Page last updated: 2024-12-06

brinzolamide

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Description

Brinzolamide is a carbonic anhydrase inhibitor used to treat open-angle glaucoma and ocular hypertension. It works by decreasing the production of aqueous humor, the fluid that fills the eye, which helps to lower intraocular pressure. Brinzolamide is available as an ophthalmic solution. Its synthesis involves a multi-step process starting from commercially available starting materials. Brinzolamide is important because it offers an effective treatment option for glaucoma, a leading cause of blindness. It is studied extensively to investigate its efficacy and safety, as well as to explore its potential in other ophthalmological conditions.'

brinzolamide: an antiglaucoma agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68844
CHEMBL ID220491
CHEBI ID3176
SCHEMBL ID24636
MeSH IDM0289415

Synonyms (112)

Synonym
AC-5277
BIDD:GT0039
MLS002153787
smr001233169
BRD-K74913225-001-03-3
nsc-760050
CHEMBL220491
al-4862
brinzolamide [usan]
(r)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2h-thieno(3,2-e)-1,2-thiazine-6-sulfonamide 1,1-dioxide
al 4862
azopt
(r)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2h-thieno(3,2-e)-1,2-thiazine-6-sulfonamide
2h-thieno(3,2-e)-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (r)-
BSPBIO_000489
BPBIO1_000539
PRESTWICK3_000365
PRESTWICK2_000365
AB00513824
C07760
138890-62-7
brinzolamide
3ZNC
DB01194
brinzolamide (brz)
CHEBI:3176 ,
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2h-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2h,3h,4h-1$l^{6},7,2-thieno[3,2-e][1,2]thiazine-6-sulfonamide
bdbm10885
azopt (tn)
(+)-4-ethylamino-3,4-dihydro-2-(methoxy)propyl-2h-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide
BZ1 ,
brinzolamide (jan/usp/inn)
D00652
PRESTWICK1_000365
PRESTWICK0_000365
SPBIO_002410
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide
AKOS005145708
HMS1569I11
(r)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2h-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
HMS2096I11
dtxsid6045531 ,
tox21_110722
dtxcid4025531
HMS2234K06
S3178
brinzolamide [usan:usp:inn:ban]
nsc 760050
unii-9451z89515
9451z89515 ,
brinzolamide component of simbrinza
brinzolamide [inn]
simbrinza component brinzolamide
brinzolamide component of azarga
brinzolamide [usp monograph]
brinzolamide [who-dd]
brinzolamide [vandf]
brinzolamide [ema epar]
brinzolamide [orange book]
azarga component brinzolamide
brinzolamide [mart.]
brinzolamide [jan]
brinzolamide [usp-rs]
brinzolamide [mi]
brinzolamide [usp impurity]
gtpl6797
(4r)-4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[4,5-e]thiazine-6-sulfonamide
CCG-220365
CCG-222516
HY-B0588
(r)-3,4-dihydro-4-ethylamino-2-(3-methoxypropyl)-2h-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide
HCRKCZRJWPKOAR-JTQLQIEISA-N
SCHEMBL24636
tox21_110722_1
NCGC00179542-03
(4r)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2h-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
Q-200751
(r)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2h-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide
B4258
AB00513824_06
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2h,3h,4h-1$l^{6},7,2-thieno[3,2-e][1$l^{6},2]thiazine-6-sulfonamide
SR-01000838832-2
sr-01000838832
brinzolamide, united states pharmacopeia (usp) reference standard
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2h-thieno[3,2-e][1,2]thiazine-6-sulfonamide-1,1-dioxide
brinzolamide, >=98% (hplc)
2h-thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4r)-
HMS3713I11
SW197152-3
138890-50-3
BCP22330
Q411517
(5r)-5-ethylamino-3-(3-methoxypropyl)-2,2-dioxo-2,9-dithia-3-azabicyclo[4.3.0]nona-1(6)7-diene-8-sulfonamide
AS-35084
NCGC00179542-10
HMS3885I11
AMY372
NCGC00179542-09
brinzolamide- bio-x
BB164262
s01ec04
brinzolamide (usp-rs)
brinzolamide (mart.)
(r)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2h-thieno(3,2,e)-1,2-thiazine-6-sulfonamide 1,1-dioxide
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2h-thieno(3,2-e)(1,2)thiazine-6-sulfonamide 1,1-dioxide
brinzolamida
brinzolamide (usp monograph)
brinzolamide (usp impurity)
brinzolamidum
EN300-7404820
(4r)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2h,3h,4h-1lambda6-thieno[3,2-e][1,2]thiazine-6-sulfonamide

Research Excerpts

Overview

Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. Its use is restricted due to inadequate aqueous solubility and permeability.

ExcerptReferenceRelevance
"Brinzolamide is an effective carbonic anhydrase inhibitor widely used in glaucoma therapy but limits its application due to inadequate aqueous solubility and permeability. "( Exploring Penetration Ability of Carbonic Anhydrase Inhibitor-Loaded Ultradeformable Bilosome for Effective Ocular Application.
Bhavana, V; Mehra, NK; Nair, VS; Rajana, N; Singh, SB; Srivastava, V; Yadav, R, 2023
)
2.35
"Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. "( Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.
Dangi, JS; Dubey, V; Kesavan, K; Mohan, P, 2020
)
3.44
"Brinzolamide (BLZ) is a drug used to treat glaucoma; however, its use is restricted due to some unwanted adverse events. "( Ophthalmic delivery of brinzolamide by liquid crystalline nanoparticles: in vitro and in vivo evaluation.
Li, J; Wang, B; Wang, Z; Wu, L; Wu, W; Xin, H; Xu, Q, 2013
)
2.14
"Brinzolamide (BRZ) is a kind of carbonic anhydrase inhibitors for glaucoma treatment."( Development of inclusion complex of brinzolamide with hydroxypropyl-β-cyclodextrin.
Chen, T; He, G; He, Z; Lei, Y; Li, H; Ren, K; Song, X; Xia, S; Xie, Y; Zhang, Y; Zheng, Y, 2013
)
1.39
"Brinzolamide is a highly specific carbonic anhydrase (CA) inhibitor which lowers intraocular pressure (IOP) by reducing the rate of aqueous humour formation. "( Brinzolamide : a review of its use in the management of primary open-angle glaucoma and ocular hypertension.
Cvetkovic, RS; Perry, CM, 2003
)
3.2
"Brinzolamide is a new topical carbonic anhydrase inhibitor for intraocular pressure (IOP) control. "( Ocular hypotensive effect and safety of brinzolamide ophthalmic solution in open angle glaucoma patients.
Chen, YF; Huang, JY; Hung, PT; Shieh, JW; Wang, TH, 2004
)
2.03
"Brinzolamide is a new topically active CAI that is safe a"( Preclinical overview of brinzolamide.
DeSantis, L, 2000
)
1.34
"Brinzolamide is a novel carbonic anhydrase inhibitor that elicits an ocular hypotensive effect when instilled topically. "( Dose-response evaluation of the ocular hypotensive effect of brinzolamide ophthalmic suspension (Azopt). Brinzolamide Dose-Response Study Group.
Silver, LH, 2000
)
1.99

Effects

Brinzolamide has been shown by the laser Doppler flowmetry technique to improve blood flow to the optic nerve head in pigmented rabbits after topical administration.

ExcerptReferenceRelevance
"Brinzolamide/brimonidine has increased by 50.0% from 2016 to 2017."( Prescribing Trends of Topical Glaucoma Medications in Australia From 2001 to 2017.
Chen, O; Jamieson, MPH; Ling, D; Perera, N; Pinnuck, BC; Williams, M, 2020
)
1.28
"Brinzolamide has been shown by the laser Doppler flowmetry technique to improve blood flow to the optic nerve head in pigmented rabbits after topical administration, without producing an increase of blood pCO2, indicating a potential for a local vasodilatory effect involving the optic nerve head circulation."( Preclinical overview of brinzolamide.
DeSantis, L, 2000
)
1.34

Actions

ExcerptReferenceRelevance
"Brinzolamide may cause a short-term increase in the human CCT, particularly on the first day."( Short-term effect of topical brinzolamide on human central corneal thickness.
Ergin, A; Gullu, R; Ogurel, T; Ornek, K,
)
1.87

Treatment

Treatment with brinzolamide/travoprost caused statistically significant sustained reduction in intraocular pressure with the reduction of 17.39% (p < 0.001) after 4 weeks and 20.08% after 12 weeks.

ExcerptReferenceRelevance
"Treatment with brinzolamide/travoprost caused statistically significant sustained reduction in intraocular pressure with the reduction of 17.39% (p < 0.001) after 4 weeks and 20.08% (p < 0.001) after 12 weeks."( [Adjunctive therapy with brinzolamide in patients on travoprost treatment].
Andreić, V; Babić, N; Barisić, S; Canadanović, V; Miljković, A,
)
0.77
"Treatment with brinzolamide 1.0% was safe, comfortable, and well tolerated."( Clinical efficacy and safety of brinzolamide (Azopt), a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension. Brinzolamide Primary Therapy Study Group.
Silver, LH, 1998
)
0.92

Toxicity

Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people. The outcome measure was the development of an adverse reaction (either ocular, systemic, or both) within at least 30 days after receipt of 1 of 4 topical glaucoma medications.

ExcerptReferenceRelevance
" One hundred forty-four patients were discontinued from the study after randomization with the most common reasons being the occurrence of an adverse event (46), inadequate intraocular pressure control (23), patient decision unrelated to study medication (11), lost to follow-up (16), and noncompliance (9)."( The long-term safety and efficacy of brinzolamide 1.0% (azopt) in patients with primary open-angle glaucoma or ocular hypertension. The Brinzolamide Long-Term Therapy Study Group.
March, WF; Ochsner, KI, 2000
)
0.58
" Brinzolamide was safe and well tolerated by patients, with minimal ocular discomfort."( The long-term safety and efficacy of brinzolamide 1.0% (azopt) in patients with primary open-angle glaucoma or ocular hypertension. The Brinzolamide Long-Term Therapy Study Group.
March, WF; Ochsner, KI, 2000
)
1.49
" The most frequent side effect was ocular pain in the case of 2% dorzolamide and blurred vision in 1% brinzolamide."( Comparisons of intraocular-pressure- lowering efficacy and side effects of 2% dorzolamide and 1% brinzolamide.
Chu, YK; Hong, YJ; Lee, JH; Lee, SC; Seong, GJ,
)
0.56
" The study medications were generally well tolerated and no serious adverse reactions occurred during the 6-week study period."( Ocular hypotensive effect and safety of brinzolamide ophthalmic solution in open angle glaucoma patients.
Chen, YF; Huang, JY; Hung, PT; Shieh, JW; Wang, TH, 2004
)
0.59
" Adverse events were recorded at each visit."( Concomitant administration of travoprost and brinzolamide versus fixed latanoprost/timolol combined therapy: three-month comparison of efficacy and safety.
Castillo, A; Fernandez-Vidal, A; Garcia-Feijoo, J; Garcia-Sanchez, J; Martinez-de-la-Casa, JM; Mendez-Hernandez, C, 2004
)
0.58
" Common adverse events were mild and included ocular hyperaemia, dysgeusia and eye irritation."( Ocular hypotensive efficacy and safety of brinzolamide ophthalmic suspension 1% added to travoprost ophthalmic solution 0.004% therapy in patients with open-angle glaucoma or ocular hypertension.
Franks, W, 2006
)
0.6
" The IOP and the side effect before and after the administration of the eyedrops were observed."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
0.55
"Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
2
" There was no significant difference for any adverse event between groups (p>0."( The efficacy and safety of timolol maleate versus brinzolamide each given twice daily added to travoprost in patients with ocular hypertension or primary open-angle glaucoma.
Berta, A; Chiselita, D; Cvenkel, B; Holló, G; Izgi, B; Liehneova, I; Petkova, N; Stewart, WC; Szaflik, J; Turacli, E,
)
0.38
" As systemic adverse events, there was one instance of malar flushing after brinzolamide addition and episodes of chest discomfort after timolol addition in 1 patient."( Comparison of ocular hypotensive effect and safety of brinzolamide and timolol added to latanoprost.
Ito, K; Matsunaga, K; Miura, K; Okawa, C; Sugimoto, K; Uji, Y,
)
0.61
" A total of 143 patients experienced at least 1 treatment-related adverse event (AE; BBFC group, n=58, 26."( Phase 3 randomized 3-month trial with an ongoing 3-month safety extension of fixed-combination brinzolamide 1%/brimonidine 0.2%.
Goode, SM; McMenemy, MG; Nguyen, QH; Realini, T; Whitson, JT, 2013
)
0.61
"To investigate whether a self-reported history of allergy to sulfa-based drugs is a predictor for subsequent adverse reactions to topical carbonic anhydrase inhibitors (CAIs)."( Evaluation of adverse events in self-reported sulfa-allergic patients using topical carbonic anhydrase inhibitors.
Guedes, GB; Karan, A; Mayer, HR; Shields, MB, 2013
)
0.39
" The outcome measure was the development of an adverse reaction (either ocular, systemic, or both) within at least 30 days after receipt of 1 of 4 classes of topical glaucoma medications: CAIs (dorzolamide and brinzolamide), prostaglandin analogues, beta-adrenergic blockers, and alpha2-adrenergic agonists."( Evaluation of adverse events in self-reported sulfa-allergic patients using topical carbonic anhydrase inhibitors.
Guedes, GB; Karan, A; Mayer, HR; Shields, MB, 2013
)
0.58
"Patients with a self-reported history of sulfa allergy had significantly more ocular adverse reactions after the initiation of any of the topical antiglaucoma medications when compared to those patients with no reported allergies."( Evaluation of adverse events in self-reported sulfa-allergic patients using topical carbonic anhydrase inhibitors.
Guedes, GB; Karan, A; Mayer, HR; Shields, MB, 2013
)
0.39
"It may be safe to use a topical CAI in patients who report a history of a sulfa allergy."( Evaluation of adverse events in self-reported sulfa-allergic patients using topical carbonic anhydrase inhibitors.
Guedes, GB; Karan, A; Mayer, HR; Shields, MB, 2013
)
0.39
" Safety was assessed with adverse event rates, ocular discomfort score, blur scale, blood pressure and heart rates, best-corrected visual acuity (BCVA) and slit lamp examinations."( Additive effects and safety of fixed combination therapy with 1% brinzolamide and 0.5% timolol versus 1% dorzolamide and 0.5% timolol in prostaglandin-treated glaucoma patients.
Adachi, M; Aihara, M; Fukuchi, T; Matsuo, H; Sasaki, N; Togano, T, 2017
)
0.69
" Thus, BTFC can be considered as a safe and effective agent for glaucoma treatment."( Additive effects and safety of fixed combination therapy with 1% brinzolamide and 0.5% timolol versus 1% dorzolamide and 0.5% timolol in prostaglandin-treated glaucoma patients.
Adachi, M; Aihara, M; Fukuchi, T; Matsuo, H; Sasaki, N; Togano, T, 2017
)
0.69
" The intraocular pressure (IOP), mean deviation value, and adverse drug reactions were evaluated."( The Efficacy and Safety of the Fixed Combination of Brinzolamide 1% and Brimonidine 0.2% in Normal Tension Glaucoma: An 18-Month Retrospective Study.
Jin, SW; Lee, SM, 2018
)
0.73
" There were no serious adverse drug reactions."( The Efficacy and Safety of the Fixed Combination of Brinzolamide 1% and Brimonidine 0.2% in Normal Tension Glaucoma: An 18-Month Retrospective Study.
Jin, SW; Lee, SM, 2018
)
0.73
"BBFC provides a significant IOP reduction and is a safe antiglaucoma medication for NTG patients."( The Efficacy and Safety of the Fixed Combination of Brinzolamide 1% and Brimonidine 0.2% in Normal Tension Glaucoma: An 18-Month Retrospective Study.
Jin, SW; Lee, SM, 2018
)
0.73
"BBFC had satisfactory IOP-lowering effects without serious adverse reactions in patients who switched medications."( Intraocular pressure-lowering effects and safety of brimonidine/brinzolamide fixed combination after switching from other medications.
Inoue, K; Ishida, K; Kunimatsu-Sanuki, S; Tomita, G, 2022
)
0.96

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters (C(max), T(max), and AUC(0-24)) were estimated by noncompartmental analysis."( Ocular pharmacokinetics of dorzolamide and brinzolamide after single and multiple topical dosing: implications for effects on ocular blood flow.
Jadhav, G; Kadam, RS; Kompella, UB; Ogidigben, M, 2011
)
0.63
" The pharmacodynamic studies were conducted for CPNCs on glaucoma induced rabbit eye model and compared with marketed product."( Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.
Dangi, JS; Dubey, V; Kesavan, K; Mohan, P, 2020
)
2
" In pharmacodynamic study, greater intraocular pressure lowering effect was achieved by CPNCs as compared to marketed drug product."( Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.
Dangi, JS; Dubey, V; Kesavan, K; Mohan, P, 2020
)
2

Compound-Compound Interactions

Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people.

