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Assay Detail

CHEMBL887285

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Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
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 Intermediate

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.
Shearer BG, Chao EY, Uehling DE, Deaton DN, Cowan C, Sherman BW, Milliken T, Faison W, Brown K, Adkison KK, Lee F.
Bioorg Med Chem Lett (2007) 17 : 4670 -4677
PubMed 17560786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.63 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL154419 1 7.30
CHEMBL247518 1 7.30
CHEMBL430390 1 7.30
CHEMBL247520 1 7.10
CHEMBL393470 1 7.00
CHEMBL246908 1 7.00
CHEMBL245673 1 6.90
CHEMBL393469 1 6.90
CHEMBL247315 1 6.80
CHEMBL393471 1 6.50
CHEMBL247519 1 6.40
CHEMBL153558 1 6.40
CHEMBL395834 1 6.20
CHEMBL245873 1 6.10
CHEMBL245874 1 5.60
CHEMBL245875 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL154419 EC50 = 50.12 nM 7.30
CHEMBL247518 EC50 = 50.12 nM 7.30
CHEMBL430390 EC50 = 50.12 nM 7.30
CHEMBL247520 EC50 = 79.43 nM 7.10
CHEMBL393470 EC50 = 100.0 nM 7.00
CHEMBL246908 EC50 = 100.0 nM 7.00
CHEMBL245673 EC50 = 125.89 nM 6.90
CHEMBL393469 EC50 = 125.89 nM 6.90
CHEMBL247315 EC50 = 158.49 nM 6.80
CHEMBL393471 EC50 = 316.23 nM 6.50
CHEMBL247519 EC50 = 398.11 nM 6.40
CHEMBL153558 EC50 = 398.11 nM 6.40
CHEMBL395834 EC50 = 630.96 nM 6.20
CHEMBL245873 EC50 = 794.33 nM 6.10
CHEMBL245874 EC50 = 2511.89 nM 5.60
CHEMBL245875 EC50 = 5011.87 nM 5.30