|
Inhibitory activity of compound against human carbonic anhydrase II
|
None
|
40.0
nM
|
|
|
Inhibitory activity of compound against bovine carbonic anhydrase IV
|
None
|
620.0
nM
|
|
|
The IC50 value was reported as apparent, since [3H]NCA was purported to be irreversible (dopamine receptor from Canine striatal membranes). Result indicates the mean of two separate experiments, each performed in triplicate.
|
None
|
200.0
nM
|
|
|
In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane
|
None
|
233.0
nM
|
|
|
Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain
|
None
|
33.0
nM
|
|
|
Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain
|
None
|
36.0
nM
|
|
|
Tested in vitro for inhibition of [3H]spiperone binding to dopamine receptor D2
|
None
|
210.0
nM
|
|
|
Affinity constant of compound was evaluated in rat striatum tissue preparation.
|
None
|
1.5
nM
|
|
|
Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells
|
Homo sapiens
|
8.0
nM
|
|
|
Binding affinity which represents concentration giving half-maximal inhibition of [3H]spiperone (Dopamine receptor D2) binding to rat tissue homogenate
|
None
|
240.0
nM
|
|
|
Compound was tested for its ability to displace [3H]- spiperone from Dopamine receptor D2 in rat striatal membranes
|
None
|
5.51
nM
|
|
|
Ki value against human carbonic anhydrase II (hCA II)
|
Homo sapiens
|
40.0
nM
|
|
|
Ki value against human carbonic anhydrase XII (hCA XII)
|
Homo sapiens
|
3.9
nM
|
|
|
Binding affinity for human dopamine receptor D3
|
Homo sapiens
|
120.0
nM
|
|
|
Binding affinity for human dopamine receptor D2 long
|
Homo sapiens
|
120.0
nM
|
|
|
Inhibitory activity against human recombinant cytosolic CA2
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibitory activity against human recombinant mitochondrial isozyme CA VA
|
Homo sapiens
|
174.0
nM
|
|
|
Inhibitory activity against human recombinant mitochondrial isozyme CA VB
|
Homo sapiens
|
18.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay
|
Helicobacter pylori
|
204.0
nM
|
|
|
Inhibition of human recombinant CA2
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Helicobacter pylori recombinant CA
|
Helicobacter pylori
|
179.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 9 by stopped-flow CO2 hydrase assay
|
Homo sapiens
|
31.0
nM
|
|
|
Inhibition of full length human recombinant CA VI
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of human recombinant cytosolic isozyme CA II by stopped-flow CO2 hydrase method
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of catalytic domain of human recombinant CA IX
|
Homo sapiens
|
46.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay
|
Saccharomyces cerevisiae
|
124.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay
|
Homo sapiens
|
46.0
nM
|
|
|
Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay
|
Mus musculus
|
73.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay
|
Candida albicans
|
760.0
nM
|
|
|
Inhibition of Cryptococcus neoformans recombinant Can2 by stopped-flow CO2 hydration assay
|
Cryptococcus neoformans
|
812.0
nM
|
|
|
Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay
|
Helicobacter pylori
|
40.0
nM
|
|
|
Inhibition of human recombinant CA2 by stopped-flow CO2 assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay
|
Stylophora pistillata
|
430.0
nM
|
|
|
Inhibition of human recombinant CA2 by stopped-flow hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay
|
Mycobacterium tuberculosis
|
266.0
nM
|
|
|
Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay
|
Stylophora pistillata
|
430.0
nM
|
|
|
Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay
|
Stylophora pistillata
|
415.0
nM
|
|
|
Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.5
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Brucella suis carbonic anhydrase II by spectrophotometry at pH 8.3
|
Brucella suis
|
84.0
nM
|
|
|
Inhibition of Brucella suis carbonic anhydrase I by spectrophotometry at pH 8.3
|
Brucella suis
|
19.0
nM
|
|
|
Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
|
Homo sapiens
|
66.22
nM
|
|
|
Antagonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
|
Homo sapiens
|
10.28
nM
|
|
|
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells assessed as inhibition of dopamine-induced recruitment of beta-arrestin-2 after 90 mins by beta-galactosidase assay
|
Homo sapiens
|
560.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
757.0
nM
|
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
205.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
68.0
nM
|
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
169.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
57.0
nM
|
|
|
Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay
|
Astrosclera willeyana
|
378.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method
|
Cryptococcus neoformans
|
812.0
nM
|
|
|
Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method
|
Candida albicans
|
760.0
nM
|
|
|
Inhibition 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 method
|
Malassezia globosa CBS 7966
|
320.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Trypanosoma cruzi CL Brener recombinant alpha-carbonic anhydrase expressed in insect Sf9 cell Baculovirus system by stopped flow CO2 hydration assay
|
Trypanosoma cruzi
|
87.9
nM
|
|
|
Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay
|
Candida glabrata
|
113.0
nM
|
|
|
Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 recombinant carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay
