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Assay Detail

CHEMBL681632

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

Binding
Inhibition of [3H]Ro-151788 binding to human alpha-5-beta-3-gamma-2 GABA-A receptor expressed in L(tk-) cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.
Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM.
J Med Chem (2004) 47 : 3642 -3657
PubMed 15214791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.12 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122154 1 9.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122154 Ki = 0.75 nM 9.12