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Assay Detail

CHEMBL745479

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

Binding
Binding affinity at human cloned acetylcholine receptor M2 in CHO cells.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.
Boyle CD, Chackalamannil S, Chen LY, Dugar S, Pushpavanam P, Billard W, Binch H, Crosby G, Cohen-Williams M, Coffin VL, Duffy RA, Ruperto V, Lachowicz JE.
Bioorg Med Chem Lett (2000) 10 : 2727 -2730
PubMed 11133078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 9.20 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76164 1 11.00
CHEMBL328094 1 10.52
CHEMBL90700 1 10.51
CHEMBL308566 1 10.15
CHEMBL94189 1 10.14
CHEMBL94247 1 9.96
CHEMBL91404 1 9.89
CHEMBL328059 1 9.80
CHEMBL433011 1 9.14
CHEMBL93017 1 9.09
CHEMBL90638 1 9.09
CHEMBL91232 1 8.99
CHEMBL90507 1 8.91
CHEMBL328093 1 8.74
CHEMBL92110 1 8.54
CHEMBL92569 1 8.29
CHEMBL328550 1 8.04
CHEMBL328120 1 7.92
CHEMBL90199 1 7.84
CHEMBL328659 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76164 Ki = 0.01 nM 11.00
CHEMBL328094 Ki = 0.03 nM 10.52
CHEMBL90700 Ki = 0.031 nM 10.51
CHEMBL308566 Ki = 0.07 nM 10.15
CHEMBL94189 Ki = 0.073 nM 10.14
CHEMBL94247 Ki = 0.11 nM 9.96
CHEMBL91404 Ki = 0.13 nM 9.89
CHEMBL328059 Ki = 0.16 nM 9.80
CHEMBL433011 Ki = 0.72 nM 9.14
CHEMBL93017 Ki = 0.823 nM 9.09
CHEMBL90638 Ki = 0.82 nM 9.09
CHEMBL91232 Ki = 1.02 nM 8.99
CHEMBL90507 Ki = 1.22 nM 8.91
CHEMBL328093 Ki = 1.82 nM 8.74
CHEMBL92110 Ki = 2.91 nM 8.54
CHEMBL92569 Ki = 5.07 nM 8.29
CHEMBL328550 Ki = 9.09 nM 8.04
CHEMBL328120 Ki = 12.1 nM 7.92
CHEMBL90199 Ki = 14.3 nM 7.84
CHEMBL328659 Ki = 34.8 nM 7.46