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Assay Detail

CHEMBL749216

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

Binding
Dissociation constant towards Muscarinic acetylcholine receptor in guinea pig ileum
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL2094109)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
Lundkvist JR, Vargas HM, Caldirola P, Ringdahl B, Hacksell U.
J Med Chem (1990) 33 : 3182 -3189
PubMed 2258904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 16 6.11 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 9.05
CHEMBL2092930 1 7.10
CHEMBL107456 1 7.01
CHEMBL432629 1 6.96
CHEMBL1788225 1 6.79
CHEMBL1788202 1 6.70
CHEMBL1788224 1 5.94
CHEMBL110892 1 5.85
CHEMBL2092932 1 5.49
CHEMBL106056 1 5.45
CHEMBL1788219 1 5.20
CHEMBL108557 1 5.16
CHEMBL2092931 1 5.11
CHEMBL108582 1 5.08
CHEMBL322126 1 4.80
CHEMBL323032 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Kd = 0.9 nM 9.05
CHEMBL2092930 Kd = 80.0 nM 7.10
CHEMBL107456 Kd = 97.0 nM 7.01
CHEMBL432629 Kd = 110.0 nM 6.96
CHEMBL1788225 Kd = 161.0 nM 6.79
CHEMBL1788202 Kd = 200.0 nM 6.70
CHEMBL1788224 Kd = 1160.0 nM 5.94
CHEMBL110892 Kd = 1400.0 nM 5.85
CHEMBL2092932 Kd = 3230.0 nM 5.49
CHEMBL106056 Kd = 3550.0 nM 5.45
CHEMBL1788219 Kd = 6320.0 nM 5.20
CHEMBL108557 Kd = 7000.0 nM 5.16
CHEMBL2092931 Kd = 7850.0 nM 5.11
CHEMBL108582 Kd = 8300.0 nM 5.08
CHEMBL322126 Kd = 16010.0 nM 4.80
CHEMBL323032 Kd = 125000.0 nM -