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Assay Detail

CHEMBL745744

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

Binding
Binding affinity towards muscarinic m1 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.
Calderon SN, Izenwasser S, Heller B, Gutkind JS, Mattson MV, Su TP, Newman AH.
J Med Chem (1994) 37 : 2285 -2291
PubMed 8057277 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.69 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 8.70
CHEMBL75217 1 7.70
CHEMBL73017 1 7.20
CHEMBL72219 1 7.12
CHEMBL73234 CARBETAPENTANE 4.0 1 7.12
CHEMBL74736 1 6.87
CHEMBL73501 1 6.24
CHEMBL451542 1 6.07
CHEMBL72506 1 6.04
CHEMBL74305 1 5.98
CHEMBL308707 1 5.77
CHEMBL307628 1 5.51
CHEMBL309172 1 -
CHEMBL307668 1 -
CHEMBL73762 1 -
CHEMBL440686 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Ki = 2.0 nM 8.70
CHEMBL75217 Ki = 20.0 nM 7.70
CHEMBL73017 Ki = 63.0 nM 7.20
CHEMBL72219 Ki = 75.0 nM 7.12
CHEMBL73234 CARBETAPENTANE Ki = 76.0 nM 7.12
CHEMBL74736 Ki = 135.0 nM 6.87
CHEMBL73501 Ki = 581.0 nM 6.24
CHEMBL451542 Ki = 843.0 nM 6.07
CHEMBL72506 Ki = 910.0 nM 6.04
CHEMBL74305 Ki = 1058.0 nM 5.98
CHEMBL308707 Ki = 1697.0 nM 5.77
CHEMBL307628 Ki = 3110.0 nM 5.51
CHEMBL309172 Ki > 10000.0 nM -
CHEMBL307668 Ki > 10000.0 nM -
CHEMBL73762 Ki > 10000.0 nM -
CHEMBL440686 Ki > 10000.0 nM -