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Assay Detail

CHEMBL747590

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

Binding
Binding affinity against muscarinic acetylcholine receptor from rat brain crude membrane, using [3H]OXO-M (oxotremorine) as the radioligand.
48
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

In vitro muscarinic activity of spiromuscarones and related analogs.
Wu ES, Griffith RC, Loch JT, Kover A, Murray RJ, Mullen GB, Blosser JC, Machulskis AC, McCreedy SA.
J Med Chem (1995) 38 : 1558 -1570
PubMed 7739014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 6.64 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290723 1 9.12
CHEMBL43191 1 8.30
CHEMBL40121 1 8.15
CHEMBL7303 ARECOLINE -1.0 1 8.13
CHEMBL289657 2 7.85
CHEMBL20835 ACECLIDINE 3.0 1 7.80
CHEMBL550 PILOCARPINE 4.0 1 7.58
CHEMBL2114433 1 7.57
CHEMBL40032 1 7.54
CHEMBL448736 1 7.52
CHEMBL39564 1 7.50
CHEMBL288113 1 7.46
CHEMBL40063 1 7.44
CHEMBL1794944 1 7.11
CHEMBL1794942 1 7.05
CHEMBL290208 2 7.05
CHEMBL1794941 1 6.89
CHEMBL1794939 1 6.72
CHEMBL38540 1 6.72
CHEMBL1794938 1 6.52
CHEMBL542350 1 6.47
CHEMBL417707 1 6.40
CHEMBL40803 1 6.40
CHEMBL553369 1 6.34
CHEMBL1744377 1 6.26
CHEMBL287747 1 6.26
CHEMBL543292 1 6.19
CHEMBL41879 1 6.19
CHEMBL1794943 1 6.10
CHEMBL1794937 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290723 Ki = 0.76 nM 9.12
CHEMBL43191 Ki = 5.0 nM 8.30
CHEMBL40121 Ki = 7.0 nM 8.15
CHEMBL7303 ARECOLINE Ki = 7.4 nM 8.13
CHEMBL289657 Ki = 14.0 nM 7.85
CHEMBL20835 ACECLIDINE Ki = 16.0 nM 7.80
CHEMBL550 PILOCARPINE Ki = 26.0 nM 7.58
CHEMBL2114433 Ki = 27.0 nM 7.57
CHEMBL40032 Ki = 29.0 nM 7.54
CHEMBL448736 Ki = 30.0 nM 7.52
CHEMBL39564 Ki = 32.0 nM 7.50
CHEMBL288113 Ki = 35.0 nM 7.46
CHEMBL40063 Ki = 36.0 nM 7.44
CHEMBL289657 Ki = 64.0 nM 7.19
CHEMBL1794944 Ki = 77.0 nM 7.11
CHEMBL290208 Ki = 90.0 nM 7.05
CHEMBL1794942 Ki = 90.0 nM 7.05
CHEMBL1794941 Ki = 130.0 nM 6.89
CHEMBL1794939 Ki = 190.0 nM 6.72
CHEMBL38540 Ki = 190.0 nM 6.72
CHEMBL1794938 Ki = 300.0 nM 6.52
CHEMBL290208 Ki = 300.0 nM 6.52
CHEMBL542350 Ki = 340.0 nM 6.47
CHEMBL40803 Ki = 400.0 nM 6.40
CHEMBL417707 Ki = 400.0 nM 6.40
CHEMBL553369 Ki = 460.0 nM 6.34
CHEMBL1744377 Ki = 550.0 nM 6.26
CHEMBL287747 Ki = 550.0 nM 6.26
CHEMBL543292 Ki = 640.0 nM 6.19
CHEMBL41879 Ki = 650.0 nM 6.19
CHEMBL1794943 Ki = 800.0 nM 6.10
CHEMBL1794937 Ki = 910.0 nM 6.04
CHEMBL289139 Ki = 980.0 nM 6.01
CHEMBL41524 Ki = 1470.0 nM 5.83
CHEMBL39291 Ki = 1500.0 nM 5.82
CHEMBL287943 Ki = 1800.0 nM 5.75
CHEMBL1794940 Ki = 1810.0 nM 5.74
CHEMBL288465 Ki = 2500.0 nM 5.60
CHEMBL442154 Ki = 2710.0 nM 5.57
CHEMBL38519 Ki = 3030.0 nM 5.52
CHEMBL39486 Ki = 3070.0 nM 5.51
CHEMBL288717 Ki = 3500.0 nM 5.46
CHEMBL289552 Ki = 4000.0 nM 5.40
CHEMBL555094 Ki = 8200.0 nM 5.09
CHEMBL553322 Ki = 8540.0 nM 5.07
CHEMBL40045 Ki = 175000.0 nM -
CHEMBL290501 Ki = 330000.0 nM -
CHEMBL40524 Ki = 1000000.0 nM -