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Assay Detail

CHEMBL753100

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Functional
Antagonist activity against Nicotinic acetylcholine receptor (nAChR) of isolated Frog rectus Abdominis Muscle
18
Total Activities
18
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. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.
Bolognesi ML, Bixel MG, Marucci G, Bartolini M, Krauss M, Angeli P, Antonello A, Rosini M, Tumiatti V, Hucho F, Melchiorre C.
J Med Chem (2002) 45 : 3286 -3295
PubMed 12109912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.31 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55587 1 7.02
CHEMBL323655 1 6.80
CHEMBL324975 1 6.77
CHEMBL430708 1 6.72
CHEMBL110308 1 6.64
CHEMBL325740 1 6.62
CHEMBL111404 1 6.49
CHEMBL326532 1 6.48
CHEMBL324001 1 6.35
CHEMBL300930 1 6.30
CHEMBL110045 1 6.28
CHEMBL327100 1 6.23
CHEMBL325505 1 6.15
CHEMBL298833 TRIPHENYLMETHYLPHOSPHONIUM BROMIDE 1 6.05
CHEMBL27673 METHOCTRAMINE 1 5.93
CHEMBL111324 1 5.92
CHEMBL325994 1 5.46
CHEMBL322731 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55587 IC50 = 95.5 nM 7.02
CHEMBL323655 IC50 = 158.49 nM 6.80
CHEMBL324975 IC50 = 169.82 nM 6.77
CHEMBL430708 IC50 = 190.55 nM 6.72
CHEMBL110308 IC50 = 229.09 nM 6.64
CHEMBL325740 IC50 = 239.88 nM 6.62
CHEMBL111404 IC50 = 323.59 nM 6.49
CHEMBL326532 IC50 = 331.13 nM 6.48
CHEMBL324001 IC50 = 446.68 nM 6.35
CHEMBL300930 IC50 = 501.19 nM 6.30
CHEMBL110045 IC50 = 524.81 nM 6.28
CHEMBL327100 IC50 = 588.84 nM 6.23
CHEMBL325505 IC50 = 707.95 nM 6.15
CHEMBL298833 TRIPHENYLMETHYLPHOSPHONIUM BROMIDE IC50 = 891.25 nM 6.05
CHEMBL27673 METHOCTRAMINE IC50 = 1174.9 nM 5.93
CHEMBL111324 IC50 = 1202.26 nM 5.92
CHEMBL325994 IC50 = 3467.37 nM 5.46
CHEMBL322731 IC50 = 4265.8 nM 5.37