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Assay Detail

CHEMBL2317358

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human MAOA after 1 hr by luminescence assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] A (CHEMBL1951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.
Rivara S, Piersanti G, Bartoccini F, Diamantini G, Pala D, Riccioni T, Stasi MA, Cabri W, Borsini F, Mor M, Tarzia G, Minetti P.
J Med Chem (2013) 56 : 1247 -1261
PubMed 23281824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.88 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8706 CLORGILINE 2.0 1 7.91
CHEMBL2312981 1 6.14
CHEMBL2313296 1 6.09
CHEMBL2313294 1 5.91
CHEMBL2312988 1 5.89
CHEMBL2312989 1 5.79
CHEMBL2313286 1 5.69
CHEMBL2312975 1 5.54
CHEMBL2313291 1 5.51
CHEMBL2313295 1 5.25
CHEMBL2313297 1 5.00
CHEMBL2313285 1 -
CHEMBL2313284 1 -
CHEMBL2313279 1 -
CHEMBL2313277 1 -
CHEMBL2312987 1 -
CHEMBL2313298 1 -
CHEMBL2312976 1 -
CHEMBL2313292 1 -
CHEMBL2312977 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8706 CLORGILINE IC50 = 12.4 nM 7.91
CHEMBL2312981 IC50 = 726.3 nM 6.14
CHEMBL2313296 IC50 = 812.3 nM 6.09
CHEMBL2313294 IC50 = 1237.0 nM 5.91
CHEMBL2312988 IC50 = 1300.0 nM 5.89
CHEMBL2312989 IC50 = 1632.0 nM 5.79
CHEMBL2313286 IC50 = 2022.0 nM 5.69
CHEMBL2312975 IC50 = 2870.0 nM 5.54
CHEMBL2313291 IC50 = 3110.0 nM 5.51
CHEMBL2313295 IC50 = 5690.0 nM 5.25
CHEMBL2313297 IC50 = 10000.0 nM 5.00
CHEMBL2313285 IC50 > 10000.0 nM -
CHEMBL2313284 IC50 > 10000.0 nM -
CHEMBL2313279 IC50 > 10000.0 nM -
CHEMBL2313277 IC50 > 10000.0 nM -
CHEMBL2312987 IC50 > 1000.0 nM -
CHEMBL2313298 IC50 > 10000.0 nM -
CHEMBL2312976 IC50 > 10000.0 nM -
CHEMBL2313292 IC50 > 10000.0 nM -
CHEMBL2312977 IC50 > 10000.0 nM -