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Assay Detail

CHEMBL678730

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

Functional
Antagonistic activity against isolated frog rectus abdominus muscle (FRA)
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism frog
Tissue Muscle tissue
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, and biological evaluation of symmetrically and unsymmetrically substituted methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists.
Rosini M, Budriesi R, Bixel MG, Bolognesi ML, Chiarini A, Hucho F, Krogsgaard-Larsen P, Mellor IR, Minarini A, Tumiatti V, Usherwood PN, Melchiorre C.
J Med Chem (1999) 42 : 5212 -5223
PubMed 10602706 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.58 6.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553023 1 6.69
CHEMBL342756 1 6.39
CHEMBL542756 1 6.35
CHEMBL553264 1 6.23
CHEMBL540608 1 6.10
CHEMBL554889 1 5.96
CHEMBL1256938 1 5.93
CHEMBL556027 1 5.90
CHEMBL1161299 1 5.82
CHEMBL542512 1 5.79
CHEMBL543452 1 5.75
CHEMBL557429 1 5.64
CHEMBL542982 1 5.61
CHEMBL538292 1 5.60
CHEMBL1161309 1 5.28
CHEMBL552809 1 5.27
CHEMBL543931 1 5.27
CHEMBL557224 1 5.22
CHEMBL542504 1 5.19
CHEMBL552626 1 5.14
CHEMBL147338 1 4.92
CHEMBL542507 1 4.64
CHEMBL555772 1 4.62
CHEMBL542509 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553023 IC50 = 204.17 nM 6.69
CHEMBL342756 IC50 = 407.38 nM 6.39
CHEMBL542756 IC50 = 446.68 nM 6.35
CHEMBL553264 IC50 = 588.84 nM 6.23
CHEMBL540608 IC50 = 794.33 nM 6.10
CHEMBL554889 IC50 = 1096.48 nM 5.96
CHEMBL1256938 IC50 = 1174.9 nM 5.93
CHEMBL556027 IC50 = 1258.93 nM 5.90
CHEMBL1161299 IC50 = 1513.56 nM 5.82
CHEMBL542512 IC50 = 1621.81 nM 5.79
CHEMBL543452 IC50 = 1778.28 nM 5.75
CHEMBL557429 IC50 = 2290.87 nM 5.64
CHEMBL542982 IC50 = 2454.71 nM 5.61
CHEMBL538292 IC50 = 2511.89 nM 5.60
CHEMBL1161309 IC50 = 5248.07 nM 5.28
CHEMBL552809 IC50 = 5370.32 nM 5.27
CHEMBL543931 IC50 = 5370.32 nM 5.27
CHEMBL557224 IC50 = 6025.6 nM 5.22
CHEMBL542504 IC50 = 6456.54 nM 5.19
CHEMBL552626 IC50 = 7244.36 nM 5.14
CHEMBL147338 IC50 = 12022.64 nM 4.92
CHEMBL542507 IC50 = 22908.68 nM 4.64
CHEMBL555772 IC50 = 23988.33 nM 4.62
CHEMBL542509 IC50 = 25118.86 nM 4.60