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Assay Detail

CHEMBL1924273

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

Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
85
Total Activities
85
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of AZD9164, a novel muscarinic M3 antagonist.
Mete A, Bowers K, Chevalier E, Donald DK, Edwards H, Escott KJ, Ford R, Grime K, Millichip I, Teobald B, Russell V.
Bioorg Med Chem Lett (2011) 21 : 7440 -7446
PubMed 22047691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 85 9.28 10.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1924027 1 10.50
CHEMBL1921908 1 10.30
CHEMBL1924040 1 10.30
CHEMBL1921925 1 10.20
CHEMBL1921907 1 10.20
CHEMBL1921935 1 10.20
CHEMBL1921917 1 10.10
CHEMBL1921937 1 10.10
CHEMBL1921945 1 10.00
CHEMBL1922053 1 10.00
CHEMBL1924036 1 10.00
CHEMBL1921946 1 9.90
CHEMBL1924049 1 9.90
CHEMBL1921919 1 9.90
CHEMBL1921941 1 9.90
CHEMBL1921918 1 9.80
CHEMBL1924025 1 9.80
CHEMBL1922051 1 9.80
CHEMBL1921904 AZD-9164 2.0 1 9.80
CHEMBL1922054 1 9.80
CHEMBL1921911 1 9.80
CHEMBL1922050 1 9.70
CHEMBL1921944 1 9.70
CHEMBL1921914 1 9.70
CHEMBL1921943 1 9.70
CHEMBL1921927 1 9.70
CHEMBL1921910 1 9.70
CHEMBL1922055 1 9.70
CHEMBL1921942 1 9.70
CHEMBL1921940 1 9.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1924027 IC50 = 0.03162 nM 10.50
CHEMBL1921908 IC50 = 0.05012 nM 10.30
CHEMBL1924040 IC50 = 0.05012 nM 10.30
CHEMBL1921925 IC50 = 0.0631 nM 10.20
CHEMBL1921907 IC50 = 0.0631 nM 10.20
CHEMBL1921935 IC50 = 0.0631 nM 10.20
CHEMBL1921917 IC50 = 0.07943 nM 10.10
CHEMBL1921937 IC50 = 0.07943 nM 10.10
CHEMBL1924036 IC50 = 0.1 nM 10.00
CHEMBL1921945 IC50 = 0.1 nM 10.00
CHEMBL1922053 IC50 = 0.1 nM 10.00
CHEMBL1921941 IC50 = 0.1259 nM 9.90
CHEMBL1921919 IC50 = 0.1259 nM 9.90
CHEMBL1924049 IC50 = 0.1259 nM 9.90
CHEMBL1921946 IC50 = 0.1259 nM 9.90
CHEMBL1921918 IC50 = 0.1585 nM 9.80
CHEMBL1921911 IC50 = 0.1585 nM 9.80
CHEMBL1922054 IC50 = 0.1585 nM 9.80
CHEMBL1921904 AZD-9164 IC50 = 0.1585 nM 9.80
CHEMBL1922051 IC50 = 0.1585 nM 9.80
CHEMBL1924025 IC50 = 0.1585 nM 9.80
CHEMBL1922052 IC50 = 0.1995 nM 9.70
CHEMBL1921940 IC50 = 0.1995 nM 9.70
CHEMBL1921942 IC50 = 0.1995 nM 9.70
CHEMBL1922055 IC50 = 0.1995 nM 9.70
CHEMBL1921927 IC50 = 0.1995 nM 9.70
CHEMBL1921943 IC50 = 0.1995 nM 9.70
CHEMBL1921914 IC50 = 0.1995 nM 9.70
CHEMBL1921944 IC50 = 0.1995 nM 9.70
CHEMBL1922050 IC50 = 0.1995 nM 9.70
CHEMBL1921910 IC50 = 0.1995 nM 9.70
CHEMBL1201335 GLYCOPYRRONIUM IC50 = 0.2512 nM 9.60
CHEMBL1921928 IC50 = 0.2512 nM 9.60
CHEMBL1922058 IC50 = 0.2512 nM 9.60
CHEMBL1924029 IC50 = 0.2512 nM 9.60
CHEMBL1921921 IC50 = 0.3162 nM 9.50
CHEMBL1921924 IC50 = 0.3162 nM 9.50
CHEMBL1922056 IC50 = 0.3162 nM 9.50
CHEMBL1921932 IC50 = 0.3162 nM 9.50
CHEMBL1922057 IC50 = 0.3981 nM 9.40
CHEMBL1921926 IC50 = 0.3981 nM 9.40
CHEMBL1921939 IC50 = 0.5012 nM 9.30
CHEMBL1924046 IC50 = 0.631 nM 9.20
CHEMBL1921929 IC50 = 0.631 nM 9.20
CHEMBL1921936 IC50 = 0.631 nM 9.20
CHEMBL1924031 IC50 = 0.7943 nM 9.10
CHEMBL1924030 IC50 = 0.7943 nM 9.10
CHEMBL1921938 IC50 = 0.7943 nM 9.10
CHEMBL1924033 IC50 = 1.0 nM 9.00
CHEMBL1922049 IC50 = 1.0 nM 9.00