ExcerptReferenceRelevance
"To evaluate the intraocular pressure (IOP) lowering efficacy and safety of Brinzolamide combined with Betaxolol for the Chinese glaucomatous patients."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
0.78
"Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
2
"The multiple drug interactions in which CAIs are involved should be carefully considered when such drugs are used in combination with the drug classes mentioned above, as the risks of developing toxicity and serious side effects if the dosages are not adjusted are high."( Drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors.
Supuran, CT, 2016
)
0.43
"To examine the relevance of concentration of benzalkonium chloride (BAK) on the cornea, we investigated the effects of latanoprost containing BAK alone and in combination with other antiglaucoma drug classes on corneal epithelium in vitro in a cultured rabbit corneal cell line (SIRC) and in vivo, using a corneal resistance device (CRD)."( In vitro and in vivo corneal effects of latanoprost combined with brimonidine, timolol, dorzolamide, or brinzolamide.
Fukuda, M; Sasaki, H; Shibata, N; Shibata, S; Shibata, T; Sugiyama, K; Takeda, N, 2016
)
0.65

Bioavailability

Brinzolamide, a lipophilic drug belongs to carbonic anhydrase inhibitors, which cause reduction of intraocular pressure in patients suffering from glaucoma. This formulation is safe for ophthalmic use and significantly increases brinZolamide bioavailability in aqueous humor.

ExcerptReferenceRelevance
" Furthermore, the bioavailability of these derivatives in rabbits is comparable to that of acetazolamide, being in the range of 85-90%, showing them as promising candidates for systemically acting CA inhibitors."( Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails.
Scozzafava, A; Supuran, CT, 2002
)
0.31
" Thus this formulation is safe for ophthalmic use and significantly increases brinzolamide bioavailability in aqueous humor."( Design and evaluation of a brinzolamide drug-resin in situ thermosensitive gelling system for sustained ophthalmic drug delivery.
Cai, CN; Li, J; Liu, H; Liu, LL; Liu, W; Xin, HX, 2014
)
0.93
" However, the conventional formulation of TM and BRZ exhibits sub optimal therapeutic effects attributable to the poor ocular bioavailability of these drugs."( Fabrication and Characterization of Timolol Maleate and Brinzolamide Loaded Nanostructured Lipid Carrier System for Ocular Drug Delivery.
Ali, J; Baboota, S; Khan, S; Shrivastava, N, 2018
)
0.73
"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
"The result concluded that CPNCs are a feasible choice to conventional eye drops because of its ability to improve the bioavailability via its longer precorneal retention time and its ability to sustained release of the drug."( Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.
Dangi, JS; Dubey, V; Kesavan, K; Mohan, P, 2020
)
2
"In recent years, the hydrophobic active substances have led researchers to develop new formulations to enhance bioavailability and dissolution rate; brinzolamide, a lipophilic drug belongs to carbonic anhydrase inhibitors, which cause reduction of intraocular pressure in patients suffering from glaucoma."( Ocular microemulsion of brinzolamide: Formulation, physicochemical characterization, and in vitro irritation studies based on EpiOcular™ eye irritation assay.
Aydın, A; Çağlar, EŞ; Charehsaz, M; Siafaka, PI; Sipahi, H; Üstündağ Okur, N, 2021
)
1.13

Dosage Studied

The current study reveals that 1 drop of brinzolamide 1% is sufficient to control IOP within the first 4 to 6 hours following uneventful phacoemulsification. 12-hour dosing is necessary for prolonged control of IOP.

ExcerptRelevanceReference
" The degree of tolerability in the eye is considered an important determinant of a patient's willingness to comply with the dosing regimen for a long-term glaucoma medication."( Preclinical overview of brinzolamide.
DeSantis, L, 2000
)
0.61
"0%, dosed two times (b."( The efficacy and safety of brinzolamide 1% ophthalmic suspension (Azopt) as a primary therapy in patients with open-angle glaucoma or ocular hypertension. Brinzolamide Primary Therapy Study Group.
Sall, K, 2000
)
0.6
"9 mm Hg with brinzolamide twice-daily dosing and -2."( The long-term safety and efficacy of brinzolamide 1.0% (azopt) in patients with primary open-angle glaucoma or ocular hypertension. The Brinzolamide Long-Term Therapy Study Group.
March, WF; Ochsner, KI, 2000
)
0.95
"Brinzolamide produced significant and equivalent reductions in intraocular pressure when dosed two and three times daily for 18 months."( The long-term safety and efficacy of brinzolamide 1.0% (azopt) in patients with primary open-angle glaucoma or ocular hypertension. The Brinzolamide Long-Term Therapy Study Group.
March, WF; Ochsner, KI, 2000
)
2.02
" No differences between groups were observed preinstillation nor following dosing at 3 or 10-min postinstillation."( Short-term ocular tolerability of dorzolamide 2% and brinzolamide 1% vs placebo in primary open-angle glaucoma and ocular hypertension subjects.
Day, DG; Holmes, KT; Jenkins, JN; Stewart, JA; Stewart, WC, 2004
)
0.57
" However, pain symptoms are fewer following chronic dosing and are generally characterized as mild."( Short-term ocular tolerability of dorzolamide 2% and brinzolamide 1% vs placebo in primary open-angle glaucoma and ocular hypertension subjects.
Day, DG; Holmes, KT; Jenkins, JN; Stewart, JA; Stewart, WC, 2004
)
0.57
"Qualified patients at Visit 1 were placed on travoprost dosed every evening for 4 weeks and then were randomized at baseline (Visit 2) to the addition of timolol maleate or brinzolamide each given twice daily."( The efficacy and safety of timolol maleate versus brinzolamide each given twice daily added to travoprost in patients with ocular hypertension or primary open-angle glaucoma.
Berta, A; Chiselita, D; Cvenkel, B; Holló, G; Izgi, B; Liehneova, I; Petkova, N; Stewart, WC; Szaflik, J; Turacli, E,
)
0.58
"5%, both dosed twice daily."( Efficacy of brinzolamide and levobetaxolol in pediatric glaucomas: a randomized clinical trial.
Bergamini, MV; Dickerson, JE; Gross, RD; Hua, SY; Landry, TA; Roarty, JD; Robin, AL; Scheib, SA; Scott, H; Vijaya, L; Whitson, JT; Woodside, AM, 2008
)
0.72
"5%, dosed twice daily and were followed up while receiving therapy for 6 months."( Intraocular pressure-lowering efficacy of brinzolamide 1%/timolol 0.5% fixed combination compared with brinzolamide 1% and timolol 0.5%.
Arzeno, G; Bergamini, MV; Dickerson, JE; Hua, SY; James, JE; Kaback, M; Landry, TA; Salem, C; Scoper, SV, 2008
)
0.61
"To compare the effectiveness of only 1 drop of topical brinzolamide 1% with dosing every 12 hours and with no ocular hypotensive medication following clear corneal phacoemulsification surgery."( Medical control of intraocular pressure with brinzolamide 1% after phacoemulsification.
Cakmak, H; Dayanir, V; Kir, E, 2008
)
0.85
"The current study reveals that 1 drop of brinzolamide 1% is sufficient to control IOP within the first 4 to 6 hours following uneventful phacoemulsification, whereas 12-hour dosing is necessary for prolonged control of IOP."( Medical control of intraocular pressure with brinzolamide 1% after phacoemulsification.
Cakmak, H; Dayanir, V; Kir, E, 2008
)
0.87
"Of the 437 patients enrolled, 220 dosed Brinz/Tim whereas 217 dosed Dorz/Tim twice daily."( The safety and efficacy of brinzolamide 1%/timolol 0.5% fixed combination versus dorzolamide 2%/timolol 0.5% in patients with open-angle glaucoma or ocular hypertension.
Aung, T; Chew, P; Coote, MA; Denis, P; Filatori, I; James, J; Laganovska, G; Manni, G; Orengo-Nania, S; Sharpe, ED; Volksone, L; Zeyen, T,
)
0.43
" However, their short duration of action requiring multiple daily dosing can hamper patient compliance."( Cyclodextrin solubilization of carbonic anhydrase inhibitor drugs: formulation of dorzolamide eye drop microparticle suspension.
Bas, JF; Jansook, P; Kristjánsdóttir, SS; Loftsson, T; Sigurdsson, BB; Sigurdsson, HH; Stefánsson, E; Thorsteinsdóttir, M, 2010
)
0.36
" For multiple dosing, rabbits were dosed twice per day with an 8-h interval between two doses, groups of rabbits were euthanized at 7, 14, and 21 days at 1 h after the last dose, and ocular tissues and plasma samples were collected."( Ocular pharmacokinetics of dorzolamide and brinzolamide after single and multiple topical dosing: implications for effects on ocular blood flow.
Jadhav, G; Kadam, RS; Kompella, UB; Ogidigben, M, 2011
)
0.63
" Targeting of multiple mechanisms in combination therapies has proven effective both clinically and commercially although potential improvements with regards to efficacy, tolerability and dosing frequency remain."( A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma.
Frieman, B; Hegde, SS; Hill, CM; Jiang, L; Kintz, S; Long, DD; Marquess, DG; Purkey, H; Shaw, JP; Steinfeld, T; Wilson, MS; Wrench, K, 2013
)
0.39
"2% monotherapy, all dosed 2 times per day (BID)."( Twice-daily brinzolamide/brimonidine fixed combination versus brinzolamide or brimonidine in open-angle glaucoma or ocular hypertension.
Aung, T; Branch, JD; Goldberg, I; Hernandez Paredes, TJ; Laganovska, G; Tsorbatzoglou, A, 2014
)
0.78
"Timolol is a non-cardioselective beta blocker and has different combined ophthalmic dosage forms for treatment of glaucoma."( A versatile HPLC method with an isocratic single mobile phase system for simultaneous determination of anti-glaucoma formulations containing timolol.
El Abass, SA; Elmansi, HM; Ibrahim, FA, 2019
)
0.51
"Despite the advances in the field of pharmaceutical materials and technology, topical administration remains a method of choice for the treatment of eye diseases such as glaucoma, with eye drops being a leading dosage form."( Mucoadhesive brinzolamide-loaded nanofibers for alternative glaucoma treatment.
Cegielska, O; Kogermann, K; Lorenz, K; Sajkiewicz, P; Sierakowski, M, 2022
)
1.09
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antiglaucoma drugAny drug which can be used to prevent or alleviate glaucoma, a disease in which the optic nerve is damaged, resulting in progressive, irreversible loss of vision. It is often, though not always, associated with increased pressure of the fluid in the eye.
EC 4.2.1.1 (carbonic anhydrase) inhibitorAn EC 4.2.1.* (hydro-lyases) inhibitor that interferes with the action of carbonic anhydrase (EC 4.2.1.1). Such compounds reduce the secretion of H(+) ions by the proximal kidney tubule.
[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 (2)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
thienothiazine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (54)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency2.98490.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency0.92000.000811.382244.6684AID686978
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency43.64860.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency38.90180.00108.379861.1304AID1645840
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency0.70790.707936.904389.1251AID504333
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
importin subunit beta-1 isoform 1Homo sapiens (human)Potency29.09295.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency29.09295.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency29.09295.804816.996225.9290AID540253
[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)
Chain A, CARBONIC ANHYDRASE IVMus musculus (house mouse)IC50 (µMol)0.04530.04530.04530.0453AID977608
Carbonic anhydrase Astrosclera willeyanaKi0.27800.03201.51729.6000AID644379
Carbonic anhydrase Sulfurihydrogenibium sp. YO3AOP1Ki0.01230.00450.16240.8760AID1268964
Carbonic anhydrase Stylophora pistillataKi0.04820.00000.686710.0000AID436565; AID552130
Carbonic anhydraseStylophora pistillataKi0.16900.00000.50715.7100AID552131
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Carbonic anhydraseHelicobacter pylori 26695Ki0.22800.02000.54864.3600AID261581; AID263638
Carbonic anhydrase 12Homo sapiens (human)Ki0.00300.00021.10439.9000AID1067227; AID1204091; AID1593068; AID238316; AID239126; AID239284; AID272527; AID293193; AID311032; AID327767; AID353231; AID770582; AID780321
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Carbonic anhydrase 1Homo sapiens (human)Ki25.86380.00001.372610.0000AID1067230; AID1142833; AID1188134; AID1190063; AID1194024; AID1195369; AID1262263; AID1268962; AID1275913; AID1287517; AID1434427; AID1453412; AID1593065; AID1605088; AID1628036; AID1796552; AID1796755; AID1796855; AID1797360; AID1797528; AID1798769; AID261579; AID263636; AID271710; AID275807; AID281082; AID300867; AID311023; AID317579; AID327758; AID349605; AID353228; AID367820; AID369271; AID414955; AID427125; AID436563; AID47725; AID47726; AID50361; AID50371; AID50374; AID552127; AID577526; AID587130; AID612725; AID644380; AID725955; AID743515; AID764719; AID770586
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)0.02420.00021.10608.3000AID1200902; AID1796686; AID47746
Carbonic anhydrase 2Homo sapiens (human)Ki3,634.67370.00000.72369.9200AID1061069; AID1067229; AID1142834; AID1188135; AID1190064; AID1194025; AID1195370; AID1240217; AID1262264; AID1268963; AID1275912; AID1278409; AID1287518; AID1434428; AID1453413; AID1593066; AID1605089; AID1628037; AID1796552; AID1796582; AID1796687; AID1796755; AID1796855; AID1797360; AID1797528; AID1798769; AID238220; AID238255; AID238300; AID238635; AID238768; AID238787; AID238850; AID256963; AID261580; AID263049; AID263637; AID271711; AID272521; AID275808; AID281083; AID300868; AID311024; AID317580; AID327759; AID349606; AID353229; AID367821; AID369272; AID414956; AID427124; AID436564; AID437749; AID448552; AID47902; AID47915; AID47929; AID47931; AID47935; AID47939; AID47940; AID47942; AID552128; AID577527; AID587131; AID612726; AID644381; AID669115; AID725956; AID726603; AID743514; AID764718; AID770585; AID780325
Carbonic anhydrase 3Homo sapiens (human)Ki110.00000.00022.010210.0000AID301578; AID327760
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.00300.00020.667710.0000AID47929; AID47942
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00300.00010.601710.0000AID47929; AID47942
Carbonic anhydrase 4Homo sapiens (human)IC50 (µMol)0.03130.00320.31712.0000AID1796686; AID48293
Carbonic anhydrase 4Homo sapiens (human)Ki3.95000.00021.97209.9200AID1605090; AID327761
Carbonic anhydrase 6Homo sapiens (human)Ki0.00840.00011.47109.9200AID1798769; AID275806; AID311029; AID327764; AID369273; AID552129; AID780324
Carbonic anhydrase 5A, mitochondrialMus musculus (house mouse)Ki0.03300.00300.45603.0000AID1797528
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.00300.00020.590910.0000AID47929; AID47942
Delta-type opioid receptorMus musculus (house mouse)Ki22.50150.00000.53939.4000AID1188134; AID1188135
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00300.00000.60689.2330AID1188135
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki45.00000.00000.38458.6000AID1188134
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.04040.00001.27259.9000AID1796582; AID256964; AID272523; AID311027; AID327762
Carbonic anhydrase 7Homo sapiens (human)Ki0.00280.00021.37379.9000AID1605091; AID238256; AID272525; AID311030; AID327765; AID764717; AID770584; AID780323
Carbonic anhydraseSaccharomyces cerevisiae S288CKi0.11400.08200.56098.7000AID367822
Carbonic anhydrase Mycobacterium tuberculosis H37RvKi0.20100.01202.72389.1200AID448554
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00300.00000.27869.0000AID1188135
Beta-carbonic anhydrase 1Mycobacterium tuberculosis H37RvKi0.83900.00483.38419.8400AID1798985; AID349607; AID448553
Carbonic anhydrase 2Mycobacterium tuberculosis H37RvKi0.12700.00902.20969.8400AID437750
Carbonic anhydrase 9Homo sapiens (human)Ki0.03460.00010.78749.9000AID1067228; AID1593067; AID1796755; AID1796855; AID1797360; AID1798769; AID238224; AID238769; AID238788; AID239048; AID239102; AID271712; AID272526; AID275809; AID281084; AID300869; AID311031; AID317581; AID327766; AID353230; AID369274; AID48296; AID48299; AID48300; AID48301; AID770583; AID780322
Carbonic anhydrase, alpha family Hydrogenovibrio crunogenus XCL-2Ki0.00420.00250.32341.1000AID1268965
Carbonic anhydrase Cryptococcus neoformans var. grubiiKi0.08700.01000.73648.3470AID669116
Carbonic anhydraseCandida albicans SC5314Ki0.84300.01051.44448.3470AID1799266; AID427122; AID669117
Carbonic anhydrase Anopheles gambiae (African malaria mosquito)Ki0.03140.00980.51174.3600AID1195371
Delta carbonic anhydraseConticribra weissflogiiKi0.11800.04960.99789.2000AID1061066
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ki4.35000.00701.21749.1700AID744415
Carbonic anhydrase 13Homo sapiens (human)Ki0.01100.00031.23099.8000AID780320
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Carbonic anhydrase 4Bos taurus (cattle)Ki3,483,830.80420.00300.59349.6500AID1796755; AID1797528; AID263050; AID48122; AID48123; AID48132; AID48280; AID48281; AID48286
Carbonic anhydrase 15Mus musculus (house mouse)Ki0.04100.00091.884610.0000AID1798769; AID369275
Carbonic anhydrase 13Mus musculus (house mouse)Ki0.01000.00021.39749.9000AID327768
Carbonic anhydrase 14Homo sapiens (human)Ki0.02400.00021.50999.9000AID239703; AID272529; AID293194; AID311034; AID327769; AID780319
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki0.02900.00001.34129.9700AID1796582; AID256965; AID272524; AID311028; AID327763
[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)
Carbonic anhydrase 2Homo sapiens (human)Kd0.00010.00000.41575.5500AID1200901; AID1796823
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Carbonic anhydrase Brucella suis 1330Kinact0.02600.01700.86285.8700AID459696
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC500.03980.039815.002550.0000AID743267
Carbonic anhydrase 12Homo sapiens (human)Kinact0.00300.00300.66749.6000AID299547; AID408472
Carbonic anhydrase 1Homo sapiens (human)Kinact45.00000.01000.93878.6000AID299242; AID299538; AID408469
Carbonic anhydrase 2Homo sapiens (human)Kinact0.00300.00300.794610.0000AID299243; AID299539; AID408470
Carbonic anhydrase 4Homo sapiens (human)Kinact3.95000.07402.39348.5900AID300467
Carbonic anhydrase 6Homo sapiens (human)Kinact0.00090.00090.72615.3000AID299544
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Kinact0.05000.02000.85809.4000AID299542
Carbonic anhydrase 7Homo sapiens (human)Kinact0.00280.00020.28525.7300AID299545
Carbonic anhydrase 9Homo sapiens (human)Kinact0.03700.00500.31976.6700AID299546; AID408471
Carbonic anhydrase 14Homo sapiens (human)Kinact0.02400.00021.44958.5900AID299549
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Kinact0.03000.00900.92319.0400AID299543
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (61)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
estrous cycleCarbonic anhydrase 12Homo sapiens (human)
chloride ion homeostasisCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 12Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
response to bacteriumCarbonic anhydrase 3Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 3Homo sapiens (human)
bicarbonate transportCarbonic anhydrase 4Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 4Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter tasteCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 7Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 7Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 7Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 7Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 7Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 7Homo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 13Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 14Homo sapiens (human)
response to bacteriumCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 12Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 12Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 3Homo sapiens (human)
protein bindingCarbonic anhydrase 3Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 3Homo sapiens (human)
nickel cation bindingCarbonic anhydrase 3Homo sapiens (human)
protein bindingCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 13Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 13Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 13Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Bos taurus (cattle)
zinc ion bindingCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 12Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 12Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytoplasmCarbonic anhydrase 3Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 4Homo sapiens (human)
rough endoplasmic reticulumCarbonic anhydrase 4Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentCarbonic anhydrase 4Homo sapiens (human)
Golgi apparatusCarbonic anhydrase 4Homo sapiens (human)
trans-Golgi networkCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
external side of plasma membraneCarbonic anhydrase 4Homo sapiens (human)
cell surfaceCarbonic anhydrase 4Homo sapiens (human)
membraneCarbonic anhydrase 4Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 4Homo sapiens (human)
transport vesicle membraneCarbonic anhydrase 4Homo sapiens (human)
secretory granule membraneCarbonic anhydrase 4Homo sapiens (human)
brush border membraneCarbonic anhydrase 4Homo sapiens (human)
perinuclear region of cytoplasmCarbonic anhydrase 4Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
extracellular regionCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
cytosolCarbonic anhydrase 6Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytosolCarbonic anhydrase 7Homo sapiens (human)
cytoplasmCarbonic anhydrase 7Homo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
cytosolCarbonic anhydrase 13Homo sapiens (human)
myelin sheathCarbonic anhydrase 13Homo sapiens (human)
intracellular membrane-bounded organelleCarbonic anhydrase 13Homo sapiens (human)
cytoplasmCarbonic anhydrase 13Homo sapiens (human)
cytosolCarbonic anhydrase 13Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
side of membraneCarbonic anhydrase 4Bos taurus (cattle)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
membraneCarbonic anhydrase 14Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 14Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 14Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (435)

