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Assay Detail

CHEMBL2215570

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Binding
Binding affinity to M4 muscarinic receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A σ(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
Banister SD, Manoli M, Doddareddy MR, Hibbs DE, Kassiou M.
Bioorg Med Chem Lett (2012) 22 : 6053 -6058
PubMed 22959245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 5.90 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2205812 1 6.33
CHEMBL2205823 1 6.29
CHEMBL2205825 1 6.18
CHEMBL2205836 1 6.16
CHEMBL2205811 1 6.01
CHEMBL2205817 1 5.95
CHEMBL2205827 1 5.91
CHEMBL2205829 1 5.88
CHEMBL1189234 1 5.85
CHEMBL2205813 1 5.63
CHEMBL2205816 1 5.53
CHEMBL2205832 1 5.09
CHEMBL2205835 1 -
CHEMBL2205818 1 -
CHEMBL2205815 1 -
CHEMBL2205830 1 -
CHEMBL2205828 1 -
CHEMBL2205826 1 -
CHEMBL1779060 1 -
CHEMBL1779059 1 -
CHEMBL1779058 1 -
CHEMBL602850 1 -
CHEMBL2205831 1 -
CHEMBL2205820 1 -
CHEMBL2205821 1 -
CHEMBL2205819 1 -
CHEMBL2205834 1 -
CHEMBL608560 1 -
CHEMBL2205822 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2205812 Ki = 470.0 nM 6.33
CHEMBL2205823 Ki = 514.0 nM 6.29
CHEMBL2205825 Ki = 659.0 nM 6.18
CHEMBL2205836 Ki = 685.0 nM 6.16
CHEMBL2205811 Ki = 977.0 nM 6.01
CHEMBL2205817 Ki = 1118.0 nM 5.95
CHEMBL2205827 Ki = 1233.0 nM 5.91
CHEMBL2205829 Ki = 1302.0 nM 5.88
CHEMBL1189234 Ki = 1415.0 nM 5.85
CHEMBL2205813 Ki = 2338.0 nM 5.63
CHEMBL2205816 Ki = 2961.0 nM 5.53
CHEMBL2205832 Ki = 8135.0 nM 5.09
CHEMBL2205835 Ki - -
CHEMBL2205818 Ki - -
CHEMBL2205815 Ki - -
CHEMBL2205830 Ki - -
CHEMBL2205828 Ki - -
CHEMBL2205826 Ki - -
CHEMBL1779060 Ki - -
CHEMBL1779059 Ki - -
CHEMBL1779058 Ki - -
CHEMBL602850 Ki - -
CHEMBL2205831 Ki - -
CHEMBL2205820 Ki - -
CHEMBL2205821 Ki - -
CHEMBL2205819 Ki - -
CHEMBL2205834 Ki - -
CHEMBL608560 Ki - -
CHEMBL2205822 Ki - -