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Assay Detail

CHEMBL834517

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

Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-3 adrenergic receptor
16
Total Activities
16
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

Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.
Sawa M, Mizuno K, Harada H, Tateishi H, Arai Y, Suzuki S, Oue M, Tsujiuchi H, Furutani Y, Kato S.
Bioorg Med Chem Lett (2005) 15 : 1061 -1064
PubMed 15686912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 8.00 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181440 1 9.27
CHEMBL182018 1 9.00
CHEMBL425161 1 8.92
CHEMBL183552 1 8.54
CHEMBL182689 1 8.49
CHEMBL360133 1 8.19
CHEMBL181603 1 8.05
CHEMBL181300 1 8.00
CHEMBL362293 1 7.96
CHEMBL182614 1 7.82
CHEMBL181964 1 7.77
CHEMBL184584 1 7.50
CHEMBL182770 1 7.44
CHEMBL361577 1 7.28
CHEMBL365669 1 7.00
CHEMBL182708 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181440 EC50 = 0.54 nM 9.27
CHEMBL182018 EC50 = 1.0 nM 9.00
CHEMBL425161 EC50 = 1.2 nM 8.92
CHEMBL183552 EC50 = 2.9 nM 8.54
CHEMBL182689 EC50 = 3.2 nM 8.49
CHEMBL360133 EC50 = 6.5 nM 8.19
CHEMBL181603 EC50 = 9.0 nM 8.05
CHEMBL181300 EC50 = 10.0 nM 8.00
CHEMBL362293 EC50 = 11.0 nM 7.96
CHEMBL182614 EC50 = 15.0 nM 7.82
CHEMBL181964 EC50 = 17.0 nM 7.77
CHEMBL184584 EC50 = 32.0 nM 7.50
CHEMBL182770 EC50 = 36.0 nM 7.44
CHEMBL361577 EC50 = 52.0 nM 7.28
CHEMBL365669 EC50 = 100.0 nM 7.00
CHEMBL182708 EC50 = 160.0 nM 6.80