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Assay Detail

CHEMBL948526

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

Binding
Binding affinity to GABAA alpha-1-beta-3-gamma-2 receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
Harris D, Clayton T, Cook J, Sahbaie P, Halliwell RF, Furtmüller R, Huck S, Sieghart W, DeLorey TM.
J Med Chem (2008) 51 : 3788 -3803
PubMed 18537233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.68 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415290 Ro-151310 1 8.17
CHEMBL458319 1 7.79
CHEMBL458147 1 7.76
CHEMBL58757 1 7.57
CHEMBL471978 1 7.55
CHEMBL471977 1 6.71
CHEMBL458321 1 6.39
CHEMBL461511 1 6.30
CHEMBL459031 1 6.30
CHEMBL45346 1 6.04
CHEMBL511685 1 5.80
CHEMBL471115 1 5.69
CHEMBL458320 1 4.76
CHEMBL510963 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415290 Ro-151310 Ki = 6.8 nM 8.17
CHEMBL458319 Ki = 16.4 nM 7.79
CHEMBL458147 Ki = 17.3 nM 7.76
CHEMBL58757 Ki = 26.9 nM 7.57
CHEMBL471978 Ki = 28.4 nM 7.55
CHEMBL471977 Ki = 197.0 nM 6.71
CHEMBL458321 Ki = 408.0 nM 6.39
CHEMBL461511 Ki = 500.0 nM 6.30
CHEMBL459031 Ki = 500.0 nM 6.30
CHEMBL45346 Ki = 920.0 nM 6.04
CHEMBL511685 Ki = 1580.0 nM 5.80
CHEMBL471115 Ki = 2050.0 nM 5.69
CHEMBL458320 Ki = 17500.0 nM 4.76
CHEMBL510963 Ki > 300.0 nM -