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Assay Detail

CHEMBL5235572

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

Binding
Binding affinity to human recombinant GABAA alpha6 receptor assessed as inhibition constant incubated for 1 hrs by liquid scintillation counting analysis
21
Total Activities
21
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-6 (CHEMBL2579)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Beato A, Gori A, Boucherle B, Peuchmaur M, Haudecoeur R.
J Med Chem (2021) 64 : 1392 -1422
PubMed 33528252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.91 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5275690 1 7.12
CHEMBL5290579 1 6.89
CHEMBL5280240 1 6.32
CHEMBL5266498 1 5.92
CHEMBL49141 1 5.89
CHEMBL1270038 1 5.70
CHEMBL454606 1 5.57
CHEMBL5290464 1 5.52
CHEMBL1270841 1 5.52
CHEMBL453066 BETA-CCM 1 5.36
CHEMBL454095 ABECARNIL 2.0 1 5.19
CHEMBL5281056 1 -
CHEMBL2008708 1 -
CHEMBL497197 1 -
CHEMBL496990 1 -
CHEMBL301605 1 -
CHEMBL1518572 1 -
CHEMBL5290746 1 -
CHEMBL499814 1 -
CHEMBL510764 1 -
CHEMBL509197 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5275690 Ki = 75.0 nM 7.12
CHEMBL5290579 Ki = 130.0 nM 6.89
CHEMBL5280240 Ki = 480.0 nM 6.32
CHEMBL5266498 Ki = 1200.0 nM 5.92
CHEMBL49141 Ki = 1300.0 nM 5.89
CHEMBL1270038 Ki = 2000.0 nM 5.70
CHEMBL454606 Ki = 2700.0 nM 5.57
CHEMBL5290464 Ki = 3000.0 nM 5.52
CHEMBL1270841 Ki = 3000.0 nM 5.52
CHEMBL453066 BETA-CCM Ki = 4400.0 nM 5.36
CHEMBL454095 ABECARNIL Ki = 6400.0 nM 5.19
CHEMBL5281056 Ki > 10000.0 nM -
CHEMBL2008708 Ki > 10000.0 nM -
CHEMBL497197 Ki > 10000.0 nM -
CHEMBL496990 Ki > 10000.0 nM -
CHEMBL301605 Ki > 1000.0 nM -
CHEMBL1518572 Ki > 1000.0 nM -
CHEMBL5290746 Ki > 10000.0 nM -
CHEMBL499814 Ki > 1000.0 nM -
CHEMBL510764 Ki > 3000.0 nM -
CHEMBL509197 Ki > 5000.0 nM -