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Assay Detail

CHEMBL745680

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

Binding
Displacement of [3H]pirenzepine from M1 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Büttelmann B, Alanine A, Bourson A, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.
Bioorg Med Chem Lett (2003) 13 : 829 -832
PubMed 12617901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.80 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL167004 1 6.82
CHEMBL169469 1 6.29
CHEMBL169695 1 6.06
CHEMBL354482 1 5.96
CHEMBL166599 1 5.92
CHEMBL166991 1 5.72
CHEMBL166935 1 5.60
CHEMBL166697 1 5.58
CHEMBL170552 1 5.42
CHEMBL299294 1 5.21
CHEMBL168496 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL167004 Ki = 150.0 nM 6.82
CHEMBL169469 Ki = 510.0 nM 6.29
CHEMBL169695 Ki = 870.0 nM 6.06
CHEMBL354482 Ki = 1100.0 nM 5.96
CHEMBL166599 Ki = 1200.0 nM 5.92
CHEMBL166991 Ki = 1900.0 nM 5.72
CHEMBL166935 Ki = 2500.0 nM 5.60
CHEMBL166697 Ki = 2600.0 nM 5.58
CHEMBL170552 Ki = 3800.0 nM 5.42
CHEMBL299294 Ki = 6100.0 nM 5.21
CHEMBL168496 Ki = 6500.0 nM 5.19