Assay IDTitleYearJournalArticle
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
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.
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
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID1434430Inhibition of Vibrio cholerae Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID47720Inhibitory activity against Human Carbonic anhydrase I2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID587132Inhibition of Leptonychotes weddellii alpha-carbonic anhydrase after 15 mins by CO2 hydrase assay at pH 7.52011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii.
AID1434429Inhibition of Burkholderia pseudomallei Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID711212Inhibition of recombinant Vibrio cholerae carbonic anhydrase expressed in Escherichia coli (DE3) preincubated for 15 mins by stopped-flow CO2 hydrase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID437750Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c.
AID1142838Inhibition of Helicobacter pylori carbonic anhydrase by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID1726079Inhibition of Vibrio cholerae beta carbonic anhydrase pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in
AID238620Inhibitory activity against cytosolic human carbonic anhydrase I2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
AID1188135Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID408469Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII.
AID552131Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1628036Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID780321Inhibition of human carbonic anhydrase12 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID1200919Inhibition of carbonic anhydrase in pigmented male Dutch-belted rabbit treated with 3% 2 x 25 uL topical dose of formulated compound in each eye after 2 to 8 hrs by pH-STAT method2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID448552Inhibition of human cloned full length carbonic anhydrase 2 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides.
AID577531Inhibition of Brucella suis carbonic anhydrase I by spectrophotometry at pH 8.32011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID275809Inhibition of catalytic domain of human recombinant CA IX2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID1142834Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID408470Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII.
AID166441In vivo intraocular pressure (IOP) lowering at 30 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID764717Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID327769Inhibition of human full length carbonic anhydrase 14 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID369272Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID244399Selectivity ratio of Inhibitory constant against human carbonic anhydrase II to carbonic anhydrase IX2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
AID1453411Inhibition of Burkholderia pseudomallei beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID1188136Inhibition of Helicobacter pylori Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID1190065Inhibition of Plasmodium falciparum Eta-carbonic anhydrase pre-incubated for 15 mins before CO2 substrate addition by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID1278409Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID272522Inhibition of human cloned CA4 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID327767Inhibition of human catalytic domain carbonic anhydrase 12 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID263049Inhibition of human CA22006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
QSAR study on topically acting sulfonamides incorporating GABA moieties: a molecular connectivity approach.
AID1809976Solubility of compound in water2021Bioorganic & medicinal chemistry letters, 12-01, Volume: 53Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors.
AID1278410Inhibition of Porphyromonas gingivalis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1275913Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID1200925Reduction in intraocular pressure in pigmented male Dutch-belted rabbit treated with 1% 2 x 25 uL topical dose of formulated compound in right eye and measured after 1 to 2 hrs by non-contact tonometry2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID437749Inhibition of human recombinant CA2 by stopped-flow hydration assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c.
AID272526Inhibition of catalytic domain of human cloned CA9 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID261581Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID166333Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 60 min at a pH of 5.52003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
AID300870Selectivity ratio of Ki for human cloned CA1 to Ki for human cloned catalytic domain CA92007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.
AID256965Inhibitory activity against human recombinant mitochondrial isozyme CA VB2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID1200901Binding affinity to human carbonic anhydrase 2 incubated for 1 hr using labeled BODIPY558/568-acetazolamide as tracer by fluorescence polarization tight binding assay2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID349605Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID369274Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID1204106Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Sulfonamide inhibition study of the β-class carbonic anhydrase from the caries producing pathogen Streptococcus mutans.
AID48122Inhibitory activity against bovine carbonic anhydrase IV2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID272528Inhibition of murine CA13 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID1204093Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-2 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-92015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII.
AID317582Selectivity for human CA9 over human CA12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
AID146521In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 60 min2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID1190064Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID349606Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID587130Inhibition of human carbonic anhydrase 1 after 15 mins by CO2 hydrase assay at pH 7.52011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii.
AID577526Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.52011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID311031Inhibition of human carbonic anhydrase 92007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID299543Inhibition of human CA5B2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID47726Inhibitory activity against human cloned isoenzyme carbonic anhydrase II (hCA II) by esterase method2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives.
AID1287520Inhibition of recombinant Enterobacter sp. B13 beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID427122Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID48281Inhibitory activity against bovine lung microsomes carbonic anhydrase isozyme IV (bCA IV).1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring?
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1268963Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID1194024Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID299243Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID272525Inhibition of human cloned CA7 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID299551Inhibition of Helicobacter pylori beta CA2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID353229Inhibition of human recombinant CA2 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties.
AID780322Inhibition of human carbonic anhydrase9 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID327766Inhibition of human catalytic domain carbonic anhydrase 9 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID238567Ki value against murine carbonic anhydrase XIII was determined; (not tested)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.
AID1262263Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID50361Compound was evaluated for binding affinity against human carbonic anhydrase II (hCA -II)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID293193Inhibition of human recombinant CA12 by CO2 hydration assay2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides.
AID261579Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID1142836Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-1 assessed as CO2 hydrase activity by stopped-flow assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID243011Selectivity ratio against human carbonic anhydrases II and XII2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID770586Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1195370Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID1194026Inhibition of recombinant Methanosarcina thermophila gamma-carbonic anhydrase by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID300869Inhibition of human cloned catalytic domain CA9 by CO2 hydration method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID770584Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID612731Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 1 at pH 8.3 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID146519In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 0 min2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID47940Inhibitory activity against human carbonic anhydrase II2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
AID726232Inhibition of Trypanosoma cruzi CL Brener recombinant alpha-carbonic anhydrase expressed in insect Sf9 cell Baculovirus system by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID1195369Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID272523Inhibition of human cloned CA5A by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID48123Inhibitory activity against human cloned Carbonic Anhydrase isozyme(bCA IV)2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails.
AID644380Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID1200917Inhibition of carbonic anhydrase in pigmented male Dutch-belted rabbit treated with 1% 2 x 25 uL topical dose of formulated compound in each eye after 2 to 8 hrs by pH-STAT method2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID47942Inhibitory activity against human carbonic anhydrase II2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
AID1593067Inhibition of human CA 9 catalytic domain2019European journal of medicinal chemistry, Apr-15, Volume: 168Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines.
AID1061169Inhibition of recombinant Methanosarcina thermophila gamma-CA CAM by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
AID299541Inhibition of human CA42007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID166568In vivo intraocular pressure (IOP) lowering at 90 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID166335Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 90 min at a pH of 5.52003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
AID1605090Inhibition of recombinant human carbonic anhydrase 4 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action.
AID778725Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Leishmania donovani chagasi, the protozoan parasite responsible for leishmaniasis.
AID238753Inhibitory activity against Carbonic anhydrase I2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
AID369271Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID414961Inhibition of Mycobacterium tuberculosis H37Rv recombinant beta-carbonic anhydrase 1 expressed in Escherichia coli BL21 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID780318Selectivity ratio of Ki for human carbonic anhydrase9 to Ki for human carbonic anhydrase22013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID238224Inhibitory constant against human Carbonic anhydrase IX2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
AID1593068Inhibition of human CA 12 catalytic domain2019European journal of medicinal chemistry, Apr-15, Volume: 168Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines.
AID1605088Inhibition of recombinant human carbonic anhydrase 1 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action.
AID238850Inhibitory activity against human carbonic anhydrase II2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma.
AID327764Inhibition of human full length carbonic anhydrase 6 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID353230Inhibition of human recombinant CA9 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties.
AID238984Inhibitory activity against human carbonic anhydrase I expressed in Escherichia coli BL21; not tested2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
AID238316Ki value against human carbonic anhydrase XII (hCA XII)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID1453410Inhibition of Francisella tularensis beta-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID299538Inhibition of human CA12007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID1240215Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase by CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID1204092Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-1 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-92015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII.
AID238300Ki value against human carbonic anhydrase II (hCA II)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1278412Inhibition of Pseudoalteromonas haloplanktis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID644379Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID299547Inhibition of human CA122007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID414956Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID47935Inhibitory activity against human recombinant carbonic anhydrase II1999Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring?
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID414955Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID47929Inhibition of human carbonic anhydrase II2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits.
AID47915Compound was evaluated for binding affinity against bovine carbonic anhydrase IV (bCA IV)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID1190063Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
Sulfonamide inhibition studies of the η-class carbonic anhydrase from the malaria pathogen Plasmodium falciparum.
AID1142837Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-2 assessed as CO2 hydrase activity by stopped-flow assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID281086Selectivity ratio of human CA9 over human CA22007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
AID1593065Inhibition of full length human CA 12019European journal of medicinal chemistry, Apr-15, Volume: 168Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines.
AID281085Selectivity ratio of human CA9 over human CA12007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
AID317581Inhibition of human CA9 catalytic domain by CO2 hydration method2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
AID780320Inhibition of human carbonic anhydrase13 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID47746Concentration which produces 50% inhibition of human Carbonic anhydrase II2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV.
AID311024Inhibition of human carbonic anhydrase 22007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID367820Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID726603Inhibition of human recombinant carbonic anhydrase 2 by dansylamide (DNSA) competition assay2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma.
AID725956Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID166565In vivo intraocular pressure (IOP) lowering at 60 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID300868Inhibition of human cloned CA2 by CO2 hydration method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.
AID281084Inhibition of catalytic domain of human recombinant isozyme CA9 by CO2 hydration method2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
AID1061069Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID239126Inhibitory constant against catalytic domain of human carbonic anhydrase XII2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
AID1275912Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID369275Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID1061067Inhibition of Porphyromonas gingivalis recombinant gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID644381Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.
AID311032Inhibition of human carbonic anhydrase 122007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID271711Inhibition of human cloned CA2 by CO2 hydration method2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
AID743512Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 recombinant carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID1204091Inhibition of recombinant human transmembrane, tumor-associated form of carbonic anhydrase-12 preincubated for 15 mins by stopped flow CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII.
AID299548Inhibition of mouse CA132007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID1434428Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID552129Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID408472Inhibition of human cloned CA12 catalytic domain by stopped flow CO2 hydration assay2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII.
AID238686Ki value against human carbonic anhydrase I; ND means not determined2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.
AID1809108Solubility of the compound2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis.
AID271712Inhibition of human cloned CA9 catalytic domain by CO2 hydration method2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
AID1061170Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
AID764718Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID48301Inhibitory activity against human carbonic anhydrase IX2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
AID317579Inhibition of human cloned CA1 by CO2 hydration method2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
AID239703Inhibitory constant against human carbonic anhydrase XIV in CO2 hydrase assay2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
AID1278411Inhibition of Nostoc commune gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1200902Inhibition of human carbonic anhydrase 2 assessed as reduction in enzyme activity incubated for 30 mins by fluorescence polarization assay2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID744415Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Carbonic anhydrase inhibitors: inhibition of the β-class enzyme from the pathogenic yeast Candida glabrata with sulfonamides, sulfamates and sulfamides.
AID327760Inhibition of human full length carbonic anhydrase 3 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID166438In vivo intraocular pressure (IOP) lowering at 120 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID261582Selectivity ratio for human carbonic anhydrase 2 over Helicobacter pylori carbonic anhydrase2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID50374Inhibitory activity against human recombinant carbonic anhydrase I (CA1)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route.
AID238256Ki value against human carbonic anhydrase VII2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.
AID238413Inhibitory constant against human Carbonic anhydrase I; NT, Not tested2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
AID436565Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID243098Ratio of inhibitory activity of human cytosolic carbonic anhydrase II to tumor associated carbonic anhydrase IX2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
AID271710Inhibition of human cloned CA1 by CO2 hydration method2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
AID1061068Inhibition of Leishmania donovani chagasi recombinant beta-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID275807Inhibition of human recombinant cytosolic isozyme CA I by stopped-flow CO2 hydrase method2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID48286Inhibitory activity against Carbonic anhydrase IV isolated from bovine lung2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
AID48300Inhibitory activity against human cloned carbonic anhydrase isozyme IX, by CO2 hydrase assay method.2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.
AID1142833Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Sulfonamide inhibition studies of two β-carbonic anhydrases from the bacterial pathogen Legionella pneumophila.
AID47902Inhibitory activity against human recombinant carbonic anhydrase II (CA2)2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails.
AID743514Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID239102Inhibitory constant against catalytic domain of human carbonic anhydrase IX2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
AID1194025Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID1291363Inhibition of recombinant Vibrio cholerae gamma-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Comparison of the sulfonamide inhibition profiles of the α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.
AID47715Inhibition constant of compound was determined against human cloned carbonic anhydrase I; Not tested2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.
AID1268965Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID311027Inhibition of human carbonic anhydrase 5A2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID47725Inhibitory activity against Human Carbonic anhydrase II2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID1067225Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 122014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID669119Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID311028Inhibition of human carbonic anhydrase 5B2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID408471Inhibition of human cloned CA9 catalytic domain by stopped flow CO2 hydration assay2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Carbonic anhydrase inhibitors: bioreductive nitro-containing sulfonamides with selectivity for targeting the tumor associated isoforms IX and XII.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID272524Inhibition of human cloned CA5B by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID311033Inhibition of mouse carbonic anhydrase 132007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID327768Inhibition of mouse full length carbonic anhydrase 13 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID1188134Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID48299Inhibition constant determined against catalytic domain of human cloned carbonic anhydrase IX2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.
