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Assay Detail

CHEMBL1924278

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

Functional
Antagonist potency at M3 receptor in Dunkin Hartley guinea pig trachea assessed as inhibition of methacholine-induced airway smooth muscle contraction after 1 hr by organ-bath technique
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

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
Kd 47 9.64 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1921917 — — 1 10.70
CHEMBL1922052 — — 1 10.60
CHEMBL1924025 — — 1 10.60
CHEMBL1922051 — — 1 10.50
CHEMBL1921941 — — 1 10.50
CHEMBL1921918 — — 1 10.50
CHEMBL1921919 — — 1 10.50
CHEMBL1924029 — — 1 10.40
CHEMBL1921943 — — 1 10.40
CHEMBL1921904 AZD-9164 2.0 1 10.30
CHEMBL1924047 — — 1 10.30
CHEMBL551466 ACLIDINIUM BROMIDE 4.0 1 10.10
CHEMBL3545181 TIOTROPIUM BROMIDE 4.0 1 10.10
CHEMBL1924050 — — 1 9.90
CHEMBL1921940 — — 1 9.90
CHEMBL1922057 — — 1 9.80
CHEMBL1921916 — — 1 9.80
CHEMBL1921911 — — 1 9.80
CHEMBL1921921 — — 1 9.70
CHEMBL1924048 — — 1 9.70
CHEMBL1921926 — — 1 9.60
CHEMBL1921908 — — 1 9.60
CHEMBL1921909 — — 1 9.60
CHEMBL1924051 — — 1 9.60
CHEMBL1921937 — — 1 9.60
CHEMBL1921935 — — 1 9.60
CHEMBL1921922 — — 1 9.50
CHEMBL1921945 — — 1 9.50
CHEMBL1921906 — — 1 9.50
CHEMBL1921905 — — 1 9.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1921917 — Kd = 0.01995 nM 10.70
CHEMBL1922052 — Kd = 0.02512 nM 10.60
CHEMBL1924025 — Kd = 0.02512 nM 10.60
CHEMBL1922051 — Kd = 0.03162 nM 10.50
CHEMBL1921941 — Kd = 0.03162 nM 10.50
CHEMBL1921918 — Kd = 0.03162 nM 10.50
CHEMBL1921919 — Kd = 0.03162 nM 10.50
CHEMBL1921943 — Kd = 0.03981 nM 10.40
CHEMBL1924029 — Kd = 0.03981 nM 10.40
CHEMBL1921904 AZD-9164 Kd = 0.05012 nM 10.30
CHEMBL1924047 — Kd = 0.05012 nM 10.30
CHEMBL3545181 TIOTROPIUM BROMIDE Kd = 0.07943 nM 10.10
CHEMBL551466 ACLIDINIUM BROMIDE Kd = 0.07943 nM 10.10
CHEMBL1924050 — Kd = 0.1259 nM 9.90
CHEMBL1921940 — Kd = 0.1259 nM 9.90
CHEMBL1922057 — Kd = 0.1585 nM 9.80
CHEMBL1921911 — Kd = 0.1585 nM 9.80
CHEMBL1921916 — Kd = 0.1585 nM 9.80
CHEMBL1921921 — Kd = 0.1995 nM 9.70
CHEMBL1924048 — Kd = 0.1995 nM 9.70
CHEMBL1921935 — Kd = 0.2512 nM 9.60
CHEMBL1921937 — Kd = 0.2512 nM 9.60
CHEMBL1924051 — Kd = 0.2512 nM 9.60
CHEMBL1921908 — Kd = 0.2512 nM 9.60
CHEMBL1921926 — Kd = 0.2512 nM 9.60
CHEMBL1921909 — Kd = 0.2512 nM 9.60
CHEMBL1921922 — Kd = 0.3162 nM 9.50
CHEMBL1921945 — Kd = 0.3162 nM 9.50
CHEMBL1921906 — Kd = 0.3162 nM 9.50
CHEMBL1921905 — Kd = 0.3162 nM 9.50
CHEMBL1922050 — Kd = 0.3162 nM 9.50
CHEMBL1921942 — Kd = 0.3981 nM 9.40
CHEMBL1921915 — Kd = 0.5012 nM 9.30
CHEMBL1201335 GLYCOPYRRONIUM Kd = 0.5012 nM 9.30
CHEMBL1922053 — Kd = 0.5012 nM 9.30
CHEMBL1922058 — Kd = 0.5012 nM 9.30
CHEMBL1921927 — Kd = 0.631 nM 9.20
CHEMBL1921928 — Kd = 0.631 nM 9.20
CHEMBL1921907 — Kd = 0.7943 nM 9.10
CHEMBL1921924 — Kd = 0.7943 nM 9.10
CHEMBL1921944 — Kd = 0.7943 nM 9.10
CHEMBL1922056 — Kd = 1.259 nM 8.90
CHEMBL1921914 — Kd = 1.585 nM 8.80
CHEMBL1922055 — Kd = 1.995 nM 8.70
CHEMBL1921925 — Kd = 3.162 nM 8.50
CHEMBL1922054 — Kd = 3.162 nM 8.50
CHEMBL1921910 — Kd = 5.012 nM 8.30