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Assay Detail

CHEMBL749221

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

Binding
Ability of compound to displace (-)-[3H]3-Quinuclidinyl benzilate (-)-[3H]-QNB from Muscarinic acetylcholine receptors in the heart from Guinea Pig.
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL2094109)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.
Johansson G, Sundquist S, Nordvall G, Nilsson BM, Brisander M, Nilvebrant L, Hacksell U.
J Med Chem (1997) 40 : 3804 -3819
PubMed 9371246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 46 7.17 10.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12980 QUINUCLIDINYL BENZILATE 1 10.35
CHEMBL331497 1 9.14
CHEMBL517712 ATROPINE 4.0 1 9.05
CHEMBL123510 1 8.95
CHEMBL338801 1 8.72
CHEMBL339719 1 8.66
CHEMBL339702 1 8.64
CHEMBL333670 1 8.62
CHEMBL128035 1 8.51
CHEMBL124017 1 8.48
CHEMBL122160 1 8.16
CHEMBL124592 1 8.02
CHEMBL333937 1 7.97
CHEMBL333815 1 7.96
CHEMBL333540 1 7.96
CHEMBL433672 1 7.82
CHEMBL121974 1 7.62
CHEMBL124811 1 7.60
CHEMBL127659 1 7.46
CHEMBL125398 1 7.42
CHEMBL126387 1 7.32
CHEMBL340195 1 6.92
CHEMBL124651 1 6.89
CHEMBL341115 1 6.72
CHEMBL333501 1 6.68
CHEMBL338568 1 6.66
CHEMBL124480 1 6.64
CHEMBL339405 1 6.64
CHEMBL124553 1 6.55
CHEMBL339885 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12980 QUINUCLIDINYL BENZILATE Ki = 0.045 nM 10.35
CHEMBL331497 Ki = 0.72 nM 9.14
CHEMBL517712 ATROPINE Ki = 0.89 nM 9.05
CHEMBL123510 Ki = 1.12 nM 8.95
CHEMBL338801 Ki = 1.9 nM 8.72
CHEMBL339719 Ki = 2.2 nM 8.66
CHEMBL339702 Ki = 2.3 nM 8.64
CHEMBL333670 Ki = 2.4 nM 8.62
CHEMBL128035 Ki = 3.1 nM 8.51
CHEMBL124017 Ki = 3.3 nM 8.48
CHEMBL122160 Ki = 6.9 nM 8.16
CHEMBL124592 Ki = 9.5 nM 8.02
CHEMBL333937 Ki = 10.7 nM 7.97
CHEMBL333815 Ki = 11.0 nM 7.96
CHEMBL333540 Ki = 11.0 nM 7.96
CHEMBL433672 Ki = 15.0 nM 7.82
CHEMBL121974 Ki = 24.0 nM 7.62
CHEMBL124811 Ki = 25.0 nM 7.60
CHEMBL127659 Ki = 35.0 nM 7.46
CHEMBL125398 Ki = 38.0 nM 7.42
CHEMBL126387 Ki = 48.0 nM 7.32
CHEMBL340195 Ki = 120.0 nM 6.92
CHEMBL124651 Ki = 130.0 nM 6.89
CHEMBL341115 Ki = 190.0 nM 6.72
CHEMBL333501 Ki = 210.0 nM 6.68
CHEMBL338568 Ki = 220.0 nM 6.66
CHEMBL124480 Ki = 230.0 nM 6.64
CHEMBL339405 Ki = 230.0 nM 6.64
CHEMBL124553 Ki = 280.0 nM 6.55
CHEMBL339885 Ki = 320.0 nM 6.50
CHEMBL341476 Ki = 390.0 nM 6.41
CHEMBL339305 Ki = 400.0 nM 6.40
CHEMBL433188 Ki = 420.0 nM 6.38
CHEMBL125560 Ki = 460.0 nM 6.34
CHEMBL121945 Ki = 547.0 nM 6.26
CHEMBL124395 Ki = 575.0 nM 6.24
CHEMBL125764 Ki = 620.0 nM 6.21
CHEMBL332303 Ki = 1200.0 nM 5.92
CHEMBL125823 Ki = 1600.0 nM 5.80
CHEMBL124332 Ki = 1900.0 nM 5.72
CHEMBL332731 Ki = 2000.0 nM 5.70
CHEMBL340597 Ki = 2460.0 nM 5.61
CHEMBL124564 Ki = 2530.0 nM 5.60
CHEMBL123691 Ki = 2840.0 nM 5.55
CHEMBL125692 Ki = 3200.0 nM 5.50
CHEMBL338561 Ki = 3600.0 nM 5.44