l 671152 profile

dorzolamide hydrochloride : The hydrochloride salt of dorzolamide. It is used in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension. [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]

ID Source	ID
PubMed CID	6918132
CHEMBL ID	1201162
CHEBI ID	4703
SCHEMBL ID	41152
MeSH ID	M0173573

Synonym
AC-5244
dorzolomide hydrochloride
smr001233461
MLS002154162
mk-507
trusopt
dorzolamide hydrochloride
l-671152
cas-130693-82-2
NCGC00016977-01
dorzolamide hydrochloride (jp17/usp)
D00653
130693-82-2
dorzolamide hydrochloride [usan]
l-671,152
mk 0507
l 671152
cosopt
(4s,6s)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide, monohydrochloride
4h-thieno(2,3-b)thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, monohydrochloride, (4s-trans)-
4h-thieno(2,3-b)thiopyran-2-sulfonamide, 5,6-dihydro-4-(ethylamino)-6-methyl-, 7,7-dioxide, monohydrochloride, (4s,6s)-
mk-0507
dorzolamide hcl ,
(4s,6s)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride
CHEBI:4703 ,
CHEMBL1201162
dorzolamide (as hydrochloride)
AKOS005146235
HMS1571O14
unii-qzo5366ew7
dorzolamide hydrochloride [usan:usp]
qzo5366ew7 ,
dtxcid9025530
tox21_110720
dtxsid1045530 ,
D4189
S1375
AKOS015895951
dorzolamide hydrochloride, trans-(-)-
cosopt component dorzolamide hydrochloride
122028-16-4
dorzolamide hydrochloride [mart.]
dorzolamide hydrochloride [usp impurity]
dorzolamide hydrochloride component of cosopt
dorzolamide hydrochloride [mi]
dorzolamide hydrochloride [usp monograph]
dorzolamide hydrochloride [vandf]
dorzolamide hydrochloride [usp-rs]
dorzolamide hydrochloride [who-dd]
dorzolamide hydrochloride [jan]
(4s,6s)-4-(ethylamino)-5,6-dihydro-6-methyl-4h-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide, monohydrochloride
dorzolamide hydrochloride [orange book]
CCG-221116
CS-1858
dorzolamide (hydrochloride)
HY-B0109A
SCHEMBL41152
NCGC00179244-03
tox21_110720_1
KS-1348
OSRUSFPMRGDLAG-QMGYSKNISA-N
(4s,6s)-4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide 4h-thieno[2,3-b]thiopyran-2-sulfonamide hydrochloride
(4s,6s)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4h-thieno[2,3-b]thiopyran-2-sulfonamide;hydrochloride
mk507 hydrochloride
l671152 hydrochloride
mk-507 (l-671152) hcl
dorzolamide hydrochloride, united states pharmacopeia (usp) reference standard
SR-05000001449-3
dorzolamide for system suitability, european pharmacopoeia (ep) reference standard
dorzolamide hydrochloride, european pharmacopoeia (ep) reference standard
mfcd00884659
Q27106441
dorzolomide hcl
EX-A3987
C72221
(2s,4s)-4-(ethylamino)-2-methyl-1,1-dioxo-2h,3h,4h-1lambda6-thieno[2,3-b]thiopyran-6-sulfonamide hydrochloride
EN300-19768601
BD164381
dorzolamide hydrochloride- bio-x
dorzolamide hydrochloride ophthalmic
dorzolamide hydrochloride (usp monograph)
(4s,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide hydrochloride
dorzolamide hydrochloride (usp impurity)
dorzolamide hydrochloride (usan:usp)
dorzolamide hci
dorzolamide pf
dorzolamide hydrochloride (usp-rs)
(4s,6s)-4-ethylamino-6-methyl-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide monohydrochloride
(ss,6s)-n-ethyl-6-methyl-2-sulfamoyl-5,6-dihydro-4h-thieno(2,3-b)thiopyran-4-aminium 7,7-dioxide chloride
(4s,6s)-4-(ethylamino)-6-methyl-5,6-dihydro-4h-thieno(2,3-b)thiopyran-2-sulfonamide 7,7-dioxide hydrochloride
dorzolamide hydrochloride (mart.)
Z2756516872

Excerpt	Reference	Relevance
"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

