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Assay Detail

CHEMBL679647

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

Binding
Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex
14
Total Activities
14
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 B receptor (CHEMBL2111474)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Froestl W, Mickel SJ, Hall RG, von Sprecher G, Strub D, Baumann PA, Brugger F, Gentsch C, Jaekel J, Olpe HR.
J Med Chem (1995) 38 : 3297 -3312
PubMed 7650684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.14 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113310 1 7.35
CHEMBL321255 1 7.19
CHEMBL113304 1 7.11
CHEMBL113553 1 7.05
CHEMBL113396 1 6.85
CHEMBL113348 1 6.82
CHEMBL111555 1 6.67
CHEMBL109375 1 6.18
CHEMBL113385 1 5.98
CHEMBL112933 1 5.94
CHEMBL286077 1 5.17
CHEMBL430510 1 4.78
CHEMBL113092 1 4.73
CHEMBL324406 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113310 IC50 = 45.0 nM 7.35
CHEMBL321255 IC50 = 65.0 nM 7.19
CHEMBL113304 IC50 = 77.0 nM 7.11
CHEMBL113553 IC50 = 89.0 nM 7.05
CHEMBL113396 IC50 = 140.0 nM 6.85
CHEMBL113348 IC50 = 152.0 nM 6.82
CHEMBL111555 IC50 = 213.0 nM 6.67
CHEMBL109375 IC50 = 665.0 nM 6.18
CHEMBL113385 IC50 = 1050.0 nM 5.98
CHEMBL112933 IC50 = 1160.0 nM 5.94
CHEMBL286077 IC50 = 6810.0 nM 5.17
CHEMBL430510 IC50 = 16580.0 nM 4.78
CHEMBL113092 IC50 = 18500.0 nM 4.73
CHEMBL324406 IC50 = 67600.0 nM 4.17