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Assay Detail

CHEMBL3420198

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

Binding
Displacement of [3H]NMS from human muscarinic M1 acetylcholine receptor expressed in CHO cell membranes by radioligand binding assay
16
Total Activities
16
Compounds Tested
3
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

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
Kd 12 6.18 7.14
Imax 2 - -
pKd 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414840 1 7.14
CHEMBL3414842 1 7.13
CHEMBL3414839 1 6.85
CHEMBL3414838 1 6.82
CHEMBL3414844 1 6.82
CHEMBL3414847 1 6.78
CHEMBL3414841 1 6.31
CHEMBL3414843 1 6.07
CHEMBL3121473 1 5.67
CHEMBL550 PILOCARPINE 4.0 1 5.57
CHEMBL667 ACETYLCHOLINE 4.0 1 4.76
CHEMBL608112 1 4.26
CHEMBL3414854 1 -
CHEMBL3414851 1 -
CHEMBL3414845 1 -
CHEMBL3414846 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414840 Kd = 72.44 nM 7.14
CHEMBL3414842 Kd = 74.13 nM 7.13
CHEMBL3414839 Kd = 141.25 nM 6.85
CHEMBL3414838 Kd = 151.36 nM 6.82
CHEMBL3414844 Kd = 151.36 nM 6.82
CHEMBL3414847 Kd = 165.96 nM 6.78
CHEMBL3414841 Kd = 489.78 nM 6.31
CHEMBL3414843 Kd = 851.14 nM 6.07
CHEMBL3121473 Kd = 2137.96 nM 5.67
CHEMBL550 PILOCARPINE Kd = 2691.53 nM 5.57
CHEMBL667 ACETYLCHOLINE Kd = 17378.01 nM 4.76
CHEMBL608112 Kd = 54954.09 nM 4.26
CHEMBL3414854 Imax = 10.0 uM -
CHEMBL3414851 Imax = 3.0 uM -
CHEMBL3414845 pKd - -
CHEMBL3414846 pKd - -