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Assay Detail

CHEMBL749927

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

Binding
Inhibition of [3H]pirenzepine binding against muscarinic acetylcholine receptor in rat brain.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.
Triggle DJ, Kwon YW, Abraham P, Pitner JB, Mascarella SW, Carroll FI.
J Med Chem (1991) 34 : 3164 -3171
PubMed 1956033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.95 9.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320611 1 9.93
CHEMBL321214 1 9.78
CHEMBL318812 1 9.71
CHEMBL326640 1 8.54
CHEMBL110808 1 8.24
CHEMBL110339 1 7.90
CHEMBL322582 1 7.55
CHEMBL111529 1 5.01
CHEMBL325322 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320611 Ki = 0.118 nM 9.93
CHEMBL321214 Ki = 0.166 nM 9.78
CHEMBL318812 Ki = 0.197 nM 9.71
CHEMBL326640 Ki = 2.87 nM 8.54
CHEMBL110808 Ki = 5.73 nM 8.24
CHEMBL110339 Ki = 12.7 nM 7.90
CHEMBL322582 Ki = 27.9 nM 7.55
CHEMBL111529 Ki = 9810.0 nM 5.01
CHEMBL325322 Ki = 12500.0 nM 4.90