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Assay Detail

CHEMBL686245

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

Functional
Antimuscarinic activity was assayed for its ability to block the acetyl-choline induced contraction of the guinea pig ileum
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 1 — Organism
Curated By Intermediate

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
Carroll FI, Abraham P, Parham K, Griffith RC, Ahmad A, Richard MM, Padilla FN, Witkin JM, Chiang PK.
J Med Chem (1987) 30 : 805 -809
PubMed 3494849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 7.99 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287868 AZAPROPHEN 1 10.40
CHEMBL517712 ATROPINE 4.0 1 8.70
CHEMBL12980 QUINUCLIDINYL BENZILATE 1 8.70
CHEMBL26505 APROFENE 2.0 1 8.50
CHEMBL70352 BENACTYZINE 2.0 1 8.20
CHEMBL353846 ADIPHENINE 2.0 1 7.10
CHEMBL9967 PIRENZEPINE 2.0 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287868 AZAPROPHEN Kd = 0.03981 nM 10.40
CHEMBL517712 ATROPINE Kd = 1.995 nM 8.70
CHEMBL12980 QUINUCLIDINYL BENZILATE Kd = 1.995 nM 8.70
CHEMBL26505 APROFENE Kd = 3.162 nM 8.50
CHEMBL70352 BENACTYZINE Kd = 6.31 nM 8.20
CHEMBL353846 ADIPHENINE Kd = 79.43 nM 7.10
CHEMBL9967 PIRENZEPINE Kd = 50118.72 nM 4.30