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Assay Detail

CHEMBL748895

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Binding
Binding affinity for human Muscarinic acetylcholine receptor M2
13
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE.
J Med Chem (2002) 45 : 5415 -5418
PubMed 12459007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.29 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74141 1 9.29
CHEMBL418446 3 9.05
CHEMBL276239 1 9.05
CHEMBL12098 SCH-211803 1 9.05
CHEMBL150624 3 8.89
CHEMBL150845 1 8.02
CHEMBL150707 1 7.50
CHEMBL412421 1 6.98
CHEMBL52203 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74141 Ki = 0.51 nM 9.29
CHEMBL276239 Ki = 0.9 nM 9.05
CHEMBL12098 SCH-211803 Ki = 0.89 nM 9.05
CHEMBL418446 Ki = 0.89 nM 9.05
CHEMBL150624 Ki = 1.3 nM 8.89
CHEMBL150624 Ki = 2.4 nM 8.62
CHEMBL150624 Ki = 2.7 nM 8.57
CHEMBL418446 Ki = 6.6 nM 8.18
CHEMBL150845 Ki = 9.6 nM 8.02
CHEMBL418446 Ki = 12.0 nM 7.92
CHEMBL150707 Ki = 32.0 nM 7.50
CHEMBL412421 Ki = 104.0 nM 6.98
CHEMBL52203 Ki = 221.0 nM 6.66