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Assay Detail

CHEMBL653130

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

Binding
In vitro inhibition of [3H]diazepam binding to rat cerebral cortical membrane benzodiazepine receptors
24
Total Activities
22
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

Biomimetic approach to potential benzodiazepine receptor agonists and antagonists.
Guzman F, Cain M, Larscheid P, Hagen T, Cook JM, Schweri M, Skolnick P, Paul SM.
J Med Chem (1984) 27 : 564 -570
PubMed 6325688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 5.18 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307061 1 7.00
CHEMBL11709 1 6.00
CHEMBL453066 BETA-CCM 1 6.00
CHEMBL273491 1 5.41
CHEMBL153069 1 5.00
CHEMBL156897 CANTHIN-6-ONE 1 5.00
CHEMBL154343 1 5.00
CHEMBL346663 1 4.95
CHEMBL416152 1 4.88
CHEMBL152492 1 4.50
CHEMBL11863 1 4.24
CHEMBL346218 1 4.17
CHEMBL154573 1 -
CHEMBL152548 1 -
CHEMBL440184 1 -
CHEMBL417982 1 -
CHEMBL154813 1 -
CHEMBL346949 1 -
CHEMBL152662 1 -
CHEMBL357950 2 -
CHEMBL273939 1 -
CHEMBL152566 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307061 Ki = 100.0 nM 7.00
CHEMBL453066 BETA-CCM Ki = 1000.0 nM 6.00
CHEMBL11709 Ki = 1000.0 nM 6.00
CHEMBL273491 Ki = 3890.0 nM 5.41
CHEMBL153069 Ki = 10000.0 nM 5.00
CHEMBL156897 CANTHIN-6-ONE Ki = 10000.0 nM 5.00
CHEMBL154343 Ki = 10000.0 nM 5.00
CHEMBL346663 Ki = 11200.0 nM 4.95
CHEMBL416152 Ki = 13200.0 nM 4.88
CHEMBL152492 Ki = 32000.0 nM 4.50
CHEMBL11863 Ki = 58000.0 nM 4.24
CHEMBL346218 Ki = 68000.0 nM 4.17
CHEMBL152566 Ki > 50000.0 nM -
CHEMBL273939 Ki > 50000.0 nM -
CHEMBL357950 Ki > 50000.0 nM -
CHEMBL152662 Ki > 50000.0 nM -
CHEMBL154573 Ki > 50000.0 nM -
CHEMBL346949 Ki > 50000.0 nM -
CHEMBL152566 Ki > 50000.0 nM -
CHEMBL417982 Ki = 1470000.0 nM -
CHEMBL357950 Ki > 50000.0 nM -
CHEMBL440184 Ki = 750000.0 nM -
CHEMBL152548 Ki > 50000.0 nM -
CHEMBL154813 Ki > 50000.0 nM -