteinHomo sapiens (human)Potency0.707928.183828.183828.1838AID1159614
SMAD family member 3Homo sapiens (human)Potency21.87240.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency12.20650.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency13.32560.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency28.18380.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency9.02850.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID743035; AID743036; AID743040; AID743042; AID743053; AID743054; AID743063
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.38720.011212.4002100.0000AID1030
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency17.01250.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency0.22750.000417.946075.1148AID1346784; AID1347036
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.46710.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.89400.000214.376460.0339AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency23.53540.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency22.26780.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency26.95460.001530.607315,848.9004AID1224848; AID1224849; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency21.68990.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.15640.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743091
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency14.99830.001024.504861.6448AID743212; AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency34.66540.001019.414170.9645AID743094
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency30.50760.023723.228263.5986AID743222; AID743223
IDH1Homo sapiens (human)Potency9.20000.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency89.12510.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.09380.001723.839378.1014AID743083
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency19.493819.739145.978464.9432AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.10650.057821.109761.2679AID1159526; AID1159528
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency1.12200.10009.191631.6228AID1346983
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.92900.00419.984825.9290AID504444
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency30.63790.000323.4451159.6830AID743065; AID743067
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID1454
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency41.35340.000627.21521,122.0200AID743202; AID743219
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency3.98110.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency3.98110.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency3.98110.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.48130.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency18.83440.004611.374133.4983AID624296; AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency1.77830.125912.234435.4813AID1458
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency68.58960.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency37.35650.00339.158239.8107AID1347407
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency68.58960.001551.739315,848.9004AID1259244
TAR DNA-binding protein 43Homo sapiens (human)Potency19.95261.778316.208135.4813AID652104
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 3Rattus norvegicus (Norway rat)IC50 (µMol)8.40004.90006.65008.4000AID678784
Bile salt export pumpHomo sapiens (human)IC50 (µMol)17.06000.11007.190310.0000AID1449628
Corticosteroid-binding globulinHomo sapiens (human)Ki0.02240.01323.248110.0000AID51055
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC50 (µMol)1.90001.00004.446710.0000AID681591
[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)
Sex hormone-binding globulinHomo sapiens (human)Kd0.04170.00020.34964.7863AID318680
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
glucocorticoid metabolic processCorticosteroid-binding globulinHomo sapiens (human)
negative regulation of endopeptidase activityCorticosteroid-binding globulinHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
androgen bindingSex hormone-binding globulinHomo sapiens (human)
protein bindingSex hormone-binding globulinHomo sapiens (human)
steroid bindingSex hormone-binding globulinHomo sapiens (human)
steroid bindingCorticosteroid-binding globulinHomo sapiens (human)
serine-type endopeptidase inhibitor activityCorticosteroid-binding globulinHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionSex hormone-binding globulinHomo sapiens (human)
extracellular exosomeSex hormone-binding globulinHomo sapiens (human)
extracellular regionCorticosteroid-binding globulinHomo sapiens (human)
extracellular spaceCorticosteroid-binding globulinHomo sapiens (human)
extracellular exosomeCorticosteroid-binding globulinHomo sapiens (human)
extracellular spaceCorticosteroid-binding globulinHomo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (109)