AID48103Binding affinity against Carbonic anhydrase II2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.
AID50364Inhibition of human carbonic anhydrase I2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits.
AID669115Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID238746Ki value against hCA I; ND means not determined2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID311030Inhibition of human carbonic anhydrase 72007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID1593066Inhibition of full length human CA 22019European journal of medicinal chemistry, Apr-15, Volume: 168Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines.
AID436564Inhibition of human recombinant CA2 by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID299242Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID1287519Inhibition of Vibrio cholerae beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID50371Inhibitory activity against human cloned carbonic anhydrase isozyme I by esterase assay method.2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.
AID764719Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
AID770581Selectivity ratio of Ki for human carbonic anhydrase 2 to Ki for human carbonic anhydrase 92013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID436563Inhibition of human recombinant CA1 by stopped-flow CO2 assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.
AID48132Inhibition constant against bovine Carbonic anhydrase IV, isolated from lung microsomes2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID577527Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.52011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID256964Inhibitory activity against human recombinant mitochondrial isozyme CA VA2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID327761Inhibition of human full length carbonic anhydrase 4 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID353228Inhibition of human recombinant CA1 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties.
AID299545Inhibition of human CA72007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID146520In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 30 min2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID1628038Inhibition of recombinant Plasmodium falciparum eta-carbonic anhydrase (181 to 538 residues) expressed in Escherichia coli artic express (DE3) preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID281083Inhibition of human recombinant isozyme CA2 by CO2 hydration method2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
AID271714Selectivity for human CA9 over CA22006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
AID1188137Inhibition of Porphyromonas gingivalis Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID1067227Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID311023Inhibition of human carbonic anhydrase 12007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID1278413Inhibition of recombinant Colwellia psychrerythraea gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID743515Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID238769Inhibitory activity against Carbonic anhydrase IX2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
AID349608Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 3 expressed in Escherichia coli BL21 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID1240216Inhibition of Methanosarcina thermophila recombinant gamma carbonic anhydrase by stopped flow CO2 hydrase assay method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID300871Selectivity ratio of Ki for human cloned CA1 to Ki for human cloned catalytic domain CA92007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.
AID587131Inhibition of human carbonic anhydrase 2 after 15 mins by CO2 hydrase assay at pH 7.52011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii.
AID669117Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID669116Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
AID770582Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID299544Inhibition of human CA62007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID1204094Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-1 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-122015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII.
AID272520Inhibition of human cloned CA1 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID1188138Inhibition of Porphyromonas gingivalis Gamma-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Sulfonamide inhibition study of the carbonic anhydrases from the bacterial pathogen Porphyromonas gingivalis: the β-class (PgiCAb) versus the γ-class (PgiCA) enzymes.
AID369273Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID552128Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID299552Inhibition of Methanosarcina thermophila gamma CA2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID367821Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID238787Inhibitory activity against human carbonic anhydrase II expressed in Escherichia coli BL212004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
AID448553Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID263637Inhibition of human recombinant CA22006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID427125Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID238255Ki value against human carbonic anhydrase II2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.
AID239284Inhibitory activity against catalytic domain of human carbonic anhydrase XII2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma.
AID577530Inhibition of Brucella suis carbonic anhydrase II by spectrophotometry at pH 8.32011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
A new β-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth.
AID300867Inhibition of human cloned CA1 by CO2 hydration method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Inhibition of carbonic anhydrase isozymes I, II and IX with benzenesulfonamides containing an organometallic moiety.
AID1067229Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID552130Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID299542Inhibition of human CA5A2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID166196Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 240 min at a pH of 5.52003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
AID239048Inhibitory activity against membrane bound tumor associated human carbonic anhydrase IX2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
AID1240217Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID166435In vivo intraocular pressure (IOP) lowering at 0 min in normotensive rabbits after treatment with one drop (50 uL) 2% solution of CA inhibitor directly into the eye, at 5.5pH2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties.
AID1195371Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
AID272529Inhibition of human cloned CA14 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID770585Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID780319Inhibition of human carbonic anhydrase14 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID311026Inhibition of human carbonic anhydrase 42007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID725955Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1067226Selectivity ratio of Ki for human transmembrane carbonic anhydrase 2 to Ki for human cytosolic carbonic anhydrase 92014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1262267Inhibition of Chionodraco hamatus alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID1262264Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID299540Inhibition of human CA32007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID612726Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID327759Inhibition of human full length carbonic anhydrase 2 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID238220Inhibitory constant against human Carbonic anhydrase II2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
AID1061066Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii.
AID770583Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID780324Inhibition of human carbonic anhydrase6 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID612725Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID244127Ratio of Ki for human carbonic anhydrases II and IX2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
AID48280Inhibitory activity against bovine carbonic anhydrase isozyme IV isolated from bovine lung microsomes, by esterase assay method.2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.
AID48293Concentration which produces 50% Inhibition of human Carbonic anhydrase IV2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV.
AID272527Inhibition of catalytic domain of human cloned CA12 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID448554Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID299250Inhibition of Helicobacter pylori beta carbonic anhydrase by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID1200926Reduction in intraocular pressure unilaterally lasered ocular hypertensive cynomolgus monkey treated with 1% 2 x 25 uL topical dose of formulated compound in right eye and measured after 2 hrs by ocular hypertension primate tonometry2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID299249Inhibition of Helicobacter pylori alpha carbonic anhydrase by stopped-flow CO2 hydrase assay2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors: the beta-carbonic anhydrase from Helicobacter pylori is a new target for sulfonamide and sulfamate inhibitors.
AID311029Inhibition of human carbonic anhydrase 62007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID275808Inhibition of human recombinant cytosolic isozyme CA II by stopped-flow CO2 hydrase method2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID238788Inhibitory activity against human carbonic anhydrase IX expressed in Escherichia coli BL212004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
AID1200918Inhibition of carbonic anhydrase in pigmented male Dutch-belted rabbit treated with 2% 2 x 25 uL topical dose of formulated compound in each eye after 2 to 8 hrs by pH-STAT method2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID238635Inhibitory activity against cytosolic human carbonic anhydrase II2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
AID281082Inhibition of human recombinant isozyme CA1 by CO2 hydration method2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
AID299550Inhibition of Helicobacter pylori alpha CA2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID317580Inhibition of human cloned CA2 by CO2 hydration method2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1434427Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
AID233702Selectivity ratio, inhibition (Ki) of human carbonic anhydrase IX compared to human carbonic anhydrase II2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1204095Selectivity ratio Ki for recombinant human cytosolic form of carbonic anhydrase-2 to Ki for recombinant human transmembrane, tumor-associated form of carbonic anhydrase-122015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Synthesis of Schiff base derivatives of 4-(2-aminoethyl)-benzenesulfonamide with inhibitory activity against carbonic anhydrase isoforms I, II, IX and XII.
AID311025Inhibition of human carbonic anhydrase 32007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID256963Inhibitory activity against human recombinant cytosolic CA22005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID299549Inhibition of human CA142007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID1194028Inhibition of recombinant Nostoc commune gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID299539Inhibition of human CA22007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID367822Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Carbonic anhydrase inhibitors: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
AID263638Inhibition of Helicobacter pylori recombinant CA2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID299546Inhibition of human CA9 catalytic domain2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Carbonic anhydrase inhibitors: inhibition of human, bacterial, and archaeal isozymes with benzene-1,3-disulfonamides--solution and crystallographic studies.
AID1194027Inhibition of recombinant Porphyromonas gingivalis gamma-carbonic anhydrase by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic cyanobacterium Nostoc commune.
AID272521Inhibition of human cloned CA2 by stopped-flow CO2 hydration method2006Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
AID327763Inhibition of human full length carbonic anhydrase 5B by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID48296Inhibitory activity against human tumor-associated transmembrane carbonic anhydrase IX.2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Carbonic anhydrase inhibitors: the first QSAR study on inhibition of tumor-associated isoenzyme IX with aromatic and heterocyclic sulfonamides.
AID353231Inhibition of human recombinant CA12 by stopped flow CO2 hydration assay2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties.
AID238768Inhibitory activity against Carbonic anhydrase II2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
AID1605089Inhibition of recombinant human carbonic anhydrase 2 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action.
AID1268964Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID311034Inhibition of human carbonic anhydrase 142007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Carbonic anhydrases as targets for medicinal chemistry.
AID1453413Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID1200903Solubility of the compound2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.
AID427123Inhibition of Cryptococcus neoformans recombinant Can2 by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID47931Inhibition constant (Ki) against human cloned carbonic anhydrase II (CAH)2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.
AID743513Inhibition of Helicobacter pylori recombinant alpha carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay2013Bioorganic & medicinal chemistry, Mar-15, Volume: 21, Issue:6
The alpha-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1 is highly susceptible to inhibition by sulfonamides.
AID317583Selectivity for human CA9 over human CA22008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
AID275806Inhibition of full length human recombinant CA VI2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.
AID349607Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID166198Fall of intraocular pressure (IOP) after treatment with 50 ug into normotensive rabbit at time interval 30 min at a pH of 5.52003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
AID146522In vivo intraocular pressure lowering in Normotensive Rabbits after the administration at a pH of 5.5, at time interval 90 min2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.
AID1240214Inhibition of Nostoc commune gamma carbonic anhydrase by CO2 hydration assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Sulfonamide inhibition studies of the γ-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.
AID612732Inhibition of Salmonella Typhimurium recombinant carbonic anhydrase 2 at pH 8.3 by stopped flow CO2 hydration assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates.
AID263639Selectivity for Helicobacter pylori recombinant CA over human recombinant CA22006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID300467Inhibition of human recombinant full length CA4 by stopped-flow technique2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Carbonic anhydrase inhibitors. Interaction of the antiepileptic drug sulthiame with twelve mammalian isoforms: kinetic and X-ray crystallographic studies.
AID1275910Inhibition of Vibrio cholerae beta-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID271713Selectivity for human CA9 over CA12006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
AID1067228Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID293194Inhibition of human recombinant CA14 by CO2 hydration assay2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides.
AID327765Inhibition of human full length carbonic anhydrase 7 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID1262266Inhibition of weddell seal alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Anion and sulfonamide inhibition studies of an α-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.
AID327762Inhibition of human full length carbonic anhydrase 5A by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID780325Inhibition of human carbonic anhydrase2 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID301578Inhibition of human recombinant CA 3 assessed as CO2 hydration by stopped flow kinetic assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides.
AID1605091Inhibition of recombinant human carbonic anhydrase 7 incubated for 6 hrs prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action.
AID552127Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.
AID1275911Inhibition of Vibrio cholerae alpha-carbonic anhydrase using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Sulfonamide inhibition studies of the β-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.
AID263636Inhibition of human recombinant CA12006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
AID1287517Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID1287518Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Sulfonamide inhibition studies of the β-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.
AID327758Inhibition of human full length carbonic anhydrase 1 by stopped flow CO2 hydrase assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
AID1268962Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Sulfonamide inhibition studies of the α-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.
AID427124Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID1067230Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
AID1453412Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
AID263050Inhibition of bovine CA42006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
QSAR study on topically acting sulfonamides incorporating GABA moieties: a molecular connectivity approach.
AID47939Inhibitory activity against human recombinant carbonic anhydrase II (CA2)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route.
AID1628037Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Cloning, expression, purification and sulfonamide inhibition profile of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.
AID459696Inhibition of Brucella suis CA1 expressed in Escherichia coli BL21(DE3) by stopped-flow CO2-hydration assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis.
AID780323Inhibition of human carbonic anhydrase7 preincubated for 15 mins by stopped-flow CO2 hydration assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Structural study of interaction between brinzolamide and dorzolamide inhibition of human carbonic anhydrases.
AID261580Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1346202Human carbonic anhydrase 7 (4.2.1.1 Carbonate dehydratases)2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1345957Human carbonic anhydrase 14 (4.2.1.1 Carbonate dehydratases)1992The Journal of biological chemistry, Dec-15, Volume: 267, Issue:35
Inhibition of carbonic anhydrases I and II by N-unsubstituted carbamate esters.
AID1346210Human carbonic anhydrase 12 (4.2.1.1 Carbonate dehydratases)2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
AID1345928Human carbonic anhydrase 1 (4.2.1.1 Carbonate dehydratases)2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1798769CA Inhibition Assay from Article 10.1021/jm801267c: \\Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.\\2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
AID1796686CA Inhibition Assay from Article 10.1016/s0968-0896(00)00026-2: \\2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.\\2000Bioorganic & medicinal chemistry, May, Volume: 8, Issue:5
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.
AID1796552CA Inhibition Assay from Article 10.1021/jm0512600: \\Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.\\2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
AID1796755CA Inhibition Assay from Article 10.1021/jm021123s: \\Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.\\2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.
AID1796855CA Inhibition Assay from Article 10.1021/jm0494826: \\Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.\\2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
AID1798985CA Inhibition Assay from Article 10.1021/jm9000488: \\Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.\\2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.
AID1797360CA Inhibition Assay from Article 10.1021/jm061320h: \\Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.\\2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.
AID1797528Esterase Assay from Article 10.1021/jm031057+: \\Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.\\2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.
AID1796582CA Inhibition Assay from Article 10.1021/jm050483n: \\Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.\\2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
AID1799266CA Inhibition Assay from Article 10.1016/j.bmc.2009.05.002: \\Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.\\2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides.
AID1798982CA Inhibition Assay from Article 10.1021/jm9003126: \\Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.\\2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
AID1796823In Vitro Binding for Human Carbonic Anhydrase II from Article 10.1002/pro.5560071201: \\Structural analysis of inhibitor binding to human carbonic anhydrase II.\\1998Protein science : a publication of the Protein Society, Dec, Volume: 7, Issue:12
Structural analysis of inhibitor binding to human carbonic anhydrase II.
AID1796687In vitro binding of inhibitor to hCA-II from Article 10.1016/s0968-0896(00)00026-2: \\2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.2000Bioorganic & medicinal chemistry, May, Volume: 8, Issue:5
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.
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).
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB1998Protein science : a publication of the Protein Society, Mar, Volume: 7, Issue:3
Structures of murine carbonic anhydrase IV and human carbonic anhydrase II complexed with brinzolamide: molecular basis of isozyme-drug discrimination.
AID1811Experimentally measured binding affinity data derived from PDB1998Protein science : a publication of the Protein Society, Mar, Volume: 7, Issue:3
Structures of murine carbonic anhydrase IV and human carbonic anhydrase II complexed with brinzolamide: molecular basis of isozyme-drug discrimination.
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 (332)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (2.41)18.2507
2000's124 (37.35)29.6817
2010's152 (45.78)24.3611
2020's48 (14.46)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 76.95

