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Assay Detail

CHEMBL4403720

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Binding
Binding affinity to GABA-A alpha5 (unknown origin)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gamma-aminobutyric acid receptor subunit alpha-5 (CHEMBL5112)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABA<sub>A</sub>R) Modulators Acting at the Benzodiazepine Binding Site: An Update.
Maramai S, Benchekroun M, Ward SE, Atack JR.
J Med Chem (2020) 63 : 3425 -3446
PubMed 31738537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.76 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306422 1 9.18
CHEMBL204696 1 8.96
CHEMBL363211 1 8.85
CHEMBL1077391 1 8.70
CHEMBL1080588 1 8.34
CHEMBL3681419 BASMISANIL 2.0 1 8.33
CHEMBL45346 1 8.22
CHEMBL4581355 1 8.10
CHEMBL12 DIAZEPAM 4.0 1 7.82
CHEMBL4228824 1 7.26
CHEMBL4553352 1 7.10
CHEMBL1783282 AZD7325 2.0 1 6.64
CHEMBL1783256 AZD6280 1.0 1 5.78
CHEMBL4537552 1 5.30
CHEMBL4441634 1 -
CHEMBL4537371 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306422 Ki = 0.66 nM 9.18
CHEMBL204696 Ki = 1.1 nM 8.96
CHEMBL363211 Ki = 1.4 nM 8.85
CHEMBL1077391 Ki = 2.0 nM 8.70
CHEMBL1080588 Ki = 4.6 nM 8.34
CHEMBL3681419 BASMISANIL Ki = 4.7 nM 8.33
CHEMBL45346 Ki = 6.0 nM 8.22
CHEMBL4581355 Ki = 7.9 nM 8.10
CHEMBL12 DIAZEPAM Ki = 15.0 nM 7.82
CHEMBL4228824 Ki = 55.0 nM 7.26
CHEMBL4553352 Ki = 79.0 nM 7.10
CHEMBL1783282 AZD7325 Ki = 230.0 nM 6.64
CHEMBL1783256 AZD6280 Ki = 1680.0 nM 5.78
CHEMBL4537552 Ki = 5000.0 nM 5.30
CHEMBL4441634 Ki - -
CHEMBL4537371 Ki - -