osilodrostat profile

Osilodrostat: an orally active aldosterone-synthase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	44139752
CHEMBL ID	3099695
SCHEMBL ID	12460772
MeSH ID	M0551461

Synonym
osilodrostat
5yl4iq1078 ,
isturisa
928134-65-0
(+)-osilodrostat
4-((5r)-6,7-dihydro-5h-pyrrolo(1,2-c)imidazol-5-yl)-3-fluoro-benzonitrile
lci 699
benzonitrile, 4-((5r)-6,7-dihydro-5h-pyrrolo(1,2-c)imidazol-5-yl)-3-fluoro-
lci-699
lci699
unii-5yl4iq1078
osilodrostat [usan:inn]
bdbm50444549
lci699-nx
CHEMBL3099695 ,
lci-699-nx
S7456
SCHEMBL12460772
osilodrostat [inn]
osilodrostat [mi]
osilodrostat [who-dd]
osilodrostat [usan]
gtpl8310
4-[(5r)-6,7-dihydro-5h-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
AC-32907
DTXSID40156570
AKOS027323750
osilodrostat (usan/inn)
D11061
HY-16276
osilodrostat;4-[(5r)-6,7-dihydro-5h-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
CS-6896
DB11837
EX-A1397
(r)-4-(6,7-dihydro-5h-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile
BS-17881
Q27088216
1304733-26-3
4-[(5r)-6,7-dihydro-5h-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzo nitrile
CCG-266774
osilodrostat free base
A909743
4-[(4r,5r)-6,7-dihydro-5h-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
3-fluoro-4-[(5r)-5h,6h,7h-pyrrolo[1,2-c]imidazol-5-yl]benzonitrile
EN300-14284797
(r)-4-(6,7-dihydro-5h-pyrrolo(1,2-c)imidazol-5-yl)-3-fluorobenzonitrile
h02ca02
osilodrostatum

Excerpt	Reference	Relevance
"Osilodrostat acts as a potent, reversible inhibitor of 11β-hydroxylase (CYP11B1) and 18-hydroxylase (or aldosterone synthase, CYP11B2), counteracting both gluco- and mineralocorticoid production. "	( Osilodrostat oral tablets for adults with Cushing's disease. Aboud, N; Arnaldi, G; Lucchetti, B; Martino, M; Salvio, G, 2022)	3.61
"Osilodrostat is a potent oral steroidogenesis inhibitor that has lately been shown as an effective adjuvant therapy in the management of patients with CD."	( Osilodrostat - an emerging drug for the medical management of Cushing's disease. Bolanowski, M; Jawiarczyk-Przybyłowska, A; Mehlich, A; Stasiewicz, A; Witek, P, 2022)	2.89
"Osilodrostat is a new 11β-hydroxylase inhibitor with a mode of action analogous to Metyrapone. "	( Differences in the spectrum of steroidogenic enzyme inhibition between Osilodrostat and Metyrapone in ACTH-dependent Cushing syndrome patients. Assié, G; Baron, S; Bertherat, J; Bessiene, L; Blanchet, B; Bonnet-Serrano, F; Bricaire, L; Groussin, L; Guibourdenche, J; Guignat, L; Laguillier-Morizot, C; Poirier, J; Vaczlavik, A, 2022)	2.4
"Osilodrostat is a rapidly efficient therapy for PNCS/EAS with severe/intense hypercortisolism. "	( Efficacy and Safety of Osilodrostat in Paraneoplastic Cushing Syndrome: A Real-World Multicenter Study in France. Baudin, E; Boullay, HD; Castinetti, F; Chabre, O; Chanson, P; Do Cao, C; Dormoy, A; Drui, D; François, M; Geslot, A; Haissaguerre, M; Lasolle, H; Laurent, C; Mayer, A; Puerto, M; Raverot, G; Reznik, Y; Rod, A; Salenave, S; Tabarin, A; Vieira-Pinto, O; Vitellius, G; Young, J, 2023)	2.66
"Osilodrostat (LCI699) is a potent inhibitor of the human steroidogenic cytochromes P450 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2). "	( Selectivity of osilodrostat as an inhibitor of human steroidogenic cytochromes P450. Auchus, RJ; Liu, J; Oommen, J; Peng, HM; Valentín-Goyco, J, 2023)	2.71
"Osilodrostat is an effective long-term treatment for patients with Cushing's disease."	( Long-term efficacy and safety of osilodrostat in patients with Cushing's disease: results from the LINC 4 study extension. Auchus, RJ; Belaya, Z; Bex, M; Feelders, RA; Gadelha, M; Heaney, AP; Paul, M; Pedroncelli, AM; Snyder, PJ; Turcu, AF; Witek, P, 2023)	1.91
"Osilodrostat is an effective new treatment option that is approved in Europe for the treatment of endogenous Cushing's syndrome and in the USA for Cushing's disease."	( Efficacy and safety of osilodrostat in patients with Cushing's disease (LINC 3): a multicentre phase III study with a double-blind, randomised withdrawal phase. Auchus, R; Bertagna, X; Biller, BMK; Findling, J; Fleseriu, M; Gu, F; Kim, JH; Lacroix, A; Laplanche, A; Lee, EJ; Leelawattana, R; Newell-Price, J; O'Connell, P; Pedroncelli, AM; Pivonello, R; Shimatsu, A; Tauchmanova, L, 2020)	1.59
"Osilodrostat (LCI699) is a new steroidogenesis inhibitor of 11β-hydroxylase (CYP11β1) that induced remission of hypercortisolism in 86% of patients with refractory CD in the randomized placebo-controlled trial LINC-3 (NCT02180217)."	( Corticotroph tumor progression during long-term therapy with osilodrostat in a patient with persistent Cushing's disease. Berthelet, F; Fontaine-Sylvestre, C; Lacroix, A; Létourneau-Guillon, L; Moumdjian, RA, 2021)	1.58
"Osilodrostat is an effective, new treatment option for CD, with positive effects on cardiovascular and quality of life parameters as well as tolerable adverse effects. "	( Osilodrostat: A Review of Recent Clinical Studies and Practical Recommendations for its Use in the Treatment of Cushing Disease. Yuen, KCJ, 2021)	3.51
"Osilodrostat is a CYP11B1 and CYP11B2 inhibitor, with unknown effects on other steroidogenic enzymes."	( Osilodrostat Is a Potential Novel Steroidogenesis Inhibitor for the Treatment of Cushing Syndrome: An In Vitro Study. Creemers, SG; de Jong, FH; de Rijke, YB; Feelders, RA; Franssen, GJH; Hofland, LJ; van Koetsveld, PM, 2019)	2.68
"Osilodrostat is a promising treatment option for Cushing syndrome, and in vivo differences with metyrapone are potentially driven by pharmacokinetic differences."	( Osilodrostat Is a Potential Novel Steroidogenesis Inhibitor for the Treatment of Cushing Syndrome: An In Vitro Study. Creemers, SG; de Jong, FH; de Rijke, YB; Feelders, RA; Franssen, GJH; Hofland, LJ; van Koetsveld, PM, 2019)	2.68
"Osilodrostat (LCI699) is an adrenal steroidogenesis inhibitor currently in late-phase clinical development as a potential treatment for Cushing's disease. "	( Drug Interaction Potential of Osilodrostat (LCI699) Based on Its Effect on the Pharmacokinetics of Probe Drugs of Cytochrome P450 Enzymes in Healthy Adults. Armani, S; Chun, DY; Darstein, C; Einolf, HJ; Gu, H; Kulkarni, S; Sauter, N; Ting, L; Tripathi, AP; Wang, L; Zhu, B, 2017)	2.19
"Osilodrostat is a moderate inhibitor of CYP1A2 and CYP2C19 and a weak inhibitor of CYP2D6 and the most clinically important CYP enzyme, CYP3A4. "	( Drug Interaction Potential of Osilodrostat (LCI699) Based on Its Effect on the Pharmacokinetics of Probe Drugs of Cytochrome P450 Enzymes in Healthy Adults. Armani, S; Chun, DY; Darstein, C; Einolf, HJ; Gu, H; Kulkarni, S; Sauter, N; Ting, L; Tripathi, AP; Wang, L; Zhu, B, 2017)	2.19

