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Assay Detail

CHEMBL747589

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]-NMS (N-Methylscopolamine) as the radioligand.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 23 4.90 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290723 1 6.16
CHEMBL1794941 1 5.83
CHEMBL1794940 1 5.83
CHEMBL40032 1 5.79
CHEMBL40063 1 5.59
CHEMBL40121 1 5.57
CHEMBL550 PILOCARPINE 4.0 1 5.43
CHEMBL7303 ARECOLINE -1.0 1 5.15
CHEMBL20835 ACECLIDINE 3.0 1 5.08
CHEMBL288113 1 4.60
CHEMBL290501 1 4.52
CHEMBL288465 1 4.48
CHEMBL1794937 1 4.47
CHEMBL1794938 1 4.42
CHEMBL41524 1 4.40
CHEMBL1794939 1 4.35
CHEMBL543292 1 4.15
CHEMBL39564 1 4.08
CHEMBL39486 1 4.06
CHEMBL288717 1 4.01
CHEMBL442154 1 -
CHEMBL555094 1 -
CHEMBL553322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290723 Ki = 700.0 nM 6.16
CHEMBL1794941 Ki = 1470.0 nM 5.83
CHEMBL1794940 Ki = 1470.0 nM 5.83
CHEMBL40032 Ki = 1630.0 nM 5.79
CHEMBL40063 Ki = 2580.0 nM 5.59
CHEMBL40121 Ki = 2680.0 nM 5.57
CHEMBL550 PILOCARPINE Ki = 3670.0 nM 5.43
CHEMBL7303 ARECOLINE Ki = 7120.0 nM 5.15
CHEMBL20835 ACECLIDINE Ki = 8260.0 nM 5.08
CHEMBL288113 Ki = 25100.0 nM 4.60
CHEMBL290501 Ki = 30000.0 nM 4.52
CHEMBL288465 Ki = 33000.0 nM 4.48
CHEMBL1794937 Ki = 34000.0 nM 4.47
CHEMBL1794938 Ki = 38100.0 nM 4.42
CHEMBL41524 Ki = 39900.0 nM 4.40
CHEMBL1794939 Ki = 44800.0 nM 4.35
CHEMBL543292 Ki = 71000.0 nM 4.15
CHEMBL39564 Ki = 83300.0 nM 4.08
CHEMBL39486 Ki = 87400.0 nM 4.06
CHEMBL288717 Ki = 98700.0 nM 4.01
CHEMBL442154 Ki = 141000.0 nM -
CHEMBL555094 Ki = 430000.0 nM -
CHEMBL553322 Ki = 734000.0 nM -