Page last updated: 2024-12-08

cortodoxone

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

Description

Cortodoxone: 17,21-Dihydroxypregn-4-ene-3,20-dione. A 17-hydroxycorticosteroid with glucocorticoid and anti-inflammatory activities. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

11-deoxycortisol : A deoxycortisol that is cortisol in which the hydroxy group at position 11 has been replaced by a hydrogen. [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 CID440707
CHEMBL ID253144
CHEBI ID28324
SCHEMBL ID42590
MeSH IDM0005222
PubMed CID227112
CHEMBL ID1705958
CHEBI ID125417
SCHEMBL ID13352414
MeSH IDM0005222

Synonyms (158)

Synonym
smr000059123
LMST02030086
cortodoxone (usan)
EU-0101040
D03595
reichstein's substance s, >=98%
cortexolone
17-hydroxy-11-deoxycorticosterone
11-desoxyhydrocortisone
cortisol, 11-deoxy-
substance s
skf 3050
11-deoxy-17-hydroxycorticosterone
11-deoxyhydrocortisone
reichstein s
17,21-dihydroxyprogesterone
17.alpha.-hydroxycortexone
reichstein's substance s
sk&f 3050
nsc-18317
reichstein's compound s
11-dioxycortisol
corticosterone, 11-deoxy-17-hydroxy-
11-desoxy-17-hydroxycorticosterone
11-desoxycortisol
LOPAC0_001040
11-desoxycortisone
substance s, reichstein's
brn 2511358
einecs 205-805-2
cortodoxone [usan:inn:ban]
MLS001333072
MLS001333071
17,21-dihydroxypregn-4-ene-3,20-dione
pregn-4-ene-3,20-dione, 17,21-dihydroxy-
17-(1-keto-2-hydroxyethyl)-4-androsten-17alpha, 21-ol-3-one
4-pregnene-17alpha,21-diol-3,20-dione
17-hydroxydesoxycorticosterone
cmc_13429
17alpha-hydroxycortexone
17-alpha-hydroxycortexone
cortodoxona [inn-spanish]
cortodoxonum [inn-latin]
17,21-dihydroxy-4-pregnene-3,20-dione
11-deoxycortisol
152-58-9
cortodoxone
C05488
11 deoxycortisol
CHEBI:28324 ,
MLS000069440 ,
NCGC00021222-04
NCGC00021222-03
33BB233B-CC8F-413B-8901-3A73030BBA68
R 0500
NCGC00021222-05
CHEMBL253144
cortifen
skf-3050
11-deoxycortisone
17alpha,21-dihydroxy-4-pregnene-3,20-dione
(8r,9s,10r,13s,14s,17r)-17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-3-one
11-deoxy cortisol
HMS3263O21
unii-wdt5slp0hq
4-08-00-02913 (beilstein handbook reference)
wdt5slp0hq ,
cortodoxonum
cortodoxona
cas-152-58-9
dtxcid6025642
dtxsid8045642 ,
tox21_110867
CCG-205117
HMS2234L16
AKOS015969740
LP01040
S4775
(1s,2r,10r,11s,14r,15s)-14-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
gtpl5100
17.alpha.,21-dihydroxy-4-pregnen-3,20-dione
.delta.4-pregnene-17.alpha.,21-diol-3,20-dione
11-desoxy-17.alpha.-hydroxycorticosterone
17.alpha.,21-dihydroxypregn-4-ene-3,20-dione
11-desoxy-17-hydroxycorticosterone [mi]
hydrocortisone impurity f [ep impurity]
cortodoxone [inn]
4-pregnene-17.alpha.,21-diol-3,20-dione
4-pregnen-17.alpha.,21-diol-3,20-dione
cortodoxone [usan]
17.alpha.,21-dihydroxyprogesterone
bdbm50423539
sk&f-3050
SCHEMBL42590
NCGC00021222-06
tox21_110867_1
17alpha,21-dihydroxy-pregna-4-ene-3,20-dione
tox21_501040
CS-5182
HY-77839
NCGC00261725-01
17,21-dihydroxy-pregn-4-ene-3,20-dione
OPERA_ID_1433
mfcd00003662
17a,21-dihydroxyprogesterone
sr-01000076100
SR-01000076100-1
17|a inverted exclamation mark,21-dihydroxypregna-4-ene-3,20-dione
C72891
hydrocortisone imp. f (ep); 17,21-dihydroxypregn-4-ene-3,20-dione; reichstein's substance s; 11-deoxycortisol; cortexolone; hydrocortisone impurity f
11-deoxycortisol (17,21-dihydroxypregn-4-ene-3,20-dione)
11-deoxycortisol (17,21-dihydroxypregn-4-ene-3,20-dione) 1.0 mg/ml in methanol
17,21-dihydroxypregn-4-ene-3,20-dione (reichstein's substance s)
20-dione 17,21-dihydroxypregn-4-ene-3
(8r,10r,13s,17r)-17-hydroxy-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
11-deoxycortisol;cortexolone;reichstein's substance s
(8r,9s,10r,13s,14s,17r)-17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3h-cyclopenta[a]phenanthren-3-one
Q2064915
SDCCGSBI-0051010.P002
NCGC00021222-07
A936328
AS-56275
11-deoxycortisol, 1mg/ml in acetonitrile
MLS001076465
HMS3394E07
17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-3-one
17alpha,21dihydroxy progesterone
OPREA1_732056
4-pregnene-17.alpha.,20-dione
cortisol, 11-dioxy-
pregn-4-ene-3, 17,21-dihydroxy-
17,20-dione
nsc18317
smr000466922
MLS001424203
reichsteins substance s
MLS001240241
CHEBI:125417
HMS2052E07
AKOS000621769
FT-0665779
FT-0665171
HMS2232H23
CCG-101089
HMS3369P15
AB00698346-05
NC00339
SCHEMBL13352414
AKOS024304316
CHEMBL1705958
Q27216034
17-hydroxy-17-(2-hydroxy-1-oxoethyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-3-one
sr-01000310463
SR-01000310463-1
37-60-5
DTXSID00859297
pcb no.101-2,2',4,5,5'-pentachlorobiphenyl
hydrocortisone ep impurity f

