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Assay Detail

CHEMBL753101

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Functional
Antagonism of carbachol action on nAChR of isolated frog rectus abdominus.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism frog
Tissue Rectus abdominis muscle
Confidence 0 — Uncurated / Unknown
Curated By Expert

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 2. Role of polymethylene chain lengths separating amine functions and of substituents on the terminal nitrogen atoms.
Rosini M, Bixel MG, Marucci G, Budriesi R, Krauss M, Bolognesi ML, Minarini A, Tumiatti V, Hucho F, Melchiorre C.
J Med Chem (2002) 45 : 1860 -1878
PubMed 11960498 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.11 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55343 1 7.11
CHEMBL55587 1 7.02
CHEMBL292391 1 6.68
CHEMBL55463 1 6.66
CHEMBL51850 1 6.44
CHEMBL54725 1 6.43
CHEMBL56043 1 6.42
CHEMBL54113 1 6.39
CHEMBL55568 1 6.31
CHEMBL300930 1 6.30
CHEMBL55549 1 6.30
CHEMBL293128 1 6.27
CHEMBL52619 1 6.21
CHEMBL54680 1 6.17
CHEMBL54469 METHYLTRIPHENYLPHOSPHONIUM BROMIDE 1 6.05
CHEMBL27673 METHOCTRAMINE 1 5.93
CHEMBL294613 1 5.88
CHEMBL300964 1 5.80
CHEMBL27739 1 5.62
CHEMBL55765 1 5.48
CHEMBL55333 1 5.36
CHEMBL294865 1 5.14
CHEMBL55975 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55343 IC50 = 77.62 nM 7.11
CHEMBL55587 IC50 = 95.5 nM 7.02
CHEMBL292391 IC50 = 208.93 nM 6.68
CHEMBL55463 IC50 = 218.78 nM 6.66
CHEMBL51850 IC50 = 363.08 nM 6.44
CHEMBL54725 IC50 = 371.54 nM 6.43
CHEMBL56043 IC50 = 380.19 nM 6.42
CHEMBL54113 IC50 = 407.38 nM 6.39
CHEMBL55568 IC50 = 489.78 nM 6.31
CHEMBL300930 IC50 = 501.19 nM 6.30
CHEMBL55549 IC50 = 501.19 nM 6.30
CHEMBL293128 IC50 = 537.03 nM 6.27
CHEMBL52619 IC50 = 616.6 nM 6.21
CHEMBL54680 IC50 = 676.08 nM 6.17
CHEMBL54469 METHYLTRIPHENYLPHOSPHONIUM BROMIDE IC50 = 891.25 nM 6.05
CHEMBL27673 METHOCTRAMINE IC50 = 1174.9 nM 5.93
CHEMBL294613 IC50 = 1318.26 nM 5.88
CHEMBL300964 IC50 = 1584.89 nM 5.80
CHEMBL27739 IC50 = 2398.83 nM 5.62
CHEMBL55765 IC50 = 3311.31 nM 5.48
CHEMBL55333 IC50 = 4365.16 nM 5.36
CHEMBL294865 IC50 = 7244.36 nM 5.14
CHEMBL55975 IC50 = 23988.33 nM 4.62