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Assay Detail

CHEMBL858105

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

Functional
Inotropic responses, induced by the compound in electrically paced (Hz) guinea pig left atria
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 1 — Organism
Curated By Intermediate

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
Melchiorre C, Bolognesi ML, Budriesi R, Ghelardini C, Chiarini A, Minarini A, Rosini M, Tumiatti V, Wade EJ.
J Med Chem (2001) 44 : 4035 -4038
PubMed 11708906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 9.15 9.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127273 PIPERTRAMINE 1 9.65
CHEMBL129680 1 9.47
CHEMBL130835 PIPERTRAMINE AMIDE 1 9.40
CHEMBL340804 1 9.28
CHEMBL128786 1 9.22
CHEMBL128493 1 8.89
CHEMBL128365 ARECAIDINE PROPARGYL ESTER 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127273 PIPERTRAMINE EC50 = 0.2239 nM 9.65
CHEMBL129680 EC50 = 0.3388 nM 9.47
CHEMBL130835 PIPERTRAMINE AMIDE EC50 = 0.3981 nM 9.40
CHEMBL340804 EC50 = 0.5248 nM 9.28
CHEMBL128786 EC50 = 0.6026 nM 9.22
CHEMBL128493 EC50 = 1.288 nM 8.89
CHEMBL128365 ARECAIDINE PROPARGYL ESTER EC50 = 7.079 nM 8.15