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Secondary safety endpoints included clinical laboratory testing, local and systemic adverse events (AEs), physical examination/vital signs, and electrocardiogram (ECG)."( Pharmacokinetic Profile, Safety, and Tolerability of Clascoterone (Cortexolone 17-alpha propionate, CB-03-01) Topical Cream, 1% in Subjects With Acne Vulgaris: An Open-Label Phase 2a Study
Cartwright, M; Gerloni, M; Mazzetti, A; Moro, L, 2019
)
0.51
" Safety measures included adverse event frequency and severity."( Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials.
Cartwright, M; Fragasso, E; Gerloni, M; Hebert, A; Mazzetti, A; Stein Gold, L; Thiboutot, D, 2020
)
0.56
" Adverse events rates were low and mostly mild; the predominant local skin reaction was trace or mild erythema."( Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials.
Cartwright, M; Fragasso, E; Gerloni, M; Hebert, A; Mazzetti, A; Stein Gold, L; Thiboutot, D, 2020
)
0.56
"Use of clascoterone cream, 1%, for acne treatment appears to demonstrate favorable efficacy and safety with low adverse event rates."( Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials.
Cartwright, M; Fragasso, E; Gerloni, M; Hebert, A; Mazzetti, A; Stein Gold, L; Thiboutot, D, 2020
)
0.56
" Treatment-emergent adverse events (TEAEs) and local skin reactions were evaluated at months 1, 3, 6, and 9, and at any unscheduled visit(s)."( Open-label, long-term extension study to evaluate the safety of clascoterone (CB-03-01) cream, 1% twice daily, in patients with acne vulgaris.
Cartwright, M; Eichenfield, L; Fragasso, E; Gold, LS; Hebert, A; Mazzetti, A; Moro, L, 2020
)
0.56
" Safety outcomes included the proportion of patients with any treatment-emergent adverse event (TEAE) as well as incidence of any TEAE, serious adverse events (AEs), AEs related to study drug, AEs leading to study drug discontinuation, nasopharyngitis, headache, oropharyngeal pain, and vomiting."( Efficacy and safety of topical clascoterone cream for treatment of acne vulgaris: A systematic review and meta-analysis of randomized placebo-controlled trials.
Abu-Zaid, A; Al Hawsawi, KA; Alkhodaidi, ST; Alkhudaidi, IT; Magzoub, D, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" The primary objectives of this study were to determine the pharmacokinetic (PK) properties and adrenal suppression potential of clascoterone topical cream, 1% in subjects with acne vulgaris."( Pharmacokinetic Profile, Safety, and Tolerability of Clascoterone (Cortexolone 17-alpha propionate, CB-03-01) Topical Cream, 1% in Subjects With Acne Vulgaris: An Open-Label Phase 2a Study
Cartwright, M; Gerloni, M; Mazzetti, A; Moro, L, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" It has been proposed that the increased bioavailability of unmetabolized corticosterone and cortisol following 11 beta-OHSD inhibition allows these steroids to act on renal mineralocorticoid receptors to elicit the mineralocorticoid action."( The 11 beta-OHSD inhibitor, carbenoxolone, enhances Na retention by aldosterone and 11-deoxycorticosterone.
Morris, DJ; Souness, GW, 1990
)
0.28
"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