Role	Description
EC 4.2.1.1 (carbonic anhydrase) inhibitor	An 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.
antihypertensive agent	Any drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
antiglaucoma drug	Any 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.
[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]

Class	Description
hydrochloride	A salt formally resulting from the reaction of hydrochloric acid with an organic base.
organoammonium salt
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Beta-lactamase	Escherichia coli K-12	Potency	5.6234	0.0447	17.8581	100.0000	AID485294
TDP1 protein	Homo sapiens (human)	Potency	3.6626	0.0008	11.3822	44.6684	AID686978
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	2.9849	0.0010	22.6508	76.6163	AID1224838
chromobox protein homolog 1	Homo sapiens (human)	Potency	100.0000	0.0060	26.1688	89.1251	AID540317
nuclear factor erythroid 2-related factor 2 isoform 2	Homo sapiens (human)	Potency	14.5810	0.0041	9.9848	25.9290	AID504444
DNA polymerase iota isoform a (long)	Homo sapiens (human)	Potency	100.0000	0.0501	27.0736	89.1251	AID588590
geminin	Homo sapiens (human)	Potency	5.8048	0.0046	11.3741	33.4983	AID624296
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (75)

Assay ID	Title	Year	Journal	Article
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS 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.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The 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.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The 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.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID166276	In vivo fall of IOP of normotensive rabbits after treatment with 1 drop(50 microL) of 2% solution of CA inhibitor with pH value 5.5 into the eye at 60 min	1999	Journal 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?
AID251065	Tested for the fall of intraocular pressure of glaucomatous rabbits, after treatment with one drop (50 uL) 2% solution at a pH 5.5, directly into the eye after 90 minutes of administration	2005	Bioorganic & 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.
AID1322634	Reduction in intraocular pressure in New Zealand albino rabbit model of hypertonic saline-induced ocular hypertension at 1 to 2% instilled immediately after hypertonic saline injection measured after 4 hrs post dose	2016	Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23	Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure Lowering Investigations.
AID1357850	Anti-glaucoma activity in albino New Zealand rabbit transient glaucoma model assessed as inhibition of hypertonic saline-induced intraocular pressure at 1% administered topically and measured after 24 to 96 mins	2018	European journal of medicinal chemistry, May-10, Volume: 151	2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents.
AID166500	Drug concentration was tested in ocular fluids and tissues after 1 hour following the corneal application in normotensive albino rabbits on aqueous humor	1999	Journal 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?
AID1385751	Reduction in hypertonic saline solution-induced elevated intraocular pressure in New Zealand White rabbit at 1 % (w/v) dosed topically before hypertonic saline solution injection measured after 60 mins
AID1322633	Reduction in intraocular pressure in New Zealand albino rabbit model of hypertonic saline-induced ocular hypertension at 1 to 2% instilled immediately after hypertonic saline injection measured after 60 mins post dose	2016	Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23	Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure Lowering Investigations.
AID251064	Tested for the fall of intraocular pressure of glaucomatous rabbits, after treatment with one drop (50 uL) 2% solution at a pH 5.5, directly into the eye after 60 minutes of administration	2005	Bioorganic & 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.
AID166273	In vivo fall of IOP of normotensive rabbits after treatment with 1 drop(50 microL) of 2% solution of CA inhibitor with pH value 5.5 into the eye at 0 min	1999	Journal 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?
AID166277	In vivo fall of IOP of normotensive rabbits after treatment with 1 drop(50 microL) of 2% solution of CA inhibitor with pH value 5.5 into the eye at 90 min.	1999	Journal 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?
AID1656170	Suppression of hypertonic saline solution-induced increase in intraocular pressure in New Zealand rabbit model of glaucoma assessed as reduction in intraocular pressure dosed as 1% eye drops formulation via direct instillation into eye conjunctive pocket	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.
AID1168855	Antiglaucoma activity in hypertensive New Zealand rabbit assessed as drop in intraocular pressure at 2% solution administered as topical ocular instillation after 4 hrs relative to control	2014	Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21	Structural insights on carbonic anhydrase inhibitory action, isoform selectivity, and potency of sulfonamides and coumarins incorporating arylsulfonylureido groups.
AID1626030	Ocular hypotensive activity in sterile hypertonic saline injected hypertensive New Zealand white rabbit assessed as reduction in intraocular pressure at 1 % administered as eye drops measured up to 120 mins post injection	2016	Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12	Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma.
AID1170163	Antiglaucoma activity in New Zealand albino rabbit assessed as reduction in hypertonic saline-induced intraocular pressure at 2% solution administered topically measured after 4 hrs	2014	Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22	A class of 4-sulfamoylphenyl-ω-aminoalkyl ethers with effective carbonic anhydrase inhibitory action and antiglaucoma effects.
AID1357848	Anti-glaucoma activity in albino New Zealand rabbit transient glaucoma model assessed as inhibition of hypertonic saline-induced intraocular pressure at 1% administered topically and measured after 60 mins	2018	European journal of medicinal chemistry, May-10, Volume: 151	2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents.
AID1656169	Suppression of hypertonic saline solution-induced increase in intraocular pressure in New Zealand rabbit model of glaucoma assessed as reduction in intraocular pressure dosed as 1% eye drops formulation via direct instillation into eye conjunctive pocket	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.
