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Assay Detail

CHEMBL649663

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

Functional
Stimulated increase in cAMP in CHO cells expressing human beta-3 receptor
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.
Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.
Bioorg Med Chem Lett (2000) 10 : 1971 -1973
PubMed 10987429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 7.98 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58241 1 8.92
CHEMBL58407 1 8.70
CHEMBL294753 1 8.62
CHEMBL292598 1 8.57
CHEMBL291516 1 8.31
CHEMBL418308 1 8.30
CHEMBL291306 1 8.24
CHEMBL430594 1 8.21
CHEMBL293994 1 8.15
CHEMBL293577 1 8.14
CHEMBL57908 1 8.04
CHEMBL58798 1 8.02
CHEMBL291593 1 8.01
CHEMBL60281 1 8.00
CHEMBL61429 1 7.92
CHEMBL433248 1 7.66
CHEMBL294172 1 7.58
CHEMBL59270 1 7.48
CHEMBL294492 1 7.40
CHEMBL61962 1 7.35
CHEMBL291594 1 7.35
CHEMBL294849 1 7.30
CHEMBL291992 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58241 EC50 = 1.2 nM 8.92
CHEMBL58407 EC50 = 2.0 nM 8.70
CHEMBL294753 EC50 = 2.4 nM 8.62
CHEMBL292598 EC50 = 2.7 nM 8.57
CHEMBL291516 EC50 = 4.9 nM 8.31
CHEMBL418308 EC50 = 5.0 nM 8.30
CHEMBL291306 EC50 = 5.8 nM 8.24
CHEMBL430594 EC50 = 6.2 nM 8.21
CHEMBL293994 EC50 = 7.1 nM 8.15
CHEMBL293577 EC50 = 7.3 nM 8.14
CHEMBL57908 EC50 = 9.1 nM 8.04
CHEMBL58798 EC50 = 9.5 nM 8.02
CHEMBL291593 EC50 = 9.8 nM 8.01
CHEMBL60281 EC50 = 10.0 nM 8.00
CHEMBL61429 EC50 = 12.0 nM 7.92
CHEMBL433248 EC50 = 22.0 nM 7.66
CHEMBL294172 EC50 = 26.0 nM 7.58
CHEMBL59270 EC50 = 33.0 nM 7.48
CHEMBL294492 EC50 = 40.0 nM 7.40
CHEMBL61962 EC50 = 45.0 nM 7.35
CHEMBL291594 EC50 = 45.0 nM 7.35
CHEMBL294849 EC50 = 50.0 nM 7.30
CHEMBL291992 EC50 = 51.0 nM 7.29