Excerpt	Reference	Relevance
"Osilodrostat has been shown to be highly effective at maintaining normal urinary free cortisol in patients with CD."	( Updates in adrenal steroidogenesis inhibitors for Cushing's syndrome - A practical guide. Fleseriu, M; Han, AJ; Varlamov, EV, 2021)	1.34

Excerpt	Reference	Relevance
"Osilodrostat might inhibit CYP11B1 and CYP11B2, in some conditions to a lesser extent CYP17A1 activity, and a proximal step in the steroidogenesis."	( Osilodrostat Is a Potential Novel Steroidogenesis Inhibitor for the Treatment of Cushing Syndrome: An In Vitro Study. Creemers, SG; de Jong, FH; de Rijke, YB; Feelders, RA; Franssen, GJH; Hofland, LJ; van Koetsveld, PM, 2019)	2.68

Excerpt	Reference	Relevance
"Osilodrostat treatment reduced UFC in all patients; 78.9% (n/N = 15/19) had normal UFC at week 22. "	( Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Bertagna, X; Biller, BM; Fleseriu, M; Hamrahian, AH; Hilliard, A; Molitch, ME; Pivonello, R; Sauter, N; Shimatsu, A; Shimizu, C; Tanaka, T; Tian, C; White, T; Young, J, 2016)	3.32
"Treatment with osilodrostat was generally well tolerated."	( Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Bertagna, X; Biller, BM; Fleseriu, M; Hamrahian, AH; Hilliard, A; Molitch, ME; Pivonello, R; Sauter, N; Shimatsu, A; Shimizu, C; Tanaka, T; Tian, C; White, T; Young, J, 2016)	2.22