Dosage Studied

ExcerptRelevanceReference
" This dosage resulted in partial adrenal suppression, manifested by reduced levels of plasma cortisol."( Topical corticosteroid therapy and pituitary-adrenal function.
Becker, B; Krupin, T; Mandell, AI; Podos, SM, 1976
)
0.26
" The cytolytic effect exhibits well-defined dose-response relationships and specificity for glucocorticoids."( Long-term incubation of rat thymus cells: Cytolytic actions of glucocorticoids in vitro.
Leung, K; Munck, A, 1975
)
0.25
" Dose-response experiments with 20 beta-S and 17 alpha,20 beta-dihydroxy-4-pregnen-3-one (17 alpha,20 beta-P) over a range of incubation times yielded similar results for both steroids, suggesting that conversion of 17 alpha,20 beta-P to 20 beta-S is not required for 17 alpha,20 beta-P-induced GVBD."( Induction of maturation of Atlantic croaker oocytes by 17 alpha,20 beta,21-trihydroxy-4-pregnen-3-one in vitro: consideration of some biological and experimental variables.
Patiño, R; Thomas, P, 1990
)
0.28
" When the ambient cortisol level was equalized (and suppressed) in all subjects at the time of study with a threshold dosage of corticotropin-releasing hormone, we found an augmented response to corticotropin-releasing hormone in depressives."( Augmented pituitary corticotropin response to a threshold dosage of human corticotropin-releasing hormone in depressives pretreated with metyrapone.
Britton, D; Fava, GA; Hochla, P; Lisansky, J; Meikle, AW; Peake, GT; Qualls, C; Risch, SC; Strassman, RJ; Zownir-Brazis, M, 1989
)
0.28
" A dose-response curve with a high sensitivity was obtained in each 11-deoxycortisol assay system by the use of a minimum amount of the enzyme-labeled antigen at an appropriate dilution of monoclonal anti-11-deoxycortisol antibody (Ka = 2 x 10(10) M-1)."( Sensitivity of steroid enzyme immunoassays. Comparison of four label enzymes in an assay system using a monoclonal anti-steroid antibody.
Hosoda, H; Nambara, T; Tsukamoto, R, 1989
)
0.28
"We studied the effect of low dosage (0."( Missing effect of etomidate on testosterone secretion in man.
Allolio, B; Stuttmann, R; Winkelmann, W, 1986
)
0.27
"The effects of administering ketoconazole at a high dosage (30 mg/kg of body weight/day) and at a low dosage (10 mg/kg/day) on steroidogenesis in the dog were compared."( Ketoconazole-induced changes in selected canine hormone concentrations.
McDonald, R; Nachreiner, R; Roudebush, P; Willard, MD, 1986
)
0.27
" We suggest that, in children being treated with ACTH, the dosage of ACTH should be gradually tapered, AM cortisol levels should be monitored, and high-dose steroids should be included when treating medical stress."( Hypothalamo-pituitary-adrenal function in infantile spasms: effects of ACTH therapy.
Rao, JK; Willis, J, 1987
)
0.27
" RU 28 362 was more potent than either hydrocortisone or betamethasone, but all three glucocorticoids had a parallel dose-response curve in suppression of the increase in cell volume that occurs with activation during the first day in culture."( Suppression of growth of PHA-stimulated human lymphocytes by a novel steroid (RU 28 362) lacking the 21-OH group.
