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Assay Detail

CHEMBL745743

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

Binding
Binding affinity towards human muscarinic M1 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 M1 (CHEMBL216)
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 6.58 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355854 1 8.37
CHEMBL277642 HIMBACINE 1 8.35
CHEMBL354636 1 7.42
CHEMBL353311 1 6.87
CHEMBL170977 1 6.75
CHEMBL352618 1 6.65
CHEMBL352756 1 6.52
CHEMBL172272 1 6.51
CHEMBL426032 1 6.47
CHEMBL355193 1 6.45
CHEMBL355475 1 6.42
CHEMBL366819 1 6.40
CHEMBL352596 1 6.38
CHEMBL170205 1 6.37
CHEMBL366640 1 6.35
CHEMBL171520 1 6.33
CHEMBL172969 1 6.26
CHEMBL170922 1 6.24
CHEMBL173950 1 6.24
CHEMBL354934 1 6.22
CHEMBL368990 1 6.07
CHEMBL423438 1 5.87
CHEMBL172646 1 5.81
CHEMBL445134 1 -
CHEMBL173155 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355854 Ki = 4.3 nM 8.37
CHEMBL277642 HIMBACINE Ki = 4.5 nM 8.35
CHEMBL354636 Ki = 38.0 nM 7.42
CHEMBL353311 Ki = 136.0 nM 6.87
CHEMBL170977 Ki = 179.0 nM 6.75
CHEMBL352618 Ki = 222.0 nM 6.65
CHEMBL352756 Ki = 304.0 nM 6.52
CHEMBL172272 Ki = 312.0 nM 6.51
CHEMBL426032 Ki = 341.0 nM 6.47
CHEMBL355193 Ki = 353.0 nM 6.45
CHEMBL355475 Ki = 376.0 nM 6.42
CHEMBL366819 Ki = 399.0 nM 6.40
CHEMBL352596 Ki = 416.0 nM 6.38
CHEMBL170205 Ki = 427.0 nM 6.37
CHEMBL366640 Ki = 445.0 nM 6.35
CHEMBL171520 Ki = 464.0 nM 6.33
CHEMBL172969 Ki = 554.0 nM 6.26
CHEMBL170922 Ki = 579.0 nM 6.24
CHEMBL173950 Ki = 581.0 nM 6.24
CHEMBL354934 Ki = 601.0 nM 6.22
CHEMBL368990 Ki = 857.0 nM 6.07
CHEMBL423438 Ki = 1361.0 nM 5.87
CHEMBL172646 Ki = 1533.0 nM 5.81
CHEMBL445134 Ki > 900.0 nM -
CHEMBL173155 Ki > 420.0 nM -