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Assay Detail

CHEMBL4026880

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

Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design and Discovery of New M2 Receptor Agonists.
Fish I, Stößel A, Eitel K, Valant C, Albold S, Huebner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P.
J Med Chem (2017) 60 : 9239 -9250
PubMed 29094937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 5.26 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100938 1 7.39
CHEMBL4065555 1 6.85
CHEMBL4102555 1 6.68
CHEMBL4069313 1 6.26
CHEMBL4081662 1 6.21
CHEMBL4093215 1 6.16
CHEMBL4073256 1 6.11
CHEMBL4075227 1 6.08
CHEMBL4085150 1 5.70
CHEMBL4103375 1 5.41
CHEMBL4085451 1 5.40
CHEMBL4072787 1 5.39
CHEMBL4071109 1 5.33
CHEMBL667 ACETYLCHOLINE 4.0 1 5.33
CHEMBL4094819 1 5.24
CHEMBL4070055 1 5.24
CHEMBL4060823 1 5.20
CHEMBL4061384 1 5.06
CHEMBL4083241 1 5.00
CHEMBL4089027 1 4.96
CHEMBL4061390 1 4.92
CHEMBL4084607 1 4.92
CHEMBL4092348 1 4.89
CHEMBL4064668 1 4.85
CHEMBL4103087 1 4.80
CHEMBL4092769 1 4.70
CHEMBL4099667 1 4.68
CHEMBL4097248 1 4.62
CHEMBL4095626 1 4.60
CHEMBL146953 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100938 Ki = 41.0 nM 7.39
CHEMBL4065555 Ki = 140.0 nM 6.85
CHEMBL4102555 Ki = 210.0 nM 6.68
CHEMBL4069313 Ki = 550.0 nM 6.26
CHEMBL4081662 Ki = 620.0 nM 6.21
CHEMBL4093215 Ki = 690.0 nM 6.16
CHEMBL4073256 Ki = 780.0 nM 6.11
CHEMBL4075227 Ki = 830.0 nM 6.08
CHEMBL4085150 Ki = 2000.0 nM 5.70
CHEMBL4103375 Ki = 3900.0 nM 5.41
CHEMBL4085451 Ki = 4000.0 nM 5.40
CHEMBL4072787 Ki = 4100.0 nM 5.39
CHEMBL4071109 Ki = 4700.0 nM 5.33
CHEMBL667 ACETYLCHOLINE Ki = 4700.0 nM 5.33
CHEMBL4070055 Ki = 5800.0 nM 5.24
CHEMBL4094819 Ki = 5800.0 nM 5.24
CHEMBL4060823 Ki = 6300.0 nM 5.20
CHEMBL4061384 Ki = 8700.0 nM 5.06
CHEMBL4083241 Ki = 10000.0 nM 5.00
CHEMBL4089027 Ki = 11000.0 nM 4.96
CHEMBL4061390 Ki = 12000.0 nM 4.92
CHEMBL4084607 Ki = 12000.0 nM 4.92
CHEMBL4092348 Ki = 13000.0 nM 4.89
CHEMBL4064668 Ki = 14000.0 nM 4.85
CHEMBL4103087 Ki = 16000.0 nM 4.80
CHEMBL4092769 Ki = 20000.0 nM 4.70
CHEMBL4099667 Ki = 21000.0 nM 4.68
CHEMBL4097248 Ki = 24000.0 nM 4.62
CHEMBL4095626 Ki = 25000.0 nM 4.60
CHEMBL146953 Ki = 28000.0 nM 4.55
CHEMBL4099673 Ki = 36000.0 nM 4.44
CHEMBL4070061 Ki = 42000.0 nM 4.38
CHEMBL4074319 Ki = 43000.0 nM 4.37
CHEMBL14 CARBACHOL Ki = 51000.0 nM 4.29
CHEMBL4091032 Ki = 75000.0 nM 4.12
CHEMBL4095774 Ki > 50000.0 nM -
CHEMBL4091934 Ki > 50000.0 nM -