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Assay Detail

CHEMBL752969

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

Binding
Binding affinity towards human muscarinic M2 receptor in CHO-KI cells using [3H]- QNB as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-KI
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.
Doller D, Chackalamannil S, Czarniecki M, McQuade R, Ruperto V.
Bioorg Med Chem Lett (1999) 9 : 901 -906
PubMed 10206558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.75 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354636 1 7.89
CHEMBL353311 1 7.58
CHEMBL355854 1 7.49
CHEMBL277642 HIMBACINE 1 7.32
CHEMBL352618 1 7.29
CHEMBL172646 1 6.83
CHEMBL352756 1 6.74
CHEMBL170977 1 6.72
CHEMBL426032 1 6.68
CHEMBL352596 1 6.65
CHEMBL366819 1 6.56
CHEMBL172969 1 6.55
CHEMBL355475 1 6.51
CHEMBL170205 1 6.45
CHEMBL354934 1 6.42
CHEMBL366640 1 6.31
CHEMBL171520 1 6.28
CHEMBL355193 1 6.24
CHEMBL170922 1 6.22
CHEMBL172272 1 6.19
CHEMBL445134 1 -
CHEMBL173950 1 -
CHEMBL423438 1 -
CHEMBL368990 1 -
CHEMBL173155 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354636 Ki = 13.0 nM 7.89
CHEMBL353311 Ki = 26.0 nM 7.58
CHEMBL355854 Ki = 32.2 nM 7.49
CHEMBL277642 HIMBACINE Ki = 48.4 nM 7.32
CHEMBL352618 Ki = 51.0 nM 7.29
CHEMBL172646 Ki = 148.0 nM 6.83
CHEMBL352756 Ki = 184.0 nM 6.74
CHEMBL170977 Ki = 189.0 nM 6.72
CHEMBL426032 Ki = 209.0 nM 6.68
CHEMBL352596 Ki = 224.0 nM 6.65
CHEMBL366819 Ki = 275.0 nM 6.56
CHEMBL172969 Ki = 283.0 nM 6.55
CHEMBL355475 Ki = 312.0 nM 6.51
CHEMBL170205 Ki = 352.0 nM 6.45
CHEMBL354934 Ki = 376.0 nM 6.42
CHEMBL366640 Ki = 485.0 nM 6.31
CHEMBL171520 Ki = 520.0 nM 6.28
CHEMBL355193 Ki = 570.0 nM 6.24
CHEMBL170922 Ki = 595.0 nM 6.22
CHEMBL172272 Ki = 650.0 nM 6.19
CHEMBL445134 Ki > 280.0 nM -
CHEMBL173950 Ki > 500.0 nM -
CHEMBL423438 Ki > 500.0 nM -
CHEMBL368990 Ki > 500.0 nM -
CHEMBL173155 Ki > 42.0 nM -