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

MetricThis Compound (vs All)
Research Demand Index76.95 (24.57)
Research Supply Index6.08 (2.92)
Research Growth Index5.24 (4.65)
Search Engine Demand Index135.11 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (76.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials86 (24.57%)5.53%
Reviews25 (7.14%)6.00%
Case Studies24 (6.86%)4.05%
Observational2 (0.57%)0.25%
Other213 (60.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (60)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT01111890]Phase 470 participants (Actual)Interventional2010-04-30Completed
Brinzolamide for the Treatment of Chronic Central Serous Chorioretinopathy [NCT03542006]Phase 235 participants (Anticipated)Interventional2018-06-01Not yet recruiting
Topical Brinzolamide Ophthalmic Suspension Versus Placebo in the Treatment of Infantile Nystagmus Syndrome [NCT01312402]Phase 45 participants (Actual)Interventional2011-01-31Completed
Choroidal Thickness and Its Correlations With Ocular Parameters in Cases With Primary Open-angle Glaucoma [NCT03966560]Phase 496 participants (Actual)Interventional2014-01-31Completed
Comparison of the Effects of Latanoprost(0.005%) and Brinzolamide(1.0%) on Intraocular Pressure in Primary Open-angle Glaucoma and Ocular Hypertension [NCT01084902]130 participants (Actual)Interventional2010-02-28Active, not recruiting
A Multicentre, Double Blind, Active Controlled, Parallel Group, Two Arm, Bioequivalence Study With Clinical Endpoint Comparing Brinzolamide 1% Ophthalmic Suspension (Manufactured by Indoco Remedies Ltd. for Watson Pharma Pvt Ltd.), to Brinzolamide (Azopt® [NCT02512042]Phase 3973 participants (Actual)Interventional2015-04-30Completed
24-hr Intraocular Pressure Control With Brinzolamide 1% / Brimonidine 0.2% Ophthalmic Suspension vs Vehicle [NCT02770248]Phase 4162 participants (Actual)Interventional2016-05-23Completed
Stop Retinal Ganglion Cell Dysfunction Study [NCT02390284]Phase 3500 participants (Anticipated)Interventional2015-09-30Active, not recruiting
Safety and IOP-Lowering Efficacy of Brinzolamide 10 mg/mL/Brimonidine 2 mg/mL Fixed Combination Eye Drops, Suspension Compared to Brinzolamide 10 mg/mL Eye Drops, Suspension and Brimonidine 2 mg/mL Eye Drops, Solution in Patients With Open-Angle Glaucoma [NCT01310777]Phase 3771 participants (Actual)Interventional2011-05-31Completed
A Three-Month, Randomized, Double-Masked, Parallel-Group Study With a Planned Three-Month Safety Extension of the Efficacy and Safety of a Fixed Combination of Brinzolamide 1%/Brimonidine 0.2% Compared to Brinzolamide 1% and Brimonidine 0.2% All Dosed Thr [NCT01297920]Phase 31,062 participants (Actual)Interventional2011-03-31Completed
Efficacy and Safety of Adding the Brinzolamide/Timolol Maleate Fixed Combination (AZARGA®) to Ocular Hypertensive or Glaucoma Patients Uncontrolled on Prostaglandin Monotherapy [NCT01263444]Phase 447 participants (Actual)Interventional2011-03-31Completed
Multi-Center, Randomized, Double-Masked, Active Controlled, Parallel Group Study to Compare Perrigo's Brinzolamide Ophthalmic Suspension 1% to Azopt® in the Treatment of Primary Open Angle Glaucoma or Ocular Hypertension in Both Eyes [NCT04024072]Phase 3495 participants (Actual)Interventional2019-06-24Completed
Comparison of Brimonidine 0.15% Purite, Dorzolamide 2%, and Brinzolamide 1% as Adjunctive Therapy to Prostaglandin Analogs [NCT00675207]Phase 4120 participants (Actual)Interventional2006-01-31Completed
Safety and IOP-Lowering Efficacy of Brinzolamide/Brimonidine Fixed Combination Ophthalmic Suspension in Patients With Open-Angle Glaucoma and/or Ocular Hypertension [NCT00961649]Phase 2195 participants (Actual)Interventional2009-10-31Terminated
A BIOEQUIVALENCE STUDY OF THE GENERIC BRINZOLAMIDE 1% OPHTHALMIC SUSPENSION COMPARED TO REFERENCE LISTED DRUG AZOPT® (BRINZOLAMIDE) OPHTHALMIC SUSPENSION 1% IN SUBJECTS WITH PRIMARY OPEN ANGLE GLAUCOMA OR OCULAR HYPERTENSION [NCT03896633]Phase 1/Phase 2637 participants (Actual)Interventional2018-02-28Completed
[NCT01722604]Phase 3258 participants (Actual)Interventional2012-01-31Completed
Efficacy and Safety of Brinzolamide 10 mg/mL / Brimonidine 2 mg/mL Eye Drops, Suspension Compared to Brinzolamide 10 mg/mL Eye Drops, Suspension Plus Brimonidine 2 mg/mL Eye Drops, Solution in Subjects With Open-Angle Glaucoma or Ocular Hypertension [NCT02339584]Phase 3493 participants (Actual)Interventional2015-04-14Completed
The Efficacy and Safety of Adding the Brinzolamide/Timolol Maleate Fixed Combination (Azarga®) to Prostaglandin Monotherapy [NCT00966576]Phase 447 participants (Actual)Interventional2009-07-31Completed
Quality of 24-hour Intraocular Pressure Control Obtained With the Brinzolamide/Timolol Fixed Combination Compared With the Brimonidine/Timolol Fixed Combination When Added to Travoprost Monotherapy in Subjects With Open-angle Glaucoma [NCT00981786]Phase 451 participants (Actual)Interventional2009-08-31Completed
A Double-Masked, Parallel-Group, Efficacy and Safety Study of Brinzolamide 1.0% (AZOPT) as Adjunctive Therapy to Travoprost 0.004% (TRAVATAN) in Patients With Chronic Angle-Closure Glaucoma [NCT00758342]Phase 437 participants (Actual)Interventional2006-05-31Terminated(stopped due to difficulty of enrolling patients)
Effects of Topical Hypotensive Drugs on Circadian Ocular Perfusion Pressure and Ocular Blood Flow in Patients With Open-Angle Glaucoma [NCT00800540]Phase 435 participants (Actual)Interventional2009-02-28Completed
[NCT00767494]Phase 317 participants (Actual)Interventional2008-10-31Terminated(stopped due to Project Cancelled)
[NCT00767481]Phase 36 participants (Actual)Interventional2008-10-31Terminated(stopped due to Project Cancelled)
A Comparison of Brinzolamide Ophthalmic Suspension, 1% (Azopt) TID vs. Placebo TID Added to Latanoprost Ophthalmic Solution, 0.005% (Xalatan) in Patients With Elevated IOP on a Prostaglandin [NCT00759941]Phase 486 participants (Actual)Interventional2007-10-31Completed
Three Month Efficacy and Safety Study of a Fixed Combination of Brinzolamide 1%/Brimonidine 0.2% Compared to Brinzolamide 1% and Brimonidine 0.2% All Dosed Three Times Daily in Patients With Open-Angle Glaucoma and/or Ocular Hypertension [NCT01297517]Phase 31,001 participants (Actual)Interventional2011-02-28Completed
Comparison of Efficacy and Safety of Brinzolamide/Timolol Fixed Combination (AZARGA™) vs Brinzolamide (AZOPT®) and Timolol in Chinese Subjects With Open-Angle Glaucoma or Ocular Hypertension [NCT01357616]Phase 3328 participants (Actual)Interventional2010-11-30Completed
IOP Lowering Efficacy of Travoprost/Brinzolamide Fixed Combination Ophthalmic Suspension in Patients With Open-Angle Glaucoma or Ocular Hypertension [NCT00527501]Phase 2136 participants (Actual)Interventional2007-08-31Completed
The Effects of the Water Drinking Test on Intraocular Pressure of Glaucoma Patients Undergoing 24 Hour Continuous Monitoring With the SENSIMED Triggerfish [NCT01507584]23 participants (Actual)Interventional2011-08-31Completed
[NCT00440141]Phase 440 participants (Actual)Interventional2006-07-31Completed
Efficacy and Safety of Brinzolamide 10 mg/mL/Brimonidine 2 mg/mL Eye Drops, Suspension Compared to Brinzolamide 10 mg/mL Eye Drops, Suspension Plus Brimonidine 2 mg/mL Eye Drops, Solution in Patients With Open-Angle Glaucoma or Ocular Hypertension [NCT01309204]Phase 31,184 participants (Actual)Interventional2011-05-31Completed
Patient Preference Comparison of AZARGA Versus COSOPT After Single Doses in Patients With Open-Angled Glaucoma or Ocular Hypertension [NCT01471158]Phase 4120 participants (Actual)Interventional2010-09-30Completed
A Multiple-Dose Study of the IOP-Lowering Efficacy of Azopt 1.0% Compared to Timolol 0.5% When Added to a PGA as Adjunctive Therapy Over a 24 Hour Period in Patients With Glaucoma or Ocular Hypertension [NCT00300079]Phase 430 participants (Anticipated)Interventional2006-09-30Completed
[NCT00314158]Phase 3523 participants (Actual)Interventional2005-11-30Completed
A Study of a Glaucoma Therapy to Treat Open-Angle Glaucoma or Ocular Hypertension [NCT00326092]Phase 288 participants Interventional2006-05-31Completed
Multi-Center, Randomized, Double-Masked, Active Controlled, Parallel Group Study to Compare Perrigo's Brinzolamide/Brimonidine Ophthalmic Suspension 1% to Simbrinza® in the Treatment of Primary Open Angle Glaucoma or Ocular Hypertension in Both Eyes [NCT04944290]Phase 3447 participants (Actual)Interventional2021-05-28Completed
Safety and Efficacy Study of BETAXON 0.5% and AZOPT 1.0% in Pediatric Patients With Glaucoma or Ocular Hypertension [NCT00061516]Phase 378 participants (Actual)Interventional2003-01-31Completed
Safety and Efficacy to Reduce the IOP of the Fixed Association of Latanoprost 0.005% (50 μg/mL)/ Brinzolamide 1% (10mg/mL) Drops, Compared to Latanoprost 0.005% (50 μg/mL) Drops, in Patients With Open Angle Glaucoma or Ocular Hypertension [NCT01721707]Phase 30 participants (Actual)Interventional2012-12-31Withdrawn(stopped due to withdrawn by industry)
Earlier Intraocular Pressure Control After Ahmed Glaucoma Valve Implantation for Glaucoma [NCT00869141]Phase 452 participants (Actual)Interventional2009-03-31Completed
Patient Preference Comparison of AZARGA Versus COSOPT in Patients With Open-Angle Glaucoma or Ocular Hypertension [NCT01340014]Phase 4112 participants (Actual)Interventional2011-09-30Completed
A Study of a Glaucoma Therapy to Treat Open-Angle Glaucoma or Ocular Hypertension [NCT00314171]Phase 3437 participants (Actual)Interventional2005-10-31Completed
A Phase IV Study of Travoprost + Brinzolamide to Treat Glaucoma or Ocular Hypertension [NCT00471380]Phase 446 participants (Actual)Interventional2007-03-31Completed
Additive Effect of Brinzolamide 1%/Brimonidine 0.2% Fixed Dose Combination As Adjunctive Therapy to Travoprost [NCT01937299]Phase 4307 participants (Actual)Interventional2013-10-31Completed
Effect of Topical Prophylaxis With Brinzolamide-brimonidine Fixed Combination on Intraocular Pressure Elevation After Intravitreal Injections of Anti-vascular Endothelial Growth Factors [NCT04523844]47 participants (Actual)Interventional2020-05-11Completed
Study of the Efficacy of Brinzolamide 1% Plus Brimonidine 0.2% Versus Brimonidine 0.2% in the Prevention of Intraocular Pressure Rise After Nd-YAG Laser Capsulotomy [NCT03192826]Phase 479 participants (Actual)Interventional2016-06-20Completed
A 6-week, Double Masked, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Twice-daily Brinzolamide 1%/Brimonidine 0.2% Fixed Dose Combination as an Adjunctive Therapy to Travoprost 0.004% in Reducing Intraocular Pressure in Patients With No [NCT03150160]Phase 41 participants (Actual)Interventional2017-09-21Completed
A Descriptive Comfort Study of Brinzolamide 1% / Brimonidine Tartrate 0.2% Fixed Combination Ophthalmic Suspension, Brinzolamide 1% Ophthalmic Suspension and Brimonidine Tartrate 0.2% Ophthalmic Solution in Patients With Open-Angle Glaucoma or Ocular Hype [NCT01426867]Phase 2103 participants (Actual)Interventional2011-09-30Completed
Efficacy and Safety of Timolol Maleate 0.5% Compared to Brinzolamide 1% When Added to Travoprost 0.004% in Primary Open-angle Glaucoma or Ocular Hypertension [NCT00372827]Phase 4245 participants Interventional2004-02-29Completed
Assessing the Safety and Efficacy of Switching to AZARGA® (Brinzolamide/Timolol Fixed Combination) as Replacement Therapy in Patients With Uncontrolled Intraocular Pressure in Taiwan [NCT01484951]Phase 474 participants (Actual)Interventional2011-05-31Completed
A 6-Week Proof-of-Concept Study Evaluating the Safety and IOP-Lowering Efficacy of Travoprost/Brinzolamide Fixed Combination Ophthalmic Suspension in Subjects With Open-Angle Glaucoma or Ocular Hypertension [NCT02140060]Phase 2327 participants (Actual)Interventional2014-06-30Completed
Clinical Evaluation of Patients With X-linked Retinoschisis (XLRS) [NCT02331173]66 participants (Actual)Observational2012-11-30Completed
Therapeutic Equivalence Study of Generic Brinzolamide 1% Ophthalmic Suspension Compared to Reference Listed Drug Azopt® (Brinzolamide) Ophthalmic Suspension 1% in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension. [NCT05022004]Phase 3599 participants (Actual)Interventional2021-12-20Completed
Assessing the Efficacy and Tolerability of AZARGA® (Brinzolamide 1%/Timolol 0.5% Fixed Combination) as Replacement Therapy in Patients on COMBIGAN® (Brimonidine 0.2%/Timolol 0.5% Fixed Combination) Therapy in Canada [NCT01415401]Phase 457 participants (Actual)Interventional2011-09-30Completed
Additive Effect of Brinzolamide 1%/Brimonidine 0.2% Fixed Dose Combination as Adjunctive Therapy to a Prostaglandin Analogue [NCT01937312]Phase 4282 participants (Actual)Interventional2013-10-31Completed
Assessing the Efficacy and Tolerability of AZARGA® (Brinzolamide 1%/Timolol 0.5% Fixed Combination) as Replacement Therapy in Patients on Brimonidine 0.2%/Timolol 0.5% Fixed Combination Therapy (COMBIGAN®) in Brazil [NCT01514734]Phase 49 participants (Actual)Interventional2012-03-31Terminated(stopped due to Low recruitment rate)
Effect of Fixed Brinzolamide-brimonidine Combination on Intraocular Pressure After Phacoemulsification [NCT03494257]62 participants (Actual)Interventional2017-09-04Completed
Additive Effect of Twice Daily Brinzolamide 1%/Brimonidine 0.2% Fixed Dose Combination as an Adjunctive Therapy to a Prostaglandin Analogue [NCT02419508]Phase 4290 participants (Actual)Interventional2015-08-07Completed
Safety and Efficacy With Twice Daily Brinzolamide 1%/Brimonidine 0.2% (SIMBRINZA®) as an Adjunctive Therapy to Travoprost 0.004%/Timolol 0.5% (DUOTRAV®) [NCT02730871]Phase 4173 participants (Actual)Interventional2016-06-24Terminated(stopped due to Enrollment Challenges)
Prospective, Randomized, Single-Center Study to Evaluate 24-hour Intraocular Pressure Control With Brinzolamide 1%/Brimonidine 0.2% Fixed Dose Combination Therapy [NCT01978600]Phase 489 participants (Actual)Interventional2013-10-31Completed
The Efficacy and Safety of Brinzolamide 1%/Timolol 0.5% Fixed Combination Versus Dorzolamide 1%/Timolol 0.5% in Patients With Open-Angle Glaucoma and Ocular Hypertension [NCT02325518]Phase 4218 participants (Actual)Interventional2014-12-31Completed
Assessing the Efficacy and Tolerability of AZARGA® (Brinzolamide 1%/Timolol 0.5% Fixed Combination) as Replacement Therapy in Patients on Brimonidine 0.2%/Timolol 0.5% Fixed Combination Therapy (COMBIGAN®) in Latin America [NCT01518244]Phase 450 participants (Actual)Interventional2011-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00471380 (1) [back to overview]Intra Ocular Pressure (IOP)
NCT00758342 (1) [back to overview]Mean IOP (Intraocular Pressure)
NCT00759941 (4) [back to overview]Mean Change From Baseline in Intraocular Pressure, 12 PM, at 3 Months
NCT00759941 (4) [back to overview]Mean Change From Baseline in Intraocular Pressure, 4 PM, at 3 Months
NCT00759941 (4) [back to overview]Mean Change From Baseline in Intraocular Pressure, 8 AM, at 3 Months
NCT00759941 (4) [back to overview]Mean Change From Baseline in Intraocular Pressure, Diurnal, at 3 Months
NCT00800540 (12) [back to overview]Mean Change From Baseline in Overall Diastolic Ocular Perfusion Pressure at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in End Diastolic Velocity in the Ophthalmic Artery at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Intraocular Pressure (IOP) at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Mean Flow Value in the Inverotemporal Peripapillary Retina at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Mean Flow Value in the Superotemporal Peripapillary Retina at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Peak Systolic Velocity in the Central Retinal Artery at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Peak Systolic Velocity in the Ophthalmic Artery at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Systolic Blood Pressure at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Vascular Resistance in the Central Retinal Artery at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Vascular Resistance in the Ophthalmic Artery at 6 Weeks
NCT00800540 (12) [back to overview]Mean Change From Baseline in Circadian Diastolic Ocular Perfusion Pressure at Week 6
NCT00800540 (12) [back to overview]Mean Change From Baseline in Diastolic Blood Pressure at Week 6
NCT00869141 (3) [back to overview]Intraocular Pressure Control After Ahmed Valve Implantation for Glaucoma
NCT00869141 (3) [back to overview]Rate of Hypertensive Phase After Ahmed Valve Implantation for Glaucoma
NCT00869141 (3) [back to overview]Intraocular Pressure of Eyes With Hypertensive Phase Versus Without Hypertensive Phase
NCT00961649 (2) [back to overview]Mean Change in Intraocular Pressure (IOP) From Baseline to Each of the Assessment Time Points (8 AM, + 2 Hrs, + 7 Hrs, and + 9 Hrs) at Week 6 - Brinz/Brim, Brinz, Brim
NCT00961649 (2) [back to overview]Mean Change in Intraocular Pressure (IOP) From Baseline to Each of the Assessment Time Points (8 AM, +2 Hrs, +7 Hrs, and +9 Hrs) at Week 6 - Brinz/Brim, Brinz+Brim
NCT01263444 (4) [back to overview]Percentage of Patients Reaching the Target IOP (≤ 18 mmHg)
NCT01263444 (4) [back to overview]Mean Change From Baseline in IOP Per Prostaglandin Group at Week 12
NCT01263444 (4) [back to overview]Mean Change From Baseline in Intraocular Pressure (IOP) at Week 12
NCT01263444 (4) [back to overview]Mean Change From Baseline in IOP at Week 4
NCT01297517 (1) [back to overview]Mean IOP at Month 3 for Each Assessment Timepoint (8 AM, + 2 h, + 7 h, and + 9 h)
NCT01297920 (1) [back to overview]Mean Intraocular Pressure (IOP) at Each Assessment Timepoint (8 AM, +2 h, +7 h, and +9 h) at Month 3
NCT01309204 (1) [back to overview]Mean Diurnal IOP Change From Baseline at Month 3
NCT01310777 (1) [back to overview]Mean Diurnal IOP Change From Baseline at Month 3
NCT01340014 (2) [back to overview]Ocular Discomfort
NCT01340014 (2) [back to overview]Preferred Treatment
NCT01357616 (4) [back to overview]Mean Diurnal IOP Change From Baseline at Week 8
NCT01357616 (4) [back to overview]Mean IOP Change From Baseline at 11 AM
NCT01357616 (4) [back to overview]Mean IOP Change From Baseline (5 PM) at Week 8
NCT01357616 (4) [back to overview]Mean IOP Change From Baseline at 9 AM
NCT01415401 (2) [back to overview]Percentage of Subjects Who Reach Target IOP (≤ 18 mmHg)
NCT01415401 (2) [back to overview]Change in IOP at the Final Visit From Prior Brimonidine 0.2%/Timolol 0.5% Fixed Combination (COMBIGAN®) Therapy (i.e. From Baseline)
NCT01426867 (1) [back to overview]Mean Ocular Discomfort Score
NCT01484951 (2) [back to overview]Change in Intraocular Pressure (IOP) at the Final Visit From Prior Beta-blocker Monotherapy (Timolol 0.5% Only)
NCT01484951 (2) [back to overview]Percentage of Patients With Target IOP (≤18 mmHg), Regardless of Prior Therapy
NCT01514734 (1) [back to overview]Change in Intraocular Pressure (IOP) at 8 Weeks From Baseline (Prior Therapy).
NCT01518244 (2) [back to overview]Mean Change in Intraocular Pressure (IOP) From Baseline (Prior Therapy) at Week 8
NCT01518244 (2) [back to overview]Percentage of Subjects Who Reach Target IOP (≤18 mmHg) at Week 8
NCT01722604 (2) [back to overview]Change in Intraocular Pressure (IOP) From Baseline to Week 12
NCT01722604 (2) [back to overview]Intraocular Pressure (IOP) at Week 12
NCT01937299 (3) [back to overview]Mean Diurnal IOP Change From Baseline to Week 6
NCT01937299 (3) [back to overview]Mean Diurnal Intraocular Pressure (IOP) at Week 6
NCT01937299 (3) [back to overview]Mean Diurnal IOP Percentage Change From Baseline to Week 6
NCT01937312 (4) [back to overview]Mean Diurnal Intraocular Pressure (IOP) at Week 6
NCT01937312 (4) [back to overview]Mean Diurnal IOP Change From Baseline to Week 6
NCT01937312 (4) [back to overview]Mean Diurnal IOP Percentage Change From Baseline to Week 6
NCT01937312 (4) [back to overview]Mean IOP at Week 6 for Each Time Point (8 AM, 10 AM, 3 PM, 5 PM)
NCT01978600 (3) [back to overview]Mean 24-hour IOP at Week 4
NCT01978600 (3) [back to overview]Mean Diurnal IOP at Week 4
NCT01978600 (3) [back to overview]Mean Nocturnal IOP at Week 4
NCT02140060 (1) [back to overview]Mean IOP at Week 6
NCT02325518 (2) [back to overview]Least Squares Mean Change From Baseline in Intraocular Pressure (IOP) at 11 AM
NCT02325518 (2) [back to overview]Least Squares Mean Change From Baseline in IOP at 9 AM
NCT02339584 (1) [back to overview]Mean Diurnal IOP Change From Baseline at Month 3
NCT02419508 (7) [back to overview]Mean Diurnal IOP at Week 6
NCT02419508 (7) [back to overview]Mean Percentage Change From Baseline at 09:00 at Week 6
NCT02419508 (7) [back to overview]Mean Change From Baseline (on PGA) in Diurnal IOP (Mean of 09:00 and 11:00 Time Points) at Week 6
NCT02419508 (7) [back to overview]Mean Percentage Change From Baseline in IOP at 11:00 at Week 6
NCT02419508 (7) [back to overview]Mean Change From Baseline in IOP at 09:00 at Week 6
NCT02419508 (7) [back to overview]Mean Change From Baseline in IOP at 11:00 at Week 6
NCT02419508 (7) [back to overview]Mean Percentage Change From Baseline in Diurnal IOP at Week 6
NCT02512042 (1) [back to overview]Mean Difference in Intraocular Pressure (IOP) of Both Eyes Between the Two Treatment Groups at Four Time Points
NCT02730871 (5) [back to overview]Mean Percentage Change From Baseline in Diurnal IOP at Week 6
NCT02730871 (5) [back to overview]Mean Change From Baseline in IOP (09:00, 11:00) at Week 6
NCT02730871 (5) [back to overview]Mean Change From Baseline in Diurnal Intraocular Pressure (IOP) (Mean of Changes at 09:00 and 11:00 Time Points) at Week 6
NCT02730871 (5) [back to overview]Mean Percentage Change From Baseline in IOP (09:00, 11:00) at Week 6
NCT02730871 (5) [back to overview]Mean Diurnal IOP at Week 6
NCT02770248 (4) [back to overview]Least Squares Mean Change From Baseline in IOP for Each Time Point (8 AM Through 6 AM) at Week 4
NCT02770248 (4) [back to overview]Least Squares Mean Change From Baseline in Nocturnal IOP at Week 4
NCT02770248 (4) [back to overview]Least Squares Mean Change From Baseline in Daytime IOP at Week 4
NCT02770248 (4) [back to overview]Least Squares Mean Change From Baseline in 24-hr Intraocular Pressure (IOP) at Week 4
NCT03192826 (4) [back to overview]Intraocular Pressure (IOP) at 3 Hours After Nd-YAG Posterior Capsulotomy
NCT03192826 (4) [back to overview]Intraocular Pressure (IOP) at 24 Hourw After Nd-YAG Posterior Capsulotomy
NCT03192826 (4) [back to overview]Intraocular Pressure (IOP) at 1 Week After Nd-YAG Posterior Capsulotomy
NCT03192826 (4) [back to overview]Intraocular Pressure (IOP) at 1 Hour After Nd-YAG Posterior Capsulotomy
NCT03896633 (2) [back to overview]Change in Intraocular Pressure (IOP)
NCT03896633 (2) [back to overview]Intraocular Pressure (IOP)
NCT04024072 (1) [back to overview]Mean Change in Intra-ocular Pressure

