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Assay Detail

CHEMBL682136

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

Binding
The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-aminobutyric acid A receptor to rat whole brain membranes.
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Brain membranes
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607) ↗
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
Anderson A, Boyd AC, Byford A, Campbell AC, Gemmell DK, Hamilton NM, Hill DR, Hill-Venning C, Lambert JJ, Maidment MS, May V, Marshall RJ, Peters JA, Rees DC, Stevenson D, Sundaram H.
J Med Chem (1997) 40 : 1668 -1681
PubMed 9171876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.40 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790249 — — 1 7.50
CHEMBL1790258 — — 1 7.41
CHEMBL1790264 — — 1 7.28
CHEMBL1790250 — — 1 7.28
CHEMBL2105209 MINAXOLONE 2.0 1 7.15
CHEMBL1790277 — — 1 7.10
CHEMBL1790265 — — 1 7.05
CHEMBL207538 BREXANOLONE 4.0 1 7.04
CHEMBL1790244 — — 1 7.00
CHEMBL1790262 — — 1 6.97
CHEMBL1790248 — — 1 6.94
CHEMBL210952 ELTANOLONE 2.0 1 6.93
CHEMBL3138407 — — 1 6.90
CHEMBL1790246 — — 1 6.88
CHEMBL1790267 — — 1 6.85
CHEMBL3137819 — — 1 6.83
CHEMBL3137825 — — 1 6.77
CHEMBL1790273 — — 1 6.69
CHEMBL1790247 — — 1 6.68
CHEMBL1256760 — — 1 6.66
CHEMBL3137824 — — 1 6.64
CHEMBL3138379 — — 1 6.63
CHEMBL1790256 — — 1 6.58
CHEMBL1790276 — — 1 6.57
CHEMBL3138185 — — 1 6.57
CHEMBL1790275 — — 1 6.50
CHEMBL1790274 — — 1 6.50
CHEMBL3138386 — — 1 6.47
CHEMBL1790242 — — 1 6.43
CHEMBL1790278 — — 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790249 — IC50 = 32.0 nM 7.50
CHEMBL1790258 — IC50 = 39.0 nM 7.41
CHEMBL1790250 — IC50 = 53.0 nM 7.28
CHEMBL1790264 — IC50 = 53.0 nM 7.28
CHEMBL2105209 MINAXOLONE IC50 = 71.0 nM 7.15
CHEMBL1790277 — IC50 = 79.0 nM 7.10
CHEMBL1790265 — IC50 = 90.0 nM 7.05
CHEMBL207538 BREXANOLONE IC50 = 91.0 nM 7.04
CHEMBL1790244 — IC50 = 100.0 nM 7.00
CHEMBL1790262 — IC50 = 107.0 nM 6.97
CHEMBL1790248 — IC50 = 115.0 nM 6.94
CHEMBL210952 ELTANOLONE IC50 = 117.0 nM 6.93
CHEMBL3138407 — IC50 = 127.0 nM 6.90
CHEMBL1790246 — IC50 = 131.0 nM 6.88
CHEMBL1790267 — IC50 = 142.0 nM 6.85
CHEMBL3137819 — IC50 = 148.0 nM 6.83
CHEMBL3137825 — IC50 = 171.0 nM 6.77
CHEMBL1790273 — IC50 = 206.0 nM 6.69
CHEMBL1790247 — IC50 = 209.0 nM 6.68
CHEMBL1256760 — IC50 = 220.0 nM 6.66
CHEMBL3137824 — IC50 = 231.0 nM 6.64
CHEMBL3138379 — IC50 = 235.0 nM 6.63
CHEMBL1790256 — IC50 = 261.0 nM 6.58
CHEMBL1790276 — IC50 = 267.0 nM 6.57
CHEMBL3138185 — IC50 = 270.0 nM 6.57
CHEMBL1790275 — IC50 = 316.0 nM 6.50
CHEMBL1790274 — IC50 = 317.0 nM 6.50
CHEMBL3138386 — IC50 = 341.0 nM 6.47
CHEMBL1790242 — IC50 = 369.0 nM 6.43
CHEMBL1790278 — IC50 = 387.0 nM 6.41
CHEMBL1790254 — IC50 = 424.0 nM 6.37
CHEMBL1790243 — IC50 = 497.0 nM 6.30
CHEMBL1790261 — IC50 = 504.0 nM 6.30
CHEMBL190279 ALFAXALONE IC50 = 538.0 nM 6.27
CHEMBL1790253 — IC50 = 910.0 nM 6.04
CHEMBL1790257 — IC50 = 951.0 nM 6.02
CHEMBL1790245 — IC50 = 948.0 nM 6.02
CHEMBL1790266 — IC50 = 1140.0 nM 5.94
CHEMBL3137817 — IC50 = 1160.0 nM 5.94
CHEMBL3137822 — IC50 = 1390.0 nM 5.86
CHEMBL1790263 — IC50 = 1490.0 nM 5.83
CHEMBL1790269 — IC50 = 1990.0 nM 5.70
CHEMBL1790255 — IC50 = 2170.0 nM 5.66
CHEMBL3137815 — IC50 = 2561.0 nM 5.59
CHEMBL3137818 — IC50 = 3041.0 nM 5.52
CHEMBL1790268 — IC50 = 3195.0 nM 5.50
CHEMBL1790260 — IC50 = 5587.0 nM 5.25
CHEMBL526 PROPOFOL IC50 = 8300.0 nM 5.08
CHEMBL3138186 — IC50 = 9040.0 nM 5.04
CHEMBL441 THIOPENTAL IC50 = 29500.0 nM 4.53