Excerpt	Reference	Relevance
" The available data on mean sitting systolic blood pressure (MSSBP), mean sitting diastolic blood pressure (MSDBP), adverse effects, renin-angiotensin-aldosterone system biomarkers (RAASB) and adrenocorticotropic hormone-stimulated cortisol concentration (AHSC) were collected."	( Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review. Tian, JB; Wang, HZ; Yang, KH, 2015)	0.42
" Adverse reactions occurred in 73 of the 139 patients (52."	( Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review. Tian, JB; Wang, HZ; Yang, KH, 2015)	0.42
" Of the nine patients enrolled in the study, seven completed the 12-week core treatment period and two discontinued at or prior to week 12 due to adverse events (AEs)."	( A multicenter, phase 2 study to evaluate the efficacy and safety of osilodrostat, a new 11β-hydroxylase inhibitor, in Japanese patients with endogenous Cushing's syndrome other than Cushing's disease. Kaneko, T; Midorikawa, S; Sato, M; Satoh, F; Shimatsu, A; Suzuki, A; Takeda, T; Tanaka, T; Ujihara, M, 2020)	0.79
" Most common adverse events (ie, occurred in >25% of participants) were nausea (57 [42%]), headache (46 [34%]), fatigue (39 [28%]), and adrenal insufficiency (38 [28%])."	( Efficacy and safety of osilodrostat in patients with Cushing's disease (LINC 3): a multicentre phase III study with a double-blind, randomised withdrawal phase. Auchus, R; Bertagna, X; Biller, BMK; Findling, J; Fleseriu, M; Gu, F; Kim, JH; Lacroix, A; Laplanche, A; Lee, EJ; Leelawattana, R; Newell-Price, J; O'Connell, P; Pedroncelli, AM; Pivonello, R; Shimatsu, A; Tauchmanova, L, 2020)	0.87
" Study outcomes assessed in the extension included: mean urinary free cortisol (mUFC) response rates; changes in mUFC, serum cortisol and late-night salivary cortisol (LNSC); changes in cardiovascular and metabolic-related parameters; blood pressure, waist circumference and weight; changes in physical manifestations of Cushing's disease; changes in patient-reported outcomes for health-related quality of life; changes in tumor volume; and adverse events."	( Long-term efficacy and safety of osilodrostat in patients with Cushing's disease: results from the LINC 4 study extension. Auchus, RJ; Belaya, Z; Bex, M; Feelders, RA; Gadelha, M; Heaney, AP; Paul, M; Pedroncelli, AM; Snyder, PJ; Turcu, AF; Witek, P, 2023)	1.19

Excerpt	Reference	Relevance
" An illustration of the impact of the age of preclinical models on pharmacokinetic properties is also highlighted."	( Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors. Adams, CM; Amaral, A; Beil, ME; Carvalho, J; Fu, F; Gangl, E; Hu, CW; Hu, QY; Jeng, AY; Ksander, GM; LaSala, D; Liang, G; Logman, M; Lou, C; Maniara, WM; Papillon, JP; Rajan, S; Rigel, DF; Singh, AK; Smith, SA; Zhang, C, 2015)	0.42

Excerpt	Reference	Relevance
" Structure-activity relationships and optimization of their oral bioavailability are presented."	( Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors. Adams, CM; Amaral, A; Beil, ME; Carvalho, J; Fu, F; Gangl, E; Hu, CW; Hu, QY; Jeng, AY; Ksander, GM; LaSala, D; Liang, G; Logman, M; Lou, C; Maniara, WM; Papillon, JP; Rajan, S; Rigel, DF; Singh, AK; Smith, SA; Zhang, C, 2015)	0.42
" Osilodrostat, an orally bioavailable adrenal steroidogenesis inhibitor, was approved in the USA and EU in 2020 for the treatment of CD."	( Osilodrostat for the treatment of Cushing's disease. Rasool, S; Skinner, BW, 2021)	2.97

Excerpt	Relevance	Reference
" Investigation of pyrazoles, especially N-alkyl pyrazoles, as a new template to coordinate the heme-iron motif led to a potent and highly selective CYP11B2 inhibitor 28 with an aldosterone-lowering effect at 1 mg/kg dosing in cynomolgus monkeys."	( Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2. Akahoshi, F; Egi, Y; Hiraga, Y; Nishio, M; Ohbora, T; Onda, Y; Sakakibara, R; Sasaki, W; Sato, K; Shimizu, H; Takedomi, K; Ushirogochi, H; Yamaguchi, M, 2018)	0.48
" The common adverse effects include adrenal insufficiency, hypokalemia, edema, and hyperandrogenic symptoms, which can be minimized using a slower up-titration dosing regimen."	( Osilodrostat: A Review of Recent Clinical Studies and Practical Recommendations for its Use in the Treatment of Cushing Disease. Yuen, KCJ, 2021)	2.06
" Patient characteristics and hormonal dosage were analyzed."	( Prolonged adrenocortical blockade following discontinuation of Osilodrostat. Bertherat, J; Bonnet-Serrano, F; Bouys, L; Poirier, J; Thomeret, L, 2023)	1.15

