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Literature summary for 1.4.3.4 extracted from

  • Tzvetkov, N.T.; Stammler, H.G.; Neumann, B.; Hristova, S.; Antonov, L.; Gastreich, M.
    Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors (2017), Eur. J. Med. Chem., 127, 470-492 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
Clorgyline irreversible inhibitor of isoform MAO-A Homo sapiens
Clorgyline irreversible inhibitor of isoform MAO-A Rattus norvegicus
moclobemide reversible inhibitor of isoform MAO-A Homo sapiens
moclobemide reversible inhibitor of isoform MAO-A Rattus norvegicus
N-(3,4-dichlorophenyl)-1-(2-methoxyethyl)-1H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-dichlorophenyl)-1-(2-methoxyethyl)-1H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3,4-dichlorophenyl)-2-methyl-2H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-dichlorophenyl)-2-methyl-2H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3,4-difluorophenyl)-1-methyl-1H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-difluorophenyl)-1-methyl-1H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3,4-difluorophenyl)-1H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-difluorophenyl)-1H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3,4-difluorophenyl)-2-methyl-2H-indazole-5-carboxamide
-
Homo sapiens
N-(3,4-difluorophenyl)-2-methyl-2H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide NTZ-1441; NTZ-1441 Homo sapiens
N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide NTZ-1441; NTZ-1441 Rattus norvegicus
N-(3-chloro-4-fluorophenyl)-1H-indazole-5-carboxamide
-
Homo sapiens
N-(3-chloro-4-fluorophenyl)-1H-indazole-5-carboxamide
-
Rattus norvegicus
N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide NTZ-1442; NTZ-1442 Homo sapiens
N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide NTZ-1442; NTZ-1442 Rattus norvegicus
N-phenyl-1H-indazole-5-carboxamide
-
Homo sapiens
N-phenyl-1H-indazole-5-carboxamide
-
Rattus norvegicus
rasagiline irreversible inhibitor of isoform MAO-B Homo sapiens
rasagiline irreversible inhibitor of isoform MAO-B Rattus norvegicus
safinamide reversible inhibitor of isoform MAO-B Homo sapiens
safinamide reversible inhibitor of isoform MAO-B Rattus norvegicus
selegiline irreversible inhibitor of isoform MAO-B Homo sapiens
selegiline irreversible inhibitor of isoform MAO-B Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens P21397
-
-
Homo sapiens P27338
-
-
Rattus norvegicus P19643
-
-
Rattus norvegicus P21396
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Homo sapiens
-
brain
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-tyramine + H2O + O2
-
Homo sapiens 2-(4-hydroxyphenyl)acetaldehyde + NH3 + H2O2
-
?
4-tyramine + H2O + O2
-
Rattus norvegicus 2-(4-hydroxyphenyl)acetaldehyde + NH3 + H2O2
-
?

Synonyms

Synonyms Comment Organism
MAO-A
-
Homo sapiens
MAO-A
-
Rattus norvegicus
MAO-B
-
Homo sapiens
MAO-B
-
Rattus norvegicus
monoamine oxidase A
-
Homo sapiens
monoamine oxidase A
-
Rattus norvegicus
monoamine oxidase B
-
Homo sapiens
monoamine oxidase B
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000000386
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.000000586
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide
0.000000679
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3-chloro-4-fluorophenyl)-1H-indazole-5-carboxamide
0.00000108
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-1-(2-methoxyethyl)-1H-indazole-5-carboxamide
0.00000132
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.00000143
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide
0.00000144
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.00000152
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-difluorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.00000159
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-difluorophenyl)-1H-indazole-5-carboxamide
0.00000236
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chloro-4-fluorophenyl)-1H-indazole-5-carboxamide
0.00000382
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-1-(2-methoxyethyl)-1H-indazole-5-carboxamide
0.00000565
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.00000889
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-1H-indazole-5-carboxamide
0.0000225
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.0000384
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-difluorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.000117
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-phenyl-1H-indazole-5-carboxamide
0.000221
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.00042
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.000662
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.000708
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-phenyl-1H-indazole-5-carboxamide
0.00136
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.00174
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.00188
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.00287
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-1-(2-methoxyethyl)-1H-indazole-5-carboxamide
0.00518
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens safinamide
0.00764
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-difluorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.00808
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-phenyl-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-phenyl-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3-chloro-4-fluorophenyl)-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chloro-4-fluorophenyl)-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-difluorophenyl)-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3,4-difluorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-difluorophenyl)-1-methyl-1H-indazole-5-carboxamide
0.01
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3,4-dichlorophenyl)-1-(2-methoxyethyl)-1H-indazole-5-carboxamide
0.018
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus safinamide
0.361
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens moclobemide
0.708
-
isoform MAO-B, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide
1.69
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide
10
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide
10
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide
10
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide
10.7
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus moclobemide
45
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Homo sapiens safinamide
580
-
isoform MAO-A, at pH 7.4, temperature not specified in the publication Rattus norvegicus safinamide