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Assay Detail

CHEMBL869799

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

Functional
Spasmolytic activity in Wistar rat ileum
40
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Ileum
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Design, microwave-assisted synthesis, and spasmolytic activity of 2-(alkyloxyaryl)-1H-benzimidazole derivatives as constrained stilbene bioisosteres.
Navarrete-Vázquez G, Moreno-Diaz H, Aguirre-Crespo F, León-Rivera I, Villalobos-Molina R, Muñoz-Muñiz O, Estrada-Soto S, Estrada-Soto S.
Bioorg Med Chem Lett (2006) 16 : 4169 -4173
PubMed 16784847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.21 5.92
Emax 20 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385136 2 5.92
CHEMBL19224 PAPAVERINE 3.0 2 5.81
CHEMBL209913 2 5.76
CHEMBL209470 2 5.75
CHEMBL209734 2 5.72
CHEMBL377207 2 5.71
CHEMBL378887 2 5.47
CHEMBL209200 2 5.40
CHEMBL203360 2 5.29
CHEMBL377740 2 5.28
CHEMBL209469 2 5.25
CHEMBL426871 2 5.23
CHEMBL209369 2 5.11
CHEMBL379179 2 4.97
CHEMBL380245 2 4.82
CHEMBL209552 2 4.55
CHEMBL209544 2 4.52
CHEMBL379880 2 4.23
CHEMBL209918 2 4.11
CHEMBL379376 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385136 IC50 = 1190.0 nM 5.92
CHEMBL19224 PAPAVERINE IC50 = 1550.0 nM 5.81
CHEMBL209913 IC50 = 1720.0 nM 5.76
CHEMBL209470 IC50 = 1800.0 nM 5.75
CHEMBL209734 IC50 = 1900.0 nM 5.72
CHEMBL377207 IC50 = 1940.0 nM 5.71
CHEMBL378887 IC50 = 3400.0 nM 5.47
CHEMBL209200 IC50 = 4000.0 nM 5.40
CHEMBL203360 IC50 = 5150.0 nM 5.29
CHEMBL377740 IC50 = 5250.0 nM 5.28
CHEMBL209469 IC50 = 5600.0 nM 5.25
CHEMBL426871 IC50 = 5830.0 nM 5.23
CHEMBL209369 IC50 = 7700.0 nM 5.11
CHEMBL379179 IC50 = 10600.0 nM 4.97
CHEMBL380245 IC50 = 15000.0 nM 4.82
CHEMBL209552 IC50 = 28200.0 nM 4.55
CHEMBL209544 IC50 = 30000.0 nM 4.52
CHEMBL379880 IC50 = 59000.0 nM 4.23
CHEMBL209918 IC50 = 78600.0 nM 4.11
CHEMBL377207 Emax = 50.0 % -
CHEMBL209734 Emax = 80.0 % -
CHEMBL209552 Emax = 51.4 % -
CHEMBL379880 Emax = 38.2 % -
CHEMBL380245 Emax = 47.7 % -
CHEMBL209918 Emax = 11.1 % -
CHEMBL377740 Emax = 61.2 % -
CHEMBL379179 Emax = 54.9 % -
CHEMBL209369 Emax = 52.8 % -
CHEMBL385136 Emax = 70.0 % -
CHEMBL209469 Emax = 55.0 % -
CHEMBL209470 Emax = 65.0 % -
CHEMBL209200 Emax = 90.0 % -
CHEMBL378887 Emax = 59.0 % -
CHEMBL379376 Emax = 50.0 % -
CHEMBL209913 Emax = 60.0 % -
CHEMBL426871 Emax = 93.5 % -
CHEMBL19224 PAPAVERINE Emax = 96.7 % -
CHEMBL209544 Emax = 34.9 % -
CHEMBL203360 Emax = 42.4 % -
CHEMBL379376 IC50 = 190000.0 nM -