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Assay Detail

CHEMBL4351519

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

Binding
Displacement of [3H]-flumazenil from rat GABAA alpha1beta3gamma2 receptor expressed in CHO cell membranes measured after 2 hrs by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and Identification of a Novel, Functionally Subtype Selective GABA<sub>A</sub> Positive Allosteric Modulator (PF-06372865).
Owen RM, Blakemore D, Cao L, Flanagan N, Fish R, Gibson KR, Gurrell R, Huh CW, Kammonen J, Mortimer-Cassen E, Nickolls SA, Omoto K, Owen D, Pike A, Pryde DC, Reynolds DS, Roeloffs R, Rose C, Stead C, Takeuchi M, Warmus JS, Watson C.
J Med Chem (2019) 62 : 5773 -5796
PubMed 30964988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.39 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3647536 DARIGABAT 2.0 1 9.47
CHEMBL4545044 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3647536 DARIGABAT Ki = 0.34 nM 9.47
CHEMBL4545044 Ki = 0.5 nM 9.30