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)	IC50 (µMol)	3.9811	0.0020	0.9818	4.7300	AID1372645
Cytochrome P450 1A2	Homo sapiens (human)	IC50 (µMol)	0.0002	0.0001	1.7740	10.0000	AID1154696
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	0.0029	0.0001	1.7536	10.0000	AID1154701
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	2.0151	10.0000	AID1059817
Aromatase	Homo sapiens (human)	IC50 (µMol)	2.1109	0.0000	1.2904	10.0000	AID1059821; AID1154701; AID1177645; AID1372646
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	2.8005	10.0000	AID1059818
Cytochrome P450 11B1, mitochondrial	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.4950	0.4950	3.5289	5.0000	AID1059813
Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)	IC50 (µMol)	0.0053	0.0005	0.2902	2.7800	AID1059815; AID1154701; AID1177647; AID1191379; AID1200851; AID1266756; AID1449095; AID1498051; AID1874665
Cytochrome P450 11B2, mitochondrial	Mus musculus (house mouse)	IC50 (µMol)	0.2100	0.1900	0.2000	0.2100	AID1251773
Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)	IC50 (µMol)	0.0014	0.0001	0.2738	3.5000	AID1059816; AID1059822; AID1154696; AID1154700; AID1177651; AID1191378; AID1200850; AID1251772; AID1266712; AID1449096; AID1498050; AID1874662
Cytochrome P450 11B2, mitochondrial	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.1110	0.1110	0.3555	0.6000	AID1059814
Cytochrome P450 2C19	Homo sapiens (human)	IC50 (µMol)	0.0002	0.0000	2.3983	10.0000	AID1154696
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
steroid biosynthetic process	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
androgen biosynthetic process	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
glucocorticoid biosynthetic process	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
sex differentiation	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
steroid metabolic process	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
hormone biosynthetic process	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
progesterone metabolic process	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
porphyrin-containing compound metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
toxin biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
post-embryonic development	Cytochrome P450 1A2	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
regulation of gene expression	Cytochrome P450 1A2	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
dibenzo-p-dioxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lung development	Cytochrome P450 1A2	Homo sapiens (human)
methylation	Cytochrome P450 1A2	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
cellular respiration	Cytochrome P450 1A2	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 1A2	Homo sapiens (human)
cellular response to cadmium ion	Cytochrome P450 1A2	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of chronic inflammatory response	Aromatase	Homo sapiens (human)
steroid biosynthetic process	Aromatase	Homo sapiens (human)
estrogen biosynthetic process	Aromatase	Homo sapiens (human)
androgen catabolic process	Aromatase	Homo sapiens (human)
syncytium formation	Aromatase	Homo sapiens (human)
negative regulation of macrophage chemotaxis	Aromatase	Homo sapiens (human)
sterol metabolic process	Aromatase	Homo sapiens (human)
female genitalia development	Aromatase	Homo sapiens (human)
mammary gland development	Aromatase	Homo sapiens (human)
uterus development	Aromatase	Homo sapiens (human)
prostate gland growth	Aromatase	Homo sapiens (human)
testosterone biosynthetic process	Aromatase	Homo sapiens (human)
positive regulation of estradiol secretion	Aromatase	Homo sapiens (human)
female gonad development	Aromatase	Homo sapiens (human)
response to estradiol	Aromatase	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
C21-steroid hormone biosynthetic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
glucocorticoid biosynthetic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
immune response	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
regulation of blood pressure	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
sterol metabolic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
aldosterone biosynthetic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cellular response to hormone stimulus	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cortisol biosynthetic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cellular response to potassium ion	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
glucose homeostasis	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cortisol metabolic process	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cellular response to peptide hormone stimulus	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
cortisol biosynthetic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
regulation of blood volume by renal aldosterone	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
renal water homeostasis	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
C21-steroid hormone biosynthetic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
mineralocorticoid biosynthetic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
sterol metabolic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
aldosterone biosynthetic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
cellular response to hormone stimulus	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
cortisol biosynthetic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
cellular response to potassium ion	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
potassium ion homeostasis	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
sodium ion homeostasis	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
glucocorticoid biosynthetic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
cortisol metabolic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
cellular response to peptide hormone stimulus	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
long-chain fatty acid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C19	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
steroid 17-alpha-monooxygenase activity	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
iron ion binding	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
oxygen binding	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
heme binding	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
17-alpha-hydroxyprogesterone aldolase activity	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 1A2	Homo sapiens (human)
iron ion binding	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	Cytochrome P450 1A2	Homo sapiens (human)
electron transfer activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 1A2	Homo sapiens (human)
enzyme binding	Cytochrome P450 1A2	Homo sapiens (human)
heme binding	Cytochrome P450 1A2	Homo sapiens (human)
demethylase activity	Cytochrome P450 1A2	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 1A2	Homo sapiens (human)
aromatase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Cytochrome P450 1A2	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Aromatase	Homo sapiens (human)
steroid hydroxylase activity	Aromatase	Homo sapiens (human)
electron transfer activity	Aromatase	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Aromatase	Homo sapiens (human)
oxygen binding	Aromatase	Homo sapiens (human)
heme binding	Aromatase	Homo sapiens (human)
aromatase activity	Aromatase	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
steroid 11-beta-monooxygenase activity	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
iron ion binding	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
heme binding	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
corticosterone 18-monooxygenase activity	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
steroid 11-beta-monooxygenase activity	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
iron ion binding	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
heme binding	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
corticosterone 18-monooxygenase activity	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C19	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxygen binding	Cytochrome P450 2C19	Homo sapiens (human)
enzyme binding	Cytochrome P450 2C19	Homo sapiens (human)
heme binding	Cytochrome P450 2C19	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C19	Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C19	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endoplasmic reticulum	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
endoplasmic reticulum membrane	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
axon	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
neuronal cell body	Steroid 17-alpha-hydroxylase/17,20 lyase	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Aromatase	Homo sapiens (human)
endoplasmic reticulum membrane	Aromatase	Homo sapiens (human)
membrane	Aromatase	Homo sapiens (human)
endoplasmic reticulum	Aromatase	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
mitochondrion	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
mitochondrial inner membrane	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
mitochondrial inner membrane	Cytochrome P450 11B1, mitochondrial	Homo sapiens (human)
mitochondrion	Cytochrome P450 11B2, mitochondrial	Mus musculus (house mouse)
mitochondrion	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
mitochondrial inner membrane	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
mitochondrial inner membrane	Cytochrome P450 11B2, mitochondrial	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C19	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C19	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (84)

