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Assay Detail

CHEMBL893770

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

Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
19
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.
Provins L, Christophe B, Danhaive P, Dulieu J, Gillard M, Quéré L, Stebbins K.
Bioorg Med Chem Lett (2007) 17 : 3077 -3080
PubMed 17398090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.32 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234099 1 8.89
CHEMBL205654 2 8.50
CHEMBL389992 1 7.89
CHEMBL232419 2 7.80
CHEMBL232860 1 7.70
CHEMBL434388 1 7.50
CHEMBL232208 1 7.40
CHEMBL395571 1 7.40
CHEMBL232416 1 7.10
CHEMBL434765 1 7.10
CHEMBL396761 2 6.80
CHEMBL242822 1 6.80
CHEMBL242823 1 6.70
CHEMBL232417 1 6.30
CHEMBL436814 1 6.20
CHEMBL245137 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234099 Ki = 1.3 nM 8.89
CHEMBL205654 Ki = 3.162 nM 8.50
CHEMBL205654 Ki = 3.2 nM 8.49
CHEMBL389992 Ki = 13.0 nM 7.89
CHEMBL232419 Ki = 15.85 nM 7.80
CHEMBL232419 Ki = 16.0 nM 7.80
CHEMBL232860 Ki = 20.0 nM 7.70
CHEMBL434388 Ki = 32.0 nM 7.50
CHEMBL395571 Ki = 40.0 nM 7.40
CHEMBL232208 Ki = 40.0 nM 7.40
CHEMBL232416 Ki = 79.0 nM 7.10
CHEMBL434765 Ki = 79.0 nM 7.10
CHEMBL242822 Ki = 158.0 nM 6.80
CHEMBL396761 Ki = 158.49 nM 6.80
CHEMBL242823 Ki = 200.0 nM 6.70
CHEMBL396761 Ki = 200.0 nM 6.70
CHEMBL232417 Ki = 501.0 nM 6.30
CHEMBL436814 Ki = 631.0 nM 6.20
CHEMBL245137 Ki = 794.0 nM 6.10