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Assay Detail

CHEMBL5235566

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

Binding
Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2093872)
Type PROTEIN COMPLEX GROUP
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
IC50 25 8.34 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747460 1 9.70
CHEMBL1271047 1 9.40
CHEMBL1518572 1 9.30
CHEMBL49141 1 9.30
CHEMBL5280240 1 9.30
CHEMBL5290464 1 9.30
CHEMBL5266498 1 9.30
CHEMBL454095 ABECARNIL 2.0 1 9.00
CHEMBL453066 BETA-CCM 1 9.00
CHEMBL454606 1 9.00
CHEMBL1337028 1 9.00
CHEMBL509197 1 9.00
CHEMBL5266558 1 8.52
CHEMBL510764 1 8.52
CHEMBL2262044 1 8.52
CHEMBL499814 1 8.52
CHEMBL5276119 1 8.40
CHEMBL5290746 1 8.40
CHEMBL457794 1 6.12
CHEMBL275224 NORHARMANE 1 5.80
CHEMBL12014 HARMAN 1 5.60
CHEMBL1972187 1 4.51
CHEMBL129208 1 -
CHEMBL340807 HARMALINE 1 -
CHEMBL269538 HARMINE 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747460 IC50 = 0.2 nM 9.70
CHEMBL1271047 IC50 = 0.4 nM 9.40
CHEMBL1518572 IC50 = 0.5 nM 9.30
CHEMBL49141 IC50 = 0.5 nM 9.30
CHEMBL5280240 IC50 = 0.5 nM 9.30
CHEMBL5290464 IC50 = 0.5 nM 9.30
CHEMBL5266498 IC50 = 0.5 nM 9.30
CHEMBL454095 ABECARNIL IC50 = 1.0 nM 9.00
CHEMBL453066 BETA-CCM IC50 = 1.0 nM 9.00
CHEMBL454606 IC50 = 1.0 nM 9.00
CHEMBL1337028 IC50 = 1.0 nM 9.00
CHEMBL509197 IC50 = 1.0 nM 9.00
CHEMBL5266558 IC50 = 3.0 nM 8.52
CHEMBL510764 IC50 = 3.0 nM 8.52
CHEMBL2262044 IC50 = 3.0 nM 8.52
CHEMBL499814 IC50 = 3.0 nM 8.52
CHEMBL5276119 IC50 = 4.0 nM 8.40
CHEMBL5290746 IC50 = 4.0 nM 8.40
CHEMBL457794 IC50 = 750.0 nM 6.12
CHEMBL275224 NORHARMANE IC50 = 1600.0 nM 5.80
CHEMBL12014 HARMAN IC50 = 2500.0 nM 5.60
CHEMBL1972187 IC50 = 31000.0 nM 4.51
CHEMBL129208 IC50 > 100000.0 nM -
CHEMBL340807 HARMALINE IC50 > 100.0 microA -
CHEMBL269538 HARMINE IC50 > 100000.0 nM -