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Assay Detail

CHEMBL881234

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

Binding
Binding affinity for rat heart muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate
22
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL309)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.
Naito R, Yonetoku Y, Okamoto Y, Toyoshima A, Ikeda K, Takeuchi M.
J Med Chem (2005) 48 : 6597 -6606
PubMed 16220976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.94 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194628 1 8.17
CHEMBL1169543 1 8.06
CHEMBL371293 2 7.89
CHEMBL1231 OXYBUTYNIN 4.0 1 7.85
CHEMBL606903 1 7.82
CHEMBL372983 2 7.66
CHEMBL439867 1 7.55
CHEMBL198065 2 7.12
CHEMBL606904 1 6.96
CHEMBL1734 SOLIFENACIN 4.0 1 6.92
CHEMBL196481 1 6.85
CHEMBL198669 1 6.36
CHEMBL197588 2 6.32
CHEMBL606963 1 6.07
CHEMBL606901 1 5.80
CHEMBL606962 1 5.77
CHEMBL606902 1 5.46
CHEMBL197717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194628 Ki = 6.8 nM 8.17
CHEMBL1169543 Ki = 8.7 nM 8.06
CHEMBL371293 Ki = 13.0 nM 7.89
CHEMBL1231 OXYBUTYNIN Ki = 14.0 nM 7.85
CHEMBL606903 Ki = 15.0 nM 7.82
CHEMBL372983 Ki = 22.0 nM 7.66
CHEMBL439867 Ki = 28.0 nM 7.55
CHEMBL372983 Ki = 39.0 nM 7.41
CHEMBL198065 Ki = 76.0 nM 7.12
CHEMBL371293 Ki = 93.0 nM 7.03
CHEMBL606904 Ki = 110.0 nM 6.96
CHEMBL1734 SOLIFENACIN Ki = 120.0 nM 6.92
CHEMBL196481 Ki = 140.0 nM 6.85
CHEMBL198669 Ki = 440.0 nM 6.36
CHEMBL197588 Ki = 480.0 nM 6.32
CHEMBL606963 Ki = 850.0 nM 6.07
CHEMBL606901 Ki = 1600.0 nM 5.80
CHEMBL606962 Ki = 1700.0 nM 5.77
CHEMBL197588 Ki = 1800.0 nM 5.75
CHEMBL606902 Ki = 3500.0 nM 5.46
CHEMBL197717 Ki > 1000.0 nM -
CHEMBL198065 Ki > 1000.0 nM -