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Assay Detail

CHEMBL1685249

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

Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Trachea
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL5414)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Discovery of substituted phenyl urea derivatives as novel long-acting β2-adrenoreceptor agonists.
Pérez D, Crespo M, Solé L, Prat M, Carcasona C, Calama E, Otal R, Gavaldá A, Gómez-Angelats M, Miralpeix M, Puig C.
Bioorg Med Chem Lett (2011) 21 : 1545 -1548
PubMed 21277205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 9.54 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1682213 1 10.30
CHEMBL1682210 1 10.15
CHEMBL1682212 1 10.05
CHEMBL1682214 1 9.89
CHEMBL1682211 1 9.70
CHEMBL1682215 1 9.70
CHEMBL1682216 1 9.70
CHEMBL1682217 1 9.70
CHEMBL1682218 1 9.70
CHEMBL1682219 1 9.15
CHEMBL1682302 1 9.05
CHEMBL1682221 1 9.00
CHEMBL1346 DARIFENACIN 4.0 1 9.00
CHEMBL1682220 1 8.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1682213 EC50 = 0.05 nM 10.30
CHEMBL1682210 EC50 = 0.07 nM 10.15
CHEMBL1682212 EC50 = 0.09 nM 10.05
CHEMBL1682214 EC50 = 0.13 nM 9.89
CHEMBL1682211 EC50 = 0.2 nM 9.70
CHEMBL1682215 EC50 = 0.2 nM 9.70
CHEMBL1682216 EC50 = 0.2 nM 9.70
CHEMBL1682217 EC50 = 0.2 nM 9.70
CHEMBL1682218 EC50 = 0.2 nM 9.70
CHEMBL1682219 EC50 = 0.7 nM 9.15
CHEMBL1682302 EC50 = 0.9 nM 9.05
CHEMBL1682221 EC50 = 1.0 nM 9.00
CHEMBL1346 DARIFENACIN EC50 = 1.0 nM 9.00
CHEMBL1682220 EC50 = 3.2 nM 8.49