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Assay Detail

CHEMBL681272

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

Binding
Inhibition of [3H]muscimol binding to GABA A receptor 4-biphenylacetic acid at 10 e-4 M
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
Araki K, Kuroda T, Uemori S, Moriguchi A, Ikeda Y, Hirayama F, Yokoyama Y, Iwao E, Yakushiji T.
J Med Chem (1993) 36 : 1356 -1363
PubMed 8388467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.49 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9 NORFLOXACIN 4.0 1 7.70
CHEMBL15549 1 6.92
CHEMBL8 CIPROFLOXACIN 4.0 1 6.39
CHEMBL4 OFLOXACIN 4.0 1 4.96
CHEMBL29929 1 -
CHEMBL28858 1 -
CHEMBL27345 1 -
CHEMBL29572 1 -
CHEMBL26523 1 -
CHEMBL282127 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9 NORFLOXACIN IC50 = 20.0 nM 7.70
CHEMBL15549 IC50 = 120.0 nM 6.92
CHEMBL8 CIPROFLOXACIN IC50 = 410.0 nM 6.39
CHEMBL4 OFLOXACIN IC50 = 11000.0 nM 4.96
CHEMBL29929 IC50 > 100000.0 nM -
CHEMBL28858 IC50 > 100000.0 nM -
CHEMBL27345 IC50 > 100000.0 nM -
CHEMBL29572 IC50 > 100000.0 nM -
CHEMBL26523 IC50 > 100000.0 nM -
CHEMBL282127 IC50 > 100000.0 nM -