Assay ID	Title	Year	Journal	Article
AID1203969	Reduction in diastolic blood pressure in Cushing's disease patient at 4 mg/day in two equal doses and dose escalated every 14 days to 10, 20, 40, and 100 mg/day	2015	European journal of medicinal chemistry, , Volume: 96	Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.
AID1251767	Reduction of plasma cortisol level in non-naive cynomolgus monkey at 0.5 mg/kg, po administered prior to ACTH challenge measured after 60 mins by LC-MS/MS analysis	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1498053	Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM preincubated for 10 followed by NADPH addition measured after 20 mins by LC-MS/MS analysis	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.
AID1154700	Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycorticosterone as substrate	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
AID1177660	Decrease in aldosterone level in primary aldosteronism patient plasma at 1 mg, bid for 15 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1251737	Selectivity factor, ratio of IC50 for human CYP11B1 to IC50 for human CYP11B2	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1251768	Increase in plasma 11-deoxycortisol level in non-naive cynomolgus monkey at 0.5 mg/kg, po administered prior to ACTH challenge measured after 60 mins by LC-MS/MS analysis	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1251755	Reduction of plasma aldosterone level in obese diabetic db/db mouse at 30 mg/kg, po measured at 2 hrs by LC-MS/MS analysis relative to control	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1249914	Decrease in aldosterone level in hypertension patient plasma at 0.5 mg, po dosed twice daily	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
AID1249916	Decrease in diastolic pressure in hypertension patient at 0.5 mg, po dosed twice daily	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
AID1372645	Inhibition of CYP17A1 (unknown origin)	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
AID1203972	Reduction in plasma rennin level in Cushing's disease patient at 4 mg/day in two equal doses and dose escalated every 14 days to 10, 20, 40, and 100 mg/day (Rvb = 13 ng/L)	2015	European journal of medicinal chemistry, , Volume: 96	Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.
AID1510892	Increase in ACTH-induced 11-deoxycortisol level in cynomolgus monkey at 0.5 mg/kg, po administered 10 mins prior to ACTH stimulation for 7 days	2019	ACS medicinal chemistry letters, Jul-11, Volume: 10, Issue:7	Development of Highly Selective Pyrimidine-Based Aldosterone Synthase (CYP11B2) Inhibitors.
AID1191379	Inhibition of CYP11B1 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 25 mins by HPLC analysis	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.
AID1874663	Selectivity ratio of IC50 for inhibition of human CYP11B2 to IC50 for inhibition of human CYP11B1	2022	Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17	Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[
AID1059816	Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrate by cell-based assay	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1251757	Reduction of plasma corticosterone level in obese diabetic db/db mouse at 30 mg/kg, po measured at 2 hrs by LC-MS/MS analysis relative to control	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1177645	Inhibition of CYP19 (unknown origin)	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1498050	Inhibition of human CYP11B2 expressed in Chinese hamster V79 cell mitochondria assessed as reduction in aldosterone production using deoxycorticosterone as substrate after 1.5 hrs in presence of NADPH by HTRF assay	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.
AID1177654	Elimination half life in sodium depleted healthy human	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1177663	Increase in ACTH level in primary aldosteronism patient plasma at 0.5 mg, bid for 14 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1510897	Increase in ACTH-induced DOC level in cynomolgus monkey at 0.5 mg/kg, po administered 10 mins prior to ACTH stimulation for 7 days	2019	ACS medicinal chemistry letters, Jul-11, Volume: 10, Issue:7	Development of Highly Selective Pyrimidine-Based Aldosterone Synthase (CYP11B2) Inhibitors.
AID1658207	In vivo inhibition of CYP11B2 in cynomolgus monkey assessed as reduction in ACTH-induced 11-deoxycorticosterone at 1 mg/kg, po preincubated for 1 hr followed by ACTH challenge and measured after 60 mins by LC/MS-MS analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
AID1177653	Tmax in sodium depleted healthy human	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1251753	Increase in plasma 11-deoxycorticosterone level in obese diabetic db/db mouse at 30 mg/kg, po measured at 2 hrs by LC-MS/MS analysis relative to control	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1177659	Decrease in aldosterone level in primary aldosteronism patient plasma at 0.5 mg, bid for 14 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1177662	Increase in 11-deoxycorticosterone level in primary aldosteronism patient plasma at 1 mg, bid for 15 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1203967	Reduction in plasma aldosterone level in Cushing's disease patient at 4 mg/day in two equal doses and dose escalated every 14 days to 10, 20, 40, and 100 mg/day relative to control	2015	European journal of medicinal chemistry, , Volume: 96	Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.
AID1177655	Decrease in aldosterone level in sodium depleted healthy human urine administered daily for 7 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1372640	Inhibition of cynomolgus monkey adrenal mitochondrial CYP11B1 using 11-deoxycortisol as substrate after 90 mins in presence of NADPH by mass spectrometric analysis	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
AID1449096	Inhibition of human CYP11B2 expressed in hamster V79MZ cells using [1,2-3H]-11-deoxycorticosterone as substrate after 6 hrs by HPLC analysis	2017	Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12	Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.
AID1177646	Selectivity ratio of IC50 for CYP19 (unknown origin) to IC50 for human CYP11B1	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1449097	Selectivity ratio of IC50 for human CYP11B2 expressed in hamster V79MZ cells to IC50 for human CYP11B1 expressed in hamster V79MZ cells	2017	Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12	Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.
AID1203970	Induction of 11-deoxycorticosterone level in Cushing's disease patient at 4 mg/day in two equal doses and dose escalated every 14 days to 10, 20, 40, and 100 mg/day	2015	European journal of medicinal chemistry, , Volume: 96	Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.
AID1059814	Inhibition of rat recombinant CYP11B2 using 11-deoxycorticosterone as substrate by cell-based assay	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1200850	Inhibition of human CYP11B2 expressed in V79 MZh cells using [14C]-deoxycorticosterone substrate incubated for 6 hrs by HPTLC method	2015	Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5	Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.
