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Assay Detail

CHEMBL923036

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Binding
Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells
28
Total Activities
26
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 Autocuration

Target

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

Publication

Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.
Vistoli G, Pedretti A, Dei S, Scapecchi S, Marconi C, Romanelli MN.
Bioorg Med Chem (2008) 16 : 3049 -3058
PubMed 18182302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.93 8.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64000 1 8.58
CHEMBL1162116 1 8.44
CHEMBL21536 XANOMELINE 4.0 1 7.93
CHEMBL77793 1 6.99
CHEMBL23957 OXOTREMORINE METHIODIDE 1 6.97
CHEMBL134641 SABCOMELINE 2.0 1 6.69
CHEMBL7634 OXOTREMORINE 1 6.49
CHEMBL12587 MUSCARINE 1 6.31
CHEMBL608828 (S)-ACECLIDINE 1 6.21
CHEMBL259344 1 6.17
CHEMBL151938 MILAMELINE 2.0 1 6.00
CHEMBL105457 1 5.92
CHEMBL14 CARBACHOL 4.0 1 5.88
CHEMBL258907 1 5.85
CHEMBL402473 1 5.77
CHEMBL320820 1 5.68
CHEMBL612034 (R)-ACECLIDINE 1 5.65
CHEMBL7303 ARECOLINE -1.0 1 5.61
CHEMBL294273 1 5.56
CHEMBL258906 1 5.45
CHEMBL259131 1 5.30
CHEMBL258905 1 5.28
CHEMBL541424 3 5.03
CHEMBL550 PILOCARPINE 4.0 1 4.92
CHEMBL259662 1 4.43
CHEMBL553241 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64000 Ki = 2.63 nM 8.58
CHEMBL1162116 Ki = 3.631 nM 8.44
CHEMBL21536 XANOMELINE Ki = 11.75 nM 7.93
CHEMBL77793 Ki = 102.33 nM 6.99
CHEMBL23957 OXOTREMORINE METHIODIDE Ki = 107.15 nM 6.97
CHEMBL134641 SABCOMELINE Ki = 204.17 nM 6.69
CHEMBL7634 OXOTREMORINE Ki = 323.59 nM 6.49
CHEMBL12587 MUSCARINE Ki = 489.78 nM 6.31
CHEMBL608828 (S)-ACECLIDINE Ki = 616.6 nM 6.21
CHEMBL259344 Ki = 676.08 nM 6.17
CHEMBL151938 MILAMELINE Ki = 1000.0 nM 6.00
CHEMBL105457 Ki = 1202.26 nM 5.92
CHEMBL14 CARBACHOL Ki = 1318.26 nM 5.88
CHEMBL258907 Ki = 1412.54 nM 5.85
CHEMBL402473 Ki = 1698.24 nM 5.77
CHEMBL320820 Ki = 2089.3 nM 5.68
CHEMBL612034 (R)-ACECLIDINE Ki = 2238.72 nM 5.65
CHEMBL7303 ARECOLINE Ki = 2454.71 nM 5.61
CHEMBL294273 Ki = 2754.23 nM 5.56
CHEMBL258906 Ki = 3548.13 nM 5.45
CHEMBL259131 Ki = 5011.87 nM 5.30
CHEMBL258905 Ki = 5248.07 nM 5.28
CHEMBL541424 Ki = 9332.54 nM 5.03
CHEMBL550 PILOCARPINE Ki = 12022.64 nM 4.92
CHEMBL541424 Ki = 15488.17 nM 4.81
CHEMBL259662 Ki = 37153.52 nM 4.43
CHEMBL553241 Ki = 77624.71 nM 4.11
CHEMBL541424 Ki = 81283.05 nM 4.09