AID1656171	Suppression of hypertonic saline solution-induced increase in intraocular pressure in New Zealand rabbit model of glaucoma assessed as reduction in intraocular pressure dosed as 1% eye drops formulation via direct instillation into eye conjunctive pocket	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.
AID166505	Drug concentration was tested in ocular fluids and tissues after 2 hour following the corneal application in normotensive albino rabbits on cornea	1999	Journal 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?
AID166504	Drug concentration was tested in ocular fluids and tissues after 2 hour following the corneal application in normotensive albino rabbits on cilirary process	1999	Journal 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?
AID166275	In vivo fall of IOP of normotensive rabbits after treatment with 1 drop(50 microL) of 2% solution of CA inhibitor with pH value 5.5 into the eye at 30 min.	1999	Journal 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?
AID1357849	Anti-glaucoma activity in albino New Zealand rabbit transient glaucoma model assessed as inhibition of hypertonic saline-induced intraocular pressure at 1% administered topically and measured after 120 mins	2018	European journal of medicinal chemistry, May-10, Volume: 151	2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents.
AID251056	Tested for the fall of intraocular pressure of glaucomatous rabbits, after treatment with one drop (50 uL) 2% solution at a pH 5.5, directly into the eye after 0 minutes of administration	2005	Bioorganic & 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.
AID1656172	Suppression of hypertonic saline solution-induced increase in intraocular pressure in New Zealand rabbit model of glaucoma assessed as reduction in intraocular pressure dosed as 1% eye drops formulation via direct instillation into eye conjunctive pocket	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.
AID1170162	Antiglaucoma activity in New Zealand albino rabbit assessed as reduction in hypertonic saline-induced intraocular pressure at 2% solution administered topically measured after 1 hr	2014	Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22	A class of 4-sulfamoylphenyl-ω-aminoalkyl ethers with effective carbonic anhydrase inhibitory action and antiglaucoma effects.
AID251063	Tested for the fall of intraocular pressure of glaucomatous rabbits, after treatment with one drop (50 uL) 2% solution at a pH 5.5, directly into the eye after 30 minutes of administration	2005	Bioorganic & 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.
AID166502	Drug concentration was tested in ocular fluids and tissues after 1 hour following the corneal application in normotensive albino rabbits on cornea	1999	Journal 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?
AID166501	Drug concentration was tested in ocular fluids and tissues after 1 hour following the corneal application in normotensive albino rabbits on cilirary process	1999	Journal 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?
AID166503	Drug concentration was tested in ocular fluids and tissues after 2 hour following the corneal application in normotensive albino rabbits on aqueous humor	1999	Journal 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?
AID1385752	Reduction in hypertonic saline solution-induced elevated intraocular pressure in New Zealand White rabbit at 1 % (w/v) dosed topically before hypertonic saline solution injection measured after 120 mins
AID504812	Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. 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.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810	Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. 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.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. 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.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588519	A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities	2011	Antiviral research, Sep, Volume: 91, Issue:3	High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299	A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis	2010	Bioorganic & 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	1 (4.17)	18.2507
2000's	2 (8.33)	29.6817
2010's	14 (58.33)	24.3611
2020's	7 (29.17)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	24 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)	3.58	8	monocarboxylic acid amide; sulfonamide; thiadiazoles	anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor
dichlorphenamide Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma.	2.02	1	dichlorobenzene; sulfonamide	antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor; ophthalmology drug
ethoxzolamide Ethoxzolamide: A carbonic anhydrase inhibitor used as diuretic and in glaucoma. It may cause hypokalemia.. ethoxzolamide : A sulfonamide that is 1,3-benzothiazole-2-sulfonamide which is substituted by an ethoxy group at position 6. A carbonic anhydrase inhibitor, it has been used in the treatment of glaucoma, and as a diuretic.	2.41	2	aromatic ether; benzothiazoles; sulfonamide	antiglaucoma drug; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor
mafenide Mafenide: A sulfonamide that inhibits the enzyme CARBONIC ANHYDRASE and is used as a topical anti-bacterial agent, especially in burn therapy.	2	1	aromatic amine
methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.	2.02	1	sulfonamide; thiadiazoles
sulfanilamide [no description available]	2.41	2	substituted aniline; sulfonamide antibiotic; sulfonamide	antibacterial agent; drug allergen; EC 4.2.1.1 (carbonic anhydrase) inhibitor
4-amino-6-chloro-1,3-benzenedisulfonamide 4-amino-6-chloro-1,3-benzenedisulfonamide: metabolite of hydrochlorothiazide	2	1	sulfonamide
brinzolamide brinzolamide: an antiglaucoma agent	2.41	2	sulfonamide; thienothiazine	antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor
2-aminobenzenesulfonamide [no description available]	2	1	benzenes; sulfonamide
5-amino-1,3,4-thiadiazole-2-sulfonamide 5-amino-1,3,4-thiadiazole-2-sulfonamide: structure in first source	2	1
aminozolamide aminozolamide: used in therapy of ocular hypertension	2	1
6-hydroxyethoxzolamide 6-hydroxyethoxzolamide: structure given in first source	2	1
4-(2-aminoethyl)benzenesulfonamide [no description available]	2	1
dorzolamide dorzolamide: topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer. dorzolamide : 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration). A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension.	2.41	2	sulfonamide; thiophenes	antiglaucoma drug; antihypertensive agent; EC 4.2.1.1 (carbonic anhydrase) inhibitor
6-hydroxybenzothiazide-2-sulfonamide 6-hydroxybenzothiazide-2-sulfonamide: structure given in first source	2	1

