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Assay Detail

CHEMBL992812

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

Binding
Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells by liquid scintillation counter
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
Scapecchi S, Nesi M, Matucci R, Bellucci C, Buccioni M, Dei S, Guandalini L, Manetti D, Martini E, Marucci G, Romanelli MN, Teodori E, Cirilli R.
J Med Chem (2008) 51 : 3905 -3912
PubMed 18543900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 4.67 5.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40554 1 5.71
CHEMBL554532 1 5.28
CHEMBL551563 1 5.25
CHEMBL555475 1 5.13
CHEMBL92387 1 5.10
CHEMBL553434 1 4.86
CHEMBL461089 1 4.84
CHEMBL513277 1 4.57
CHEMBL553155 1 4.51
CHEMBL460470 1 4.48
CHEMBL450463 1 4.44
CHEMBL14 CARBACHOL 4.0 1 4.42
CHEMBL505086 1 4.42
CHEMBL450729 1 4.36
CHEMBL461709 1 4.35
CHEMBL461088 1 4.33
CHEMBL527880 1 4.29
CHEMBL451335 1 4.20
CHEMBL461502 1 4.11
CHEMBL461087 1 -
CHEMBL458416 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40554 Ki = 1949.84 nM 5.71
CHEMBL554532 Ki = 5248.07 nM 5.28
CHEMBL551563 Ki = 5623.41 nM 5.25
CHEMBL555475 Ki = 7413.1 nM 5.13
CHEMBL92387 Ki = 7943.28 nM 5.10
CHEMBL553434 Ki = 13803.84 nM 4.86
CHEMBL461089 Ki = 14454.4 nM 4.84
CHEMBL513277 Ki = 26915.35 nM 4.57
CHEMBL553155 Ki = 30902.95 nM 4.51
CHEMBL460470 Ki = 33113.11 nM 4.48
CHEMBL450463 Ki = 36307.81 nM 4.44
CHEMBL14 CARBACHOL Ki = 38018.94 nM 4.42
CHEMBL505086 Ki = 38018.94 nM 4.42
CHEMBL450729 Ki = 43651.58 nM 4.36
CHEMBL461709 Ki = 44668.36 nM 4.35
CHEMBL461088 Ki = 46773.51 nM 4.33
CHEMBL527880 Ki = 51286.14 nM 4.29
CHEMBL451335 Ki = 63095.73 nM 4.20
CHEMBL461502 Ki = 77624.71 nM 4.11
CHEMBL461087 Ki = 177827.94 nM -
CHEMBL458416 Ki = 154881.66 nM -