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

CHEMBL650071

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 brain cortical membranes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors.
Cox ED, Diaz-Arauzo H, Huang Q, Reddy MS, Ma C, Harris B, McKernan R, Skolnick P, Cook JM.
J Med Chem (1998) 41 : 2537 -2552
PubMed 9651158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.33 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10483 1 9.00
CHEMBL1518572 1 9.00
CHEMBL49141 1 8.09
CHEMBL87437 1 7.86
CHEMBL273464 1 7.66
CHEMBL85068 1 7.61
CHEMBL82736 1 7.51
CHEMBL83464 1 7.40
CHEMBL83581 1 7.37
CHEMBL87538 1 7.26
CHEMBL440880 1 7.20
CHEMBL84757 1 6.75
CHEMBL85808 1 6.57
CHEMBL420044 1 6.54
CHEMBL84668 1 6.48
CHEMBL84921 1 6.16
CHEMBL87743 1 6.14
CHEMBL85716 1 -
CHEMBL10701 1 -
CHEMBL314788 1 -
CHEMBL84842 1 -
CHEMBL87640 1 -
CHEMBL10638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10483 IC50 = 1.0 nM 9.00
CHEMBL1518572 IC50 = 1.0 nM 9.00
CHEMBL49141 IC50 = 8.1 nM 8.09
CHEMBL87437 IC50 = 13.9 nM 7.86
CHEMBL273464 IC50 = 22.0 nM 7.66
CHEMBL85068 IC50 = 24.7 nM 7.61
CHEMBL82736 IC50 = 30.8 nM 7.51
CHEMBL83464 IC50 = 40.0 nM 7.40
CHEMBL83581 IC50 = 43.2 nM 7.37
CHEMBL87538 IC50 = 55.5 nM 7.26
CHEMBL440880 IC50 = 63.8 nM 7.20
CHEMBL84757 IC50 = 176.0 nM 6.75
CHEMBL85808 IC50 = 271.4 nM 6.57
CHEMBL420044 IC50 = 290.0 nM 6.54
CHEMBL84668 IC50 = 330.0 nM 6.48
CHEMBL84921 IC50 = 697.0 nM 6.16
CHEMBL87743 IC50 = 730.0 nM 6.14
CHEMBL85716 IC50 > 1000.0 nM -
CHEMBL10701 IC50 > 5000.0 nM -
CHEMBL314788 IC50 > 1000.0 nM -
CHEMBL84842 IC50 > 1000.0 nM -
CHEMBL87640 IC50 > 1000.0 nM -
CHEMBL10638 IC50 > 5000.0 nM -