AID1498051	Inhibition of human CYP11B1 expressed in Chinese hamster V79 cells assessed as reduction in corticosterone production using deoxycorticosterone as substrate after 1.5 to 2 hrs in presence of NADPH by HTRF assay	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.
AID1177666	Decrease in diastolic blood pressure in hypertension patient at 1 mg, qd for 8 weeks	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1266712	Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrate after 2 hrs by scintillation proximity assay	2015	Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23	Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
AID1251773	Inhibition of mouse CYP11B2 expressed in renal leiomyoblastoma cells	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1251751	Increase in plasma 11-deoxycorticosterone level in obese diabetic db/db mouse at 3 mg/kg, po measured at 2 hrs by LC-MS/MS analysis relative to control	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1200852	Selectivity index, ratio of IC50 for human CYP11B1 to IC50 human CYP11B2	2015	Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5	Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.
AID1059817	Inhibition of CYP2D6 (unknown origin)	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1154696	Inhibition of CYP11B2 (unknown origin)	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
AID1059811	Time-weighted average (0 to 8 hrs) in Sprague-Dawley rat at 1 mg/kg, po	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1251772	Inhibition of human CYP11B2 expressed in renal leiomyoblastoma cells	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1177656	Decrease in aldosterone level in sodium depleted healthy human plasma administered daily for 7 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1059821	Inhibition of human CYP19 preincubated for 10 mins followed by protein addition measured after 90 mins by fluorimetric analysis	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1874662	Inhibition of human CYP11B2 expressed in Chinese hamster V79 MZh cells using [14C]-deoxycorticosteron as substrate measured after 6 hrs by phosphoimager analysis	2022	Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17	Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[
AID1154702	Selectivity factor, ratio of IC50 for human CYP11B2 to IC50 for human CYP11B1	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
AID1203968	Reduction in systolic blood pressure in Cushing's disease patient at 4 mg/day in two equal doses and dose escalated every 14 days to 10, 20, 40, and 100 mg/day	2015	European journal of medicinal chemistry, , Volume: 96	Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.
AID1266756	Inhibition human recombinant CYP11B1 using 11-deoxycorticosterone as substrate after 2 hrs by scintillation proximity assay	2015	Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23	Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
AID1372639	Inhibition of cynomolgus monkey adrenal mitochondrial CYP11B2 using corticosterone as substrate after 60 mins in presence of NADPH by mass spectrometric analysis	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
AID1874665	Inhibition of human CYP11B1 expressed in Chinese hamster V79 MZh cells using [14C]-deoxycorticosteron as substrate measured after 6 hrs by phosphoimager analysis	2022	Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17	Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[
AID1059818	Inhibition of CYP2C9 (unknown origin)	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1059810	Reduction of angiotensin 2-stimulated plasma aldosterone time-weighted average (0 to 8 hrs) in Sprague-Dawley rat at 1 mg/kg, po	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1177647	Inhibition of human CYP11B1 expressed in V79 MZ cells	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1498054	Metabolic stability in monkey liver microsomes assessed as parent compound remaining at 1 uM preincubated for 10 followed by NADPH addition measured after 20 mins by LC-MS/MS analysis	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.
AID1059813	Inhibition of rat recombinant CYP11B1 using 11-deoxycortisol as substrate by cell-based assay	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1177661	Increase in 11-deoxycorticosterone level in primary aldosteronism patient plasma at 0.5 mg, bid for 14 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1251754	Reduction of plasma aldosterone level in obese diabetic db/db mouse at 3 mg/kg, po measured at 2 hrs by LC-MS/MS analysis relative to control	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1191378	Inhibition of CYP11B2 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 45 mins by HPLC analysis	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.
AID1177651	Inhibition of human aldosterone synthase expressed in V79 MZ cells	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1203971	Reduction in plasma potassium level in Cushing's disease patient at 4 mg/day in two equal doses and dose escalated every 14 days to 10, 20, 40, and 100 mg/day	2015	European journal of medicinal chemistry, , Volume: 96	Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.
AID1251766	Reduction of plasma aldosterone level in non-naive cynomolgus monkey at 0.5 mg/kg, po administered prior to ACTH challenge measured after 60 mins by LC-MS/MS analysis	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1200851	Inhibition of human CYP11B1 expressed in V79 MZh cells using [14C]-deoxycorticosterone substrate incubated for 6 hrs by HPTLC method	2015	Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5	Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.
AID1372646	Inhibition of CYP19A1 (unknown origin)	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
AID1251756	Reduction of plasma corticosterone level in obese diabetic db/db mouse at 3 mg/kg, po measured at 2 hrs by LC-MS/MS analysis relative to control	2015	Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20	Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
AID1177664	Increase in ACTH level in primary aldosteronism patient plasma at 1 mg, bid for 15 days	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
AID1498052	Selectivity index, ratio of IC50 for human CYP11B1 expressed in Chinese hamster V79 cells to IC50 for human CYP11B2 expressed in Chinese hamster V79 cell mitochondria	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.
AID1449095	Inhibition of human CYP11B1 expressed in hamster V79MZ cells using [1,2-3H]-11-deoxycorticosterone as substrate after 6 hrs by HPLC analysis	2017	Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12	Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.
AID1059815	Inhibition of human recombinant CYP11B1 using 11-deoxycortisol as substrate by cell-based assay	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1266759	Decrease in ACTH-stimulated plasma aldosterone level of chair-trained chronically cannulated cynomolgus monkey model compound administered followed by ACTH challenge for 3 hrs measured after 24 hrs by LC/MS/MS analysis	2015	Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23	Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
