Assay Detail

CHEMBL3420956

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Binding

Binding affinity to muscarinic M1 acetylcholine receptor (unknown origin)

ChEMBL ↗

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Target

Muscarinic acetylcholine receptor M1 (CHEMBL216) ↗

Open DB target context

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Muscarinic acetylcholine receptor M1 (CHEMBL216) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Muscarinic acetylcholine receptor M1

CHEMBL216

Anchored from Assay target.

Protein identity Muscarinic acetylcholine receptor M1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.

Chen X, Klöckner J, Holze J, Zimmermann C, Seemann WK, Schrage R, Bock A, Mohr K, Tränkle C, Holzgrabe U, Decker M.
J Med Chem (2015) 58 : 560 -576
PubMed 25478907 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	5.00	5.10
Kd	2	5.17	5.57

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL550	PILOCARPINE	4.0	2	5.57
CHEMBL667	ACETYLCHOLINE	4.0	2	4.90

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL550	PILOCARPINE	Kd	=	2691.53	nM	5.57
CHEMBL550	PILOCARPINE	Ki	=	7943.28	nM	5.10
CHEMBL667	ACETYLCHOLINE	Ki	=	12589.25	nM	4.90
CHEMBL667	ACETYLCHOLINE	Kd	=	17378.01	nM	4.76