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Assay Detail

CHEMBL923035

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Binding
Binding affinity to human cloned muscarinic M1 receptor expressed in CHO cells
23
Total Activities
23
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 M1 (CHEMBL216)
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 23 5.43 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7634 OXOTREMORINE 1 8.95
CHEMBL21536 XANOMELINE 4.0 1 8.10
CHEMBL1162116 1 7.04
CHEMBL77793 1 6.92
CHEMBL134641 SABCOMELINE 2.0 1 6.64
CHEMBL151938 MILAMELINE 2.0 1 5.25
CHEMBL258907 1 5.23
CHEMBL550 PILOCARPINE 4.0 1 5.18
CHEMBL259662 1 5.08
CHEMBL259344 1 5.08
CHEMBL320820 1 4.96
CHEMBL105457 1 4.96
CHEMBL14 CARBACHOL 4.0 1 4.92
CHEMBL258906 1 4.85
CHEMBL12587 MUSCARINE 1 4.74
CHEMBL258905 1 4.72
CHEMBL23957 OXOTREMORINE METHIODIDE 1 4.69
CHEMBL64000 1 4.67
CHEMBL402473 1 4.67
CHEMBL7303 ARECOLINE -1.0 1 4.53
CHEMBL259131 1 4.28
CHEMBL541424 1 4.03
CHEMBL294273 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7634 OXOTREMORINE Ki = 1.122 nM 8.95
CHEMBL21536 XANOMELINE Ki = 7.943 nM 8.10
CHEMBL1162116 Ki = 91.2 nM 7.04
CHEMBL77793 Ki = 120.23 nM 6.92
CHEMBL134641 SABCOMELINE Ki = 229.09 nM 6.64
CHEMBL151938 MILAMELINE Ki = 5623.41 nM 5.25
CHEMBL258907 Ki = 5888.44 nM 5.23
CHEMBL550 PILOCARPINE Ki = 6606.93 nM 5.18
CHEMBL259662 Ki = 8317.64 nM 5.08
CHEMBL259344 Ki = 8317.64 nM 5.08
CHEMBL320820 Ki = 10964.78 nM 4.96
CHEMBL105457 Ki = 10964.78 nM 4.96
CHEMBL14 CARBACHOL Ki = 12022.64 nM 4.92
CHEMBL258906 Ki = 14125.38 nM 4.85
CHEMBL12587 MUSCARINE Ki = 18197.01 nM 4.74
CHEMBL258905 Ki = 19054.61 nM 4.72
CHEMBL23957 OXOTREMORINE METHIODIDE Ki = 20417.38 nM 4.69
CHEMBL64000 Ki = 21379.62 nM 4.67
CHEMBL402473 Ki = 21379.62 nM 4.67
CHEMBL7303 ARECOLINE Ki = 29512.09 nM 4.53
CHEMBL259131 Ki = 52480.75 nM 4.28
CHEMBL541424 Ki = 93325.43 nM 4.03
CHEMBL294273 Ki = 281838.29 nM -