AID1059819	Inhibition of CYP3A (unknown origin)	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1372641	Selectivity index, ratio of IC50 for cynomolgus monkey adrenal mitochondrial CYP11B1 to IC50 for cynomolgus monkey adrenal mitochondrial CYP11B2	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
AID1059812	Oral bioavailability in Sprague-Dawley rat at 1 mg/kg	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1059809	Reduction of ACTH-stimulated plasma corticosterone concentration in Sprague-Dawley rat	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1059822	Inhibition of CYP11B2 in human NCI-H295R cells assessed as inhibition of angiotensin-2-induced aldosterone production after 24 hrs by RIA	2013	ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12	Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
AID1249915	Decrease in systolic pressure in hypertension patient at 0.5 mg, po dosed twice daily	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
AID1191380	Selectivity factor, ratio of IC50 for CYP11B1 in human V79MZ cells to IC50 for CYP11B2 in human V79MZ cells	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.
AID1658241	Upregulation of cortisol level in ACTH-induced cynomolgus monkey at 1 mg/kg, po preincubated for 1 hr followed by ACTH challenge and measured after 60 mins by LC/MS-MS analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
AID1154701	Inhibition of human CYP11B1 expressed in hamster V79MZh cells using deoxycorticosterone as substrate	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
AID1345266	Human CYP11B1 (CYP11, CYP17, CYP19, CYP20 and CYP21 families)	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
AID1345245	Human CYP11B2 (CYP11, CYP17, CYP19, CYP20 and CYP21 families)	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	36 (46.75)	24.3611
2020's	41 (53.25)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	12 (15.58%)	5.53%
Reviews	21 (27.27%)	6.00%
Case Studies	7 (9.09%)	4.05%
Observational	0 (0.00%)	0.25%
Other	37 (48.05%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
caffeine [no description available]	3.53	1	1	purine alkaloid; trimethylxanthine	adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	6.77	8	0	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
metyrapone Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency.	7.08	11	0	aromatic ketone	antimetabolite; diagnostic agent; EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor
midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.	3.53	1	1	imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative
mitotane Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.	5.68	3	0	diarylmethane
omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.	3.53	1	1	aromatic ether; benzimidazoles; pyridines; sulfoxide
temozolomide [no description available]	4.22	1	0	imidazotetrazine; monocarboxylic acid amide; triazene derivative	alkylating agent; antineoplastic agent; prodrug
corticosterone [no description available]	2.11	1	0	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone	human metabolite; mouse metabolite
spironolactone Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.	4.44	2	2	3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester	aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic
aldosterone [no description available]	11.17	12	6	11beta-hydroxy steroid; 18-oxo steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; mineralocorticoid; primary alpha-hydroxy ketone; steroid aldehyde	human metabolite; mouse metabolite
androstenedione Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads.	2.41	1	0	17-oxo steroid; 3-oxo-Delta(4) steroid; androstanoid	androgen; Daphnia magna metabolite; human metabolite; mouse metabolite
desoxycorticosterone Desoxycorticosterone: A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE	7.51	4	4	20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; mineralocorticoid; primary alpha-hydroxy ketone	human metabolite; mouse metabolite
staurosporine [no description available]	2.1	1	0	indolocarbazole alkaloid; organic heterooctacyclic compound	apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector
cabergoline Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.	5.05	2	0	N-acylurea	antineoplastic agent; antiparkinson drug; dopamine agonist
mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.	4.1	2	0	3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound	abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive
fadrozole Fadrozole: A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer.	5.62	8	0	imidazopyridine
mespirenone mespirenone: structure given in first source	2.1	1	0
gefitinib [no description available]	4.22	1	0	aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound	antineoplastic agent; epidermal growth factor receptor antagonist
cyc 202 seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.	4.22	1	0	2,6-diaminopurines	antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
cortodoxone Cortodoxone: 17,21-Dihydroxypregn-4-ene-3,20-dione. A 17-hydroxycorticosteroid with glucocorticoid and anti-inflammatory activities.. 11-deoxycortisol : A deoxycortisol that is cortisol in which the hydroxy group at position 11 has been replaced by a hydrogen.	2.69	2	0	deoxycortisol; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	human metabolite; mouse metabolite
eplerenone Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.	4.96	4	2	3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester	aldosterone antagonist; antihypertensive agent
tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.	5.05	2	0	retinoic acid; vitamin A	anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule
etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.	11.73	6	0	ethyl ester; imidazoles	intravenous anaesthetic; sedative
dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.	3.53	1	1	6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene	antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic
ergoline Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.. ergoline : An indole alkaloid whose structural skeleton is found in many naturally occurring and synthetic ergolines which are known to bind to neurotransmitter receptors, such as dopamine, noradrenaline and serotonin receptors and function as unselective agonists or antagonists at these receptors.	3.17	1	0	diamine; ergoline alkaloid; indole alkaloid fundamental parent; indole alkaloid; organic heterotetracyclic compound
pasireotide pasireotide : A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing's disease.	11.35	5	0	homodetic cyclic peptide; peptide hormone	antineoplastic agent
angiotensinogen Angiotensinogen: An alpha-globulin of about 453 amino acids, depending on the species. It is produced by the liver in response to lowered blood pressure and secreted into blood circulation. Angiotensinogen is the inactive precursor of the ANGIOTENSINS produced in the body by successive enzyme cleavages. Cleavage of angiotensinogen by RENIN yields the decapeptide ANGIOTENSIN I. Further cleavage of angiotensin I (by ANGIOTENSIN CONVERTING ENZYME) yields the potent vasoconstrictor octapeptide ANGIOTENSIN II; and then, via other enzymes, other angiotensins also involved in the hemodynamic-regulating RENIN-ANGIOTENSIN SYSTEM.	3.48	1	1