Intra Ocular Pressure (IOP)

Intra Ocular Pressure, calculated as AUC (area under the curve) of IOP measured from 8.00 a.m. to 8.00 p.m, at different time-points (NCT00471380)
Timeframe: Baseline, end of each period (week 8, week 16, week 24)

,
Interventionmm Hg (millimeters mercury)*week (Mean)
Week 8Week 16Week 24
Crossover Group ABB179.20188.82201.50
Crossover Group BAA191.89196.26191.93

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Mean IOP (Intraocular Pressure)

(NCT00758342)
Timeframe: Screening: Week 12; (At 9 am and 4 pm time points)

,
Interventionmm Hg (millimeters mercury) (Mean)
9 AM measurement4 PM measurement
Travoprost 0.004% + Brinzolamide 1.0%17.5817.11
Travoprost 0.004% + Tears Natural20.5918.50

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Mean Change From Baseline in Intraocular Pressure, 12 PM, at 3 Months

Intraocular pressure was measured by Goldmann applanation tonometry. A negative number indicated a reduction in intraocular pressure. (NCT00759941)
Timeframe: Day 0, 3 months

InterventionmmHg (Mean)
Xalatan + Azopt-3.30
Xalatan + Placebo-2.48

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Mean Change From Baseline in Intraocular Pressure, 4 PM, at 3 Months

Intraocular pressure was measured by Goldmann applanation tonometry. A negative number indicated a reduction in intraocular pressure. (NCT00759941)
Timeframe: Day 0, 3 months

InterventionmmHg (Mean)
Xalatan + Azopt-3.00
Xalatan + Placebo-2.33

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Mean Change From Baseline in Intraocular Pressure, 8 AM, at 3 Months

Intraocular pressure was measured by Goldmann applanation tonometry. A negative number indicated a reduction in intraocular pressure. (NCT00759941)
Timeframe: Day 0, 3 months

InterventionmmHg (Mean)
Xalatan + Azopt-3.13
Xalatan + Placebo-2.57

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Mean Change From Baseline in Intraocular Pressure, Diurnal, at 3 Months

Diurnal intraocular pressure is the mean of the three timepoints measured (8AM, 12PM & 4PM). Intraocular pressure was measured by Goldmann applanation tonometry. A negative number indicated a reduction in mean intraocular pressure. (NCT00759941)
Timeframe: Day 0, 3 months

InterventionmmHg (Mean)
Xalatan + Azopt-3.20
Xalatan + Placebo-2.48

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Mean Change From Baseline in Overall Diastolic Ocular Perfusion Pressure at Week 6

Diastolic ocular perfusion pressure (DOPP) is defined as the difference between diastolic arterial pressure and intraocular pressure. Diastolic arterial pressure was measured with a calibrated automated sphygmomanometer. Intraocular pressure was measured with a calibrated pneumatonometer. A lower DOPP indicates a lower optic blood supply, which can be a risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

InterventionmmHg (millimeters of mercury) (Mean)
AZARGA2.6
COMBIGAN0.8

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Mean Change From Baseline in End Diastolic Velocity in the Ophthalmic Artery at Week 6

End diastolic velocity in the ophthalmic artery was assessed using Color Doppler Imaging (CDI). Assessments were made at 7 time points over a 24-hour period. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
Interventioncm/s (centimeters per second) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-0.0-0.60.50.4-0.8-0.1-0.2
COMBIGAN-0.8-1.20.2-0.8-1.4-0.6-0.5

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Mean Change From Baseline in Intraocular Pressure (IOP) at Week 6

Intraocular pressure (IOP) is defined as the fluid pressure inside the eye. Intraocular pressure was measured with a calibrated pneumatonometer at 7 time points over a 24-hour period. High IOP (outside the normal range) can be a risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
InterventionmmHg (millimeters of mercury) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-6.3-6.0-5.6-4.3-1.9-1.3-2.3
COMBIGAN-6.5-6.5-5.2-4.9-1.6-0.6-1.2

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Mean Change From Baseline in Mean Flow Value in the Inverotemporal Peripapillary Retina at Week 6

Retinal perfusion assessments were made using Heidelberg Retinal Flowmetry (HRF). Assessments were made at 4 timepoints over a 12-hour period. Intensity of blood flow was measured in arbitrary units, with a higher number indicating an increased blood flow. An increase in ocular blood flow may reduce the risk of glaucoma progression. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
InterventionArbitrary Units (Mean)
9:00 am1:00 pm5:00 pm9:00 pm
AZARGA15.9-40.7-38.7182.3
COMBIGAN-70.0-89.2-69.1-91.0

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Mean Change From Baseline in Mean Flow Value in the Superotemporal Peripapillary Retina at Week 6

Retinal perfusion assessments were made using Heidelberg Retinal Flowmetry (HRF). Assessments were made at 4 timepoints over a 12-hour period. Intensity of blood flow was measured in arbitrary units, with a higher number indicating an increased blood flow. An increase in ocular blood flow may reduce the risk of glaucoma progression. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
InterventionArbitrary Units (Mean)
9:00 am1:00 pm5:00 pm9:00 pm
AZARGA-272.4-12.1-26.714.0
COMBIGAN-43.5248.9-51.3-33.2

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Mean Change From Baseline in Peak Systolic Velocity in the Central Retinal Artery at Week 6

Peak systolic velocity in the central retinal artery was assessed using Color Doppler Imaging (CDI). Assessments were made at 7 time points over a 24-hour period. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
Interventioncm/s (centimeters per second) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA0.9-0.21.00.91.90.20.2
COMBIGAN0.70.30.6-0.5-0.5-1.10.9

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Mean Change From Baseline in Peak Systolic Velocity in the Ophthalmic Artery at Week 6

Peak systolic velocity in the ophthalmic artery was assessed using Color Doppler Imaging (CDI). Assessments were made at 7 time points over a 24-hour period. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
Interventioncm/s (centimeters per second) (Median)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-1.0-0.72.22.2-2.30.2-0.6
COMBIGAN-3.8-1.41.3-1.4-3.10.01.5

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Mean Change From Baseline in Systolic Blood Pressure at Week 6

Blood pressure is defined as the pressure exerted by circulating blood upon the walls of the blood vessels, that is, arterial pressure of the systemic circulation of blood. Systolic blood pressure refers to the maximum pressure, that is, the pressure while the heart is beating, and was measured at 7 timepoints in a 24-hour period using a calibrated sphygmomonometer. Higher blood pressure (outside the normal range) can be a risk factor for developing cardiovascular events, such as heart attack, stroke, or heart failure. Lower blood pressure (outside the normal range) can be a risk factor for dizziness or fainting. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
InterventionmmHg (millimeters of mercury) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-4.2-2.6-2.9-1.4-2.9-2.9-0.1
COMBIGAN4.5-1.9-0.4-0.6-12.2-3.03.0

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Mean Change From Baseline in Vascular Resistance in the Central Retinal Artery at Week 6

Vascular resistance in the central retinal artery was assessed using Color Doppler Imaging (CDI). Assessments were made at 7 time points over a 24-hour period. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
Interventioncm/s (centimeters per second) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-0.00-0.010.000.000.020.01-0.02
COMBIGAN0.010.01-0.000.02-0.010.010.02

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Mean Change From Baseline in Vascular Resistance in the Ophthalmic Artery at 6 Weeks

Vascular resistance in the ophthalmic artery was assessed using Color Doppler Imaging (CDI). Assessments were made at 7 time points over a 24-hour period. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
Interventioncm/s (centimeters per second) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-0.010.020.010.01-0.010.010.01
COMBIGAN-0.010.020.010.010.020.030.03

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Mean Change From Baseline in Circadian Diastolic Ocular Perfusion Pressure at Week 6

Circadian diastolic ocular perfusion pressure (COPP) is defined as the variations in diastolic OPP during the day and night. Diastolic ocular perfusion pressure was calculated at 7 timepoints over a 24-hour period. Changes in the diastolic ocular perfusion pressure rhythm throughout the day (outside the normal range) may affect glaucoma progression. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
InterventionmmHg (millimeters of mercury) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA2.83.04.44.50.80.32.0
COMBIGAN6.52.13.92.0-5.6-4.00.9

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Mean Change From Baseline in Diastolic Blood Pressure at Week 6

