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Assay Detail

CHEMBL1019684

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Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
8
Total Activities
8
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-1 adrenergic receptor (CHEMBL5471)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Butchers PR, Coe DM, Conroy R, Edney DD, Field RN, Ford AJ, Guntrip SB, Looker BE, McLay IM, Monteith MJ, Morrison VS, Mutch PJ, Richards SA, Sasse R, Smith CE.
J Med Chem (2009) 52 : 2280 -2288
PubMed 19317397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.90 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443435 1 10.40
CHEMBL1256786 FORMOTEROL 4.0 1 9.50
CHEMBL483200 1 9.10
CHEMBL475389 1 8.70
CHEMBL520313 1 8.60
CHEMBL474616 1 8.60
CHEMBL1263 SALMETEROL 4.0 1 8.30
CHEMBL514032 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443435 EC50 = 0.03981 nM 10.40
CHEMBL1256786 FORMOTEROL EC50 = 0.3162 nM 9.50
CHEMBL483200 EC50 = 0.7943 nM 9.10
CHEMBL475389 EC50 = 1.995 nM 8.70
CHEMBL520313 EC50 = 2.512 nM 8.60
CHEMBL474616 EC50 = 2.512 nM 8.60
CHEMBL1263 SALMETEROL EC50 = 5.012 nM 8.30
CHEMBL514032 EC50 = 10.0 nM 8.00