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Assay Detail

CHEMBL680687

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

Binding
In vitro binding affinity to the Gamma-aminobutyric acid A receptor complex in absence of GABA in rat cerebellum tissue
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

gamma-Aminobutyrate-A receptor modulation by 3-aryl-1-(arylsulfonyl)- 1,4,5,6-tetrahydropyridazines.
Rybczynski PJ, Combs DW, Jacobs K, Shank RP, Dubinsky B.
J Med Chem (1999) 42 : 2403 -2408
PubMed 10395481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.41 5.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76367 1 5.95
CHEMBL78307 1 5.86
CHEMBL82083 1 5.70
CHEMBL207538 BREXANOLONE 4.0 1 5.58
CHEMBL79029 1 5.58
CHEMBL1256760 1 5.52
CHEMBL76738 1 5.42
CHEMBL79238 1 5.27
CHEMBL79231 1 5.08
CHEMBL78599 1 5.00
CHEMBL309204 1 5.00
CHEMBL311213 1 5.00
CHEMBL80685 1 -
CHEMBL80518 1 -
CHEMBL312660 1 -
CHEMBL312265 1 -
CHEMBL311927 1 -
CHEMBL78483 1 -
CHEMBL78695 1 -
CHEMBL78461 1 -
CHEMBL79273 1 -
CHEMBL78422 1 -
CHEMBL79384 1 -
CHEMBL82476 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76367 IC50 = 1120.0 nM 5.95
CHEMBL78307 IC50 = 1390.0 nM 5.86
CHEMBL82083 IC50 = 2000.0 nM 5.70
CHEMBL207538 BREXANOLONE IC50 = 2610.0 nM 5.58
CHEMBL79029 IC50 = 2610.0 nM 5.58
CHEMBL1256760 IC50 = 3050.0 nM 5.52
CHEMBL76738 IC50 = 3770.0 nM 5.42
CHEMBL79238 IC50 = 5400.0 nM 5.27
CHEMBL79231 IC50 = 8300.0 nM 5.08
CHEMBL78599 IC50 = 10000.0 nM 5.00
CHEMBL309204 IC50 = 10000.0 nM 5.00
CHEMBL311213 IC50 = 10000.0 nM 5.00
CHEMBL80685 IC50 > 11000.0 nM -
CHEMBL80518 IC50 > 11000.0 nM -
CHEMBL312660 IC50 > 11000.0 nM -
CHEMBL312265 IC50 > 11000.0 nM -
CHEMBL311927 IC50 > 11000.0 nM -
CHEMBL78483 IC50 > 11000.0 nM -
CHEMBL78695 IC50 > 11000.0 nM -
CHEMBL78461 IC50 > 11000.0 nM -
CHEMBL79273 IC50 > 11000.0 nM -
CHEMBL78422 IC50 > 11000.0 nM -
CHEMBL79384 IC50 > 11000.0 nM -
CHEMBL82476 IC50 > 11000.0 nM -