Blood pressure is defined as the pressure exerted by circulating blood upon the walls of the blood vessels, that is, arterial pressure of the systemic circulation of blood. Diastolic blood pressure refers to the minimum pressure, that is, the pressure between heartbeats. Diastolic glood pressure was measured at 7 timepoints in a 24-hour period using a calibrated sphygmomonometer. Higher blood pressure (outside the normal range) can be a risk factor for developing cardiovascular events, such as heart attack, stroke, or heart failure. Lower blood pressure (outside the normal range) can be a risk factor for dizziness or fainting. (NCT00800540)
Timeframe: Week 0, Week 6 (period-based)

,
InterventionmmHg (millimeters of mercury) (Mean)
9:00 am1:00 pm5:00 pm9:00 pm12:00 am3:00 am6:00 am
AZARGA-3.3-3.5-1.5-0.5-1.4-1.5-0.5
COMBIGAN0.6-4.3-0.9-2.1-7.3-3.8-0.7

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Intraocular Pressure Control After Ahmed Valve Implantation for Glaucoma

intraocular pressure comparison between groups after the Ahmed valve implantation (NCT00869141)
Timeframe: 3 weeks after surgery

InterventionmmHg at postop 3-week (Mean)
Research Arm15.6
Standard of Care Arm20.6

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Rate of Hypertensive Phase After Ahmed Valve Implantation for Glaucoma

Intraocular pressure more than 21 mmHg during the first 6 months after Ahmed valve implantation after the pressure has been reduced to less than 22 mmHg in the first postoperative week (NCT00869141)
Timeframe: within 6 months after surgery

Interventionparticipants (Number)
Research Arm9
Standard of Care Arm12

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Intraocular Pressure of Eyes With Hypertensive Phase Versus Without Hypertensive Phase

intraocular pressure of eyes with hypertensive phase versus without hypertensive phase (NCT00869141)
Timeframe: 1 year after surgery

InterventionmmHg in 1 year postop (Mean)
Hypertensive Phase Group15.1
Non-hypertensive Phase Group11.4

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Mean Change in Intraocular Pressure (IOP) From Baseline to Each of the Assessment Time Points (8 AM, + 2 Hrs, + 7 Hrs, and + 9 Hrs) at Week 6 - Brinz/Brim, Brinz, Brim

The study drug was instilled at 8 AM and +7 hours relative to the 8 AM dosing (approximately 15 minutes after conducting the IOP measurements). Intraocular pressure was measured by Goldmann applanation tonometry. One eye from each patient was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). Intent-to-Treat (ITT) analysis data set was pre-specified for the comparison of Brinz/Brim to its individual components (Brinz and Brim). (NCT00961649)
Timeframe: Baseline, Week 6

,,
Interventionmillimeters mercury (mmHg) (Least Squares Mean)
Change from Baseline (BL) at 8 AMChange from BL at +2 hours relative to 8 AM dosingChange from BL at +7 hours relative to 8 AM dosingChange from BL at +9 hours relative to 8 AM dosing
Brim-4.1-5.3-3.0-5.9
Brinz-5.7-4.7-2.8-3.9
Brinz/Brim-5.5-8.5-5.4-6.8

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Mean Change in Intraocular Pressure (IOP) From Baseline to Each of the Assessment Time Points (8 AM, +2 Hrs, +7 Hrs, and +9 Hrs) at Week 6 - Brinz/Brim, Brinz+Brim

The study drug was instilled at 8 AM and +7 hours relative to the 8 AM dosing (approximately 15 minutes after conducting the IOP measurements). Intraocular pressure was measured by Goldmann applanation tonometry. One eye from each patient was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). Per-Protocol (PP) analysis data set was pre-specified for the comparison of Brinz/Brim to Brinz+Brim. (NCT00961649)
Timeframe: Baseline, Week 6

,
Interventionmillimeters mercury (mmHg) (Least Squares Mean)
Change from Baseline (BL) at 8 AMChange from BL at +2 hours relative to 8 AM dosingChange from BL at +7 hours relative to 8 AM dosingChange from BL at +9 hours relative to 8 AM dosing
Brinz/Brim-5.5-8.4-5.0-6.3
Brinz+Brim-5.7-8.3-4.4-6.3

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Percentage of Patients Reaching the Target IOP (≤ 18 mmHg)

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and measured in millimeters of mercury (mmHg). A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). Only one eye (study eye) was assessed. (NCT01263444)
Timeframe: Week 12

Interventionpercentage of participants (Number)
Azarga70.0

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Mean Change From Baseline in IOP Per Prostaglandin Group at Week 12

IOP (fluid pressure inside the eye) was measured by Goldmann applanation tonometry. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater amount of improvement. Only prostaglandin subgroups with ≥ 15 patients were analyzed. Only one eye (study eye) contributed to the mean. (NCT01263444)
Timeframe: Baseline, Week 12

InterventionmmHg (Mean)
AZARGA + Latanoprost (n=22)AZARGA + Travoprost (n=15)
Azarga-7.1-5.1

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Mean Change From Baseline in Intraocular Pressure (IOP) at Week 12

IOP (fluid pressure inside the eye) was measured by Goldmann applanation tonometry. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater amount of improvement. Only one eye (study eye) contributed to the mean. (NCT01263444)
Timeframe: Baseline, Week 12

InterventionmmHg (Mean)
Azarga-6.0

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Mean Change From Baseline in IOP at Week 4

IOP (fluid pressure inside the eye) was measured by Goldmann applanation tonometry. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater amount of improvement. Only one eye (study eye) contributed to the mean. (NCT01263444)
Timeframe: Baseline, Week 4

InterventionmmHg (Mean)
Azarga-6.0

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Mean IOP at Month 3 for Each Assessment Timepoint (8 AM, + 2 h, + 7 h, and + 9 h)

At the Month 3 (Exit) visit, the 8 am IOP measurement was taken before instillation of study drug. The study drug was instilled approximately 15 minutes after the 8 am measurement. An additional dose was given at 3 pm. Intraocular pressure was measured by Goldmann applanation tonometry. One eye from each patient was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01297517)
Timeframe: Month 3

,,
Interventionmillimeters mercury (mm Hg) (Least Squares Mean)
8 am (before study drug instillation)+2 hrs relative to 8 am dosing+7 hrs relative to 8 am dosing+9 hrs relative to 8 am dosing
Brimonidine23.319.721.318.8
Brinzolamide21.620.420.420.0
Brinzolamide/Brimonidine20.517.218.717.0

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Mean Intraocular Pressure (IOP) at Each Assessment Timepoint (8 AM, +2 h, +7 h, and +9 h) at Month 3

The study drug was instilled at 8 AM and 3 PM (approximately 15 minutes after conducting the IOP measurements). Intraocular pressure was measured by Goldmann applanation tonometry. One eye from each patient was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01297920)
Timeframe: Month 3

,,
Interventionmillimeters mercury (mm HG) (Least Squares Mean)
8 AM (before study drug instillation)+ 2 hours relative to 8 AM dosing+ 7 hours relative to 8 AM dosing+ 9 hours relative to 8 AM dosing
Brimonidine23.219.921.518.9
Brinz/Brim21.118.019.517.2
Brinzolamide22.020.820.720.4

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Mean Diurnal IOP Change From Baseline at Month 3

Mean Diurnal IOP Change from Baseline at Month 3 (ie, the subject IOP change from baseline averaged over the 9 AM and + 2 h time points at Month 3) was measured by Goldmann applanation tonometry. The study drug was instilled approximately 15 minutes after conducting the 9AM IOP measurement. One eye from each subject was chosen as the study eye, and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01309204)
Timeframe: Baseline (Day 1), Month 3

Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Brinz/Brim-8.5
Brinz+Brim-8.3

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Mean Diurnal IOP Change From Baseline at Month 3

Mean Diurnal IOP Change from Baseline at Month 3 (ie, the subject IOP change from baseline averaged over the 9 AM, + 2 h, and + 7 h time points at Month 3) was measured by Goldmann applanation tonometry. The study drug was instilled approximately 15 minutes after conducting the 9AM IOP measurement. One eye from each subject was chosen as the study eye, and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01310777)
Timeframe: Baseline (Day 1), Month 3

Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Brinz/Brim-7.9
Brinz-6.5
Brim-6.4

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Ocular Discomfort

Ocular discomfort was assessed by the participant 1 minute after instillation of the study medication. Ocular discomfort was rated on a 10-point scale (0=no discomfort, 9=substantial discomfort). (NCT01340014)
Timeframe: Day 7 of each period

InterventionUnits on a scale (Mean)
AZARGA2.6
COSOPT3.7

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Preferred Treatment

"The participant completed a questionnaire on the Day 15 visit (ie, after administration of both study medications) consisting of a single preference question: Thinking about the comfort of the two medications (1st and 2nd) that you took during this study, which medication do you prefer? Preferred treatment is presented as a percentage." (NCT01340014)
Timeframe: At the end of both periods, Day 15

InterventionPercentage of participants (Number)
AZARGA60.2
COSOPT39.8

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Mean Diurnal IOP Change From Baseline at Week 8

Mean diurnal IOP change from baseline at Week 8 (ie, the subject IOP change from baseline averaged over the 9 AM, 11AM and 5 PM time points at Week 8) was measured by Goldmann applanation tonometry. One eye from each subject was chosen as the study eye, and only data for the study eye were used for the efficacy analysis. A higher IOP (fluid pressure inside the eye) can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater improvement.. (NCT01357616)
Timeframe: Baseline, Week 8

Interventionmillimeters mercury (mmHg) (Least Squares Mean)
AZARGA-6.84
AZOPT + Timolol-6.00

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Mean IOP Change From Baseline at 11 AM

Mean IOP change from baseline at 11 AM was measured by Goldmann applanation tonometry. One eye from each subject was chosen as the study eye, and only data for the study eye were used for the efficacy analysis. A higher IOP (fluid pressure inside the eye) can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater improvement. (NCT01357616)
Timeframe: Baseline, Up to Week 8

,
InterventionmmHg (Least Squares Mean)
Change from baseline at Week 2Change from baseline at Week 4Change from baseline at Week 8
AZARGA-7.5-7.6-7.4
AZOPT + Timolol-6.8-6.8-6.5

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Mean IOP Change From Baseline (5 PM) at Week 8

Mean IOP change from baseline (5 PM) at Week 8 was measured by Goldmann applanation tonometry. One eye from each subject was chosen as the study eye, and only data for the study eye were used for the efficacy analysis. A higher IOP (fluid pressure inside the eye) can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater improvement. (NCT01357616)
Timeframe: Baseline, Week 8

InterventionmmHg (Least Squares Mean)
AZARGA-6.3
AZOPT + Timolol-5.1

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Mean IOP Change From Baseline at 9 AM

Mean IOP change from baseline at 9 AM was measured by Goldmann applanation tonometry. One eye from each subject was chosen as the study eye, and only data for the study eye were used for the efficacy analysis. A higher IOP (fluid pressure inside the eye) can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater improvement. (NCT01357616)
Timeframe: Baseline, Up to Week 8

,
InterventionmmHg (Least Squares Mean)
Change from baseline at Week 2Change from baseline at Week 4Change from baseline at Week 8
AZARGA-6.9-7.3-6.7
AZOPT + Timolol-6.5-6.4-6.2

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Percentage of Subjects Who Reach Target IOP (≤ 18 mmHg)

IOP (fluid pressure inside the eye) was assessed by Goldmann applanation tonometry and measured in mmHg. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). One eye was chosen as the study eye, and only data from the study eye were used for the efficacy analysis. (NCT01415401)
Timeframe: Week 8

Interventionpercentage of participants (Number)
AZARGA36.2

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Change in IOP at the Final Visit From Prior Brimonidine 0.2%/Timolol 0.5% Fixed Combination (COMBIGAN®) Therapy (i.e. From Baseline)

IOP (fluid pressure inside the eye) was assessed by Goldmann applanation tonometry and measured in millimeters of mercury (mmHg). A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater amount of improvement. One eye was chosen as the study eye, and only data from the study eye were used for the efficacy analysis. (NCT01415401)
Timeframe: Baseline, Week 8

InterventionmmHg (Mean)
BaselineChange from baseline at Week 8
AZARGA22.24-2.24

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Mean Ocular Discomfort Score

Ocular discomfort was assessed by the subject immediately following the 8 AM instillation of study drug and rated on a 5-point scale: 0 (none), 1 (mild), 2 (moderate), 3 (severe), and 4 (very severe). (NCT01426867)
Timeframe: Week 1

InterventionUnits on a scale (Mean)
Brinz/Brim0.8
Brinzolamide0.4
Brimonidine0.3

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Change in Intraocular Pressure (IOP) at the Final Visit From Prior Beta-blocker Monotherapy (Timolol 0.5% Only)

As measured at baseline and final visit with Goldmann applanation tonometry. The outcome measure was pre-specified for Timolol 0.5% only participants. (NCT01484951)
Timeframe: Baseline, Week 8

Interventionmillimeters mercury (mmHg) (Mean)
BaselineChange at Week 8
AZARGA18.22-3.56

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Percentage of Patients With Target IOP (≤18 mmHg), Regardless of Prior Therapy

As measured with Goldmann applanation tonometry. The outcome measure was pre-specified for all participants. (NCT01484951)
Timeframe: Week 8

InterventionPercentage of Participants (Number)
AZARGA54.3

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Change in Intraocular Pressure (IOP) at 8 Weeks From Baseline (Prior Therapy).

Intraocular pressure was measured by Goldmann applanation tonometry. Data for the worse eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01514734)
Timeframe: 8 weeks

Interventionmillimeters mercury (mmHg) (Mean)
AZARGA-0.89

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Mean Change in Intraocular Pressure (IOP) From Baseline (Prior Therapy) at Week 8

IOP (fluid pressure inside the eye) was measured by Goldmann applanation tonometry. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates a greater amount of improvement. One eye was chosen as the study eye, and only data from the study eye were used for the efficacy analysis. (NCT01518244)
Timeframe: Baseline, Week 8

Interventionmilllimeters mercury (mmHg) (Mean)
AZARGA®-3.60

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Percentage of Subjects Who Reach Target IOP (≤18 mmHg) at Week 8

IOP (fluid pressure inside the eye) was measured by Goldmann applanation tonometry. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). One eye was chosen as the study eye, and only data from the study eye were used for the efficacy analysis. (NCT01518244)
Timeframe: Week 8

Interventionpercentage of participants (Number)
AZARGA®55.3

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Change in Intraocular Pressure (IOP) From Baseline to Week 12

(NCT01722604)
Timeframe: Baseline, Week 12

InterventionmmHg (Mean)
Brinzolamide 1% Ophthalmic Suspension-5.3
Azopt 1% Ophthalmic Suspension-5.4

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Intraocular Pressure (IOP) at Week 12

(NCT01722604)
Timeframe: Week 12

InterventionmmHg (Mean)
Brinzolamide 1% Ophthalmic Suspension20.6
Azopt 1% Ophthalmic Suspension20.8

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Mean Diurnal IOP Change From Baseline to Week 6

Baseline IOP was defined as the average of the timepoint-matched IOP measurements at Eligibility 1 and Eligibility 2 Visits. Diurnal IOP change was defined as the average of the four changes from baseline (timepoints 8 AM, 10 AM, 3 PM, and 5 PM). IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in millimeters mercury (mmHg). One eye was chosen as the study eye and only data for the study eye were used for the analyses. A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. (NCT01937299)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
SIMBRINZA-5.10
Vehicle-2.22

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Mean Diurnal Intraocular Pressure (IOP) at Week 6

Diurnal IOP was defined as the average of the four timepoints measured (8 AM, 10 AM, 3 PM, and 5 PM). IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in millimeters mercury (mmHg). One eye was chosen as the study eye and only data for the study eye were used for the analyses. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01937299)
Timeframe: Week 6

InterventionmmHg (Mean)
SIMBRINZA17.44
Vehicle20.34

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Mean Diurnal IOP Percentage Change From Baseline to Week 6

Baseline IOP was defined as the average of the timepoint-matched IOP measurements at Eligibility 1 and Eligibility 2 Visits. Diurnal IOP Percentage Change was defined as the average of the four percent changes from baseline (timepoints 8 AM, 10 AM, 3 PM, and 5 PM). IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in millimeters mercury (mmHg). One eye was chosen as the study eye and only data for the study eye were used for the analyses. A more negative percent change from baseline indicates a greater amount of improvement, i.e., a reduction of IOP. (NCT01937299)
Timeframe: Baseline, Week 6

Interventionpercent change (Mean)
SIMBRINZA-22.27
Vehicle-9.57

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Mean Diurnal Intraocular Pressure (IOP) at Week 6

