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Assay Detail

CHEMBL819428

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

Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-2 adrenergic receptor (CHEMBL3754)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of novel N-phenylglycine derivatives as potent and selective beta(3)-adrenoceptor agonists for the treatment of frequent urination and urinary incontinence.
Tanaka N, Tamai T, Mukaiyama H, Hirabayashi A, Muranaka H, Akahane S, Miyata H, Akahane M.
J Med Chem (2001) 44 : 1436 -1445
PubMed 11311067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.05 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284782 1 8.04
CHEMBL83063 RITODRINE 4.0 1 7.62
CHEMBL32933 1 7.21
CHEMBL32470 1 6.60
CHEMBL289670 1 6.55
CHEMBL32532 1 6.19
CHEMBL284520 1 5.89
CHEMBL32586 1 5.85
CHEMBL32939 1 5.85
CHEMBL33360 1 5.80
CHEMBL285888 1 5.77
CHEMBL35738 1 5.66
CHEMBL33399 1 5.59
CHEMBL32670 1 5.48
CHEMBL32590 1 5.01
CHEMBL35459 1 4.96
CHEMBL32391 1 4.85
CHEMBL32115 1 -
CHEMBL417137 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284782 IC50 = 9.12 nM 8.04
CHEMBL83063 RITODRINE IC50 = 23.99 nM 7.62
CHEMBL32933 IC50 = 61.66 nM 7.21
CHEMBL32470 IC50 = 251.19 nM 6.60
CHEMBL289670 IC50 = 281.84 nM 6.55
CHEMBL32532 IC50 = 645.65 nM 6.19
CHEMBL284520 IC50 = 1288.25 nM 5.89
CHEMBL32586 IC50 = 1412.54 nM 5.85
CHEMBL32939 IC50 = 1412.54 nM 5.85
CHEMBL33360 IC50 = 1584.89 nM 5.80
CHEMBL285888 IC50 = 1698.24 nM 5.77
CHEMBL35738 IC50 = 2187.76 nM 5.66
CHEMBL33399 IC50 = 2570.4 nM 5.59
CHEMBL32670 IC50 = 3311.31 nM 5.48
CHEMBL32590 IC50 = 9772.37 nM 5.01
CHEMBL35459 IC50 = 10964.78 nM 4.96
CHEMBL32391 IC50 = 14125.38 nM 4.85
CHEMBL32115 IC50 < 100000.0 nM -
CHEMBL417137 IC50 < 100000.0 nM -