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Assay Detail

CHEMBL655820

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

Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
14
Total Activities
14
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-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.
Uehling DE, Donaldson KH, Deaton DN, Hyman CE, Sugg EE, Barrett DG, Hughes RG, Reitter B, Adkison KK, Lancaster ME, Lee F, Hart R, Paulik MA, Sherman BW, True T, Cowan C.
J Med Chem (2002) 45 : 567 -583
PubMed 11806709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.57 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL154370 1 9.00
CHEMBL345304 1 8.50
CHEMBL153916 1 8.30
CHEMBL154150 1 8.10
CHEMBL348269 1 8.00
CHEMBL155072 1 8.00
CHEMBL157210 1 7.70
CHEMBL347616 1 7.50
CHEMBL154036 1 7.30
CHEMBL152535 1 7.30
CHEMBL154419 1 7.30
CHEMBL348501 1 7.10
CHEMBL153558 1 6.40
CHEMBL155092 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL154370 EC50 = 1.0 nM 9.00
CHEMBL345304 EC50 = 3.162 nM 8.50
CHEMBL153916 EC50 = 5.012 nM 8.30
CHEMBL154150 EC50 = 7.943 nM 8.10
CHEMBL348269 EC50 = 10.0 nM 8.00
CHEMBL155072 EC50 = 10.0 nM 8.00
CHEMBL157210 EC50 = 19.95 nM 7.70
CHEMBL347616 EC50 = 31.62 nM 7.50
CHEMBL154036 EC50 = 50.12 nM 7.30
CHEMBL152535 EC50 = 50.12 nM 7.30
CHEMBL154419 EC50 = 50.12 nM 7.30
CHEMBL348501 EC50 = 79.43 nM 7.10
CHEMBL153558 EC50 = 398.11 nM 6.40
CHEMBL155092 EC50 = 3162.28 nM 5.50