Assay IDTitleYearJournalArticle
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID162613Relative binding affinity for progestin receptor of uterus of rabbit at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID126128In vivo relative Mineralocorticoid activity in Male Sprague-Dawley rats1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives.
AID126431Relative binding affinity against Mineralocorticoid Receptor in Male Sprague-Dawley rats1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives.
AID39320Relative binding affinity for androgen receptor of prostate of rat at 2 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID51062In silico steroid binding affinity to transport protein corticosteroid binding globulin1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Compass: predicting biological activities from molecular surface properties. Performance comparisons on a steroid benchmark.
AID74373Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID23271Partition coefficient (logD7.4)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID681853TP_TRANSPORTER: inhibition of Digoxin uptake (Digoxin: 0.05 uM, Deoxycorticosterone: 100 uM) in Oatp2-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID681591TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT2-expressing HRPE cells1998The Journal of biological chemistry, Dec-04, Volume: 273, Issue:49
Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.
AID50906Inhibition of mouse constitutive androstane receptor (mCAR) activity at 10 uM was determined as percent remaining activity2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Molecular determinants of steroid inhibition for the mouse constitutive androstane receptor.
AID45742Effect on collateral sensitivity of CHRC5 cells to local anesthetics/steroids.1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID51059Binding affinity to corticosteroid binding globulin1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Three-dimensional quantitative similarity-activity relationships (3D QSiAR) from SEAL similarity matrices.
AID318680Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
An updated steroid benchmark set and its application in the discovery of novel nanomolar ligands of sex hormone-binding globulin.
AID624619Specific activity of expressed human recombinant UGT2B72000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID51055Binding affinity to human CBG receptor (corticosteroid-binding globulins)2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR.
AID74376Relative binding affinity to glucocorticoid receptor on cytosol from liver at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID468984Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 0.3 uM after 7 hrs2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone.
AID74374Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID212737Binding affinity against testosterone-binding globulin (TeBG)1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Structure-activity relationships from molecular similarity matrices.
AID1150124Relative binding affinity to guinea pig progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID468985Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone.
AID212919Binding affinity towards testosterone binding globulin is expressed as log(1/k).1996Journal of medicinal chemistry, May-24, Volume: 39, Issue:11
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.
AID680619TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.1 uM, Deoxycorticosterone: 100 uM) in Oatp1-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID51049Binding affinity against corticosteroid-binding globulin1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Structure-activity relationships from molecular similarity matrices.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID74377Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID51048In silico binding affinity to human corticosteriod binding globulin1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.
AID51054Binding affinity for corticosteroid binding globulin is expressed as log(1/k)1996Journal of medicinal chemistry, May-24, Volume: 39, Issue:11
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.
AID327555Displacement of [131I]IMTO from CYP450c 11 in Wistar rat adrenal membrane2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
New selective inhibitors of steroid 11beta-hydroxylation in the adrenal cortex. Synthesis and structure-activity relationship of potent etomidate analogues.
AID212931Binding affinity towards human testosterone binding globulin.1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.
AID680156TP_TRANSPORTER: ATP hydrolysis in membranes from DC-3F/ADX cells1996The Biochemical journal, Jul-15, Volume: 317 ( Pt 2)Effects of steroids and verapamil on P-glycoprotein ATPase activity: progesterone, desoxycorticosterone, corticosterone and verapamil are mutually non-exclusive modulators.
AID1150122Relative binding affinity to sheep progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID74375Relative binding affinity to glucocorticoid receptor on cytosol from liver at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID126435Relative binding affinity for mineralocorticoid receptor of rat kidney at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1150123Relative binding affinity to rabbit progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID220020Binding affinity towards human corticosteroid binding globulin.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID228061Binding affinity towards human testosterone binding globulin.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
AID1150121Relative binding affinity to human progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID74378Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID51058Binding affinity towards corticosteroid-binding globulin (CBG)2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique.
AID51056Binding affinity to the corticosteroid-binding globulin (CBG) receptor.2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.
AID679210TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Deoxycorticosterone: 100 uM) in OCT1-expressing HRPE cells1998The Journal of biological chemistry, Dec-04, Volume: 273, Issue:49
Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.
AID213396Glucocorticoid induced Tyrosine Aminotransferase activity relative to Dexamethasone1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID678784TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT3-expressing HRPE cells1998The Journal of biological chemistry, Dec-04, Volume: 273, Issue:49
Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.
AID212920Binding affinity against transport protein testosterone binding globulin.1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Compass: predicting biological activities from molecular surface properties. Performance comparisons on a steroid benchmark.
AID23943Diffusion constant for permeability of stratum corneum1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
The role of solvent-accessible surface area in determining partition coefficients.
AID51052In silico binding affinity to corticosteroid binding globulin (CBG)1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 1. Method and validations.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1346849Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors)2000The Journal of biological chemistry, Jun-23, Volume: 275, Issue:25
Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
AID1346902Human Mineralocorticoid receptor (3C. 3-Ketosteroid receptors)1993European journal of pharmacology, Oct-15, Volume: 247, Issue:2
Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
AID1346849Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors)1993European journal of pharmacology, Oct-15, Volume: 247, Issue:2
Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7,060)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905155 (73.02)18.7374
1990's951 (13.47)18.2507
2000's608 (8.61)29.6817
2010's294 (4.16)24.3611
2020's52 (0.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.44

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

MetricThis Compound (vs All)
Research Demand Index46.44 (24.57)
Research Supply Index8.94 (2.92)
Research Growth Index4.14 (4.65)
Search Engine Demand Index85.17 (26.88)
Search Engine Supply Index2.11 (0.95)

This Compound (46.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials52 (0.69%)5.53%
Reviews232 (3.06%)6.00%
Case Studies154 (2.03%)4.05%
Observational0 (0.00%)0.25%
Other7,150 (94.23%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]