Condition	Indicated	Relationship Strength	Studies	Trials
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	2.1	1	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	1	5.43	2	0
Blood Pressure, High [description not available]	0	13.51	23	18
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	1	15.51	23	18
Adrenocorticotropic Hormone, Inappropriate Secretion [description not available]	0	13.4	35	7
Pituitary ACTH Hypersecretion A disease of the PITUITARY GLAND characterized by the excess amount of ADRENOCORTICOTROPIC HORMONE secreted. This leads to hypersecretion of cortisol (HYDROCORTISONE) by the ADRENAL GLANDS resulting in CUSHING SYNDROME.	1	15.4	35	7
Cushing's Syndrome [description not available]	0	10.32	24	1
Cushing Syndrome A condition caused by prolonged exposure to excess levels of cortisol (HYDROCORTISONE) or other GLUCOCORTICOIDS from endogenous or exogenous sources. It is characterized by upper body OBESITY; OSTEOPOROSIS; HYPERTENSION; DIABETES MELLITUS; HIRSUTISM; AMENORRHEA; and excess body fluid. Endogenous Cushing syndrome or spontaneous hypercortisolism is divided into two groups, those due to an excess of ADRENOCORTICOTROPIN and those that are ACTH-independent.	1	12.32	24	1
Adrenocortical Carcinoma A malignant neoplasm of the ADRENAL CORTEX. Adrenocortical carcinomas are unencapsulated anaplastic (ANAPLASIA) masses sometimes exceeding 20 cm or 200 g. They are more likely to be functional than nonfunctional, and produce ADRENAL CORTEX HORMONES that may result in hypercortisolism (CUSHING SYNDROME); HYPERALDOSTERONISM; and/or VIRILISM.	0	7.41	1	0
Adrenal Cortex Cancer [description not available]	0	2.41	1	0
Adrenal Cortex Neoplasms Tumors or cancers of the ADRENAL CORTEX.	0	2.41	1	0
Adenoma, Basal Cell [description not available]	0	6.39	5	0
Cancer of Pituitary [description not available]	0	4.86	4	0
Adenoma A benign epithelial tumor with a glandular organization.	0	6.39	5	0
Pituitary Neoplasms Neoplasms which arise from or metastasize to the PITUITARY GLAND. The majority of pituitary neoplasms are adenomas, which are divided into non-secreting and secreting forms. Hormone producing forms are further classified by the type of hormone they secrete. Pituitary adenomas may also be characterized by their staining properties (see ADENOMA, BASOPHIL; ADENOMA, ACIDOPHIL; and ADENOMA, CHROMOPHOBE). Pituitary tumors may compress adjacent structures, including the HYPOTHALAMUS, several CRANIAL NERVES, and the OPTIC CHIASM. Chiasmal compression may result in bitemporal HEMIANOPSIA.	0	4.86	4	0
Local Neoplasm Recurrence [description not available]	0	4.28	2	0
Orphan Diseases Rare diseases that have not been well studied.	0	2.41	1	0
Diseases of Endocrine System [description not available]	0	2.41	1	0
Endocrine System Diseases Pathological processes of the ENDOCRINE GLANDS, and diseases resulting from abnormal level of available HORMONES.	0	2.41	1	0
2019 Novel Coronavirus Disease [description not available]	0	3.81	2	0
Adrenal Gland Hypofunction [description not available]	0	3.86	6	0
Adrenal Insufficiency Conditions in which the production of adrenal CORTICOSTEROIDS falls below the requirement of the body. Adrenal insufficiency can be caused by defects in the ADRENAL GLANDS, the PITUITARY GLAND, or the HYPOTHALAMUS.	0	8.86	6	0
Adrenal Gland Hyperfunction [description not available]	0	2.6	1	0
Adrenocortical Hyperfunction Excess production of ADRENAL CORTEX HORMONES such as ALDOSTERONE; HYDROCORTISONE; DEHYDROEPIANDROSTERONE; and/or ANDROSTENEDIONE. Hyperadrenal syndromes include CUSHING SYNDROME; HYPERALDOSTERONISM; and VIRILISM.	0	2.6	1	0
Benign Neoplasms [description not available]	0	2.76	2	0
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	2.76	2	0
Ectopic ACTH Syndrome [description not available]	0	4.49	2	0
ACTH Syndrome, Ectopic Symptom complex due to ACTH production by non-pituitary neoplasms.	0	4.49	2	0
Aldosteronism [description not available]	0	11.57	18	17
Hyperaldosteronism A condition caused by the overproduction of ALDOSTERONE. It is characterized by sodium retention and potassium excretion with resultant HYPERTENSION and HYPOKALEMIA.	1	13.57	18	17
Adrenal Cancer [description not available]	0	4.04	1	0
ACTH-Producing Pituitary Adenoma [description not available]	0	4.84	2	0
Cirrhosis [description not available]	0	3.92	1	0
Innate Inflammatory Response [description not available]	0	3.92	1	0
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	0	3.92	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	3.92	1	0
Hypertension, Essential [description not available]	0	11.33	16	16
Essential Hypertension Hypertension that occurs without known cause, or preexisting renal disease. Associated polymorphisms for a number of genes have been identified, including AGT, GNB3, and ECE1. OMIM: 145500	1	13.33	16	16
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	3.48	1	1
Cardiac Hypertrophy Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.	0	3.04	1	0
Cardiomegaly Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.	0	3.04	1	0

osilodrostat

Description

Cross-References

Synonyms (48)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (12)

Inhibition Measurements

Biological Processes (77)

Molecular Functions (38)

Ceullar Components (10)

Bioassays (84)

Research

Studies (77)

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Research Demand Index: 61.60

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osilodrostat

Description

Cross-References

Synonyms (48)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (12)

Inhibition Measurements

Biological Processes (77)

Molecular Functions (38)

Ceullar Components (10)

Bioassays (84)

Research

Studies (77)

Market Indicators

Research Demand Index: 61.60

Study Types

Related Drugs (27)

Related Conditions (41)