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Assay Detail

CHEMBL746308

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

Binding
Ability to displace [3H]- pirenzepine from M1 receptor in rat hippocampal membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Acylhydrazones as M1/M3 selective muscarinic agonists
Wu ES, Kover A, Loch JT, Rosenberg L, Semus SF, Verhoest PR, Gordon JC, Machulskis AC, McCreedy SA, Zongrone J, Blosser JC
Bioorg Med Chem Lett (1996) 6 : 2525 -2530
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 4.62 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40121 1 5.42
CHEMBL312957 1 5.32
CHEMBL313565 1 5.10
CHEMBL81954 1 5.06
CHEMBL420596 1 5.05
CHEMBL84985 1 5.02
CHEMBL84109 1 5.00
CHEMBL85952 1 4.87
CHEMBL314796 1 4.84
CHEMBL82012 1 4.82
CHEMBL278681 1 4.80
CHEMBL314421 1 4.60
CHEMBL418933 1 4.60
CHEMBL83410 1 4.60
CHEMBL85729 1 4.55
CHEMBL85999 1 4.52
CHEMBL85953 1 4.52
CHEMBL84135 1 4.47
CHEMBL84222 1 4.42
CHEMBL432186 1 4.39
CHEMBL84278 1 4.22
CHEMBL83905 1 4.19
CHEMBL84825 1 4.12
CHEMBL421531 1 4.11
CHEMBL86224 1 4.05
CHEMBL83874 1 4.00
CHEMBL312200 1 4.00
CHEMBL315347 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40121 Ki = 3800.0 nM 5.42
CHEMBL312957 Ki = 4800.0 nM 5.32
CHEMBL313565 Ki = 8000.0 nM 5.10
CHEMBL81954 Ki = 8800.0 nM 5.06
CHEMBL420596 Ki = 9000.0 nM 5.05
CHEMBL84985 Ki = 9500.0 nM 5.02
CHEMBL84109 Ki = 10000.0 nM 5.00
CHEMBL85952 Ki = 13600.0 nM 4.87
CHEMBL314796 Ki = 14400.0 nM 4.84
CHEMBL82012 Ki = 15200.0 nM 4.82
CHEMBL278681 Ki = 16000.0 nM 4.80
CHEMBL314421 Ki = 25000.0 nM 4.60
CHEMBL418933 Ki = 25000.0 nM 4.60
CHEMBL83410 Ki = 25000.0 nM 4.60
CHEMBL85729 Ki = 28000.0 nM 4.55
CHEMBL85999 Ki = 30000.0 nM 4.52
CHEMBL85953 Ki = 30000.0 nM 4.52
CHEMBL84135 Ki = 34000.0 nM 4.47
CHEMBL84222 Ki = 38000.0 nM 4.42
CHEMBL432186 Ki = 41000.0 nM 4.39
CHEMBL84278 Ki = 60000.0 nM 4.22
CHEMBL83905 Ki = 65000.0 nM 4.19
CHEMBL84825 Ki = 76000.0 nM 4.12
CHEMBL421531 Ki = 78000.0 nM 4.11
CHEMBL86224 Ki = 90000.0 nM 4.05
CHEMBL83874 Ki = 100000.0 nM 4.00
CHEMBL312200 Ki = 100000.0 nM 4.00
CHEMBL315347 Ki = 180000.0 nM -