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Assay Detail

CHEMBL863987

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

Functional
Antagonism at muscarinic M2 receptor in isolated guinea pig urinary bladder
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.
Starck JP, Talaga P, Quéré L, Collart P, Christophe B, Lo Brutto P, Jadot S, Chimmanamada D, Zanda M, Wagner A, Mioskowski C, Massingham R, Guyaux M.
Bioorg Med Chem Lett (2006) 16 : 373 -377
PubMed 16275087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 8.40 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381623 1 9.30
CHEMBL370232 1 9.30
CHEMBL200319 1 9.10
CHEMBL200693 1 9.10
CHEMBL200171 1 9.10
CHEMBL382213 1 8.70
CHEMBL200957 1 8.50
CHEMBL201933 1 8.20
CHEMBL1346 DARIFENACIN 4.0 1 7.80
CHEMBL1382 TOLTERODINE 4.0 1 7.80
CHEMBL200210 1 7.50
CHEMBL1231 OXYBUTYNIN 4.0 1 7.40
CHEMBL372566 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381623 Kd = 0.5012 nM 9.30
CHEMBL370232 Kd = 0.5012 nM 9.30
CHEMBL200319 Kd = 0.7943 nM 9.10
CHEMBL200693 Kd = 0.7943 nM 9.10
CHEMBL200171 Kd = 0.7943 nM 9.10
CHEMBL382213 Kd = 1.995 nM 8.70
CHEMBL200957 Kd = 3.162 nM 8.50
CHEMBL201933 Kd = 6.31 nM 8.20
CHEMBL1346 DARIFENACIN Kd = 15.85 nM 7.80
CHEMBL1382 TOLTERODINE Kd = 15.85 nM 7.80
CHEMBL200210 Kd = 31.62 nM 7.50
CHEMBL1231 OXYBUTYNIN Kd = 39.81 nM 7.40
CHEMBL372566 Kd = 39.81 nM 7.40