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Assay Detail

CHEMBL746303

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Binding
Binding affinity against human muscarine receptor (hM2) cloned in CHO cells
10
Total Activities
9
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 M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.
Gao LJ, Waelbroeck M, Hofman S, Van Haver D, Milanesio M, Viterbo D, De Clercq PJ.
Bioorg Med Chem Lett (2002) 12 : 1909 -1912
PubMed 12113806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.65 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277642 HIMBACINE 2 8.33
CHEMBL301670 1 7.02
CHEMBL57485 1 6.77
CHEMBL294663 1 6.51
CHEMBL56275 1 6.17
CHEMBL58824 1 6.07
CHEMBL291562 1 5.94
CHEMBL430587 1 5.93
CHEMBL55698 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277642 HIMBACINE Ki = 4.677 nM 8.33
CHEMBL277642 HIMBACINE Ki = 10.0 nM 8.00
CHEMBL301670 Ki = 95.5 nM 7.02
CHEMBL57485 Ki = 169.82 nM 6.77
CHEMBL294663 Ki = 309.03 nM 6.51
CHEMBL56275 Ki = 676.08 nM 6.17
CHEMBL58824 Ki = 851.14 nM 6.07
CHEMBL291562 Ki = 1148.15 nM 5.94
CHEMBL430587 Ki = 1174.9 nM 5.93
CHEMBL55698 Ki = 1737.8 nM 5.76