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Assay Detail

CHEMBL818919

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Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-3-andrenergic receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Beta-3 adrenergic receptor (CHEMBL246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,4-Thiazolidinediones as potent and selective human beta3 agonists.
Hu B, Ellingboe J, Gunawan I, Han S, Largis E, Li Z, Malamas M, Mulvey R, Oliphant A, Sum FW, Tillett J, Wong V.
Bioorg Med Chem Lett (2001) 11 : 757 -760
PubMed 11277513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.20 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164378 1 8.52
CHEMBL424167 1 8.22
CHEMBL163262 1 8.00
CHEMBL166085 1 7.92
CHEMBL161949 1 7.89
CHEMBL162711 1 7.62
CHEMBL165893 1 7.40
CHEMBL162380 1 6.77
CHEMBL165892 1 6.66
CHEMBL350131 1 6.42
CHEMBL440924 1 6.18
CHEMBL161950 1 6.05
CHEMBL32590 1 5.94
CHEMBL164065 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164378 EC50 = 3.0 nM 8.52
CHEMBL424167 EC50 = 6.0 nM 8.22
CHEMBL163262 EC50 = 10.0 nM 8.00
CHEMBL166085 EC50 = 12.0 nM 7.92
CHEMBL161949 EC50 = 13.0 nM 7.89
CHEMBL162711 EC50 = 24.0 nM 7.62
CHEMBL165893 EC50 = 40.0 nM 7.40
CHEMBL162380 EC50 = 170.0 nM 6.77
CHEMBL165892 EC50 = 220.0 nM 6.66
CHEMBL350131 EC50 = 380.0 nM 6.42
CHEMBL440924 EC50 = 660.0 nM 6.18
CHEMBL161950 EC50 = 900.0 nM 6.05
CHEMBL32590 EC50 = 1150.0 nM 5.94
CHEMBL164065 EC50 > 10000.0 nM -