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Assay Detail

CHEMBL861669

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

Binding
Increase in [3H]flunitrazepam binding to GABA-A receptor in mouse embryo cortical neurons
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2094133)
Type PROTEIN COMPLEX GROUP
Organism Mus musculus

Publication

Activity of B-nor analogues of neurosteroids on the GABA(A) receptor in primary neuronal cultures.
Suñol C, García DA, Bujons J, Kristofíková Z, Matyás L, Babot Z, Kasal A.
J Med Chem (2006) 49 : 3225 -3234
PubMed 16722640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 10 - -
EC50 4 6.16 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379949 1 6.61
CHEMBL207538 BREXANOLONE 4.0 1 6.06
CHEMBL210767 1 6.03
CHEMBL210952 ELTANOLONE 2.0 1 5.93
CHEMBL210387 1 -
CHEMBL378742 1 -
CHEMBL383839 1 -
CHEMBL379786 1 -
CHEMBL379583 1 -
CHEMBL211043 1 -
CHEMBL210998 1 -
CHEMBL207412 1 -
CHEMBL207079 1 -
CHEMBL207302 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379949 EC50 = 245.47 nM 6.61
CHEMBL207538 BREXANOLONE EC50 = 870.96 nM 6.06
CHEMBL210767 EC50 = 933.25 nM 6.03
CHEMBL210952 ELTANOLONE EC50 = 1174.9 nM 5.93
CHEMBL210387 Activity - -
CHEMBL378742 Activity - -
CHEMBL383839 Activity - -
CHEMBL379786 Activity - -
CHEMBL379583 Activity - -
CHEMBL211043 Activity - -
CHEMBL210998 Activity - -
CHEMBL207412 Activity - -
CHEMBL207079 Activity - -
CHEMBL207302 Activity - -