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Assay Detail

CHEMBL745569

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

Binding
Ability to dissociate radioligand [3H]NMS from muscarinic acetylcholine receptor M2 of porcine heart
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL4781)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique.
Stiefl N, Baumann K.
J Med Chem (2003) 46 : 1390 -1407
PubMed 12672239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 5.90 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL609382 1 7.35
CHEMBL609120 1 7.22
CHEMBL30939 1 7.20
CHEMBL31376 1 7.18
CHEMBL32530 1 7.15
CHEMBL284393 1 7.07
CHEMBL27743 1 6.94
CHEMBL31380 1 6.83
CHEMBL285811 1 6.49
CHEMBL28407 1 6.41
CHEMBL284962 1 6.40
CHEMBL32676 1 6.34
CHEMBL31452 1 6.28
CHEMBL31518 1 6.24
CHEMBL284055 1 6.13
CHEMBL609124 1 6.13
CHEMBL31097 1 6.10
CHEMBL262124 1 6.10
CHEMBL281080 1 6.00
CHEMBL609125 1 6.00
CHEMBL285598 1 5.90
CHEMBL286892 1 5.86
CHEMBL31599 1 5.84
CHEMBL30376 1 5.80
CHEMBL31162 1 5.70
CHEMBL30361 1 5.66
CHEMBL280535 1 5.64
CHEMBL285136 1 5.63
CHEMBL31895 1 5.57
CHEMBL27673 METHOCTRAMINE 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL609382 EC50 = 44.98 nM 7.35
CHEMBL609120 EC50 = 59.98 nM 7.22
CHEMBL30939 EC50 = 63.1 nM 7.20
CHEMBL31376 EC50 = 66.07 nM 7.18
CHEMBL32530 EC50 = 70.79 nM 7.15
CHEMBL284393 EC50 = 85.11 nM 7.07
CHEMBL27743 EC50 = 114.82 nM 6.94
CHEMBL31380 EC50 = 147.91 nM 6.83
CHEMBL285811 EC50 = 323.59 nM 6.49
CHEMBL28407 EC50 = 389.05 nM 6.41
CHEMBL284962 EC50 = 398.11 nM 6.40
CHEMBL32676 EC50 = 457.09 nM 6.34
CHEMBL31452 EC50 = 524.81 nM 6.28
CHEMBL31518 EC50 = 570.16 nM 6.24
CHEMBL609124 EC50 = 739.61 nM 6.13
CHEMBL284055 EC50 = 741.31 nM 6.13
CHEMBL31097 EC50 = 799.83 nM 6.10
CHEMBL262124 EC50 = 794.33 nM 6.10
CHEMBL281080 EC50 = 1000.0 nM 6.00
CHEMBL609125 EC50 = 990.83 nM 6.00
CHEMBL285598 EC50 = 1258.93 nM 5.90
CHEMBL286892 EC50 = 1380.38 nM 5.86
CHEMBL31599 EC50 = 1438.8 nM 5.84
CHEMBL30376 EC50 = 1584.89 nM 5.80
CHEMBL31162 EC50 = 1995.26 nM 5.70
CHEMBL30361 EC50 = 2197.86 nM 5.66
CHEMBL280535 EC50 = 2290.87 nM 5.64
CHEMBL285136 EC50 = 2344.23 nM 5.63
CHEMBL31895 EC50 = 2691.53 nM 5.57
CHEMBL27673 METHOCTRAMINE EC50 = 2999.16 nM 5.52
CHEMBL282782 EC50 = 3801.89 nM 5.42
CHEMBL286686 EC50 = 4497.8 nM 5.35
CHEMBL31103 EC50 = 6025.6 nM 5.22
CHEMBL30264 EC50 = 6760.83 nM 5.17
CHEMBL31915 EC50 = 8810.49 nM 5.05
CHEMBL177732 EC50 = 9772.37 nM 5.01
CHEMBL31475 EC50 = 10000.0 nM 5.00
CHEMBL31336 EC50 = 12105.98 nM 4.92
CHEMBL31533 EC50 = 23988.33 nM 4.62
CHEMBL6966 VERAPAMIL EC50 = 30974.19 nM 4.51
CHEMBL31221 EC50 = 31988.95 nM 4.50
CHEMBL284672 EC50 = 53951.06 nM 4.27
CHEMBL30669 EC50 = 110917.48 nM -
CHEMBL31385 EC50 = 151008.02 nM -