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Assay Detail

CHEMBL681618

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

Binding
Apparent affinity by displacement of pre-incubated [35S]-TBPS from rat cortical homogenates at 600 nM
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel site-directed affinity ligands for GABA-gated chloride channels: synthesis, characterization, and molecular modeling of 1-(isothiocyanatophenyl)-4-tert-butyl-2,6,7-trioxabicyclo[2.2.2]octanes .
de Costa BR, Lewin AH, Rice KC, Skolnick P, Schoenheimer JA.
J Med Chem (1991) 34 : 1531 -1538
PubMed 2033577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 7.30 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39302 1 7.35
CHEMBL39353 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39302 Kd = 44.5 nM 7.35
CHEMBL39353 Kd = 57.3 nM 7.24