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Assay Detail

CHEMBL652557

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

Binding
In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat
15
Total Activities
15
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 anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
Albright JD, Moran DB, Wright WB, Collins JB, Beer B, Lippa AS, Greenblatt EN.
J Med Chem (1981) 24 : 592 -600
PubMed 6113284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.34 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12 DIAZEPAM 4.0 1 8.22
CHEMBL13662 CI-218872 1 6.94
CHEMBL451 CHLORDIAZEPOXIDE 4.0 1 6.61
CHEMBL157884 1 6.55
CHEMBL155571 1 6.51
CHEMBL347033 1 6.41
CHEMBL155179 1 6.29
CHEMBL347801 1 6.23
CHEMBL153823 1 6.20
CHEMBL155598 1 6.20
CHEMBL346817 1 6.15
CHEMBL157522 1 6.04
CHEMBL155215 1 5.92
CHEMBL352028 1 5.65
CHEMBL347965 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12 DIAZEPAM IC50 = 6.0 nM 8.22
CHEMBL13662 CI-218872 IC50 = 116.0 nM 6.94
CHEMBL451 CHLORDIAZEPOXIDE IC50 = 248.0 nM 6.61
CHEMBL157884 IC50 = 280.0 nM 6.55
CHEMBL155571 IC50 = 309.0 nM 6.51
CHEMBL347033 IC50 = 391.0 nM 6.41
CHEMBL155179 IC50 = 510.0 nM 6.29
CHEMBL347801 IC50 = 589.0 nM 6.23
CHEMBL153823 IC50 = 633.0 nM 6.20
CHEMBL155598 IC50 = 633.0 nM 6.20
CHEMBL346817 IC50 = 709.0 nM 6.15
CHEMBL157522 IC50 = 905.0 nM 6.04
CHEMBL155215 IC50 = 1200.0 nM 5.92
CHEMBL352028 IC50 = 2250.0 nM 5.65
CHEMBL347965 IC50 = 7450.0 nM 5.13