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Assay Detail

CHEMBL3091164

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 by SPA method
ChEMBL ↗
69
Total Activities
68
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 design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.
Mete A, Bowers K, Bull RJ, Coope H, Donald DK, Escott KJ, Ford R, Grime K, Mather A, Ray NC, Russell V.
Bioorg Med Chem Lett (2013) 23 : 6248 -6253
PubMed 24144851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 9.26 10.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087959 — — 1 10.50
CHEMBL3087235 — — 1 10.30
CHEMBL3087230 — — 1 10.30
CHEMBL3088086 — — 1 10.20
CHEMBL3088081 — — 1 10.20
CHEMBL3087961 — — 1 10.20
CHEMBL3087957 — — 1 10.10
CHEMBL3088080 — — 1 10.10
CHEMBL3088075 — — 1 10.10
CHEMBL3087949 — — 1 10.00
CHEMBL3087242 — — 1 10.00
CHEMBL3087952 — — 1 10.00
CHEMBL1201335 GLYCOPYRRONIUM 4.0 1 9.90
CHEMBL3087238 — — 1 9.90
CHEMBL3088085 — — 1 9.90
CHEMBL3088084 — — 1 9.80
CHEMBL3087368 — — 1 9.80
CHEMBL3087367 — — 1 9.80
CHEMBL3087241 — — 1 9.80
CHEMBL3087953 — — 1 9.80
CHEMBL3087232 — — 1 9.80
CHEMBL3087362 — — 1 9.80
CHEMBL3087364 — — 1 9.70
CHEMBL3087236 — — 1 9.70
CHEMBL3087946 — — 1 9.70
CHEMBL3087960 — — 1 9.60
CHEMBL3087370 — — 1 9.60
CHEMBL3087237 — — 1 9.60
CHEMBL3087375 — — 1 9.60
CHEMBL3087954 — — 1 9.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087959 — IC50 = 0.03162 nM 10.50
CHEMBL3087235 — IC50 = 0.05012 nM 10.30
CHEMBL3087230 — IC50 = 0.05012 nM 10.30
CHEMBL3088086 — IC50 = 0.0631 nM 10.20
CHEMBL3088081 — IC50 = 0.0631 nM 10.20
CHEMBL3087961 — IC50 = 0.0631 nM 10.20
CHEMBL3087957 — IC50 = 0.07943 nM 10.10
CHEMBL3088080 — IC50 = 0.07943 nM 10.10
CHEMBL3088075 — IC50 = 0.07943 nM 10.10
CHEMBL3087949 — IC50 = 0.1 nM 10.00
CHEMBL3087952 — IC50 = 0.1 nM 10.00
CHEMBL3087242 — IC50 = 0.1 nM 10.00
CHEMBL3088085 — IC50 = 0.1259 nM 9.90
CHEMBL3087238 — IC50 = 0.1259 nM 9.90
CHEMBL1201335 GLYCOPYRRONIUM IC50 = 0.1259 nM 9.90
CHEMBL3088084 — IC50 = 0.1585 nM 9.80
CHEMBL3087362 — IC50 = 0.1585 nM 9.80
CHEMBL3087232 — IC50 = 0.1585 nM 9.80
CHEMBL3087953 — IC50 = 0.1585 nM 9.80
CHEMBL3087241 — IC50 = 0.1585 nM 9.80
CHEMBL3087367 — IC50 = 0.1585 nM 9.80
CHEMBL3087368 — IC50 = 0.1585 nM 9.80
CHEMBL3087364 — IC50 = 0.1995 nM 9.70
CHEMBL3087236 — IC50 = 0.1995 nM 9.70
CHEMBL3087946 — IC50 = 0.1995 nM 9.70
CHEMBL3087960 — IC50 = 0.2512 nM 9.60
CHEMBL3087954 — IC50 = 0.2512 nM 9.60
CHEMBL3087375 — IC50 = 0.2512 nM 9.60
CHEMBL3087370 — IC50 = 0.2512 nM 9.60
CHEMBL3087237 — IC50 = 0.2512 nM 9.60
CHEMBL3087958 — IC50 = 0.3162 nM 9.50
CHEMBL3087244 — IC50 = 0.3981 nM 9.40
CHEMBL3087955 — IC50 = 0.3981 nM 9.40
CHEMBL3087377 — IC50 = 0.3981 nM 9.40
CHEMBL3087371 — IC50 = 0.5012 nM 9.30
CHEMBL3087234 — IC50 = 0.5012 nM 9.30
CHEMBL3087366 — IC50 = 0.631 nM 9.20
CHEMBL3087948 — IC50 = 0.631 nM 9.20
CHEMBL3087372 — IC50 = 0.631 nM 9.20
CHEMBL3087947 — IC50 = 0.7943 nM 9.10
CHEMBL3087373 — IC50 = 0.7943 nM 9.10
CHEMBL3087376 — IC50 = 0.7943 nM 9.10
CHEMBL3087379 — IC50 = 0.7943 nM 9.10
CHEMBL3087378 — IC50 = 1.0 nM 9.00
CHEMBL3087233 — IC50 = 1.0 nM 9.00
CHEMBL3087945 — IC50 = 2.512 nM 8.60
CHEMBL3088076 — IC50 = 2.512 nM 8.60
CHEMBL3087374 — IC50 = 2.512 nM 8.60
CHEMBL3087365 — IC50 = 2.512 nM 8.60
CHEMBL3087950 — IC50 = 3.162 nM 8.50