Diurnal IOP was defined as the average of the four timepoints measured (8 AM, 10 AM, 3 PM, and 5 PM). IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in millimeters mercury (mmHg). One eye was chosen as the study eye and only data for the study eye were used for the analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01937312)
Timeframe: Week 6

InterventionmmHg (Mean)
SIMBRINZA17.01
Vehicle20.37

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Mean Diurnal IOP Change From Baseline to Week 6

Baseline IOP was defined as the average of the timepoint-matched IOP measurements at Eligibility 1 and Eligibility 2 Visits. Diurnal IOP change was defined as the average of the four changes from baseline (timepoints 8 AM, 10 AM, 3 PM, and 5 PM). IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in millimeters mercury (mmHg). One eye was chosen as the study eye and only data for the study eye were used for the analysis. A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. (NCT01937312)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
SIMBRINZA-5.69
Vehicle-1.99

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Mean Diurnal IOP Percentage Change From Baseline to Week 6

Baseline IOP was defined as the average of the timepoint-matched IOP measurements at Eligibility 1 and Eligibility 2 Visits. Diurnal IOP Percentage Change was defined as the average of the four percent changes from baseline (timepoints 8 AM, 10 AM, 3 PM, and 5 PM). IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in millimeters mercury (mmHg). One eye was chosen as the study eye and only data for the study eye were used for the analysis. A more negative percent change from baseline indicates a greater amount of improvement, i.e., a reduction of IOP. (NCT01937312)
Timeframe: Baseline, Week 6

Interventionpercent change (Mean)
SIMBRINZA-24.88
Vehicle-8.50

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Mean IOP at Week 6 for Each Time Point (8 AM, 10 AM, 3 PM, 5 PM)

IOP was assessed using Goldmann applanation tonometry and reported in mmHg. One eye was chosen as the study eye and only data for the study eye were used for the analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01937312)
Timeframe: Week 6

,
InterventionmmHg (Mean)
8 AM10 AM3 PM5 PM
SIMBRINZA19.415.817.215.6
Vehicle21.420.219.919.9

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Mean 24-hour IOP at Week 4

24-hour IOP (fluid pressure inside the eye) is the mean of all the time points assessed (8 AM to 6 AM). IOP was measured with a calibrated applanation tonometer in millimeters of mercury (mmHg). One eye from each subject was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01978600)
Timeframe: Week 4: 8AM, 10AM, 12PM, 2PM, 4PM, 6PM, 8PM, 10PM, 12AM, 2AM, 4AM, 6AM

,
InterventionmmHg (Mean)
Baseline (Day 0)Week 4
Simbrinza23.617.9
Timolol22.818.2

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Mean Diurnal IOP at Week 4

Diurnal IOP (fluid pressure inside the eye) is the mean of the diurnal time points assessed (8 AM to 8 PM). IOP was measured with a calibrated applanation tonometer in millimeters of mercury (mmHg). One eye from each subject was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01978600)
Timeframe: Week 4: 8AM, 10AM, 12PM, 2PM, 4PM, 6PM, 8PM

,
InterventionmmHg (Mean)
Baseline (Day 0)Week 4
Simbrinza23.217.3
Timolol22.217.7

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Mean Nocturnal IOP at Week 4

Nocturnal IOP (fluid pressure inside the eye) is the mean of the nocturnal time points assessed (10 PM to 6 AM). IOP was measured with a calibrated applanation tonometer in millimeters of mercury (mmHg). One eye from each subject was chosen as the study eye and only data for the study eye were used for the efficacy analysis. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). (NCT01978600)
Timeframe: Week 4: 10PM, 12AM, 2AM, 4AM, 6AM

,
InterventionmmHg (Mean)
Baseline (Day 0)Week 4
Simbrinza24.218.6
Timolol23.618.9

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Mean IOP at Week 6

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and measured in millimeters of mercury (mmHg). A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). One eye (study eye) was used for the analysis. (NCT02140060)
Timeframe: Week 6, 8 AM, 10 AM, 12 PM, 4 PM, and 8 PM

,,,,,
InterventionmmHg (Mean)
8 AM10 AM12 PM4PM8 PM, n=44, 44, 44, 43, 45, 43
AZOPT22.019.719.519.119.3
TRAV Z19.317.417.217.617.3
TRAV Z + AZOPT20.318.218.018.018.1
TravA/Brinz20.218.918.918.518.4
TravB/Brinz18.717.217.317.517.5
TravC/Brinz19.918.217.717.317.2

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Least Squares Mean Change From Baseline in Intraocular Pressure (IOP) at 11 AM

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and measured in millimeters of mercury (mmHg). Data from 4 and 8 weeks at 11 AM were pooled, and a negative change indicates an improvement. One eye (target eye) was used for the analysis. (NCT02325518)
Timeframe: Baseline (Day 0), Week 4, Week 8 at 11 AM

,
InterventionmmHg (Least Squares Mean)
BaselineMean change pooled over Week 4 and Week 8
BRI/TIM17.0-3.3
DOR/TIM17.0-3.4

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Least Squares Mean Change From Baseline in IOP at 9 AM

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and measured in millimeters of mercury (mmHg). Data from 4 and 8 weeks at 9 AM were pooled, and a negative change indicates an improvement. One eye (target eye) was used for the analysis. (NCT02325518)
Timeframe: Baseline (Day 0), Week 4, Week 8 at 9 AM

,
InterventionmmHg (Least Squares Mean)
BaselineChange at Pool (Week 4, Week 8)
BRI/TIM17.4-3.3
DOR/TIM17.3-2.9

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Mean Diurnal IOP Change From Baseline at Month 3

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry and reported in mmHg. Diurnal IOP was defined as the average of the three timepoints measured: 9 AM, +2 Hrs and +7Hrs. Baseline was the average of the values for 2 eligibility visits. If one of the values was missing, the other non-missing value was taken as the baseline. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates greater improvement, ie, a reduction of IOP. Only one eye (study eye) contributed to the analysis. (NCT02339584)
Timeframe: Baseline (Day 0), Month 3

InterventionmmHg (Mean)
Brinz/Brim-7.2
Brinz+Brim-7.3

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Mean Diurnal IOP at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry and averaged over the 09:00 AM and 11:00 AM time points. A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Week 6

InterventionmmHg (Mean)
SIMBRINZA + PGA17.2
Vehicle + PGA20.9

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Mean Percentage Change From Baseline at 09:00 at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry at 9:00 AM. Baseline is defined as the average of the 9:00 hour values at both Eligibility visits.A more negative percent change from baseline indicates a greater improvement, i.e., a reduction of IOP. One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Baseline, Week 6

Interventionpercent change (Mean)
SIMBRINZA + PGA-21.0
Vehicle + PGA-10.9

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Mean Change From Baseline (on PGA) in Diurnal IOP (Mean of 09:00 and 11:00 Time Points) at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry and averaged over the 09:00 AM and 11:00 AM time points. A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
SIMBRINZA + PGA-5.6
Vehicle + PGA-2.1

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Mean Percentage Change From Baseline in IOP at 11:00 at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry at 11:00 AM. A more negative percent change from baseline indicates a greater improvement, i.e., a reduction of IOP. One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Baseline, Week 6

Interventionpercent change (Mean)
SIMBRINZA + PGA-31.3
Vehicle + PGA-10.8

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Mean Change From Baseline in IOP at 09:00 at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry at 09:00 AM. Baseline is defined as the average of the 9:00 hour values at both Eligibility visits. A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Baseline, Week 6

,
InterventionmmHg (Mean)
BaselineChange from baseline
SIMBRINZA + PGA23.4-4.9
Vehicle + PGA23.4-2.5

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Mean Change From Baseline in IOP at 11:00 at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry at 11:00 AM. A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Baseline, Week 6

,
InterventionmmHg (Mean)
BaselineChange from baseline
SIMBRINZA + PGA22.4-7.0
Vehicle + PGA22.6-2.4

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Mean Percentage Change From Baseline in Diurnal IOP at Week 6

IOP (fluid pressure inside the eye) was measured using Goldmann applanation tonometry and averaged over the 09:00 AM and 11:00 AM time points. A more negative percent change from baseline indicates a greater improvement, i.e., a reduction of IOP. One eye (study eye) contributed to the analysis. (NCT02419508)
Timeframe: Baseline, Week 6

Interventionpercent change (Mean)
SIMBRINZA + PGA-24.7
Vehicle + PGA-9.5

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Mean Difference in Intraocular Pressure (IOP) of Both Eyes Between the Two Treatment Groups at Four Time Points

The primary efficacy end point is the mean difference in intraocular pressure (IOP) of both eyes between the two treatment groups at four time points, i.e., at approximately 8:00 am (hour 0; before the morning drop) and 10:00 am (hour 2; after the morning drop) at the Day 14 (week 2) and Day 42 (week 6) visits (NCT02512042)
Timeframe: Day 14 and 42 at 8AM and 10AM

,
InterventionmmHg (Mean)
8AM Visit Day 148AM Visit Day 4210AM Visit Day 1410AM Visit Day 42
Azopt® (Brinzolomide Ophthalmic Suspension USP 1%)19.7518.6619.1818.16
Generic Brinzolamide Ophthalmic Suspension USP 1%19.3518.5318.7017.94

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Mean Percentage Change From Baseline in Diurnal IOP at Week 6

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry. Diurnal IOP percentage change was defined as the average of the two changes from baseline (timepoints 9 AM, 11 AM). A more negative percentage change from baseline indicates a greater improvement, i.e., a reduction of IOP. Only one eye (study eye) was used for the analyses. (NCT02730871)
Timeframe: Baseline, Week 6

Interventionpercentage change (Mean)
Simbrinza + Duotrav-20.7
Vehicle + Duotrav-11.1

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Mean Change From Baseline in IOP (09:00, 11:00) at Week 6

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry. A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. Only one eye (study eye) was used for the analyses. (NCT02730871)
Timeframe: Baseline, Week 6

,
InterventionmmHg (Mean)
Baseline 9:00 HrBaseline 11:00 HrChange from Baseline 9:00 HrChange from Baseline 11:00 Hr
Simbrinza + Duotrav22.221.4-4.4-5.4
Vehicle + Duotrav22.521.4-3.2-2.5

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Mean Change From Baseline in Diurnal Intraocular Pressure (IOP) (Mean of Changes at 09:00 and 11:00 Time Points) at Week 6

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry. Diurnal IOP change was defined as the average of the two changes from baseline (timepoints 9 AM, 11 AM). A more negative change from baseline indicates a greater improvement, i.e., a reduction of IOP. Only one eye (study eye) was used for the analyses. (NCT02730871)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
Simbrinza + Duotrav-4.5
Vehicle + Duotrav-2.4

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Mean Percentage Change From Baseline in IOP (09:00, 11:00) at Week 6

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry. A more negative percentage change from baseline indicates a greater improvement, i.e., a reduction of IOP. Only one eye (study eye) was used for the analyses. (NCT02730871)
Timeframe: Baseline, Week 6

,
Interventionpercentage change (Mean)
Percent change at 9:00 HrPercent change at 11:00 Hr
Simbrinza + Duotrav-20.2-25.0
Vehicle + Duotrav-14.1-11.7

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Mean Diurnal IOP at Week 6

IOP (fluid pressure inside the eye) was assessed using Goldmann applanation tonometry. Diurnal IOP was defined as the average of the two time points measured (9 AM, 11 AM). A higher IOP can be a greater risk factor for developing glaucoma or glaucoma progression (leading to optic nerve damage). Only one eye (study eye) was used for the analyses. (NCT02730871)
Timeframe: Week 6

InterventionmmHg (Mean)
Simbrinza + Duotrav17.1
Vehicle + Duotrav19.4

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Least Squares Mean Change From Baseline in IOP for Each Time Point (8 AM Through 6 AM) at Week 4

IOP (fluid pressure inside the eye) was measured in mmHg. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates greater improvement. Only one eye (study eye) contributed to the analysis. (NCT02770248)
Timeframe: Baseline (Day 0), Week 4

,
InterventionmmHg (Least Squares Mean)
8AM10AM12PM2PM4PM6PM8PM10PM12AM2AM4AM6AM
SIMBRINZA-3.28-5.05-4.03-3.36-3.95-4.46-3.42-2.10-1.79-2.30-1.42-1.95
Vehicle-0.49-0.61-0.27-0.66-0.51-0.32-0.72-0.67-0.83-0.55-0.98-0.63

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Least Squares Mean Change From Baseline in Nocturnal IOP at Week 4

IOP (fluid pressure inside the eye) was measured in mmHg. Change was calculated by taking the change from baseline at each time point (10 PM through 6 AM) and averaging the available changes. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates greater improvement. Only one eye (study eye) contributed to the analysis. (NCT02770248)
Timeframe: Baseline (Day 0), Week 4

InterventionmmHg (Least Squares Mean)
SIMBRINZA-1.88
Vehicle-0.73

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Least Squares Mean Change From Baseline in Daytime IOP at Week 4

IOP (fluid pressure inside the eye) was measured in mmHg. Change was calculated by taking the change from baseline at each time point (8 AM through 8 PM) and averaging the available changes. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates greater improvement. Only one eye (study eye) contributed to the analysis. (NCT02770248)
Timeframe: Baseline (Day 0), Week 4

InterventionmmHg (Least Squares Mean)
SIMBRINZA-3.93
Vehicle-0.51

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Least Squares Mean Change From Baseline in 24-hr Intraocular Pressure (IOP) at Week 4

IOP (fluid pressure inside the eye) was measured in millimeters of mercury (mmHg). Change was calculated by taking the change from baseline at each time point and averaging the available changes. A higher IOP can be a greater risk for developing glaucoma or glaucoma progression (leading to optic nerve damage). A more negative change indicates greater improvement. Only one eye (study eye) contributed to the analysis. (NCT02770248)
Timeframe: Baseline (Day 0), Week 4

InterventionmmHg (Least Squares Mean)
SIMBRINZA-3.09
Vehicle-0.60

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Intraocular Pressure (IOP) at 3 Hours After Nd-YAG Posterior Capsulotomy

Comparison of intraocular pressure at 3 hours after Nd-YAG posterior capsulotomy compared to Baseline IOP (NCT03192826)
Timeframe: 3 hours

,,
InterventionmmHg (Mean)
Baseline3 hours
Artificial Tears15.219.5
Brimonidine 0.2%15.714.7
Brinzolamide/Brimonidine FC15.612.7

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Intraocular Pressure (IOP) at 24 Hourw After Nd-YAG Posterior Capsulotomy

Comparison of intraocular pressure at 24 hours after Nd-YAG posterior capsulotomy compared to Baseline IOP (NCT03192826)
Timeframe: 24 hours

,,
InterventionmmHg (Mean)
Baseline24 hours
Artificial Tears15.215.8
Brimonidine 0.2%15.715.5
Brinzolamide/Brimonidine FC15.614.6

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Intraocular Pressure (IOP) at 1 Week After Nd-YAG Posterior Capsulotomy

Comparison of intraocular pressure at 1 week after Nd-YAG posterior capsulotomy compared to Baseline IOP (NCT03192826)
Timeframe: 1 week

,,
InterventionmmHg (Mean)
Baseline1 week
Artificial Tears15.215.6
Brimonidine 0.2%15.715.3
Brinzolamide/Brimonidine FC15.615.5

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Intraocular Pressure (IOP) at 1 Hour After Nd-YAG Posterior Capsulotomy

Comparison of intraocular pressure at 1 hour after Nd-YAG posterior capsulotomy compared to Baseline IOP (NCT03192826)
Timeframe: 1 hour

,,
InterventionmmHg (Mean)
Baseline1 hour
Artificial Tears15.219.5
Brimonidine 0.2%15.714.7
Brinzolamide/Brimonidine FC15.613.7

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Change in Intraocular Pressure (IOP)

Change in intraocular pressure (IOP) from baseline (Eligibility Visit 2) and after treatment. (NCT03896633)
Timeframe: 6 weeks

InterventionmmHg (Mean)
Brinzolamide 1% Ophthalmic Suspension-4.85
Azopt 1% Ophthalmic Suspension-4.70

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Intraocular Pressure (IOP)

(NCT03896633)
Timeframe: 6 weeks

InterventionmmHg (Mean)
Brinzolamide 1% Ophthalmic Suspension20.07
Azopt 1% Ophthalmic Suspension19.89

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Mean Change in Intra-ocular Pressure

mean change in intra-ocular pressure of both eyes at four time points : at approximately 8:00 a.m. (hour 0; before the morning drop) and approximately 10:00 a.m. (hour 2) on Day 14 (Week 2) and Day 42 (Week 6) visits. (NCT04024072)
Timeframe: 6 weeks

,
InterventionmmHG (Mean)
8AM Day 1410AM Day 148AM Day 4210AM Day 42
Perrigo Active-4.25-4.22-4.43-4.05
Reference Active-3.80-4.00-4.20-4.06

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