Beck, JS; Brown, RA; Deraedt, R; Potts, RC, 1987
)
0.27
" A dose-response study, at the range of 2-40 mg/kg, showed that a significant decrease was noted at 6 mg/kg and it was maximal (45% inhibition) at 20 and 40 mg/kg."( Inhibition of prostaglandin synthesis in brain of rat by dexamethasone: lack of effect of dexamethasone phosphate ester and various hormonal steroids.
Abu-Amer, Y; Shohami, E; Weidenfeld, J, 1988
)
0.27
" Thus it appears that CA has no untoward effect upon glucocorticoid secretion when given in high dosage for prolonged periods to hirsute women."( Effect of cyproterone acetate on glucocorticoid secretion in patients treated for hirsutism.
Croxson, MS; Evans, MC; France, J; Holdaway, IM; Ibbertson, HK; Sheehan, A; Wilson, T, 1983
)
0.27
" Parallel dose-response curves were demonstrated between dilutions of plasma with elevated 11-deoxycortisol concentrations and the standard reference preparation."( A simplified radioimmunoassay for plasma 11-deoxycortisol.
Su, JC; Walsh, PR; Wang, MC, 1981
)
0.26
" S with an ACTH-cortisol dose-response curve obtained in normal subjects shows that subnormal ACTH responses after metyrapone in the range between 13 and 33 pmol/L still generate normal comp."( Pituitary function tests: comparison of ACTH and 11-deoxy-cortisol responses in the metyrapone test and with the insulin hypoglycemia test.
Bähr, V; Exner, P; Oelkers, PW; Steiner, H, 1994
)
0.29
" No rational dosage forms make it possible to conduct clinical trials by parenteral administration."( [Pharmacological aspects in the development of liposomal medicinal preparations for the internal injection of hydrophobic cytostatics].
Baryshnikov, AIu; Oborotova, NA; Polozkova, ZS; Smirnova, ZS, 2002
)
0.31
" Stimulation of adrenal CMP-S and cortisol by pituitary ACTH demonstrated a dose-response curve with the shape of half a geometric parabola."( Combined stimulation of adrenocorticotropin and compound-S by single dose metyrapone test as an outpatient procedure to assess hypothalamic-pituitary-adrenal function.
Berneis, K; Gessler, A; Girard, J; Meier, C; Müller, B; Staub, JJ, 2002
)
0.31
" Dose-response studies using metyrapone and glucocorticoid agonists are needed to further investigate HPA axis regulation in PTSD."( Overnight metyrapone and combined dexamethasone/metyrapone tests in post-traumatic stress disorder: preliminary findings.
Jahn, H; Kellner, M; Otte, C; Schick, M; Wiedemann, K; Yassouridis, A, 2004
)
0.32
[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
deoxycortisolA 3,20-dioxo steroid having the structure of cortisol but lacking one or more of its hydroxy groups.
glucocorticoidGlucocorticoids are a class of steroid hormones that regulate a variety of physiological processes, in particular control of the concentration of glucose in blood.
primary alpha-hydroxy ketoneAn alpha-hydroxy ketone in which the carbonyl group and the hydroxy group are linked by a -CH2 (methylene) group.
tertiary alpha-hydroxy ketoneAn alpha-hydroxy ketone in which the carbonyl group and the hydroxy group are linked by a carbon bearing two organyl groups.
21-hydroxy steroid
[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 (28)

