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Assay Detail

CHEMBL745670

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

Binding
Displacement of [3H]pirenzepine binding at Muscarinic acetylcholine receptor M1 in rat brain P2 membranes.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.
Kline RH, Izenwasser S, Katz JL, Joseph DB, Bowen WD, Newman AH.
J Med Chem (1997) 40 : 851 -857
PubMed 9083473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 9.10 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084910 1 9.39
CHEMBL3084869 1 9.37
CHEMBL3084878 1 9.30
CHEMBL1201203 BENZTROPINE 4.0 1 9.23
CHEMBL3084907 1 9.22
CHEMBL3084909 1 9.07
CHEMBL3084870 1 9.01
CHEMBL3084891 AMINOBENZTROPINE 1 8.95
CHEMBL310310 1 8.83
CHEMBL3084901 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084910 Ki = 0.41 nM 9.39
CHEMBL3084869 Ki = 0.43 nM 9.37
CHEMBL3084878 Ki = 0.5 nM 9.30
CHEMBL1201203 BENZTROPINE Ki = 0.59 nM 9.23
CHEMBL3084907 Ki = 0.6 nM 9.22
CHEMBL3084909 Ki = 0.85 nM 9.07
CHEMBL3084870 Ki = 0.98 nM 9.01
CHEMBL3084891 AMINOBENZTROPINE Ki = 1.12 nM 8.95
CHEMBL310310 Ki = 1.48 nM 8.83
CHEMBL3084901 Ki = 2.52 nM 8.60