Condition	Indicated	Relationship Strength	Studies
Intraocular Pressure The pressure of the fluids in the eye.	0	3.46	7
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	3.21	5
Glaucoma An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)	1	5.36	6
Innate Inflammatory Response [description not available]	0	2.05	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.05	1
Encephalitis, Polio [description not available]	0	2.06	1
Poliomyelitis An acute infectious disease of humans, particularly children, caused by any of three serotypes of human poliovirus (POLIOVIRUS). Usually the infection is limited to the gastrointestinal tract and nasopharynx, and is often asymptomatic. The central nervous system, primarily the spinal cord, may be affected, leading to rapidly progressive paralysis, coarse FASCICULATION and hyporeflexia. Motor neurons are primarily affected. Encephalitis may also occur. The virus replicates in the nervous system, and may cause significant neuronal loss, most notably in the spinal cord. A rare related condition, nonpoliovirus poliomyelitis, may result from infections with nonpoliovirus enteroviruses. (From Adams et al., Principles of Neurology, 6th ed, pp764-5)	0	2.06	1
Benign Neoplasms [description not available]	0	2.1	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	2.1	1
Congenital Zika Syndrome [description not available]	0	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1

l 671152

Description

Cross-References

Synonyms (92)

Research Excerpts

Bioavailability

Roles (3)

Drug Classes (2)

Protein Targets (7)

Potency Measurements

Bioassays (75)

Research

Studies (24)

Market Indicators

Research Demand Index: 12.08

Study Types

l 671152

Description

Cross-References

Synonyms (92)

Research Excerpts

Bioavailability

Roles (3)

Drug Classes (2)

Protein Targets (7)

Potency Measurements

Bioassays (75)

Research

Studies (24)

Market Indicators

Research Demand Index: 12.08

Study Types

Related Drugs (15)

Related Conditions (11)