Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL650999

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

Binding
Displacement of [3H]flunitrazepam from diazepam-sensitive GABA-A benzodiazepine receptor of rat cortical membrane
23
Total Activities
23
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

Synthesis and structure-activity relationships of 3,5-disubstituted 4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-ones at diazepam-sensitive and diazepam-insensitive benzodiazepine receptors.
Ananthan S, Clayton SD, Ealick SE, Wong G, Evoniuk GE, Skolnick P.
J Med Chem (1993) 36 : 479 -490
PubMed 8386247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.16 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54069 1 8.62
CHEMBL267665 RO-147437 1 8.52
CHEMBL301513 1 8.03
CHEMBL300027 1 7.82
CHEMBL145300 1 7.63
CHEMBL53119 1 7.46
CHEMBL52934 1 7.42
CHEMBL51740 1 6.80
CHEMBL356583 1 6.79
CHEMBL148068 1 6.62
CHEMBL145431 1 6.50
CHEMBL53425 1 6.47
CHEMBL144497 1 6.47
CHEMBL143502 1 6.16
CHEMBL358734 1 6.13
CHEMBL358804 1 -
CHEMBL356721 1 -
CHEMBL357180 1 -
CHEMBL144266 1 -
CHEMBL358820 1 -
CHEMBL144655 1 -
CHEMBL436072 1 -
CHEMBL291473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54069 IC50 = 2.4 nM 8.62
CHEMBL267665 RO-147437 IC50 = 3.0 nM 8.52
CHEMBL301513 IC50 = 9.3 nM 8.03
CHEMBL300027 IC50 = 15.3 nM 7.82
CHEMBL145300 IC50 = 23.2 nM 7.63
CHEMBL53119 IC50 = 34.3 nM 7.46
CHEMBL52934 IC50 = 37.8 nM 7.42
CHEMBL51740 IC50 = 157.0 nM 6.80
CHEMBL356583 IC50 = 164.0 nM 6.79
CHEMBL148068 IC50 = 238.0 nM 6.62
CHEMBL145431 IC50 = 317.0 nM 6.50
CHEMBL53425 IC50 = 338.0 nM 6.47
CHEMBL144497 IC50 = 340.0 nM 6.47
CHEMBL143502 IC50 = 687.0 nM 6.16
CHEMBL358734 IC50 = 739.0 nM 6.13
CHEMBL358804 IC50 > 1000.0 nM -
CHEMBL356721 IC50 > 1000.0 nM -
CHEMBL357180 IC50 > 1000.0 nM -
CHEMBL144266 IC50 > 1000.0 nM -
CHEMBL358820 IC50 > 1000.0 nM -
CHEMBL144655 IC50 > 1000.0 nM -
CHEMBL436072 IC50 > 1000.0 nM -
CHEMBL291473 IC50 > 1000.0 nM -