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Assay Detail

CHEMBL652360

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

Binding
Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cerebral cortex membrane
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics.
Tomczuk BE, Taylor CR, Moses LM, Sutherland DB, Lo YS, Johnson DN, Kinnier WB, Kilpatrick BF.
J Med Chem (1991) 34 : 2993 -3006
PubMed 1681105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 5.76 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101304 1 6.82
CHEMBL103827 1 6.70
CHEMBL101192 1 6.51
CHEMBL319567 1 6.42
CHEMBL321129 1 6.34
CHEMBL317415 1 6.33
CHEMBL103835 1 6.17
CHEMBL451 CHLORDIAZEPOXIDE 4.0 1 6.15
CHEMBL102298 1 6.06
CHEMBL101329 1 6.05
CHEMBL328386 1 5.80
CHEMBL322460 1 5.76
CHEMBL99696 1 5.75
CHEMBL328407 1 5.60
CHEMBL101115 1 5.57
CHEMBL100897 1 5.57
CHEMBL327961 1 5.57
CHEMBL319146 1 5.44
CHEMBL319426 1 5.39
CHEMBL101169 1 5.35
CHEMBL319320 1 5.29
CHEMBL103453 1 5.28
CHEMBL318094 1 5.19
CHEMBL328169 1 5.14
CHEMBL103699 1 5.10
CHEMBL100866 1 5.07
CHEMBL330418 1 5.03
CHEMBL103793 1 -
CHEMBL320617 1 -
CHEMBL319785 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101304 IC50 = 150.0 nM 6.82
CHEMBL103827 IC50 = 200.0 nM 6.70
CHEMBL101192 IC50 = 310.0 nM 6.51
CHEMBL319567 IC50 = 380.0 nM 6.42
CHEMBL321129 IC50 = 460.0 nM 6.34
CHEMBL317415 IC50 = 470.0 nM 6.33
CHEMBL103835 IC50 = 680.0 nM 6.17
CHEMBL451 CHLORDIAZEPOXIDE IC50 = 710.0 nM 6.15
CHEMBL102298 IC50 = 880.0 nM 6.06
CHEMBL101329 IC50 = 900.0 nM 6.05
CHEMBL328386 IC50 = 1600.0 nM 5.80
CHEMBL322460 IC50 = 1750.0 nM 5.76
CHEMBL99696 IC50 = 1800.0 nM 5.75
CHEMBL328407 IC50 = 2500.0 nM 5.60
CHEMBL327961 IC50 = 2700.0 nM 5.57
CHEMBL100897 IC50 = 2700.0 nM 5.57
CHEMBL101115 IC50 = 2700.0 nM 5.57
CHEMBL319146 IC50 = 3600.0 nM 5.44
CHEMBL319426 IC50 = 4100.0 nM 5.39
CHEMBL101169 IC50 = 4500.0 nM 5.35
CHEMBL319320 IC50 = 5100.0 nM 5.29
CHEMBL103453 IC50 = 5200.0 nM 5.28
CHEMBL318094 IC50 = 6400.0 nM 5.19
CHEMBL328169 IC50 = 7200.0 nM 5.14
CHEMBL103699 IC50 = 8000.0 nM 5.10
CHEMBL100866 IC50 = 8500.0 nM 5.07
CHEMBL330418 IC50 = 9300.0 nM 5.03
CHEMBL100959 IC50 > 10000.0 nM -
CHEMBL103244 IC50 > 10000.0 nM -
CHEMBL328610 IC50 > 10000.0 nM -
CHEMBL318983 IC50 > 10000.0 nM -
CHEMBL432004 IC50 > 10000.0 nM -
CHEMBL329036 IC50 > 10000.0 nM -
CHEMBL422070 IC50 > 10000.0 nM -
CHEMBL101065 IC50 > 10000.0 nM -
CHEMBL103166 IC50 > 10000.0 nM -
CHEMBL321305 IC50 > 10000.0 nM -
CHEMBL323347 IC50 > 10000.0 nM -
CHEMBL2111615 IC50 > 10000.0 nM -
CHEMBL319621 IC50 > 10000.0 nM -
CHEMBL100816 IC50 > 10000.0 nM -
CHEMBL327940 IC50 > 10000.0 nM -
CHEMBL103198 IC50 > 10000.0 nM -
CHEMBL102485 IC50 > 10000.0 nM -
CHEMBL103717 IC50 > 10000.0 nM -
CHEMBL100864 IC50 > 10000.0 nM -
CHEMBL321805 IC50 > 10000.0 nM -
CHEMBL319785 IC50 > 10000.0 nM -
CHEMBL320617 IC50 > 10000.0 nM -
CHEMBL103793 IC50 > 10000.0 nM -