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Assay Detail

CHEMBL819430

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Functional
Agonistic activity towards beta-3 adrenoceptor. Mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Beta-3 adrenergic receptor (CHEMBL4031)
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
EC50 19 7.39 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32670 1 9.03
CHEMBL284782 1 8.66
CHEMBL32586 1 8.25
CHEMBL32933 1 8.14
CHEMBL32115 1 7.96
CHEMBL32470 1 7.89
CHEMBL32391 1 7.85
CHEMBL35459 1 7.64
CHEMBL32532 1 7.62
CHEMBL32590 1 7.60
CHEMBL33360 1 7.28
CHEMBL284520 1 7.21
CHEMBL33399 1 7.09
CHEMBL417137 1 6.80
CHEMBL83063 RITODRINE 4.0 1 6.72
CHEMBL285888 1 6.34
CHEMBL32939 1 6.24
CHEMBL35738 1 6.09
CHEMBL289670 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32670 EC50 = 0.9333 nM 9.03
CHEMBL284782 EC50 = 2.188 nM 8.66
CHEMBL32586 EC50 = 5.623 nM 8.25
CHEMBL32933 EC50 = 7.244 nM 8.14
CHEMBL32115 EC50 = 10.96 nM 7.96
CHEMBL32470 EC50 = 12.88 nM 7.89
CHEMBL32391 EC50 = 14.13 nM 7.85
CHEMBL35459 EC50 = 22.91 nM 7.64
CHEMBL32532 EC50 = 23.99 nM 7.62
CHEMBL32590 EC50 = 25.12 nM 7.60
CHEMBL33360 EC50 = 52.48 nM 7.28
CHEMBL284520 EC50 = 61.66 nM 7.21
CHEMBL33399 EC50 = 81.28 nM 7.09
CHEMBL417137 EC50 = 158.49 nM 6.80
CHEMBL83063 RITODRINE EC50 = 190.55 nM 6.72
CHEMBL285888 EC50 = 457.09 nM 6.34
CHEMBL32939 EC50 = 575.44 nM 6.24
CHEMBL35738 EC50 = 812.83 nM 6.09
CHEMBL289670 EC50 = 831.76 nM 6.08