|
Sulfurihydrogenibium yellowstonense
|
67.4
nM
|
|
|
Inhibition of Helicobacter pylori recombinant alpha carbonic anhydrase preincubated for 15 mins by CO2 hydration stopped-flow assay
|
Helicobacter pylori
|
204.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition 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 assay
|
Homo sapiens
|
3.9
nM
|
|
|
Inhibition 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 assay
|
Homo sapiens
|
46.0
nM
|
|
|
Inhibition 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 assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
121.78
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
106.19
%
|
|
|
Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay
|
Thalassiosira weissflogii
|
259.0
nM
|
|
|
Inhibition of Porphyromonas gingivalis recombinant gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay
|
Porphyromonas gingivalis
|
418.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Porphyromonas gingivalis gamma-carbonic anhydrase expressed in Escherichia coli preincubated for 15 mins by stopped flow CO2 hydration assay
|
Porphyromonas gingivalis
|
418.0
nM
|
|
|
Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
3.9
nM
|
|
|
Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
46.0
nM
|
|
|
Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Antagonist activity at dopamine D2 receptor (unknown origin)
|
Homo sapiens
|
7.6
nM
|
|
|
Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-1 assessed as CO2 hydrase activity by stopped-flow assay
|
Legionella pneumophila subsp. pneumophila str. Philadelphia 1
|
253.0
nM
|
|
|
Inhibition of Legionella pneumophilia subsp. Pneumophila strain Philadelphia-1 carbonic anhydrase-2 assessed as CO2 hydrase activity by stopped-flow assay
|
Legionella pneumophila subsp. pneumophila str. Philadelphia 1
|
245.0
nM
|
|
|
Inhibition of Helicobacter pylori carbonic anhydrase by stopped-flow CO2 hydration assay
|
Helicobacter pylori
|
35.0
nM
|
|
|
Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Helicobacter pylori Beta-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method
|
Helicobacter pylori
|
35.0
nM
|
|
|
Inhibition of Porphyromonas gingivalis Gamma-carbonic anhydrase compound preincubated for 15 mins by stopped flow CO2 hydrase assay method
|
Porphyromonas gingivalis
|
418.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of recombinant Porphyromonas gingivalis gamma-carbonic anhydrase by stopped flow CO2 hydrase assay
|
Porphyromonas gingivalis
|
418.0
nM
|
|
|
Inhibition of recombinant Nostoc commune gamma-carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydrase assay
|
Nostoc commune
|
60.5
nM
|
|
|
Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay
|
Anopheles gambiae
|
29.5
nM
|
|
|
Inhibition of Nostoc commune gamma carbonic anhydrase by CO2 hydration assay
|
Nostoc commune
|
60.5
nM
|
|
|
Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Chionodraco hamatus alphaCA incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay
|
Chionodraco hamatus
|
511.0
nM
|
|
|
Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay
|
Sulfurihydrogenibium yellowstonense
|
67.4
nM
|
|
|
Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay
|
Thiomicrospira crunogena XCL-2
|
873.0
nM
|
|
|
Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Porphyromonas gingivalis gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay
|
Porphyromonas gingivalis
|
418.0
nM
|
|
|
Inhibition of Nostoc commune gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay
|
Nostoc commune
|
60.5
nM
|
|
|
Inhibition of recombinant Colwellia psychrerythraea gamma carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay
|
Colwellia psychrerythraea
|
505.0
nM
|
|
|
Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of recombinant Enterobacter sp. B13 beta carbonic anhydrase incubated for 15 mins by stopped-flow CO2 hydration assay
|
Enterobacter sp.
|
132.0
nM
|
|
|
Inhibition of recombinant Vibrio cholerae gamma-carbonic anhydrase preincubated for 15 mins by stopped-flow CO2 hydration assay
|
Vibrio cholerae
|
77.9
nM
|
|
|
Inhibition 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
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition 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
|
Vibrio cholerae
|
77.9
nM
|
|
|
Inhibition 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
|
Homo sapiens
|
40.0
nM
|
|
|
Competitive antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as induction of rightward shift in the dopamine dose response curve for beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
|
Homo sapiens
|
39.81
nM
|
|
|
Competitive antagonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay
|
Homo sapiens
|
2.818
nM
|
|
|
Displacement of [3H]-sulpiride from human D3 receptor expressed in HEK293 cells at 100 nM after 150 mins by liquid scintillation counting method relative to control
|
Homo sapiens
|
87.9
%
|
|
|
Displacement of [3H]-sulpiride from human D2 receptor expressed in HEK293 cells at 100 nM after 150 mins by liquid scintillation counting method relative to control
|
Homo sapiens
|
92.2
%
|
|
|
Antagonist activity at human D2R expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 120 mins by beta-galactosidase based PathHunter assay
|
Homo sapiens
|
42.0
nM
|
|
|
Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of Vibrio cholerae beta carbonic anhydrase pre-incubated for 15 mins prior to testing by phenol red-based stopped-flow CO2 hydration assay
|
Vibrio cholerae
|
68.0
nM
|
|