PathwayProteinsCompounds
Metabolism14961108
Metabolism of lipids500463
Metabolism of steroids111135
Metabolism of steroid hormones2537
Glucocorticoid 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 CYP11B1 causes AH404
Steroid hormone precursor biosynthesis015
Glucocorticoid biosynthesis1411
Biosynthesis of aldosterone and cortisol010
Biochemical pathways: part I0466
Classical pathway of steroidogenesis with glucocorticoid and mineralocorticoid metabolism325

Protein Targets (48)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
endonuclease IVEscherichia coliPotency50.11870.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency42.28410.100020.879379.4328AID588453
phosphopantetheinyl transferaseBacillus subtilisPotency10.00000.141337.9142100.0000AID1490
ATAD5 protein, partialHomo sapiens (human)Potency29.08100.004110.890331.5287AID493107
TDP1 proteinHomo sapiens (human)Potency16.02970.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency1.26490.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID743036; AID743040; AID743042; AID743053; AID743054
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency29.84930.001022.650876.6163AID1224838
progesterone receptorHomo sapiens (human)Potency5.88890.000417.946075.1148AID1346784; AID1346795; AID1347036
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency7.58640.000214.376460.0339AID720691; AID720692; AID720719
retinoid X nuclear receptor alphaHomo sapiens (human)Potency23.91450.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency15.09110.001530.607315,848.9004AID1224841; AID1224848; AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency2.46650.000229.305416,493.5996AID743069; AID743075; AID743078; AID743079
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency0.70790.707936.904389.1251AID504333
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency10.59010.001019.414170.9645AID743191
arylsulfatase AHomo sapiens (human)Potency8.49211.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.93690.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.26600.001723.839378.1014AID743083
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00280.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency95.283423.934123.934123.9341AID1967
chromobox protein homolog 1Homo sapiens (human)Potency65.81140.006026.168889.1251AID488953; AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency1.63600.00419.984825.9290AID504444
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency19.96820.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency0.00460.004611.374133.4983AID624296
survival motor neuron protein isoform dHomo sapiens (human)Potency19.95260.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency0.02510.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency5.96220.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency3.15730.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency0.02511.000012.224831.6228AID885
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency6.51310.00419.984825.9290AID504444
gemininHomo sapiens (human)Potency0.11580.004611.374133.4983AID624297
TAR DNA-binding protein 43Homo sapiens (human)Potency0.35481.778316.208135.4813AID652104
[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)
Corticosteroid-binding globulinHomo sapiens (human)Ki0.01320.01323.248110.0000AID51055
[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)Kd0.03630.00020.34964.7863AID318680
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
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 (13)

Processvia Protein(s)Taxonomy
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 (13)

Processvia Protein(s)Taxonomy
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 membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-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 (119)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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).
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.
AID1198140Permeability of the compound in PBS and EtOH by PAMPA method2015European journal of medicinal chemistry, Mar-26, Volume: 93Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
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.
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.
AID51049Binding affinity against corticosteroid-binding globulin1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Structure-activity relationships from molecular similarity matrices.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
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.
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.
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.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID53796Binding 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.
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.
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.
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.
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.
AID679242TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells2002The Journal of endocrinology, Oct, Volume: 175, Issue:1
The role of the efflux transporter P-glycoprotein in brain penetration of prednisolone.
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.
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.
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.
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.
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.
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.
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.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID212737Binding affinity against testosterone-binding globulin (TeBG)1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Structure-activity relationships from molecular similarity matrices.
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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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.
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.
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.
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.
AID1745845Primary 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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (918)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990449 (48.91)18.7374
1990's170 (18.52)18.2507
2000's147 (16.01)29.6817
2010's84 (9.15)24.3611
2020's68 (7.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.16

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

MetricThis Compound (vs All)
Research Demand Index20.16 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials50 (5.11%)5.53%
Trials0 (0.00%)5.53%
Reviews34 (3.47%)6.00%
Reviews0 (0.00%)6.00%
Case Studies53 (5.41%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other842 (86.01%)84.16%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]