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Assay Detail

CHEMBL680443

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

Binding
Displacement of [3H]-Ro- 15-4513 from alpha-6 beta2 gamma2 subunits of Rat GABA-A receptor expressed in Sf-9 insect cell membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Expert

Target

GABA A receptor alpha-6/beta-2/gamma-2 (CHEMBL2111365)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
Mickelson JW, Jacobsen EJ, Carter DB, Im HK, Im WB, Schreur PJ, Sethy VH, Tang AH, McGee JE, Petke JD.
J Med Chem (1996) 39 : 4654 -4666
PubMed 8917654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.33 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142750 1 7.88
CHEMBL15093 PNU-91571 1 7.88
CHEMBL279867 PANADIPLON 2.0 1 6.22
CHEMBL343489 1 -
CHEMBL143864 1 -
CHEMBL343688 1 -
CHEMBL264999 1 -
CHEMBL141243 1 -
CHEMBL140631 1 -
CHEMBL142792 1 -
CHEMBL12 DIAZEPAM 4.0 1 -
CHEMBL357637 1 -
CHEMBL142329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142750 Ki = 13.2 nM 7.88
CHEMBL15093 PNU-91571 Ki = 13.2 nM 7.88
CHEMBL279867 PANADIPLON Ki = 603.0 nM 6.22
CHEMBL343489 Ki > 589.0 nM -
CHEMBL143864 Ki > 589.0 nM -
CHEMBL343688 Ki > 589.0 nM -
CHEMBL264999 Ki > 589.0 nM -
CHEMBL141243 Ki > 589.0 nM -
CHEMBL140631 Ki > 589.0 nM -
CHEMBL142792 Ki > 589.0 nM -
CHEMBL12 DIAZEPAM Ki > 7000.0 nM -
CHEMBL357637 Ki > 589.0 nM -
CHEMBL142329 Ki > 589.0 nM -