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Assay Detail

CHEMBL1685250

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Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL3252)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 12 5.64 6.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1682220 1 6.53
CHEMBL1682215 1 6.26
CHEMBL1682211 1 6.05
CHEMBL1682217 1 5.80
CHEMBL1346 DARIFENACIN 4.0 1 5.64
CHEMBL1682219 1 5.24
CHEMBL1682216 1 5.20
CHEMBL1682218 1 5.05
CHEMBL1682221 1 5.00
CHEMBL1682210 1 -
CHEMBL1682212 1 -
CHEMBL1682213 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1682220 EC50 = 296.0 nM 6.53
CHEMBL1682215 EC50 = 550.0 nM 6.26
CHEMBL1682211 EC50 = 900.0 nM 6.05
CHEMBL1682217 EC50 = 1600.0 nM 5.80
CHEMBL1346 DARIFENACIN EC50 = 2310.0 nM 5.64
CHEMBL1682219 EC50 = 5770.0 nM 5.24
CHEMBL1682216 EC50 = 6300.0 nM 5.20
CHEMBL1682218 EC50 = 8890.0 nM 5.05
CHEMBL1682221 EC50 = 10000.0 nM 5.00
CHEMBL1682210 EC50 > 10000.0 nM -
CHEMBL1682212 EC50 > 10000.0 nM -
CHEMBL1682213 EC50 > 10000.0 nM -